PYRROLIDINONE DERIVATIVES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS (Fri, 18 Apr 2014)
The present invention relates to pyrrolidinone derivatives of formula (I). The pyrrolidinone derivatives of formula (I) are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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EXENDIN-4 DERIVATIVES AS DUAL GLP1/GLUCAGON AGONISTS (Fri, 18 Apr 2014)
The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.
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INDOLYLDIHYDROIMIDAZOPYRIMIDINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 11 Apr 2014)
The invention relates to the novel products of formula (I): in which R1 represents H, Alk or cycloalkyl optionally substituted with one or more Hal; R2 represents H or Hal; and R3 represents H; Hal, OH; NO2; C2-C6 alkenyl; C2-C6 alkynyl; -Y-alkyl; R; OR; -CO2H; -CO2R; -NRxRy, -CONRxRy or -CO2NRxRy, all optionally substituted; where Y represents S, SO or SO2; NRxRy is such that either Rx represents H, alk or cycloalkyl and Ry represents H, alk, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, COR or SO2R, all optionally substituted; or Rx and Ry form, with N, an optionally substituted cyclic radical; R represents alk, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, all optionally substituted; with one or more H representing a deuterium atom; these products being in any of the isomer forms, and the salts, as medicaments, in particular as anticancer agents.
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ACYLAMINO-SUBSTITUTED CYCLIC CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 28 Mar 2014)
<p id="p-0001" num="0000">The present invention relates to compounds of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.57mm" wi="70.02mm" file="US20140088158A1-20140327-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A, Y, Z, R<sup>20 </sup>to R<sup>22 </sup>and R<sup>50 </sup>have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA<sub>1 </sub>receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.</p>
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MACROLIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 28 Mar 2014)
The patent application relates to compounds of formula (I) below: formula (I) to a process for preparing them and to the therapeutic use thereof.
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BENZOIMIDAZOLE-CARBOXYLIC ACID AMIDE DERIVATIVES AS APJ RECEPTOR MODULATORS (Fri, 28 Mar 2014)
The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R', R", R"', R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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PROCESS FOR THE PREPARATION OF DEUTERATED COMPOUNDS CONTAINING N-ALKYL GROUPS (Fri, 21 Mar 2014)
<p id="p-0001" num="0000">The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.</p>
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CRYSTALLINE COMPOUNDS (Fri, 21 Mar 2014)
Provided herein are polymorph E, a mixed DMAC/toluene solvate and a DMSO solvate of N-(3-{[(2Z)-3-[(2-chloro-5- methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]sulfamoyl}phenyl)-2- methylalaninamide.
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Spirocyclic nitriles as protease inhibitors (Fri, 14 Mar 2014)
<p id="p-0001" num="0000">The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.</p>
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OXATHIAZINE DERIVATIVES WHICH ARE SUBSTITUTED WITH BENZYL OR HETEROMETHYLENE GROUPS, METHOD FOR PRODUCING THEM, THEIR USE AS MEDICINE AND DRUG CONTAINING SAID DERIVATIVES AND THE USE THEREOF (Fri, 07 Mar 2014)
<p id="p-0001" num="0000">The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.30mm" wi="62.23mm" file="US20140066437A1-20140306-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PROCESS FOR SYNTHESIZING KETO BENZOFURAN DERIVATIVES (Fri, 14 Feb 2014)
<p id="p-0001" num="0000">The invention relates to a method for synthesizing benzofuran derivatives, in particular the dronedarone of formula (D), including carrying out a Fries rearrangement reaction using a sulfonamido-benzofuran ester intermediate.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.61mm" wi="74.17mm" file="US20140046078A1-20140213-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL (HETEROCYCLE/CONDENSED PIPERIDINE)-(PIPERAZINYL)-1-ALKANONE OR (HETEROCYCLE/CONDENSED PYRROLIDINE)-(PIPERAZINYL)-1-ALKANONE DERIVATIVES AND USE THEREOF AS p75 INHIBITORS (Fri, 07 Feb 2014)
<p id="p-0001" num="0000">The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="11.35mm" wi="23.37mm" file="US20140038946A1-20140206-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.</p>
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POLYSACCHARIDES COMPRISING TWO ANTITHROMBIN III-BINDING SITES, PREPARATION THEREOF AND USE THEREOF AS ANTITHROMBOTIC MEDICAMENTS (Fri, 31 Jan 2014)
<p id="p-0001" num="0000">The invention relates to sulphated polysaccharides which have the general structure of the constituent polysaccharides of heparin and which have a molecular weight of less than 8000 Daltons, comprising two antithrombin III-binding hexasaccharide sequences corresponding to formula (I) in which: R1 represents an OH group when the hexasaccharide of formula (I) is located at the reducing end of the polysaccharide, or else R1 represents a bond with another saccharide unit of said polysaccharide; R2 represents a hydrogen atom when the hexasaccharide of formula (I) is located at the non-reducing end of the polysaccharide, in which case the bond between carbon atoms 4 and 5 of the first saccharide unit of said hexasaccharide is a double bond, or else R2 represents a bond with another saccharide unit of said polysaccharide, in which case the bond between carbon atoms 4 and 5 of the first saccharide unit is a single bond. Preparation thereof, use thereof as antithrombotic medicaments, and also use thereof in a method for analysing a sample of a heparin derivative.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="111.51mm" wi="76.20mm" file="US20140031316A1-20140130-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BENZOIC ACID SALT OF OTAMIXABAN (Fri, 24 Jan 2014)
<p id="p-0001" num="0000">The invention relates to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate, and to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.</p>
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USE OF VEGFR-3 INHIBITORS FOR TREATING HEPATOCELLULAR CARCINOMA (Fri, 24 Jan 2014)
This invention is related to the use of inhibitors of vascular endothelial growth factor receptor 3 for treating hepatocellular carcinoma.
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REDUCTIVE AMINATION PROCESS FOR PREPARATION OF DRONEDARONE USING AMINE INTERMEDIARY COMPOUND (Fri, 17 Jan 2014)
<p id="p-0001" num="0000">The invention relates to a novel process for preparation of drohedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) is reacted in the presence of a reductive agent with butyraldehyde and/or butanoic acid, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some hovel intermediary compounds and the preparation thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="60.79mm" wi="76.20mm" file="US20140018554A1-20140116-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PROCESS FOR SYNTHESIZING KETO-BENZOFURAN DERIVATIVES (Fri, 17 Jan 2014)
<p id="p-0001" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.48mm" wi="75.86mm" file="US20140018553A1-20140116-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0002" num="0000">The invention relates to a process for synthesizing benzofuran derivatives, in particular dronedarone of formula (D), comprising a step of Friedel-Crafts acylation starting from a sulfonamido-benzofuran ester intermediate.</p>
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CYCLIC PEPTIDES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF THE PLATELET ADHESION (Fri, 10 Jan 2014)
<p id="p-0001" num="0000">The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="69.00mm" wi="76.20mm" file="US20140011734A1-20140109-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL 6-TRIAZOLOPYRIDAZINE SULFANYL BENZOTHIAZOLE DERIVATIVES AS MET INHIBITORS (Fri, 03 Jan 2014)
<p id="p-0001" num="0000">The disclosure relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.25mm" wi="63.08mm" file="US20140005189A1-20140102-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein <img id="CUSTOM-CHARACTER-00001" he="3.56mm" wi="4.57mm" file="US20140005189A1-20140102-P00001.TIF" alt="custom-character" img-content="character" img-format="tif"/>, A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.</p>
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METHOD FOR PRODUCING 2-(2-AMINOPYRIMIDIN-4-YL)-1H-INDOLE-5-CARBOXYLIC ACID DERIVATIVES (Fri, 03 Jan 2014)
<p id="p-0001" num="0000">This disclosure relates to a novel process for obtaining a compound of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.65mm" wi="69.43mm" file="US20140005392A1-20140102-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the values of R1, R2, and R3 and P are as described in the specification, and intermediates thereof.</p>
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PYRIMIDINONE DERIVATIVES AS ANTIMALARIAL AGENTS (Sat, 28 Dec 2013)
The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n = 0 or 1 and R2 is a methyl group when n = 0 and a hydrogen atom when n = 1. Process for the preparation thereof and therapeutic use thereof.
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NOVEL 2,3-DIHYDRO-1H-IMIDAZO{1,2-a}PYRIMIDIN-5-ONE and this1,2,3,4-TETRAHYDROPYRIMIDO{1,2-a}PYRIMIDIN-6-ONE DERIVATIVES COMPRISING A SUBSTITUTED MORPHOLINE, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF (Sat, 28 Dec 2013)
The invention relates to the novel products of formula (I) with p, q = 0, 1 or 2; R1 = phenyl, pyridyl; -(CH2) m -Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; -SO2 -Rb; -CO-Re; m = 1 or 2; Ra = aryl, heteroaryl, -CO-cycloalkyl, -CO-heterocycloalkyl, -CO-Rb, -C(Rb)=N-ORc, -CO 2 Rd, -CONRxRy; Rb = alkyl, aryl, heteroaryl; Rc = H, alkyl; Rd = alkyl, cycloalkyl; Re = alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry = H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3 = H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4 = H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
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EXENDIN-4 PEPTIDE ANALOGUES (Fri, 20 Dec 2013)
The present invention relates to exendin-4 peptide analogues and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.
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PROCESS FOR PREPARATION OF DRONEDARONE BY GRIGNARD REACTION (Fri, 06 Dec 2013)
The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof, which comprises reacting of compound of formula (IV) with compound of formula (VI) in a Grignard reaction, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and processes for the preparation thereof.
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SUBSTITUTED ß-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS (Fri, 29 Nov 2013)
The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Substituted B-amino acid derivatives as CXCR3 receptor antagonist (Thu, 28 Nov 2013)
The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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BENZO[1,3]DIOXINE DERIVATIVES AND THEIR USE AS LPAR5 ANTAGONISTS (Fri, 22 Nov 2013)
The present invention relates to compounds of the formula (I), wherein the residues A, R1 to R5, Z1 and Z2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.
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METHOD FOR PRODUCING RECOMBINANT 11-DE-O-METHYLTOMAYMYCIN (Fri, 22 Nov 2013)
The present invention provides a tomaymycin biosynthetic gene cluster of Streptomyces species FH6421,and its use for producing 11-de-O-methyltomaymycin.
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METHODS FOR THE ACTIVATION OF SILENT GENES IN A MICROORGANISM (Fri, 22 Nov 2013)
The present invention relates to a method for the activation of silent genes in microorganisms by co-cultivation of an inducer and a recipient microorganism. The inducer is selected from a chemical inducer, a microorganism inducer which is selected from a killed microorganism cell and/or inactivated culture medium in which said microorganism cell had been cultured and/or medium inducer. The present invention furthermore relates to a method for screening for an inducer and to a method of screening for a recipient microorganism by co-cultivation of an inducer and a recipient organism. The methods are useful for the detection of medicaments, such as antibiotics. The present invention further relates to media for culturing microorganisms comprising an inducer.
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PHOTOCHEMICAL PROCESS FOR PRODUCING ARTEMISININ (Fri, 15 Nov 2013)
<p id="p-0001" num="0000">Provided is a new photochemical process for preparing artemisinin. Also provided are certain dihydroartemisinic acid derivatives useful for preparing artemisinin.</p>
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NOVEL (HETEROCYCLE/TETRAHYDROPYRIDINE)-(PIPERAZINYL)-1-ALCANONE AND (HETEROCYCLE/DIHYDROPYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE DERIVATIVES, AND USE THEREOF AS p75 INHIBITORS (Fri, 15 Nov 2013)
<p id="p-0001" num="0000">The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="17.19mm" wi="45.04mm" file="US20130303520A1-20131114-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.</p>
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SUBSTITUTED 6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE DERIVATIVES AS KINASE INHIBITORS (Fri, 15 Nov 2013)
Substituted 6-(4-Hydroxy-phenyl)-l H-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula, in which R', R2 , R3, R4, R5 and R6 are defined as indicated below. The compounds of the formula I are proteine kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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NOVEL PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS (Fri, 18 Oct 2013)
<p id="p-0001" num="0000">The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.</p>
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NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF (Fri, 11 Oct 2013)
The present invention relates to compounds of formula (I): wherein R6 is -CONH2 or a -C(Rα)(Rβ)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
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NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.91mm" wi="56.22mm" file="US20130261106A1-20131003-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R6 is —CONH<sub>2 </sub>or a —C(R<sub>α</sub>)(R<sub>β</sub>)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group.</p> <p id="p-0004" num="0000">Process for the preparation thereof and therapeutic use thereof.</p>
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PROCESS FOR THE PREPARATION OF DRONEDARONE (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">The subject of the present invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.24mm" wi="74.76mm" file="US20130261321A1-20131003-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and the new intermediates of the preparation process.</p>
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5,6-bisaryl-2-pyridine-carboxamide derivatives, preparation thereof and therapeutic application thereof as urotensin II receptor antagonists (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">The present invention is directed to compounds of the general formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.20mm" wi="69.85mm" file="US08653276-20140218-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as defined herein, and pharmaceutical compositions thereof. The invention is also directed to their therapeutic use as urotensin II receptor antagonists, e.g., in the treatment of cardiac, coronary, and central nervous system disorders. In particular embodiments, the invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists. </p>
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A MIXTURE OF POLAR GLYCOLIPIDS FOR USE IN THE TREATMENT OF PAIN AND COPD (Fri, 27 Sep 2013)
The present invention concerns a method for the treatment and/or prevention of pain and/or Chronic Obstructive Pulmonary Disease (COPD) comprising administering to a subject a composition comprising a polar glycolipid obtainable from cells of a cyanobacterium Oscillatoria species (CyP).
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A mixture of polar glycolipids for use in the treatment of pain and COPD (Thu, 26 Sep 2013)
The present invention concerns a composition comprising a polar glycolipid obtainable from cells of a cyanobacterium Oscillatoria species (CyP), for use for the treatment and/or the prevention of pain and/or of Chronic Obstructive Pulmonary Disease (COPD).
