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, R₁, R₂, R₃, R₄and 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">R₂and R₃together 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 R₂and R₃are 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">R₃and R₄together 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 R₃and R₄are 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="US20130096306A1-20130418-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="US20130096306A1-20130418-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 R₂represents a group C_1-10-alkyl, C_3-10-cycloalkyl, C_3-7-cycloalkyl-C_1-6-alkyl, C_1-6-alkyl-C_3-7-cycloalkyl, C_3-7-cycloalkyl-C_3-7-cycloalkyl, C_1-6- alkylthio-C-_1-10-alkyl, C_1-6-alkoxy-C_1-10-alkyl, hydroxy-C_1-10-alkyl, hydroxy-C_1-6-alkyl-C_3-7-cycloalkyl-C_1-6-alkyl, hydroxy-C_3-10-cycloalkyl, C_1-10-fluoroalkyl or C_3-10- fluorocycloalkyl; an optionally substituted heterocyclic group; a group C_1-10-alkyl substituted with an optionally substituted heterocyclic group; X₆represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C_1-6-alkyl, C_3-7-cycloalkyl, C_3-7-cycloalkyl-C_1-6-alkyl, C_1-6-fluoroalkyl or cyano; and R₇represents 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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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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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, 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, R¹, R², R³and 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, R¹, R², R³, R⁴and 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), (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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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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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, R¹, R², R³, 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, R¹and R²are 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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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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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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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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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 R₁, R₂, R₃, R₄, 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 R¹, R², R³, R⁴and R⁵are 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-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, 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 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-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 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 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-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="69.68mm" file="US20130059838A1-20130307-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">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 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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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 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 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-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 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 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-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, 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 disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.</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="US20130030008A1-20130131-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A, Y, Z, R³to R⁶, R²⁰to R²²and R⁵⁰have 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 LPA₁receptor, 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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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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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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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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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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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="US20130023677A1-20130124-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which R₁and R₂are as defined in the description, <br/> by treating a 5-N-alkylamidobenzofuran derivative of general formula (II): </p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="21.25mm" wi="75.86mm" file="US20130023677A1-20130124-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">in which R₁, R₂, and R₃are 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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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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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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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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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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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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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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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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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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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 R₁, R₂, 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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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^a, R¹⁰, R²⁰, R³⁰, R⁴⁰, 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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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.
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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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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, Z₁, Z₂, Z₃, Z₄, Z₅, Z₆, Z₇, Z₈, R₃and R₃′ 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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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: R₂is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C_1-6-alkyl, C_1-6-alkoxy, or NR₈R₉group; 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_1-6-alkylene group or a —O—C_1-6-alkylene group in which the end that is an oxygen atom is bonded to the R₁group and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R₁is an optionally substituted aryl or heteroaryl group; R₃is a hydrogen or fluorine atom or a C_1-6-alkyl or trifluoromethyl group; R₄is 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 (C₂-C₅)alkylene radical which is unsubstituted or substituted one or more times by an Alk group; R₁represents a phenyl, a naphthyl, a pyridyl, a 1-benzothienyl or a 1,3-benzodioxolyl; R₂represents a hydrogen atom, a halogen atom, an Alk group, an OAlk group or else a group chosen from —S-Alk, —SO-Alk, —SO₂-Alk, —CO—N(R₄)-Alk, —N(R₄)SO₂-Alk, —N(R₄)CO-Alk, —N(R₄)SO₂—N(Alk)₂; R₃represents a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R₄represents a hydrogen atom or a (C₁-C₄)alkyl; Alk represents an unsubstituted or substituted (C₁-C₄)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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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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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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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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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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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, R₁, R₂and R₃are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use. </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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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, R₁, R₂, R₃and R₄are 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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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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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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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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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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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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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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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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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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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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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 R₂is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C_1-6-alkyl, C_1-6-alkoxy, NR₈R₉group; m, n, o and p are independently an integer equal to 0, 1, 2 or 3; A is a covalent bond or a C_1-8-alkylene group; R₁is an optionally substituted aryl or heteroaryl group; R₃is a hydrogen or fluorine atom or a C_1-6-alkyl group or a trifluoromethyl group; R₄is 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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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: R₂is a C_1-6-alkyl, C_3-7-cycloalkyl, C_3-7-cycloalkyl-C_1-4-alkyl, C_1-4-alkyloxy-C-M-alkyl, C_3-7-cycloalkyloxy-C_1-4-alkyl>C_3-7-cycloalkyl-C_1-4-alkyloxy-C_1-4-alkyl, hydroxy-C_1-6-alkyl, C_1-4-fluoroalkyl group; R₃is a hydrogen atom or a substituent selected from halogen atoms and the C_1-3alkyl, —NR₄R₅, hydroxyl or C_1-4alkyloxy groups; A is a C_1-7-alkylene group optionally substituted by one or two R_agroups; B is a C_1-7-alkylene group optionally substituted by one or two R_bgroups; L is either a nitrogen atom optionally substituted by an R_cor R_dgroup or a carbon atom substituted by an R_e1group and an R_dgroup or by two R_e2groups; Rd is a group selected from a hydrogen atom or a C_1-6-alkyl, C_3-7-cycloalkyl, C_3-7-cycloalkyl-C_1-6-alkyl, C_1-6-alkylthio-C_1-6-alkyl, C_1-6-alkyloxy-C_1-6-alkyl, C_1-6-fluoroalkyl, hydroxy-C_1-6-alkyl group; R_fis a C_1-6-alkyl, C_3-7-cycloalkyl, C_3-7-cycloalkyl-C_1-6-alkyl, C_1-6-alkyloxy-C_1-6-alkyl, C_3-7-cycloalkyloxy-C_1-4-alkyl, C_3-7-cycloalkyl-C_1-4-alkyloxy-C_1-4-alkyl, hydroxy-C_1-6-allyl, C_1-6-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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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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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—(C₁-C₆)-alkyl, NH₂or NH—(C₁-C₆)-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,(C₁-C₆)alkyl, C(═O)—(C₁-C₆)-alkyl or (C₁-C