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POLYMERIC CONJUGATES OF ACTIVE PRINCIPLES, THEIR PROCESS OF PREPARATION AND THEIR POLYMERIC INTERMEDIATES (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">The present invention relates to novel conjugates of active principles grafted to a polymer, to the nanoparticles comprising them, to their preparation and to their polymeric intermediates.</p>
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NITROBENZOTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATIONS THEREOF (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.31mm" wi="69.85mm" file="US20130245008A1-20130919-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL INDOLIZINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">The invention relates to indolizine derivatives of general formula (I), where A, B, m, W, n and R2 are as defined in claim <b>1</b>, as well as to the method for preparing same and to the therapeutic use thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.24mm" wi="55.96mm" file="US20130245006A1-20130919-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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6-CYCLOAMINO-3-(PYRIDAZIN-4-YL)IMIDAZO[1,2-b]-PYRIDAZINE AND DERIVATIVES THEREOF PREPARATION AND THERAPEUTIC APPLICATION THEREOF (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">The invention relates to the 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.83mm" wi="58.00mm" file="US20130245023A1-20130919-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein R<sub>2</sub>, R<sub>7</sub>, R<sub>8</sub>, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.</p>
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Process for the preparation of 3-(6-amino-pyridin-3yl)-2-acrylic acid derivatives (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">The present invention relates to a process for the preparation of a compound of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.69mm" wi="69.85mm" file="US20130245274A1-20130919-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">which comprises reacting a compound of the formula IV</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="28.28mm" wi="69.85mm" file="US20130245274A1-20130919-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">with the compound of formula VII R15-A2-CHO and to novel intermediate compounds used therein.</p>
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AZETIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY (Fri, 13 Sep 2013)
<p id="p-0001" num="0000">The invention relates to azetidine derivatives having the formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.19mm" wi="75.44mm" file="US20130237513A1-20130912-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein R′, R1, R2, R3, R6, R7, R, Y, A and B are as defined herein. The invention also relates to a method for preparing the same and therapeutic use thereof.</p>
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FUNCTIONAL PLA-PEG COPOLYMERS, THE NANOPARTICLES THEREOF, THEIR PREPARATION AND USE FOR TARGETED DRUG DELIVERY AND IMAGING (Sat, 07 Sep 2013)
Functional PLA-PEG copolymers, the nanoparticles thereof, their preparation and use for targeted drug delivery and imaging The present invention concerns novel functional PEG-PLA containing copolymers, the nanoparticles containing the same, their process of preparation and their use for site specific targeted drug delivery and imaging.
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PROCESS FOR PREPARATION OF DRONEDARONE BY THE USE OF DIBUTYLAMINOPROPANOL REAGENT (Sat, 07 Sep 2013)
The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof, characterized in that a compound of formula (II) - where L is leaving group - is reacted with compound of formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
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Functional PLA-PEG copolymers, the nanoparticles thereof, their preparation and use for targeted drug delivery and imaging (Thu, 05 Sep 2013)
The present invention concerns novel functional PEG-PLA containing copolymers, the nanoparticles containing the same, their process of preparation and their use for site specific targeted drug delivery and imaging.
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PROCESS FOR PREPARATION OF DRONEDARONE BY OXIDATION OF A HYDROXYL GROUP (Fri, 30 Aug 2013)
The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof (formula I), which comprises oxidizing a compound of formula (VI), or a salt thereof and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (VI) and process for the preparation thereof.
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Multivalent Meningococcal Polysaccharide-Protein Conjugate Vaccine (Fri, 23 Aug 2013)
<p id="p-0001" num="0000">The present invention describes a combined vaccine that offers broad protection against meningococcal disease caused by the pathogenic bacteria <i>Neisseria meningitidis</i>. The vaccine is comprised of four distinct polysaccharide-protein conjugates that are formulated as a single dose of vaccine. Purified capsular polysaccharides from <i>Neisseria meningitidis </i>serogroups A, C, W-135, and Y are chemically activated and selectively attached to a carrier protein by means of a covalent chemical bond, forming polysaccharide-protein conjugates capable of eliciting long-lasting immunity to a variety of <i>N. meningitidis </i>strains in children as well as adults.</p>
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PROCESS FOR PREPARATION OF DRONEDARONE BY REMOVAL OF HYDROXYL GROUP (Fri, 23 Aug 2013)
The invention relates to a process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that from the compound of formula (II). the hydroxyl group is removed,. and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
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PROCESS FOR THE PREPARATION OF DRONEDARONE BY OXIDATION OF A SULPHENYL GROUP (Fri, 23 Aug 2013)
The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (IV) or a salt thereof with an oxidizing agent in an organic or inorganic solvent or solvent mixture, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (IV), and a process for the preparation thereof.
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7-AZA-SPIRO[3,5]NONANE-7-CARBOXYLATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 16 Aug 2013)
<p id="p-0001" num="0000">The present invention is directed to 7-aza-spiro[3.5]nonane-7-carboxylate derivatives of the Formula I. The compounds of the invention are inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The invention also relates to processes for the preparation of compounds of the Formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.</p>
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PROCESS FOR PREPARING TAXOL DERIVATIVES AND CERTAIN INTERMEDIATE COMPOUNDS (Fri, 09 Aug 2013)
The present invention relates to a novel process for preparing taxol derivatives, comprising a step of esterification of a baccatin III derivative with a carboxylic acid comprising an oxazolidine ring. A subject of the present invention is also certain novel intermediates involved in this process, and in particular the compound resulting from this esterification step. Said process can be carried out in order to prepare tesetaxel.
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FUSED PYRROLEDICARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS (Fri, 09 Aug 2013)
The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
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PYRIMIDOOXAZOCINE DERIVATIVES AS MTOR - INHIBITORS (Fri, 02 Aug 2013)
The invention relates to bicydic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
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Process for preparation of dronedarone by the use of dibutylaminopropanol reagent (Thu, 25 Jul 2013)
The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) - where L is leaving group - is reacted with compound of formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
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Multivalent Meningococcal Polysaccharide-Protein Conjugate Vaccine (Fri, 12 Jul 2013)
<p id="p-0001" num="0000">The present invention describes a combined vaccine that offers broad protection against meningococcal disease caused by the pathogenic bacteria <i>Neisseria meningitidis. </i>The vaccine is comprised of four distinct polysaccharide-protein conjugates that are formulated as a single dose of vaccine. Purified capsular polysaccharides from <i>Neisseria meningitidis </i>serogroups A, C, W-135, and Y are chemically activated and selectively attached to a carrier protein by means of a covalent chemical bond, forming polysaccharide-protein conjugates capable of eliciting long-lasting immunity to a variety of <i>N. meningitidis </i>strains in children as well as adults.</p>
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ARYLSULFONAMIDE PYRIDINE-PYRIDINONE DERIVATIVES, PREPARATION OF SAME, AND THERAPEUTIC USE THEREOF (Fri, 12 Jul 2013)
<p id="p-0001" num="0000">The invention relates to pyridine-pyridinone derivatives general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.48mm" wi="74.85mm" file="US20130178472A1-20130711-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">in which R1, R2, R3, R4, n, n′, V, W, Y, Z, Ar are as defined in the description, and to their methods of preparation and their therapeutic applications.</li> </ul> </li> </ul> </p>
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THERAPEUTIC USE OF IMIDAZOPYRIDINE DERIVATIVES (Fri, 12 Jul 2013)
The invention relates to the use of compounds corresponding to formula (I) in which R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of the formulae (A), (B) and (C) in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached, or of a pharmaceutically acceptable salt thereof, for preparing a medicament for the treatment of bladder cancer.
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3-[4-(PHENYLAMINOOXALYLAMINO)PHENYL]HEX-4-YNOIC ACIDS, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS A MEDICAMENT (Fri, 12 Jul 2013)
The invention relates to 3-[4-(phenylaminooxalylamino)phenyl]hex-4-ynoic acids, and to physiologically compatible salts thereof. The invention relates to compounds of the formula (I) in which R1, R2, R3 and R4 are each defined as specified, and to physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
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FGF RECEPTOR (FGFR) AGONIST DIMERIC COMPOUNDS, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 05 Jul 2013)
The invention relates to novel heterocyclic compounds which are pyrazolopyridine derivatives that induce FGFR dimerization, having the general formula: M -L-M 2 in which M and M 2, which may be identical or different, each represent, independently of one another, a monomer unit Mand L represents a linker group which links M1 and M2 covalently with the monomer unit which follows (Formula M). Process for the preparation thereof and therapeutic use thereof.
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FGF RECEPTOR (FGFR) AGONIST DIMERIC COMPOUNDS, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 05 Jul 2013)
The invention relates to novel heterocyclic compounds which are pyrazolopyridine derivatives that induce fibroblast growth factor receptor (FGFR) dimerization, having the general formula: M1-L-M2 in which M1 or M2, which may be identical or different, each represent, independently of one another, a monomer unit M and L represents a linker group which links M1 and M2 covalently with the monomer unit which follows: Process for the preparation thereof and therapeutic use thereof.
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HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 28 Jun 2013)
<p id="p-0001" num="0000">The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.18mm" wi="64.09mm" file="US20130165422A1-20130627-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which: <br/> R, Z, A, m, and n are as defined in the disclosure; <br/> in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof. </p>
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METHOD FOR PREPARING 3-KETO-BENZOFURANE DERIVATIVES (Fri, 28 Jun 2013)
<p id="p-0001" num="0000">The invention relates to a method for preparing 3-keto-benzofurane derivatives of the general formula: Formula (I), where R is an alkyl or aryl group, R<sub>1 </sub>is hydrogen or an alkyl or aryl group, and R<sub>2 </sub>is a substituted alkyl or phenyl group. Said preparation method involves coupling a derivative of Formula III, where X is chlorine, bromine, or iodine or a sulfonate grouping: Formula (III) with a sulfonamide derivative of the formula R—SO<sub>2</sub>—NH<sub>2 </sub>in the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand.</p>
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ISOTHIAZOLOPYRIDINE-2-CARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS (Fri, 28 Jun 2013)
The present invention relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
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SULPHONYLAMINOPYRROLIDINONE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 28 Jun 2013)
The invention relates to new sulphonylaminopyrrolidinone compounds having antithrombotic activity which, in particular, inhibit blood clotting factor IXa and/ or factor Xa, to processes for their preparation and to use thereof as drugs.
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METHOD FOR RECOMBINANT PRODUCTION OF LABYRINTHOPEPTINS AND FUNCTIONAL DERIVATIVES THEREOF (Fri, 28 Jun 2013)
The present invention relates to a method for recombinant production of Labyrinthopeptins and functional derivatives thereof. Moreover, the present invention relates to novel functional derivatives of Labyrinthopeptins.
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IN SILICO AFFINITY MATURATION (Fri, 28 Jun 2013)
Methods are disclosed for increasing the binding affinity of binding proteins using in silico affinity maturation.
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Sulphonylaminopyrrolidinone derivatives, their preparation and their therapeutic application (Thu, 27 Jun 2013)
The invention relates to new sulphonylaminopyrrolidinone compounds having antithrombotic activity which, in particular, inhibit blood clotting factor IXa and/ or factor Xa, to processes for their preparation and to use thereof as drugs.
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Method for recombinant production of labyrinthopeptins and functional derivatives thereof (Thu, 27 Jun 2013)
The present invention relates to a method for recombinant production of Labyrinthopeptins and functional derivatives thereof. Moreover, the present invention relates to novel functional derivatives of Labyrinthopeptins.
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HETEROCYCLIC CARBOXYLIC ACID DERIVATIVES HAVING A 2,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE RING (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">The invention relates to oxazolopyrimidine compounds of formula (I), where A, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, X and Y are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.60mm" wi="73.74mm" file="US20130158051A1-20130620-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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1,3,5 -TRIAZINE-2-AMINE DERIVATIVES, PREPARATION THEREOF AND DIAGNOSTIC AND THERAPEUTIC USE THEREOF (Fri, 21 Jun 2013)
The present invention relates to compounds corresponding to formula (I) in which: - R1 represents a substituted phenyl; - R2 represents: - a substituted phenyl; - a heteroaromatic group, the said group being unsubstituted or substituted one or more times; - R3 represents a group Alk; - R4 represents a hydrogen atom or a (C1-C4)alkyl; - R5 represents a hydrogen atom, a (C3-C6)cycloalkyl or a (C1-C4)alkyl-O-Alk; - or alternatively R4 and R5, together with the nitrogen atom to which they are attached, constitute a heterocyclic radical chosen from: azetidin-1-yl, pyrrolidin-1-yl, piperid-1-yl, morpholin-4-yl; - R6 represents a group -COOAlk, a group -CONH 2 or a group -NHSO 2 Alk; - Alk represents a (C1-C4)alkyl, which is unsubstituted or substituted one or more times with a halogen atom; in the form of the base or of an acid-addition salt. Preparation process and diagnostic and therapeutic use.
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PYRAZOLOPYRIDINE DERIVATIVES, PREPARATION PROCESS THEREFOR AND THERAPEUTIC USE THEREOF (Fri, 21 Jun 2013)
The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
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6-(4-Hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.12mm" wi="59.27mm" file="US20130150340A1-20130613-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>and R<sup>4 </sup>are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.</p>
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CYCLOALKANE CARBOXYLIC ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS (Fri, 14 Jun 2013)
The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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CRYSTALLINE FORMS OF 2-(2-METHYLAMINO-PYRIMIDIN-4-YL)-1H-INDOLE-5-CARBOXYLIC ACID [(S)-1-CARBAMOYL-2-(PHENYL-PYRIMIDIN-2-YL-AMINO)-ETHYL]-AMIDE (Fri, 14 Jun 2013)
The present invention relates to polymorphs and hydrates of 2-(2-methylamino- pyrimidin-4-yl)-1H-indole-5-carboxylic acid [(S)-1-carbamoyl-2-(phenyl-pyrimidin-2-yl- amino)-ethyl]-amide, processes for their preparation and their use, in particular in pharmaceutical compositions.
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ANTICANCER DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 31 May 2013)
<p id="p-0001" num="0000">Provided herein are compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="65.11mm" wi="75.69mm" file="US20130137659A1-20130530-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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DERIVATIVES OF OXADIAZOLE AND PYRIDAZINE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS (Fri, 31 May 2013)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="14.90mm" wi="74.34mm" file="US20130137691A1-20130530-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">in which:</li> <li id="ul0002-0002" num="0000">n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a —CH— group; X1 represents a nitrogen atom or a —CH═CH— group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1-C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a —(C3-C10)cycloalkyl- group; Y represents a —(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1-C6)alkoxy group; Z1 is absent or represents an —NH— function; Z2 and Z3 are as defined in the description.</li> </ul> </li> </ul> </p> <p id="p-0003" num="0000">The invention also relates to a process for preparing compounds of formula (I), compositions containing them and their application in therapeutics.</p>
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2,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE DERIVATIVES (Fri, 31 May 2013)
<p id="p-0001" num="0000">The invention relates to oxazolopyrimidine compounds of formula (I), where A, R<sup>1</sup>, R<sup>2 </sup>and R<sup>3 </sup>are defined as stated in the claims. The compounds of formula (I) are suitable, for example, for wound healing.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.98mm" wi="57.83mm" file="US20130137685A1-20130530-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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SODIUM SALT OF (R)-3-[6-AMINO-PYRIDIN-3-YL]-2-(1-CYCLOHEXYL-1H-IMIDAZOL-4-YL)-PROPIONIC ACID (Fri, 31 May 2013)
The invention relates to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid, and to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1-cyclohexyl-1H-imidazol-4-yl)-propionic acid which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor).
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CRYSTALLINE SALTS OF R)-3-[6-AMINO-PYRIDIN-3-YL]-2-(1-CYCLOHEXYL-1H-IMIDAZOL-4-YL)-PROPIONIC ACID (Fri, 31 May 2013)
The invention relates to a sodium salt of (R)-3-[6-amino-pyridin-3-yl]-2-(1 -cyclohexyl- 1 H-imidazol-4-yl)-propionic acid which is in a crystalline form or in at least partially crystalline form as a monohydrate or anhydrate, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor).
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DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS (Fri, 24 May 2013)
<p id="p-0001" num="0000">The instant invention relates to derivatives of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.27mm" wi="58.67mm" file="US20130131034A1-20130523-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and their application in therapeutics.</p>
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Novel Process for the Preparation of Dronedarone (Fri, 24 May 2013)
<p id="p-0001" num="0000">The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.24mm" wi="75.95mm" file="US20130131358A1-20130523-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically acceptable salts thereof wherein the acyl group of the benzofuran derivative of the general formula II:</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="24.89mm" wi="75.95mm" file="US20130131358A1-20130523-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">where R represents C<sub>1-4 </sub>alkyl-, C<sub>1-4 </sub>alkoxy- or aryl group, is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.</p>
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PROCESS FOR THE PRODUCTION OF N-SUBSTITUTED 2-(ACETYLAMINO)-N'-BENZYL-3-METHOXYPROPANAMIDES (Fri, 24 May 2013)
A process for the production of N-substituted 2-(acetylamino)-N'-benzyl-3-methoxypropanamides and subsequent treatment with acids is described. This process can be used for the production of (R)-Lacosamide.
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METHOD FOR IDENTIFYING A COMPOUND HAVING AN ANTIARRHYTHMIC EFFECT AS WELL AS USES RELATING THERETO (Fri, 17 May 2013)
<p id="p-0001" num="0000">The present invention relates to a method of identifying a compound having an antiarrhythmic effect and to a use of adenosine-diphospho-ribose cyclase (cardiac ADPRC) for the identification of a compound having said effect.</p>
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POLYSUBSTITUTED DERIVATIVES OF 2-HETEROARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 17 May 2013)
<p id="p-0001" num="0000">Compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.32mm" wi="66.97mm" file="US20130123288A1-20130516-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R, R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4 </sub>and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.</p>
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METHODS AND USES RELATING TO THE IDENTIFICATION OF COMPOUND ASSOCIATED WITH BACTERIAL INFECTION (Fri, 17 May 2013)
<p id="p-0001" num="0000">The present invention relates to a method of identifying a compound useful for the treating, reducing or preventing pathogenic infection caused by a microorganism and to the use of the PqsD protein or a functional fragment or variant thereof for the identification of a compound having said effect.</p>
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IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 10 May 2013)
<p id="p-0001" num="0000">The invention relates to compounds corresponding to formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.45mm" wi="63.33mm" file="US20130116250A1-20130509-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">in which <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000">R<sub>2 </sub>and R<sub>3 </sub>together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below:</li> </ul> </li> </ul> </li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="95.93mm" wi="50.72mm" file="US20130116250A1-20130509-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0004" num="0000">in which the wavy lines represent the phenyl nucleus to which R<sub>2 </sub>and R<sub>3 </sub>are attached.</p> <p id="p-0005" num="0000">Preparation process and therapeutic use.</p>
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INDOLIZINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 10 May 2013)
<p id="p-0001" num="0000">The invention relates to compounds corresponding to formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.45mm" wi="60.54mm" file="US20130116249A1-20130509-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">in which <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000">R<sub>3 </sub>and R<sub>4 </sub>together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below:</li> </ul> </li> </ul> </li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="89.66mm" wi="50.80mm" file="US20130116249A1-20130509-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0004" num="0000">in which the wavy lines represent the phenyl nucleus to which R<sub>3 </sub>and R<sub>4 </sub>are attached.</p> <p id="p-0005" num="0000">Preparation process and therapeutic use.</p>
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Animal Model Expressing Luciferase under Control of the Myelin Basic Protein Promoter (MBP-luci) and Use of the Model for Bioluminescence In Vivo Imaging (Fri, 10 May 2013)
<p id="p-0001" num="0000">A Myelin Basic Protein-luciferase bioimaging noninvasive model to visualize and quantify demyelination and remyelination events in the CNS at transcriptional level in vivo is provided. Luciferase-expressing transgenic animals were generated with myelin basic protein (MBP) promoter coupled to firefly luciferase reporter. The MBP-luci bioimaging model provides a means to monitor myelination status and the efficacy of a remyelination modulating test compound. An advantage of bioimaging is that a subject in a longitudinal study can serve as its own control. The same subject can be tracked over a demyelination and remyelination process continuously over a period of at least 10 weeks. This model enables normalization of individual animal imaging response and provides quality data with considerably reduced variance. In addition, because cohorts of animals need not be sacrificed at different time points, reduction in the number necessary for a compound efficacy study is possible.</p>
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(Fri, 03 May 2013)

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(Fri, 03 May 2013)

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6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS (Fri, 03 May 2013)
The present invention relates to 1 H-pyrazolo[3,4-b]pyridine compounds of the formula (I) in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are protein kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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Oxazolopyrimidines as Edg-1 receptor agonists (Thu, 25 Apr 2013)
The present invention relates to oxazolopyrimidine compounds of the formula I, in which A, R 1 , R 2 and R 3 are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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Method of synthesis of ferroquine by convergent reductive amination (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">The invention relates to a method of synthesis of ferroquine of formula (F) or of its metabolite of formula (Fm):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="84.16mm" wi="46.91mm" file="US08497375-20130730-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">comprising a reaction of reductive amination, said reaction comprising:</li> <li id="ul0002-0002" num="0000">(i) a stage of condensation of an aldehyde-amino ferrocene of formula (III), in which R represents a hydrogen atom or a methyl group, with 7-chloroquinolin-4-amine as shown below,</li> </ul> </li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="38.18mm" wi="67.82mm" file="US08497375-20130730-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000"> <ul id="ul0004" list-style="none"> <li id="ul0004-0001" num="0000">followed by</li> <li id="ul0004-0002" num="0000">(ii) a stage of reduction of the product of condensation obtained in the preceding stage and</li> <li id="ul0004-0003" num="0000">(iii) then a stage of hydrolysis of the reaction mixture in the presence of an aqueous solution of ammonia or of citric acid.</li> </ul> </li> </ul> </p>
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3,4-DIHYDROPYRROLO[1,2-A]PYRAZINE-2,8(1H)-DICARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 12 Apr 2013)
<p id="p-0001" num="0000">Compounds corresponding to the general formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.79mm" wi="60.62mm" file="US20130090340A1-20130411-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein R<sub>2 </sub>represents a group C<sub>1-10</sub>-alkyl, C<sub>3-10</sub>-cycloalkyl, C<sub>3-7</sub>-cycloalkyl-C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-alkyl-C<sub>3-7</sub>-cycloalkyl, C<sub>3-7</sub>-cycloalkyl-C<sub>3-7</sub>-cycloalkyl, C<sub>1-6</sub>- alkylthio-C-<sub>1-10</sub>-alkyl, C<sub>1-6</sub>-alkoxy-C<sub>1-10</sub>-alkyl, hydroxy-C<sub>1-10</sub>-alkyl, hydroxy-C<sub>1-6</sub>-alkyl-C<sub>3-7</sub>-cycloalkyl-C<sub>1-6</sub>-alkyl, hydroxy-C<sub>3-10</sub>-cycloalkyl, C<sub>1-10</sub>-fluoroalkyl or C<sub>3-10</sub>- fluorocycloalkyl; an optionally substituted heterocyclic group; a group C<sub>1-10</sub>-alkyl substituted with an optionally substituted heterocyclic group; X<sub>6 </sub>represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C<sub>1-6</sub>-alkyl, C<sub>3-7</sub>-cycloalkyl, C<sub>3-7</sub>-cycloalkyl-C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-fluoroalkyl or cyano; and R<sub>7 </sub>represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, <br/> in the form of the base or of an acid-addition salt, and the therapeutic use thereof. </li> </ul> </li> </ul> </p>
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PROCESS OF PREPARATION OF L-IDURONIC ACID AND DERIVATIVES COMPRISING A DECARBOXYLATION/INTRAMOLECULAR CYCLISATION TANDEM REACTION (Fri, 12 Apr 2013)
The present invention relates to a process of preparation of L-iduronic acid and derivatives comprising a decarboxylation/intramolecular cyclisation tandem reaction. The present invention also relates to the intermediates of the process, as well as their use as intermediates in the preparation of Idraparinux.
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Process of preparation of L-iduronic acid comprising a decarboxylation/intramolecular cyclisation tandem reaction (Thu, 11 Apr 2013)
The present invention relates to a process of preparation of L-iduronic acid and derivatives comprising a decarboxylation/intramolecular cyclisation tandem reaction. The present invention also relates to the intermediates of the process, as well as their use as intermediates in the preparation of Idraparinux.
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6-(4-hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors (Fri, 05 Apr 2013)
<p id="p-0001" num="0000">The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.70mm" wi="59.35mm" file="US08686150-20140401-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6 </sup>and R<sup>7 </sup>are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them. </p>
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6-(4-HYDROXY-PHENYL)-3-ALKYL-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS (Fri, 05 Apr 2013)
The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula (I), in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula (I) are protein kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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PYRAZOLOQUINOLINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 05 Apr 2013)
The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.
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PYRAZOLOQUINOLINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 29 Mar 2013)
<p id="p-0001" num="0000">The invention relates to compounds corresponding to formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.13mm" wi="56.56mm" file="US20130079337A1-20130328-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which R1, R2 and R3 are as defined in Claim <b>1</b>, and also to the process for preparing them and to their therapeutic use.</p>
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CARBOXYLIC ACID DERIVATIVES HAVING A 2,5-SUBSTITUTED OXAZOLOPYRIMIDINE RING (Fri, 29 Mar 2013)
<p id="p-0001" num="0000">The present invention relates to oxazolopyrimidine compounds of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="15.75mm" wi="66.97mm" file="US20130079358A1-20130328-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which A, R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>and X are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.</p>
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CARBOXYLIC ACID DERIVATIVES HAVING A 2,5,7-SUBSTITUTED OXAZOLOPYRIMIDINE RING (Fri, 29 Mar 2013)
<p id="p-0001" num="0000">The invention relates to oxazolopyrimidine compounds of formula (I), where A, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and X are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.89mm" wi="67.99mm" file="US20130079357A1-20130328-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS (Fri, 29 Mar 2013)
The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]- sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
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N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS (Fri, 29 Mar 2013)
The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
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Pyrazoloquinolinone derivatives, preparation thereof and therapeutic use thereof (Thu, 28 Mar 2013)
The invention relates to compounds corresponding to formula (I) in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.
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N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS (Fri, 22 Mar 2013)
<p id="p-0001" num="0000">The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.48mm" wi="64.43mm" file="US20130072493A1-20130321-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.</p>
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HETEROCYCLIC CARBOXYLIC ACID DERIVATIVES HAVING A 2,5-SUBSTITUTED OXAZOLOPYRIMIDINE RING (Fri, 22 Mar 2013)
<p id="p-0001" num="0000">Heterocyclic carboxylic acid derivatives comprising a 2,5-substituted oxazolopyrimidine ring as Edg-1 receptor agonists</p> <p id="p-0002" num="0000">The present invention relates to oxazolopyrimidine compounds of the formula I,</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.45mm" wi="73.49mm" file="US20130072502A1-20130321-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0004" num="0000">in which A, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, X and Y are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.</p>
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2,5-SUBSTITUTED OXAZOLOPYRIMIDINE DERIVATIVES (Fri, 22 Mar 2013)
<p id="p-0001" num="0000">The invention relates to oxazolopyrimidine compounds of formula I, where A, R<sup>1 </sup>and R<sup>2 </sup>are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="15.24mm" wi="56.98mm" file="US20130072501A1-20130321-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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INDANYL-SUBSTITUTED 4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[4,3-C]PYRIDINES, THEIR USE AS MEDICAMENT, AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM (Fri, 22 Mar 2013)
The invention relates to substituted 4,5,6,7-tetrahydro-1 H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
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6-(4-HYDROXY-PHENYL)-3-STYRYL-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS (Fri, 22 Mar 2013)
The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4 and R5 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS (Fri, 22 Mar 2013)
The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula (I), in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula (I) are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
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SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS (Fri, 22 Mar 2013)
The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1 ), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
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INDANYL-SUBSTITUTED 4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[4,3-C]PYRIDINES, THEIR USE AS MEDICAMENT, AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM (Fri, 22 Mar 2013)
The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula I act on the TASK-1 potassium channel. The compounds are suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
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N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals (Thu, 21 Mar 2013)
The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
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SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS (Fri, 15 Mar 2013)
<p id="p-0001" num="0000">The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.17mm" wi="63.25mm" file="US20130065859A1-20130314-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.</p>
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SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 15 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="62.82mm" wi="74.59mm" file="US20130065877A1-20130314-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.</p>
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6-(4-HYDROXY-PHENYL)-3-STYRYL-1H-PYRAZOLO[3,4-b]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS (Fri, 15 Mar 2013)
<p id="p-0001" num="0000">The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.03mm" wi="69.85mm" file="US20130065894A1-20130314-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.</p>
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SUBSTITUTED N-HETEROARYL BIPYRROLIDINE CARBOXAMIDES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 15 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.59mm" wi="69.93mm" file="US20130065923A1-20130314-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, Q<sub>1</sub>, Q<sub>2</sub>, Q<sub>3</sub>, Q<sub>4</sub>, X, m and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I) and intermediates therefor.</p>
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SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 15 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.92mm" wi="69.60mm" file="US20130065919A1-20130314-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R, R<sub>1</sub>, R<sub>2</sub>, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.</p>
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SUBSTITUTED N-PHENYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 08 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.72mm" wi="75.52mm" file="US20130059874A1-20130307-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-phenyl spirolactam bipyrrolidines of formula (I) and intermediates therefor.</p>
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SUBSTITUTED N-HETEROARYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 08 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.67mm" wi="73.41mm" file="US20130059863A1-20130307-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein R<sub>1</sub>, R<sub>2</sub>, Q<sub>1</sub>, Q<sub>2</sub>, Q<sub>3</sub>, Q<sub>4</sub>, X, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.</p>
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SUBSTITUTED N-HETEROCYCLOALKYL BIPYRROLIDINYLPHENYL AMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 08 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.79mm" wi="70.44mm" file="US20130059891A1-20130307-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R, R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.</p>
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Substituted N-heteroaryl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof (Fri, 08 Mar 2013)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.92mm" wi="69.60mm" file="US08623877-20140107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R, R<sub>1</sub>, R<sub>2</sub>, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor. </p>
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Oxygen-substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals (Fri, 22 Feb 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of the formula I, wherein A, D, E, G, R<sup>10</sup>, R<sup>30</sup>, R<sup>40</sup>, R<sup>50 </sup>and R<sup>60 </sup>have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.46mm" wi="60.03mm" file="US08664257-20140304-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TRICYCLIC PYRIDYL-VINYL PYRROLES AS PAR1 INHIBITORS (Fri, 15 Feb 2013)
<p id="p-0001" num="0000">This disclosure relates to compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.35mm" wi="62.48mm" file="US20130040943A1-20130214-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R1, R2, R3, R4, X and Y have the meanings denoted in the disclosure. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The disclosure further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.</p>
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Pyridylvinylpyrazoloquinolines as PAR1 inhibitors (Fri, 15 Feb 2013)
<p id="p-0001" num="0000">The disclosure relates to compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="45.13mm" wi="60.20mm" file="US20130040981A1-20130214-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.</p>
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals (Fri, 01 Feb 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.33mm" wi="69.93mm" file="US08445530-20130521-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, Y, Z, R<sup>3 </sup>to R<sup>6</sup>, R<sup>20 </sup>to R<sup>22 </sup>and R<sup>50 </sup>have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA<sub>1 </sub>receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them. </p>
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PROCESS FOR PREPARATION OF DRONEDARONE USING AMIDE INTERMEDIARY COMPOUND (Fri, 01 Feb 2013)
The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that the compound of formula (II) is reduced, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.
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3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 01 Feb 2013)
The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
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SUBSTITUTED 3 - (THIAZOLE - 4 - CARBONYL) - OR 3 - (THIAZOLE - 2 - CARBONYL) AMINOPROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 01 Feb 2013)
The present invention relates to compounds of the formulae (Ia) and (Ib), wherein G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae la and lb, their use and pharmaceutical compositions comprising them.
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REDUCTIVE AMINATION PROCESS FOR PREPARATION OF DRONEDARONE USING CARBOXYL INTERMEDIARY COMPOUND (Fri, 01 Feb 2013)
The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof : Formula (I) characterized in that a compound of formula (II) : Formula (II) is aminated with compound of formula (III) among reductive conditions, : Formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.
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Carboxylic acid derivatives having an oxazolo[5,4-b]pyridine ring (Fri, 25 Jan 2013)
<p id="p-0001" num="0000">The invention therefore relates to compounds of the formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.07mm" wi="73.58mm" file="US08580816-20131112-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which X, Y, R<sup>1</sup>, R<sup>2 </sup>and R<sup>3 </sup>have the given meanings. The compounds of the formula I are suitable, for example, for wound healing. </p>
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Process for preparing aminobenzofuran derivatives (Fri, 25 Jan 2013)
<p id="p-0001" num="0000">This disclosure relates to a process for preparing 5-aminobenzofuran derivatives of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.80mm" wi="69.85mm" file="US08686180-20140401-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which R<sub>1 </sub>and R<sub>2 </sub>are as defined in the description, <br/> by treating a 5-N-alkylamidobenzofuran derivative of general formula (II): </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="21.25mm" wi="75.86mm" file="US08686180-20140401-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which R<sub>1</sub>, R<sub>2</sub>, and R<sub>3 </sub>are as defined in the description, with a strong acid, so as to form an acid addition salt of the compound of formula (I), which salt is itself treated, if necessary, with a basic agent so as to form this compound of formula (I) in free base form. </p>
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CRYSTALLINE SOLVATES OF 6-(PIPERIDIN-4-YLOXY)-2H-ISOQUINOLIN-1-ONE HYDROCHLORIDE (Fri, 18 Jan 2013)
The present invention relates to crystalline solvates of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and the use thereof.
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SUBSTITUTED PHENYL COMPOUNDS (Fri, 18 Jan 2013)
The present invention relates to novel substituted phenyl compounds of the formula (VI) and to a process for making them. The compounds can be used as intermediates for making 6-substituted-1-(2H)-isoquinolinone derivatives.
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Polymorphs of 6-(piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride (Fri, 11 Jan 2013)
<p id="p-0001" num="0000">The present invention relates to new crystalline polymorphs of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and their use, in particular for the preparation of medicaments.</p>
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Pyridino-pyridinone derivatives, preparation and therapeutic use thereof (Fri, 04 Jan 2013)
<p id="p-0001" num="0000">The present invention relates to derivatives of pyridino-pyridinones, and to their preparation and use thereof, having activity as inhibitors of kinase activity of receptors for PDGF (platelet derived growth factors) ligands and optionally of receptors for the FLT3 (fms-like tyrosine kinase receptor) ligand receptors, said derivatives comprising compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.23mm" wi="74.08mm" file="US08623893-20140107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the various substituent groups are more specifically defined herein. The compounds are suitable as therapeutics for the treatment of various proliferative diseases. </p>
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Process for the preparation of dronedarone (Fri, 28 Dec 2012)
<p id="p-0001" num="0000">The subject of the present disclosure is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.66mm" wi="75.86mm" file="US08658809-20140225-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and the new intermediates of the preparation process. </p>
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Tetrahydroisoquinoline sulfonamide derivatives, the preparation thereof, and the use of the same in therapeutics (Fri, 21 Dec 2012)
<p id="p-0001" num="0000">The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.15mm" wi="63.33mm" file="US08524700-20130903-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R1, R2, n and B are as defined in the disclosure, their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness. </p>
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Substituted isoquinoline and isoquinolinone derivatives (Fri, 14 Dec 2012)
<p id="p-0001" num="0000">A method for the treatment or prevention in a mammal of a disease associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase comprising administering to the mammal in need thereof at least one compound of the formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="61.89mm" file="US08461144-20130611-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PROCESS FOR THE PREPARATION OF DEUTERATED COMPOUNDS CONTAINING N-ALKYL GROUPS (Fri, 30 Nov 2012)
The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.
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2-AMINO-3-(IMIDAZOL-2-YL)-PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS VEGF RECEPTOR KINASE INHIBITORS (Fri, 30 Nov 2012)
The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.
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ALKYL-HETEROCYCLE CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Thu, 29 Nov 2012)
The invention relates to compounds corresponding to the general formula (I) : in which R<sb>2</sb> represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C<sb>1-6</sb>-alkyl, C<sb>1-6</sb>-alkoxy or -NR<sb>8</sb>R<sb>9</sb>; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C<sb>1-6</sb>-alkylene or -O-C<sb>1-6</sb>-alkylene; R<sb>1</sb> represents a phenyl or a heterocycle which is optionally substituted; R<sb>3</sb> represents a hydrogen, fluorine, C<sb>1-6</sb>-alkyl or trifluoromethyl; R<sb>4</sb> represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4- (4- chlorophenyl) piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
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Process for the preparation of dronedarone (Fri, 16 Nov 2012)
<p id="p-0001" num="0000">The subject of the present invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.25mm" wi="75.52mm" file="US08501971-20130806-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and the new intermediates of the preparation process. </p>
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Spiro-oxindole MDM2 antagonists (Fri, 16 Nov 2012)
<p id="p-0001" num="0000">Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.</p>
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SPIRO-OXINDOLE MDM2 ANTAGONISTS (Fri, 16 Nov 2012)
Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
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NEW PROCESS FOR THE PREPARATION OF DRONEDARONE (Thu, 15 Nov 2012)
The subject of the present invention is a novel process for the preparation of <i>N-</i> [2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5- yl] methanesulfonamide of formula (I) and the new intermediates of the reparation process.
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Method and intermediates for the preparation of 2,2,2-trifluoro-N-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride (Fri, 09 Nov 2012)
<p id="p-0001" num="0000">The present invention is directed to a method for the preparation of 2,2,2-trifluoro-n-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride of the formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.56mm" wi="38.02mm" file="US08497379-20130730-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and reaction intermediates used in the method. </p>
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Derivatives of N-[(1<i>H</i>-pyrazol-1-yl)aryl]-1<i>H</i>-indole or 1<i>H</i>-indazole-3-carboxamide, preparation thereof and applications thereof in therapeutics (Fri, 02 Nov 2012)
<p id="p-0001" num="0000">The present invention relates to compounds corresponding to formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.74mm" wi="69.85mm" file="US08623862-20140107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">X represents a —CH— group or a nitrogen atom;</li> <li id="ul0002-0002" num="0000">R<sub>1 </sub>represents a (C<sub>1</sub>-C<sub>4</sub>)alkyl or a (C<sub>1</sub>-C<sub>4</sub>)alkoxy;</li> <li id="ul0002-0003" num="0000">R<sub>2 </sub>represents a group Alk;</li> <li id="ul0002-0004" num="0000">R<sub>5 </sub>represents a hydrogen atom, a halogen atom or a group Alk;</li> <li id="ul0002-0005" num="0000">R<sub>6 </sub>represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH<sub>2 </sub>group.</li> </ul> </li> </ul> </p>
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DERIVATIVES OF N- [(1H-PYRAZOL-1-YL) ARYL] - 1H - INDOLE OR 1H - INDAZOLE - 3 - CARBOXAMIDE, THEIR PREPARATION AND THEIR USE AS P2Y12 ANTAGONISTS (Fri, 02 Nov 2012)
The present invention relates to compounds corresponding to formula (I) and their use as P2Y12 antagonists for the treatment of cardiovascular diseases.
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METHOD OF TREATING LYMPHOMA USING PYRIDOPYRIMIDINONE INHIBITORS OF PI3K/MTOR (Fri, 02 Nov 2012)
The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of formula I.
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Pyrazole derivatives, preparation thereof, and therapeutic use thereof (Fri, 26 Oct 2012)
<p id="p-0001" num="0000">The invention relates to pyrazole derivatives of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.02mm" wi="73.49mm" file="US08367715-20130205-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which X represents chlorine or fluorine; to a process for preparing said derivatives, and to therapeutic uses of said derivatives. </p>
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Acetylene derivatives of 5-phenyl-pyrazolopyridine, preparation thereof, and therapeutic use thereof (Fri, 26 Oct 2012)
<p id="p-0001" num="0000">Compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.16mm" wi="72.47mm" file="US08546424-20131001-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which: <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">R1 and R2 represent, independently of one another, a hydrogen atom or a (C<sub>1</sub>-C<sub>6</sub>)alkyl group,</li> <li id="ul0001-0002" num="0000">R3 represents one or more hydrogen or halogen atoms,</li> <li id="ul0001-0003" num="0000">X represents from 1 to 4 substituents, identical to or different from one another, chosen from hydrogen, halogen or (C<sub>1</sub>-C<sub>6</sub>)alkyl,</li> <li id="ul0001-0004" num="0000">in the form of the base or of an addition salt with an acid.</li> </ul> </p> <p id="p-0003" num="0000">Therapeutic use and synthetic process.</p>
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Method for producing 2-(2-aminopyrimidin-4-yl)-1H-indole-5-carboxylic acid derivatives (Fri, 26 Oct 2012)
<p id="p-0001" num="0000">This disclosure relates to a novel process for obtaining a compound of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.56mm" wi="69.85mm" file="US08546567-20131001-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the values of R1, R2, and R3 and P are as described in the specification, and intermediates thereof. </p>
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N-(aminoheteroaryl)-1H-indole-2-carboxamide derivatives, preparation thereof and therapeutic use therof (Fri, 19 Oct 2012)
<p id="p-0001" num="0000">The invention relates to compounds of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.23mm" wi="69.85mm" file="US08481745-20130709-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> Wherein n, X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, X<sub>4</sub>, Y, Z<sub>1</sub>, Z<sub>2</sub>, Z<sub>3</sub>, Z<sub>4</sub>, Ra and Rb are as defined herein. The invention also relates to process for the preparation of compounds of formula (I) and their therapeutic use. </p>
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POLYSACCHARIDES COMPRISING TWO ANTITHROMBIN III-BINDING SITES, PREPARATION THEREOF AND USE THEREOF AS ANTITHROMBOTIC MEDICAMENTS (Fri, 19 Oct 2012)
The invention relates to sulphated polysaccharides which have the general structure of the constituent polysaccharides of heparin and which have a molecular weight of less than 8000 Daltons, comprising two antithrombin III-binding hexasaccharide sequences corresponding to formula (I) in which: R1 represents an OH group when the hexasaccharide of formula (I) is located at the reducing end of the polysaccharide, or else R1 represents a bond with another saccharide unit of said polysaccharide; R2 represents a hydrogen atom when the hexasaccharide of formula (I) is located at the non-reducing end of the polysaccharide, in which case the bond between carbon atoms 4 and 5 of the first saccharide unit of said hexasaccharide is a double bond, or else R2 represents a bond with another saccharide unit of said polysaccharide, in which case the bond between carbon atoms 4 and 5 of the first saccharide unit is a single bond. Preparation thereof, use thereof as antithrombotic medicaments, and also use thereof in a method for analysing a sample of a heparin derivative.
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Substituted piperidine spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof (Fri, 12 Oct 2012)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.14mm" wi="75.69mm" file="US08604046-20131210-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor are disclosed. </p>
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6-pyrimidinyl-pyrimid-4-one derivative (Fri, 05 Oct 2012)
<p id="p-0001" num="0000">A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.26mm" wi="72.81mm" file="US08518939-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease). </p>
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Bicyclic derivatives of azabicyclic carboxamides, preparation thereof and therapeutic use thereof (Fri, 05 Oct 2012)
<p id="p-0001" num="0000">The disclosure relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.13mm" wi="56.81mm" file="US08604050-20131210-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein X<sub>1</sub>, X<sub>2</sub>, X<sub>3</sub>, X<sub>4</sub>, Y, n, A, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof. </p>
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Substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals (Fri, 05 Oct 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.63mm" wi="60.88mm" file="US08669370-20140311-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, D, E, L, G, R<sup>10</sup>, R<sup>30</sup>, R<sup>40</sup>, R<sup>50 </sup>and R<sup>60 </sup>have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them. </p>
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BENZOIC ACID SALT OF OTAMIXABAN (Fri, 05 Oct 2012)
The invention relates to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino (imino) methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate, and to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4- yl)benzoyl]amino}butanoate which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
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PROCESS FOR PREPARATION OF DRONEDARONE BY N-BUTYLATION (Fri, 05 Oct 2012)
The invention relates to a novel process for preparation of dronedarone (I) and pharmaceutically acceptable salts thereof where the compound of formula (II) or salt thereof is reacted with a compound of formula L-(CH2)3-CH3 (III), where L is a leaving group, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.
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REDUCTIVE AMINATION PROCESS FOR PREPARATION OF DRONEDARONE USING AMINE INTERMEDIARY COMPOUND (Fri, 05 Oct 2012)
The invention relates to a novel process for preparation of drohedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) is reacted in the presence of a reductive agent with butyraldehyde and/or butanoic acid, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some hovel intermediary compounds and the preparation thereof.
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Conjugates of pyrrolo[1,4]benzodiazepine dimers as anticancer agents (Fri, 28 Sep 2012)
<p id="p-0001" num="0000">The present invention relates to pyrrolo[1,4]benzodiazepine (PBD) dimer conjugates, to the compositions comprising them and to their therapeutic application, in particular as anticancer agents. The invention also relates to the process for the preparation of the conjugates, to their application as anticancer agents and to the dimers themselves.</p>
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(Heterocycle/tetrahydropyridine)-(piperazinyl)-1-alcanone and (heterocycle/dihydropyrrolidine)-(piperazinyl)-1-alcanone derivatives, and use thereof as p75 inhibitors (Fri, 28 Sep 2012)
<p id="p-0001" num="0000">The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="17.36mm" wi="46.23mm" file="US08518947-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof. </p>
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Substituted adamantanes and their therapeutic application (Fri, 28 Sep 2012)
<p id="p-0001" num="0000">The present invention relates to tetrahydroquinoxaline urea derivatives of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.55mm" wi="75.35mm" file="US08530657-20130910-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as defined herein, and, to their preparation and to their therapeutic application. </p>
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(Heterocycle/condensed piperidine)-(piperazinyl)-1-alkanone or (heterocycle/condensed pyrrolidine)-(piperazinyl)-1-alkanone derivatives and use thereof as p75 inhibitors (Fri, 28 Sep 2012)
<p id="p-0001" num="0000">The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="11.26mm" wi="23.37mm" file="US08580790-20131112-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof. </p>
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Diphenyl-pyrazolopyridine derivatives, preparation thereof, and use thereof as nuclear receptor not modulators (Fri, 28 Sep 2012)
<p id="p-0001" num="0000">The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3.</p>
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Substituted tetrahydropyran spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof (Fri, 21 Sep 2012)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.97mm" wi="72.90mm" file="US08383814-20130226-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sub>1</sub>, R<sub>2</sub>, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed. </p>
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Derivatives of 7 alkynyl-1,8 naphthyridones, preparation method thereof and use of same in therapeutics (Fri, 21 Sep 2012)
<p id="p-0001" num="0000">The disclosure relates to method of treating a disease in which VEGFR-3 is involved, comprising administering a therapeutically effective amount of a compound of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.80mm" wi="58.34mm" file="US08586602-20131119-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, and R<sub>4 </sub>are as defined in the disclosure, to compositions containing them, to processes for preparing them, and to their use in therapeutics. </p>
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Cyclic (aza)indolizinecarboxamides, their preparation and their use as pharmaceuticals (Fri, 14 Sep 2012)
<p id="p-0001" num="0000">The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="70.27mm" wi="69.85mm" file="US08415336-20130409-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R, R<sup>a</sup>, R<sup>10</sup>, R<sup>20</sup>, R<sup>30</sup>, R<sup>40</sup>, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them. </p>
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Derivatives of (bridged piperazinyl)-1-alkanone and use thereof as p75 inhibitors (Fri, 14 Sep 2012)
<p id="p-0001" num="0000">The present invention relates to derivatives of ((phenyl)-3,6-dihydropyridin-1-yl)(bridged piperazinyl)-1-alkanone derivatives and ((phenyl)-2,5-dihydropyrrol-1-yl) (bridged piperazinyl)-1-alkanone corresponding to Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.32mm" wi="69.85mm" file="US08519143-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which the variables are as defined herein, to the preparation thereof and to the therapeutic use thereof. </p>
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Antibodies that specifically bind to the EphA2 receptor (Fri, 10 Aug 2012)
<p id="p-0001" num="0000">The present disclosure relates to an antibody or an epitope-binding fragment thereof that specifically binds to an EphA2 receptor. It further relates to a conjugate comprising a cytotoxic agent which is covalently bound to the antibody and a method for preparing such a conjugate.</p>
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SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 03 Aug 2012)
The present invention relates to compounds of the formula (I), wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
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AMINO-SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 03 Aug 2012)
Amino-substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula (I), wherein A, D, E, G, R10 R11, R30 R40 R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
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FGF RECEPTOR-ACTIVATING 3-O-ALKYL OLIGOSACCHARIDES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 03 Aug 2012)
The invention relates to the FGF receptor-activating oligosaccharides corresponding to formula (I) in which R1 represents an optionally substituted -O-alkyl group, R2 represents a hydroxyl group or an -O-alkyl group, R3, R5, R6, R7 and R8 represent -OSO3- or hydroxyl groups, R4 represents an NH-CO-alkyl or -O-alkyl group, R represents an -O-alkyl group, and n and m, which may be identical to or different from one another, represent integers equal to 0 or 1. Method for the preparation thereof and therapeutic use thereof.
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SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 03 Aug 2012)
The present invention relates to compounds of the formula (I), wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.</p>
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DISUBSTITUTED ]4-(5-AMINOMETHYL-PHENYL)-PIPERIDIN-1-YL]-1H-INDOL-3-YL]-METHANONES (Thu, 02 Aug 2012)
The present invention extends to the compound of formula I: or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed to the use of a compound of formula I as an inhibitor of tryptase, comprising introducing the compound into a composition comprising tryptase. In addition, the present invention is directed to the use of a compound of formula I for treating a patient suffering from, or subject to, a physiological condition in need of amelioration of an inhibitor of tryptase comprising administering to the patient a therapeutically effective amount of the compound of Claim 1. The present invention is directed also to the preparation of a compound of formula I.
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SUBSTITUTED DIHYDRO BENZOCYCLOALKYLOXYMETHYL OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF (Thu, 26 Jul 2012)
The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I) as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
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Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof (Fri, 20 Jul 2012)
<p id="p-0001" num="0000">The present invention is an improved method for the preparation of (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).</p>
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1H-pyrimidin-2-one derivatives, preparation thereof and pharmaceutical use thereof as inhibitors of AKT (PKB) phosphorylation (Fri, 06 Jul 2012)
<p id="p-0001" num="0000">The invention relates to the novel products of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.64mm" wi="50.97mm" file="US08507483-20130813-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">in which Z represents —O—, —NH or Nalk; n represents 0 to 4;</li> <li id="ul0001-0002" num="0000">R1 represents Hal, hydroxyl, alkyl or alkoxy; the alkyl and alkoxy radicals being optionally substituted;</li> <li id="ul0001-0003" num="0000">R2 and R3 represent H, Hal or alkyl optionally substituted with one or more halogen atoms;</li> <li id="ul0001-0004" num="0000">R4 represents H;</li> <li id="ul0001-0005" num="0000">these products being in all the isomer forms and the salts, as medicaments, in particular as inhibitors of AKT(PKB) phosphorylation.</li> </ul> </p>
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Tricyclic N-heteroaryl-carboxamide derivatives, preparation and therapeutic use thereof (Fri, 29 Jun 2012)
<p id="p-0001" num="0000">The invention relates to tricyclic N-heteroaryl-carboxamide derivatives having the formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.59mm" wi="64.43mm" file="US08420817-20130416-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> Wherein A, P, W, Z<sub>1</sub>, Z<sub>2</sub>, Z<sub>3</sub>, Z<sub>4</sub>, Z<sub>5</sub>, Z<sub>6</sub>, Z<sub>7</sub>, Z<sub>8</sub>, R<sub>3 </sub>and R<sub>3</sub>′ are as described herein. The invention also relates to a method for preparing the same and to the therapeutic use thereof. </p>
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Tetrahydroquinoxaline urea derivatives as modulators of 11-B-hydroxysteroid dehydrogenase type I (Fri, 29 Jun 2012)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.14mm" wi="75.27mm" file="US08536173-20130917-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> where A, Ar<sub>1</sub>, Ar<sub>2</sub>, R<sub>1a</sub>, R<sub>1b</sub>, R<sub>1c</sub>, R<sub>2a</sub>, R<sub>2b</sub>, R<sub>2c</sub>, R<sub>3</sub>, R<sub>4 </sub>and R<sub>8 </sub>are as described herein, and pharmaceutical compositions thereof, methods of preparation thereof, and methods of use thereof. </p>
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Fumarate salts of a histamine H3 receptor antagonist (Fri, 15 Jun 2012)
<p id="p-0001" num="0000">The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof.</p>
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CYCLIC (AZA)INDOLIZINECARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS (Thu, 07 Jun 2012)
The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, (Ia) (Ib) wherein R, R<sp>a</sp>, R<sp>10</sp>, R<sp>20</sp>, R<sp>30</sp>, R<sp>40</sp>, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.
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Tetrahydroquinoxaline urea derivatives as modulators of 11β-hydroxysteroid dehydrogenase type 1 (Fri, 01 Jun 2012)
<p id="p-0001" num="0000">The invention relates to a compound of the general formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.14mm" wi="74.85mm" file="US08530473-20130910-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as defined herein which is useful in modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are useful for treating pathologies in which such modulation is beneficial, as in the case of metabolic syndrome or of noninsulin-dependent type 2 diabetes. The invention also relates to pharmaceutical preparations containing such a compound, processes for preparing and intermediates useful in the preparation of a such a compound. </p>
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7-aza-spiro[3.5]nonane-7-carboxylate derivatives, preparation thereof and therapeutic use thereof (Fri, 25 May 2012)
<p id="p-0001" num="0000">The invention relates to compounds of the general formula (I) where: R<sub>2 </sub>is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-alkoxy, or NR<sub>8</sub>R<sub>9 </sub>group; m, n, o and p independently are a number from 0 to 3, provided that m+n≦7 and that o+p≦7; A is a covalent bond, an oxygen atom, a C<sub>1-6</sub>-alkylene group or a —O—C<sub>1-6</sub>-alkylene group in which the end that is an oxygen atom is bonded to the R<sub>1 </sub>group and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R<sub>1 </sub>is an optionally substituted aryl or heteroaryl group; R<sub>3 </sub>is a hydrogen or fluorine atom or a C<sub>1-6</sub>-alkyl or trifluoromethyl group; R<sub>4 </sub>is an optionally substituted 5-membered heterocyclic compounds; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.11mm" wi="61.47mm" file="US08394787-20130312-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Substituted 1-alkylcinnolin-4(1<i>H</i>)-one derivatives, preparation thereof and therapeutic application of same (Fri, 25 May 2012)
<p id="p-0001" num="0000">The subject of the present invention is compounds corresponding to the formula (I) in which: X represents a divalent (C<sub>2</sub>-C<sub>5</sub>)alkylene radical which is unsubstituted or substituted one or more times by an Alk group; R<sub>1 </sub>represents a phenyl, a naphthyl, a pyridyl, a 1-benzothienyl or a 1,3-benzodioxolyl; R<sub>2 </sub>represents a hydrogen atom, a halogen atom, an Alk group, an OAlk group or else a group chosen from —S-Alk, —SO-Alk, —SO<sub>2</sub>-Alk, —CO—N(R<sub>4</sub>)-Alk, —N(R<sub>4</sub>)SO<sub>2</sub>-Alk, —N(R<sub>4</sub>)CO-Alk, —N(R<sub>4</sub>)SO<sub>2</sub>—N(Alk)<sub>2</sub>; R<sub>3 </sub>represents a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R<sub>4 </sub>represents a hydrogen atom or a (C<sub>1</sub>-C<sub>4</sub>)alkyl; Alk represents an unsubstituted or substituted (C<sub>1</sub>-C<sub>4</sub>)alkyl. Preparation process and therapeutic application.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.00mm" wi="69.85mm" file="US08420651-20130416-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUND ETHYL 8-OXO-9-[3-(1H-BENZIMIDAZOL-2-YLOXY)PHENYL]-4,5,6,7,8,9-HEXAHYDRO-2H-PYRROLO[3,4-B]QUINOLINE-3-CARBOXYLATE, SALT, CRYSTALLINE FORM, COCRYSTAL, FORMULATION, PROCESSES FOR PREPARATION, APPLICATION AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NEW USE PARTICULARLY AS INHIBITOR OF AURORA KINASES (Fri, 25 May 2012)
The invention relates more particularly to a new salt, cocrystal and formulations of ethyl 8-oxo-9-[3-(1H-benzimidazol-2-yloxy)phenyl]-4,5,6,7,8,9-hexahydro-2H- pyrrolo[3,4-b]quinoline-3-carboxylate of formula (F) to preparations thereof and to the use thereof therapeutically, particularly as selective inhibitors of Aurora A and B kinases, and for their use as anti-cancer agents.
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POLYMERIC CONJUGATES OF ACTIVE PRINCIPLES, THEIR PROCESS OF PREPARATION AND THEIR POLYMERIC INTERMEDIATES (Fri, 25 May 2012)
The present invention relates to novel conjugates of active principles grafted to a polymer, to the nanoparticles comprising them, to their preparation and to their polymeric intermediates.
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SPIRO-OXINDOLE MDM2 ANTAGONISTS (Sat, 19 May 2012)
Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
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Process for the preparation of 3-(6-amino-pyridin-3yl)-2-acrylic acid derivatives (Sat, 19 May 2012)
Process for the preparation of 3-(6-amino-pyridin-3yl)-2-acrylic acid derivatives The present invention relates to a process for the preparation of a compound of the formula (I), which comprises reacting a compound of the formula IV, (IV) with the compound of formula VII R15-A2-CHO and to novel intermediate compounds used therein.
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Tricyclic <i>N</i>-heteroaryl-carboxamide derivatives containing a benzimidazole unit, method for preparing same and their therapeutic use (Fri, 18 May 2012)
<p id="p-0001" num="0000">The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.40mm" wi="69.85mm" file="US08288376-20121016-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> Wherein A, P, Y, R<sub>1</sub>, R<sub>2 </sub>and R<sub>3 </sub>are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use. </p>
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Spiro-oxindole MDM2 antagonists (Fri, 18 May 2012)
<p id="p-0001" num="0000">Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.</p>
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1-pyrazolo[4,3-c]isoquinoline derivatives, preparation thereof and therapeutic use thereof (Fri, 11 May 2012)
<p id="p-0001" num="0000">The invention relates to a compound of formula (I), where: R<sub>1 </sub>is a phenyl group optionally substituted by one or more halogen atoms; R<sub>2 </sub>is: a hydrogen atom or a halogen atom or a cyano group; a —C(═O)Y group where Y is a hydrogen atom, or a —NH<sub>2 </sub>or —OR<sub>3 </sub>group; a —C(═S)NH<sub>2 </sub>group; a —C(═NH)NH—OH group; a —CH<sub>2</sub>OH or —CH<sub>2</sub>F group; a —CH═N—OH group; a —CH═CH<sub>2 </sub>or —C═C—R<sub>3 </sub>group; a H or H R<sub>1 </sub>group being a hydrogen or (C<sub>1</sub>-C<sub>4</sub>)alkyl group; R<sub>3 </sub>is a hydrogen atom or (C<sub>1</sub>-C<sub>4</sub>)alkyl group; and R<sub>4 </sub>is a —NH<sub>2</sub>, (C<sub>1</sub>-C<sub>4</sub>)alkyl, (C<sub>1</sub>-C<sub>4</sub>)fluoroalkyl or (C<sub>3</sub>-C<sub>7</sub>)cycloalkyl group.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="94.49mm" wi="61.98mm" file="US08461175-20130611-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Derivatives of 3-alkoxy-4,5-diarylthiophene-2-carboxamide, preparation thereof, and therapeutic use thereof (Fri, 11 May 2012)
<p id="p-0001" num="0000">The invention relates to compounds of the formula (I), where: R<sub>1 </sub>is: a —NR<sub>5</sub>R<sub>6 </sub>group; an unsubstituted or substituted phenyl; R<sub>2 </sub>is: a (C<sub>1</sub>-C<sub>4</sub>)alkyl; an —X—R<sub>7 </sub>group; R<sub>3 </sub>and R<sub>4 </sub>each are independently a substituted phenyl; R<sub>5 </sub>is a hydrogen atom or a (C<sub>1</sub>-C<sub>4</sub>)alkyl; R<sub>6 </sub>is an unsubstituted or substituted (C<sub>1</sub>-C<sub>4</sub>)alkyl; or R<sub>5 </sub>and R<sub>6 </sub>together with the nitrogen atom to which they are bonded constitute an unsubstituted or substituted heterocyclic compound; X is a (C<sub>1</sub>-C<sub>5</sub>)alkylene; R<sub>7 </sub>is an —OR<sub>8 </sub>group, a —NR<sub>9</sub>R<sub>10 </sub>group, an —SO<sub>2</sub>—(C<sub>1</sub>-C<sub>4</sub>)alkyl group; R<sub>8 </sub>is a hydrogen atom or a (C<sub>1</sub>-C<sub>4</sub>)alkyl; R<sub>9 </sub>is a hydrogen atom or a (C<sub>1</sub>-C<sub>4</sub>)alkyl; R<sub>10 </sub>is a hydrogen atom, a —COR<sub>11 </sub>group, an —SO<sub>2</sub>R<sub>11 </sub>group or a —CO(CH<sub>2</sub>)<sub>m</sub>OH group; R<sub>11 </sub>is an unsubstituted or substituted (C<sub>1</sub>-C<sub>4</sub>)alkyl; m is 1, 2 or 3. The invention also relates to methods for preparing same and to the therapeutic use thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="69.85mm" file="US08486971-20130716-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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2H or 3H-benzo[E]indazol-1-YL carbamate derivatives, the preparation and therapeutic use thereof (Fri, 04 May 2012)
<p id="p-0001" num="0000">Compounds corresponding to the formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.93mm" wi="57.07mm" file="US08258168-20120904-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them. </p>
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Acylated 1,6-anhydro decasaccharide and its use as an antithrombotic agent (Fri, 04 May 2012)
<p id="p-0001" num="0000">The instant invention relates to the decasaccharide of formula (I), wherein Ac represents an acetyl group:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="62.15mm" wi="76.20mm" file="US08501711-20130806-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent. </p>
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Sulfated heptasaccharide and its use as an antithrombotic agent (Fri, 04 May 2012)
<p id="p-0001" num="0000">The instant invention relates to the heptasaccharide of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="64.26mm" wi="76.20mm" file="US08518909-20130827-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent.</li> </ul> </li> </ul> </p>
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5, 6-bisaryl-2-pyridine-carboxamide derivatives, preparation and application thereof in therapeutics as urotensin II receptor antagonists (Fri, 04 May 2012)
<p id="p-0001" num="0000">The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.</p>
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Acylated decasaccharides and their use as antithrombotic agents (Fri, 04 May 2012)
<p id="p-0001" num="0000">The instant invention relates to decasaccharides of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="60.03mm" wi="76.20mm" file="US08546354-20131001-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein Ac represents an acetyl group and R represents a group of formula —OH or —OSO<sub>3</sub><sup>−</sup>, in their acid form or in the form of any one of their pharmaceutically acceptable salts, and to their process of preparation. The oligosaccharides of formula (I) are useful as antithrombotic agents.</li> </ul> </li> </ul> </p>
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PROCESS FOR THE PRODUCTION OF BENZOFURANS (Thu, 05 Apr 2012)
A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.
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Process for the production of dronedarone intermediates (Fri, 30 Mar 2012)
<p id="p-0001" num="0000">A process for the production of Dronedarone intermediates of the formula (I), by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-(4-methoxyphenyl)-ethanone, subsequent treatment of the ester with bases and a zeolite (alumosilicate) catalyst and optional subsequent demethylation. This process can be used for the production of Dronedarone.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="64.94mm" file="US08658808-20140225-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PROCESS FOR THE PREPARATION OF A COMPOUND USEFUL AS AN INHIBITOR OF TAFIA (Thu, 22 Mar 2012)
The present invention relates to a process for the preparation of a compound of the formula (I), which comprises reacting a compound of the formula (IV) with an oxalic acid diester and to novel intermediate compounds used therein.
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Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof (Fri, 16 Mar 2012)
<p id="p-0001" num="0000">The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.53mm" wi="67.73mm" file="US08252824-20120828-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R, R<sub>1</sub>, R<sub>2</sub>, R<sub>3 </sub>and R<sub>4 </sub>are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor. </p>
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Process for the production of benzofurans (Fri, 16 Mar 2012)
<p id="p-0001" num="0000">A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.</p>
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NOVEL ACYLATED DECASACCHARIDES AND THEIR USE AS ANTITHROMBOTIC AGENTS (Thu, 15 Mar 2012)
The instant invention relates to the decasaccharides of formula (I), wherein Ac represents an acetyl group and R represents a group of formula -OH or -OSO <sb>3 </sb>-, in their acid form or in the form of any one of their pharmaceutically acceptable salts, and to their process of preparation. The oligosaccharides of formula (I) are useful as antithrombotic agents.
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NOVEL SULFATED HEPTASACCHARIDE AND ITS USE AS ANTITHROMBOTIC AGENT (Thu, 15 Mar 2012)
The instant invention relates to the heptasaccharide of formula (I) : in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent.
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NOVEL SULFATED OCTASACCHARIDE AND ITS USE AS ANTITHROMBOTIC (Thu, 15 Mar 2012)
The instant invention relates to the octasaccharide of formula (I) in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent.
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NOVEL ACYLATED 1,6-ANHYDRO DECASACCHARIDE AND ITS USE AS ANTITHROMBOTIC AGENT (Thu, 15 Mar 2012)
The instant invention relates to the decasaccharide of Formula (I), wherein Ac represents an acetyl group: in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of Formula (I) is useful as an antithrombotic agent.
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Polysubstituted derivatives of 6-heteroarylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof (Fri, 02 Mar 2012)
<p id="p-0001" num="0000">Compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.05mm" wi="65.87mm" file="US08598166-20131203-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, Het and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof. </p>
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2-(cyclic amino)-pyrimidone derivatives as TPK1 inhibitors (Thu, 01 Mar 2012)
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R 2 represents a hydrogen or the like; R 3 represents methyl group or the like; R 20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R 4 represents hydrogen or the like; R 5 represents hydrogen or the like; R 6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH 2 , oxygen atom, NH, or the like; any one or more of R 5 and R 6 , R 5 and R 4 , R 6 and R 4 , X and R 5 , X and R 4 , X and R 6 , and R 3 and R 6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
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Derivatives of 5-pyridazinyl-1-azabicyclo[3.2.1]octane, preparation method thereof and use of same in therapeutics (Fri, 24 Feb 2012)
<p id="p-0001" num="0000">The invention relates to compounds having general formula (I), wherein R is as defined herein.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.99mm" wi="52.32mm" file="US08557819-20131015-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">The invention also relates to acid addition salt, a hydrate or a solvate of compounds of formula (I). The invention further relates to the method of preparing said compounds and to the use of same in therapeutics.</p>
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Thiadiazole and oxadiazole derivatives, preparation thereof and therapeutic use thereof (Fri, 17 Feb 2012)
<p id="p-0001" num="0000">The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.40mm" wi="74.51mm" file="US08546391-20131001-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PROCESS FOR THE PREPARATION OF ENANTIOMERIC FORMS OF 2,3-DIAMINOPROPIONIC ACID DERIVATIVES (Fri, 17 Feb 2012)
The invention relates to a process for the preparation of the enantiomeric forms of 2,3-diaminopropionic acid derivatives of formula (I), wherein R1, R2 and R3 are defined as in the claims, by racemate resolution. The separation of the racemate into its enantiomers takes place through formation of diastereomeric salts upon addition of an enantiomerically pure auxiliary, and subsequent separation by fractional crystallization.
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METHOD FOR IDENTIFYING A COMPOUND HAVING AN ANTIARRHYTHMIC EFFECT AS WELL AS USES RELATING THERETO (Fri, 03 Feb 2012)
The present invention relates to a method of identifying a compound having an antiarrhythmic effect and to a use of adenosine-diphospho-ribose cyclase (cardiac ADPRC) for the identification of a compound having said effect.
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METHODS AND USES RELATING TO THE IDENTIFICATION OF COMPOUND ASSOCIATED WITH BACTERIAL INFECTION (Fri, 03 Feb 2012)
The present invention relates to a method of identifying a compound useful for the treating, reducing or preventing a pathogenic infection caused by a microorganism and to the use of the PqsD protein or a functional fragment or variant thereof for the identification of a compound having said effect.
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CYCLIC PEPTIDES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF THE PLATELET ADHESION (Fri, 03 Feb 2012)
The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb),and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.
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ANTICANCER DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 03 Feb 2012)
The present invention relates to conjugales of pyrrolo[1,4]benzodiazepine (PBD) dimers, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing the conjugates and to their use as anticancer agents, and also to the dimers themselves. Formula (I) in which : represents a single bond or a double bond.
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ANTICANCER DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 03 Feb 2012)
The present invention relates to conjugales of pyrrolo[1,4]benzodiazepine (PBD) dimers, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing the conjugates and to their use as anticancer agents, and also to the dimers themselves. Formula (I) in which : represents a single bond or a double bond.</p>
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Methods and uses relating to the identification of compound associated with bacterial infection (Thu, 02 Feb 2012)
The present invention relates to a method of identifying a compound useful for the treating, reducing or preventing a pathogenic infection caused by a microorganism and to the use of the PqsD protein or a functional fragment or variant thereof for the identification of a compound having said effect.
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Method for identifying a compound having an antiarrhythmic effect as well as uses relating thereto (Thu, 02 Feb 2012)
The present invention relates to a method of identifying a compound having an antiarrhythmic effect and to a use of adenosine-diphospho-ribose cyclase (cardiac ADPRC) for the identification of a compound having said effect.
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DERIVATIVES OF OXADIAZOLE AND PYRIDAZINE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS (Fri, 27 Jan 2012)
The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a -CH- group; X1 represents a nitrogen atom or a -CH=CH- group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1 -C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a -(C3-C10)cycloalkyl- group; Y represents a -(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1 -C6)alkoxy group; Z1 is absent or represents an -NH- function; Z2 and Z3 are as defined in the description. The invention also relates to a process for preparing compounds of formula (I), compositions containing them and their application in therapeutics.
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NOVEL PROCESS FOR THE PREPARATION OF DRONEDARONE (Fri, 27 Jan 2012)
The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)- propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula (I), and pharmaceutically acceptable salts thereof characterized in that, the acyl group of the benzofuran derivative of the general formula (II), where R represents C 1-4 alkyl-, C1-4 alkoxy- or aryl group - is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.
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ARYLOXYALKYLENE-SUBSTITUTED HYDROXYPHENYLHEXYNOIC ACIDS, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS A MEDICAMENT (Fri, 27 Jan 2012)
The invention relates to aryloxy-alkylene substituted hydroxyphenyl hexynoic acid derivatives of formula (I) and to their physiologically compatible salts. The compounds are suitable for, for example, the treatment of diabetes, because they cause an increased insulin release by activating the GPR40 receptor.</p>
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NOVEL PROCESS FOR THE PREPARATION OF DRONEDARONE (Fri, 27 Jan 2012)
The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)- propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula (I), and pharmaceutically acceptable salts thereof characterized in that, the acyl group of the benzofuran derivative of the general formula (II), where R represents C 1-4 alkyl-, C1-4 alkoxy- or aryl group - is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.</p>
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DERIVATIVES OF OXADIAZOLE AND PYRIDAZINE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS (Fri, 27 Jan 2012)
The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a -CH- group; X1 represents a nitrogen atom or a -CH=CH- group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1 -C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a -(C3-C10)cycloalkyl- group; Y represents a -(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1 -C6)alkoxy group; Z1 is absent or represents an -NH- function; Z2 and Z3 are as defined in the description. The invention also relates to a process for preparing compounds of formula (I), compositions containing them and their application in therapeutics.</p>
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Spirocyclic nitriles as protease inhibitors (Fri, 20 Jan 2012)
<p id="p-0001" num="0000">The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.</p>
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6-cycloamino-3-(1<i>H</i>-pyrrolo[2,3-<i>b</i>]pyridin-4-yl)imidazo[1,2-<i>b</i>]pyridazine derivatives, preparation thereof and therapeutic use thereof (Fri, 13 Jan 2012)
<p id="p-0001" num="0000">The invention relates to 6-cycloamino-3-(1H-pyrrolo[2,3-b]pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to the general formula (I) in which R<sub>2 </sub>represents an aryl group optionally substituted with one or more halogen atoms or C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-alkyloxy, C<sub>1-6</sub>-alkylthio, C<sub>1-6</sub>-fluoroalkyl, C<sub>1-6</sub>-fluoroalkyloxy and —CN groups or R<sub>2 </sub>represents a group chosen from C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-fluoroalkyl, C<sub>3-7</sub>-cycloalkyl or C<sub>3-7</sub>-cycloalkyl-C<sub>1-6</sub>-alkyl groups; A represents a C<sub>1-7</sub>-alkylene group; B represents a C<sub>1-7</sub>-alkylene group; L represents either a nitrogen atom optionally substituted with an R<sub>c </sub>or R<sub>d </sub>group, or a carbon atom substituted with an R<sub>e1 </sub>group and an R<sub>d </sub>group or two R<sub>e2 </sub>groups; the carbon atoms of A and of B being optionally substituted with one or more R<sub>f </sub>groups, which may be identical to or different from one another. Preparation process and therapeutic use.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.66mm" wi="60.71mm" file="US08546395-20131001-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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INDOLIZINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 13 Jan 2012)
The invention relates to compounds corresponding to formula (I): N R1 O R3 R4 R2 (I) in which - R3 and R4 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: N N O O Ra Ra' N N O Rb Rb' N O Rc Rc'' Rc' (A) (B) (C) in which the wavy lines represent the phenyl nucleus to which R3 and R4 are attached. Preparation process and therapeutic use.
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IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 13 Jan 2012)
The invention relates to compounds corresponding to formula (I): R4 NN R1 O R2 R3 (I) 5 6 7 8 in which - R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: N N O O Ra Ra' N N O Rb Rb' N O Rc Rc'' Rc' (A) (B) (C) in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached. Preparation process and therapeutic use.
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COMBINATIONS OF KINASE INHIBITORS FOR THE TREATMENT OF CANCER (Fri, 13 Jan 2012)
The present invention provides methods of treating cancer by administering a compound of formula (I), optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with an inhibitor that targets HER2 and/or HER3.</p>
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SPIROCYCLICALLY SUBSTITUTED 1,3-PROPANE DIOXIDE DERIVATIVES, METHODS FOR THE PRODUCTION THEREOF AND USE OF THE SAME AS MEDICAMENT (Fri, 13 Jan 2012)
The invention relates to spirocyclically substituted 1,3-propane dioxide derivatives and to their physiologically compatible salts. The invention relates to compounds of formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, A and X have the given meanings, and to their physiologically compatible salts. The compounds are suitable for, for example, the treatment of diabetes.</p>
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IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 13 Jan 2012)
The invention relates to compounds corresponding to formula (I): R4 NN R1 O R2 R3 (I) 5 6 7 8 in which - R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: N N O O Ra Ra' N N O Rb Rb' N O Rc Rc'' Rc' (A) (B) (C) in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached. Preparation process and therapeutic use.</p>
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INDOLIZINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 13 Jan 2012)
The invention relates to compounds corresponding to formula (I): N R1 O R3 R4 R2 (I) in which - R3 and R4 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: N N O O Ra Ra' N N O Rb Rb' N O Rc Rc'' Rc' (A) (B) (C) in which the wavy lines represent the phenyl nucleus to which R3 and R4 are attached. Preparation process and therapeutic use.</p>
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Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments (Fri, 06 Jan 2012)
<p id="p-0001" num="0000">Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments</p> <p id="p-0002" num="0000">The invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof.</p> <p id="p-0003" num="0000">The invention relates to compounds of the formula I</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="50.46mm" wi="73.24mm" file="US08530413-20130910-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which R1, R2, R3, R4, R10, X, n, B<sub>1</sub>, B<sub>2</sub>, B<sub>3 </sub>and B<sub>4 </sub>are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes. </p>
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DERIVATIVES OF AZASPIRANYL-ALKYLCARBAMATES OF 5-MEMBER HETEROCYCLIC COMPOUNDS, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 30 Dec 2011)
<p id="p-0001" num="0000">The invention relates to a compound of the general formula (I) in which R<sub>2 </sub>is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-alkoxy, NR<sub>8</sub>R<sub>9 </sub>group; m, n, o and p are independently an integer equal to 0, 1, 2 or 3; A is a covalent bond or a C<sub>1-8</sub>-alkylene group; R<sub>1 </sub>is an optionally substituted aryl or heteroaryl group; R<sub>3 </sub>is a hydrogen or fluorine atom or a C<sub>1-6</sub>-alkyl group or a trifluoromethyl group; R<sub>4 </sub>is an optionally substituted 5-member heterocyclic compound; the compound being in the form of a base or acid addition salt. The invention also relates to the therapeutic use thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="17.78mm" wi="66.72mm" file="US20110319381A1-20111229-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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3,4-DIHYDROPYRROLO[1,2-A]PYRAZINE-2,8(1H)-DICARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 30 Dec 2011)
Compounds corresponding to the general formula (I) in which R2 represents a group C1-10-alkyl, C3-10- cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl- C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6- alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy- C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10- fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; Xe represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7- cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt. Therapeutic use.
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3,4-DIHYDROPYRROLO[1,2-A]PYRAZINE-2,8(1H)-DICARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 30 Dec 2011)
Compounds corresponding to the general formula (I) in which R2 represents a group C1-10-alkyl, C3-10- cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl- C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6- alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy- C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10- fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; Xe represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7- cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt. Therapeutic use.</p>
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2-ALKYL-6-CYCLOAMINO-3-(PYRIDIN-4-YL)IMIDAZO[1,2-B]-PYRIDAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF (Fri, 23 Dec 2011)
<p id="p-0001" num="0000">The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R<sub>2 </sub>is a C<sub>1-6</sub>-alkyl, C<sub>3-7</sub>-cycloalkyl, C<sub>3-7</sub>-cycloalkyl-C<sub>1-4</sub>-alkyl, C<sub>1-4</sub>-alkyloxy-C-M-alkyl, C<sub>3-7</sub>-cycloalkyloxy-C<sub>1-4</sub>-alkyl>C<sub>3-7</sub>-cycloalkyl-C<sub>1-4</sub>-alkyloxy-C<sub>1-4</sub>-alkyl, hydroxy-C<sub>1-6</sub>-alkyl, C<sub>1-4</sub>-fluoroalkyl group; R<sub>3 </sub>is a hydrogen atom or a substituent selected from halogen atoms and the C<sub>1-3 </sub>alkyl, —NR<sub>4</sub>R<sub>5</sub>, hydroxyl or C<sub>1-4 </sub>alkyloxy groups; A is a C<sub>1-7</sub>-alkylene group optionally substituted by one or two R<sub>a </sub>groups; B is a C<sub>1-7</sub>-alkylene group optionally substituted by one or two R<sub>b </sub>groups; L is either a nitrogen atom optionally substituted by an R<sub>c </sub>or R<sub>d </sub>group or a carbon atom substituted by an R<sub>e1 </sub>group and an R<sub>d </sub>group or by two R<sub>e2 </sub>groups; Rd is a group selected from a hydrogen atom or a C<sub>1-6</sub>-alkyl, C<sub>3-7</sub>-cycloalkyl, C<sub>3-7</sub>-cycloalkyl-C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-alkylthio-C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-alkyloxy-C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-fluoroalkyl, hydroxy-C<sub>1-6</sub>-alkyl group; R<sub>f </sub>is a C<sub>1-6</sub>-alkyl, C<sub>3-7</sub>-cycloalkyl, C<sub>3-7</sub>-cycloalkyl-C<sub>1-6</sub>-alkyl, C<sub>1-6</sub>-alkyloxy-C<sub>1-6</sub>-alkyl, C<sub>3-7</sub>-cycloalkyloxy-C<sub>1-4</sub>-alkyl, C<sub>3-7</sub>-cycloalkyl-C<sub>1-4</sub>-alkyloxy-C<sub>1-4</sub>-alkyl, hydroxy-C<sub>1-6</sub>-allyl, C<sub>1-6</sub>-fluoroalkyl or benzyl group. The invention also relates to a method for preparing same and to the therapeutic application thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.95mm" wi="43.35mm" file="US20110312934A1-20111222-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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SUBSTITUTED 3-BENZOFURANYL-INDOL-2-ONE-3-ACETAMIDIDOPIPERAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF (Fri, 23 Dec 2011)
<p id="p-0001" num="0000">The invention relates to disubstituted 3-benzofuranyl-indol-2-one-3-acetamidopiperazine derivatives of the general formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are such as defined in claim <b>1</b>, to a method for preparing same, and to the therapeutic use of said compounds.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.99mm" wi="69.85mm" file="US20110312972A1-20111222-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PROCESS FOR THE PREPARATION OF DRONEDARONE (Fri, 23 Dec 2011)
This invention relates to a process for the preparation of N-[2-n-butyl-3-{4-[(3- dibutylamino)-propoxy]-benzoyl} - 1-benzofuran-5-yl]-methane-sulfonamide of formula (I) and its pharmaceutically acceptable salts, according to one of the methylsulfonyl groups of the 2-n-butyl-3-[(di-n-butylamino-3-propoxy)-benzoyl]-5- bis-(methylsulfonamido)-benzofuran of formula (II) is selectively cleaved and if desired, the resulting compound of formula (I) is transformed into its salt.
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PROCESS FOR THE PREPARATION OF DRONEDARONE (Fri, 23 Dec 2011)
This invention relates to a process for the preparation of N-[2-n-butyl-3-{4-[(3- dibutylamino)-propoxy]-benzoyl} - 1-benzofuran-5-yl]-methane-sulfonamide of formula (I) and its pharmaceutically acceptable salts, according to one of the methylsulfonyl groups of the 2-n-butyl-3-[(di-n-butylamino-3-propoxy)-benzoyl]-5- bis-(methylsulfonamido)-benzofuran of formula (II) is selectively cleaved and if desired, the resulting compound of formula (I) is transformed into its salt.</p>
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MACROLACTONE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF FOR THE TREATMENT OF CANCER (Fri, 16 Dec 2011)
<p id="p-0001" num="0000">The present invention relates to the use of a compound of the formula (I), wherein X and Y independently of one another are OH, O—(C<sub>1</sub>-C<sub>6</sub>)-alkyl, NH<sub>2 </sub>or NH—(C<sub>1</sub>-C<sub>6</sub>)-alkyl, or X and Y together form a group —O— or wherein X and Y together form a further bond between the C atoms to which they are attached; R1 and R2 independently of one another are H, Cl or Br; R3 is H,(C<sub>1</sub>-C<sub>6</sub>)alkyl, C(═O)—(C<sub>1</sub>-C<sub>6</sub>)-alkyl or (C<sub>1</sub>-C<sub>6</sub>)-alkylene-NH—(C<sub>1</sub>-C<sub>6</sub>)-alkyl; R4 is H, (C<sub>1</sub>-C<sub>6</sub>)-alkyl or C(═O)—(C<sub>1</sub>-C<sub>6</sub>)-alkyl, and R5 is methyl or ethyl; or a physiologically tolerable salt of a compound of the formula (I), for the treatment and/or prophylaxis of cancer diseases, a pharmaceutical composition for the treatment and/or prophylaxis of cancer diseases comprising a compound of the formula (I), a compound of the formula (I) and a process for the preparation of the compound (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="70.70mm" wi="68.75mm" file="US20110306563A1-20111215-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Process for preparing prophyrin derivatives, such as protoprophyrin (IX) and synthesis intermediates (Fri, 16 Dec 2011)
<p id="p-0001" num="0000">The present invention relates to a process for preparing a porphyrin of formula (I), optionally in the form of a salt with an alkali metal and/or in the form of a metal complex:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="48.01mm" wi="67.56mm" file="US08420805-20130416-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which: <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">R and R′ are as defined in claim <b>1, </b></li> <li id="ul0002-0002" num="0000">comprising:</li> <li id="ul0002-0003" num="0000">a step of condensation, in an acidic medium, between a dipyrromethane of formula (II):</li> </ul> </li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="33.02mm" wi="69.17mm" file="US08420805-20130416-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which R′b is as defined above for (I), <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000"> <ul id="ul0004" list-style="none"> <li id="ul0004-0001" num="0000">and a dipyrromethane of formula (III):</li> </ul> </li> </ul> </p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00003" num="00003"> <img id="EMI-C00003" he="24.13mm" wi="61.55mm" file="US08420805-20130416-C00003.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which R″ is as defined in claim <b>1</b>, and also the compounds of formula (III). </p>
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Polysaccharides with antithrombotic activity, including a covalent bond and an amino chain (Fri, 16 Dec 2011)
<p id="p-0001" num="0000">The present invention relates to novel synthetic polysaccharides with antithrombotic activity, having at least one covalent bond with an amino chain, and to the preparation method thereof and to the therapeutic use thereof.</p>
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METHOD OF SYNTHESIS OF FERROQUINE BY CONVERGENT REDUCTIVE AMINATION (Fri, 16 Dec 2011)
The invention relates to a method of synthesis of ferroquine of formula (F) or of its metabolite of formula (Fm): comprising a reaction of reductive amination, said reaction comprising: (i) a stage of condensation of the aldhehyde-amino ferrocene of formula (1 ), which R represents a hydrogen atom or a methyl group, with the 7-chloroquinolin- amine of formula (2) as shown below, followed by (ii) a stage of reduction of the product of condensation obtained in the preceding stage (iii) then a stage of hydrolysis of the reaction mixture in the presence of an aqueous solution of ammonia or of citric acid.
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METHOD OF SYNTHESIS OF FERROQUINE BY CONVERGENT REDUCTIVE AMINATION (Fri, 16 Dec 2011)
The invention relates to a method of synthesis of ferroquine of formula (F) or of its metabolite of formula (Fm): comprising a reaction of reductive amination, said reaction comprising: (i) a stage of condensation of the aldhehyde-amino ferrocene of formula (1 ), which R represents a hydrogen atom or a methyl group, with the 7-chloroquinolin- amine of formula (2) as shown below, followed by (ii) a stage of reduction of the product of condensation obtained in the preceding stage (iii) then a stage of hydrolysis of the reaction mixture in the presence of an aqueous solution of ammonia or of citric acid.</p>
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DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 09 Dec 2011)
<p id="p-0001" num="0000">The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.88mm" wi="43.18mm" file="US20110301148A1-20111208-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH<sub>2</sub>, —CH(R′)—, —NH(R′)— or a heteroatom chosen from O and S, it being understood that R′ represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH<sub>2</sub>-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO<sub>2</sub>—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH<sub>2</sub>-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; or (ii) form, together with the nitrogen atom that bears them, a heterocycloalkyl group optionally substituted with one or more groups chosen from the groups —(C1-C5)alkyl and —CH<sub>2</sub>-aryl; W is a group —(C1-C5)alkylene, optionally substituted with one or more hydroxyl groups; R5 and R6, which may be identical or different, represent, independently of each other, a hydrogen atom or a group chosen from the groups —(C1-C5)alkyl and the groups —(C3-C6)cycloalkyl, and also the process for preparing them and the therapeutic uses thereof.</p>
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Derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics (Fri, 09 Dec 2011)
<p id="p-0001" num="0000">The disclosure relates to derivatives of morphine-6-glucuronide of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.16mm" wi="69.85mm" file="US08461122-20130611-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R1 is as defined in the disclosure, or an acid addition salt thereof, as well as in hydrate or solvate form. The disclosure also relates to the preparation method thereof and to the use of same in therapeutics. </p>
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HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 09 Dec 2011)
The invention relates to hexafluoroisopropyl carbamate derivatives of general formula (I): wherein R, Z, A, m and n as defined in the description, in the form of the base or of an addition salt with an acid. The compounds can be used as inhibitors of the enzyme MGL (monoacyl glycerol lipase).
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HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 09 Dec 2011)
The invention relates to hexafluoroisopropyl carbamate derivatives of general formula (I): wherein R, Z, A, m and n as defined in the description, in the form of the base or of an addition salt with an acid. The compounds can be used as inhibitors of the enzyme MGL (monoacyl glycerol lipase).</p>
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SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES (Fri, 02 Dec 2011)
<p id="p-0001" num="0000">A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.97mm" wi="63.50mm" file="US20110294786A1-20111201-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.</p>
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STREPTOSPIROLE DERIVATIVES (Fri, 02 Dec 2011)
<p id="p-0001" num="0000">The invention relates to streptospirole derivatives of the general formula (I), wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, X<sub>1</sub>, X<sub>2</sub>, Y<sub>1 </sub>and Y<sub>2 </sub>are as defined herein, a process for the preparation of said compounds by fermenting the microorganism <i>Streptomyces </i>sp. ST 108140 (DSM 19369) and optionally derivatizing the compounds produced by said microorganism, a pharmaceutical composition comprising at least one compound of the formula (I), and the use of a compound of the formula (I) for the preparation of a medicament for the treatment and/or prophylaxis of bacterial infections.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.99mm" wi="60.28mm" file="US20110295009A1-20111201-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Tropane urea derivatives, preparation thereof and therapeutic application thereof as modulators of the activity of 11betaHSD1 (Fri, 02 Dec 2011)
<p id="p-0001" num="0000">The invention relates to tropane urea derivatives of general formula (I) and to the application thereof as modulators of the activity of 11β-hydroxysteroid dehydrogenose type 1 (11βHSD1).</p>
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Derivatives of 2-pyridin-2-yl-pyrazol-3(2H)-one, preparation and therapeutic use thereof as HIF activators (Fri, 02 Dec 2011)
<p id="p-0001" num="0000">The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.</p>
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SUBSTITUTED N-HETEROARYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 18 Nov 2011)
The present invention discloses and claims a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of Formula (I). Wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of Formula (I) and intermediates therefor.
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SUBSTITUTED N-HETEROCYCLOALKYL BIPYRROLIDINYLPHENYL AMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 18 Nov 2011)
The present invention discloses and claims a series of substituted N- heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). (Formula (I)) Wherein R, R1, R2, R3, R4, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.
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SUBSTITUTED N-HETEROARYL BIPYRROLIDINE CARBOXAMIDES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 18 Nov 2011)
The present invention discloses and claims a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). Wherein R1 R2, R3, R4, Q1, Q2, Q3, Q4, X, m and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I) and intermediates therefor.
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SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 18 Nov 2011)
The present invention discloses and claims a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). Wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.
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SUBSTITUTED N-PHENYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 18 Nov 2011)
The present invention discloses and claims a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I). (Formula (I)) Wherein R1, R2, R3, R4, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
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SUBSTITUTED N-HETEROARYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 18 Nov 2011)
The present invention discloses and claims a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula ( Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
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SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 18 Nov 2011)
The present invention discloses and claims respectively a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (I) (Ia) and formula (Ib) as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
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Multivalent meningococcal derivatized polysaccharide-protein conjugates and vaccine (Thu, 17 Nov 2011)
The present invention describes derivatized polysaccharide-protein conjugates, a composition comprising one or more of such derivatized polysaccharide-protein conjugates and methods of immunizing human patients with the same. The derivatized polysaccharide-protein conjugates are purified capsular polysaccharides from Neisseria meningitidis serogroups A, C, W-135, and Y, derivatized, chemically activated and selectively attached to a carrier protein by means of a covalent chemical bond, forming polysaccharide-protein conjugates capable of eliciting long-lasting immunity to a variety of N. meningitidis strains
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Cytotoxiv agents comprising new tomaymycin derivatives and their therapeutic use (Thu, 17 Nov 2011)
The present invention is related to new tomaymycin derivatives of formula (I), their process of preparation and their therapeutic uses.
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Synthesis of morphine-6-glucuronide or one of the derivatives thereof (Fri, 11 Nov 2011)
<p id="p-0001" num="0000">The disclosure relates to a method for preparing morphine-6-glucuronide or one of the deritives thereof comprising reacting a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.94mm" wi="71.54mm" file="US08258298-20120904-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sub>1 </sub>is as defined in the disclosure, <br/> with a glucuronic acid derivative of formula (II): </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="16.43mm" wi="56.56mm" file="US08258298-20120904-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein PG, X, and R<sub>4 </sub>are as defined in the disclosure, <br/> in the presence of an aromatic solvent and trimethylsilyl trifluoromethanesulfonate; <br/> (ii) reacting the product obtained in step (i) with a strong basic agent; and then (iii) recovering the product obtained in step (ii). </p>
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Bicyclic derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics (Fri, 11 Nov 2011)
<p id="p-0001" num="0000">The disclosure relates to compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.42mm" wi="71.63mm" file="US08440634-20130514-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R1, R2, and n are as defined in the disclosure, and addition salts solvates and hydrates thereof. The disclosure also relates to the preparation method of said compounds and to the use of the same in therapeutics. </p>
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Piperidinyl-substituted isoquinolone derivatives (Thu, 10 Nov 2011)
The invention relates to 6-piperidinyl-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I') useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
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NOVEL TRIAZOLO(4,3-A)PYRIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS (Fri, 28 Oct 2011)
<p id="p-0001" num="0000">The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.</p>
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NOVEL IMIDAZO[1,2-a]PYRIMIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS (Fri, 28 Oct 2011)
<p id="p-0001" num="0000">The disclosure concerns imidazo[1,2-a]pyrimidine derivatives of formula (I) and isomers and pharmaceutically acceptable salts thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.</p>
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MACROLACTONE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF FOR THE TREATMENT OF CANCER (Thu, 27 Oct 2011)
The present invention relates to the use of a compound of the formula (I), wherein X and Y independently of one another are OH, O-(C<sb>1</sb>-C<sb>6</sb>)-alkyl, NH<sb>2</sb> or NH-(C<sb>1</sb>-C<sb>6</sb>)-alkyl, or X and Y together form a group -O- or wherein X and Y together form a further bond between the C atoms to which they are attached; R1 and R2 independently of one another are H, Cl or Br; R3 is H, (C<sb>1</sb>-C<sb>6</sb>)-alkyl, C(=O)-(C<sb>1</sb>-C<sb>6</sb>)-alkyl or (C<sb>1</sb>-C<sb>6</sb>)-alkylene-NH-(C<sb>1</sb>-C<sb>6</sb>)-alkyl; R4 is H, (C<sb>1</sb>-C<sb>6</sb>)-alkyl or C(=O)-(C<sb>1</sb>-C<sb>6</sb>)-alkyl, and R5 is methyl or ethyl; or a physiologically tolerable salt of a compound of the formula (I), for the treatment and/or prophylaxis of cancer diseases, a pharmaceutical composition for the treatment and/or prophylaxis of cancer diseases comprising a compound of the formula (I), a compound of the formula (I) and a process for the preparation of the compound (I).
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NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS MET INHIBITORS (Fri, 21 Oct 2011)
<p id="p-0001" num="0000">The invention relates to the novel products of formula (I): in which: Ra is H, Hal, aryl or heteroaryl, which are optionally substituted; Rb is H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd is H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.</p>
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Substituted piperidine spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof (Fri, 21 Oct 2011)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.97mm" wi="75.69mm" file="US08227481-20120724-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor are disclosed. </p>
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INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF (Fri, 21 Oct 2011)
<p id="p-0001" num="0000">The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="97.03mm" wi="75.86mm" file="US20110257392A1-20111020-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein each symbol is as defined in the specification.</p> <p id="p-0004" num="0000">The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps:</p> <p id="p-0005" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="134.20mm" wi="75.86mm" file="US20110257392A1-20111020-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0006" num="0000">wherein each symbol is as defined in the specification.</p> <p id="p-0007" num="0000">According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4′]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.</p>
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INSULIN-SIRNA CONJUGATES (Fri, 21 Oct 2011)
This invention relates generally to therapeutic compounds and methods useful for treating disease in humans. Specifically, the present invention relates to methods and reagents useful for treating humans suffering from metabolic diseases. Specifically, the present invention relates to covalent conjugates of insulin and analogues with nucleic acid derivatives which are capable of modulating gene expression. Furthermore, this invention relates to the use of such conjugated insulins for the treatment of metabolic diseases, including diabetes mellitus.
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ANTINEOPLASTIC DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">The disclosure concerns heterobicyclic compounds of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as enantiomers, diastereoisomers and mixtures thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.</p>
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TREATMENT FOR GLOMERULONEPHRITIS WITH 2-[4-(7-ETHYL-5H-PYRROLO[2,3-B]PYRAZIN-6-YL)PHENYL]PROPAN-2-OL (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">A treatment for glomerulonephritis, and other renal dysfunctions using a compound of Formula I is disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.08mm" wi="66.29mm" file="US20110251219A1-20111013-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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CYCLOHEXYLAMIN ISOQUINOLONE DERIVATIVES (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.72mm" wi="69.85mm" file="US20110251226A1-20111013-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or isoquinoline derivatives of the formula (I′)</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="29.89mm" wi="69.85mm" file="US20110251226A1-20111013-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.</p>
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Substituted tetrahydropyran spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.97mm" wi="72.64mm" file="US08217052-20120710-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sub>1</sub>, R<sub>2</sub>, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed. </p>
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INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="85.77mm" wi="75.86mm" file="US20110251385A1-20111013-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein each symbol is as defined in the specification.</p> <p id="p-0004" num="0000">The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps:</p> <p id="p-0005" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="103.55mm" wi="75.86mm" file="US20110251385A1-20111013-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0006" num="0000">wherein each symbol is as defined in the specification.</p> <p id="p-0007" num="0000">According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4′]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.</p>
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ISOQUINOLINE DERIVATIVES (Fri, 07 Oct 2011)
<p id="p-0001" num="0000">The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="65.70mm" file="US20110245248A1-20111006-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.</p>
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Cytotoxic agents comprising new tomaymycin derivatives and their therapeutic use (Thu, 06 Oct 2011)
The present invention is related to new tomaymycin derivatives of the following formula, their process of preparation and their therapeutic uses. wherein M and L are as specified in the claims.
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DERIVATIVES OF HETEROARYL-ALKYLCARBAMATES, METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.80mm" wi="61.55mm" file="US20110237595A1-20110929-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A, n, R<sub>1</sub>, R<sub>7 </sub>and R<sub>8 </sub>are as defined herein.</p>
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Substituted pyrazoles, compositions containing these, method of production and use (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">The disclosure relates to a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.52mm" wi="69.85mm" file="US08410286-20130402-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and salts thereof; wherein Ar, L, A, X, R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>a, R<sub>4</sub>b, and R<sub>5 </sub>are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs. </p>
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Substituted pyrazoles, compositions containing these, method of production and use (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">The disclosure relates to a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.18mm" wi="69.85mm" file="US08420824-20130416-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and salts thereof; wherein Ar, L, A, X, R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>a, R<sub>4</sub>b, and R<sub>5 </sub>are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs. </p>
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Derivatives of aminoindanes, their preparation and their application in therapeutics (Thu, 29 Sep 2011)
The instant invention relates to derivatives of formula (I) and their application in therapeutics.
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CRYSTALLIZED FORM OF DRONEDARONE BASE (Fri, 23 Sep 2011)
<p id="p-0001" num="0000">The invention relates to a novel crystallized form of dronedarone base, to its process of preparation and to pharmaceutical compositions containing said novel crystallized form.</p>
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Process for the production of artemisinin intermediates (Fri, 23 Sep 2011)
<p id="p-0001" num="0000">This application relates to a process for the production of (2R)-dihydroartemisinic acid or (2R)-dihydroartemisinic acid esters from artemisinic acid or artemisinic acid esters, respectively, by diimine hydrogenation of the exocyclic CC-double bond, and use of said process in the production of the antimalarial drug artemisinin.</p>
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Cyclic pyridyl-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals (Fri, 16 Sep 2011)
<p id="p-0001" num="0000">The invention relates to cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity.</p> <p id="p-0002" num="0000">What is described are compounds of the formula I,</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.48mm" wi="75.69mm" file="US08344004-20130101-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system. </p>
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Short synthetic pathway for 1,6:2,3-dianhydro-β-D-mannopyranose (Fri, 16 Sep 2011)
<p id="p-0001" num="0000">The invention relates to a method for preparing 1,6:2,3-dianhydro-β-D-mannopyranose and is characterized in that it includes a step of cyclizing the compound B, where R is an activating agent, in the presence of a base selected from among ammonium hydroxides and mineral bases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.30mm" wi="52.92mm" file="US08461359-20130611-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Immunization method against neisseria meningitidis serogroups a and c (Thu, 15 Sep 2011)
The present invention describes methods of immunizing a patient with a combined vaccine that offers protection against meningococcal disease caused by pathogenic bacteria Neisseria meningitidis serogroups A and C. The vaccine comprises at least two distinct polysaccharide-protein conjugates that are formulated as a single dose of vaccine. The purified capsular polysaccharides of Neisseria meningitidis serogroups A and C are chemically activated and selectively attached to a carrier protein by means of a covalent chemical bond, forming polysaccharide-protein conjugates capable of eliciting long-lasting immunity to a variety of N. meningitidis strains in infants.
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DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS (Sat, 10 Sep 2011)
The instant invention relates to derivatives of formula (I) and their application in therapeutics.
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DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS (Sat, 10 Sep 2011)
The instant invention relates to derivatives of formula (I) and their application in therapeutics.</p>
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HEXADECASACCHARIDES WITH ANTITHROMBOTIC ACTIVITY, INCLUDING A COVALENT BOND AND AN AMINO CHAIN (Fri, 02 Sep 2011)
<p id="p-0001" num="0000">The present invention relates to novel synthetic hexadecasaccharides with antithrombotic activity, having at least one covalent bond with an amino chain, and to the preparation method thereof and to the therapeutic use thereof.</p>
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ALKYLTHIAZOL CARBAMATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 02 Sep 2011)
<p id="p-0001" num="0000">The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.</p>
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METHOD FOR PREPARING 1,6:2,3-DIANHYDRO-BETA-D-MANNOPYRANOSE (Fri, 02 Sep 2011)
<p id="p-0001" num="0000">The invention relates to a method for preparing 1,6:2,3-dianhydro-â-D-mannopyranose and is characterized in that it includes a step of cyclizing the compound C, where R is an alykyl group and R′ is an activating agent, in an alcohol/alcoholate mixture under anhydrous conditions.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.30mm" wi="64.09mm" file="US20110213141A1-20110901-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TREATMENT OF DERMATOLOGICAL ALLERGIC CONDITIONS (Fri, 02 Sep 2011)
A treatment for a dermatological allergic condition is disclosed, using a compound: as [4-(5-Aminomethyl-2-fluorophenyl)piperidine-1-yl][7-fluoro-1-(2-methoxyethyl)-4-trifluoromethoxy-1H-indol-3-yl]methanone.
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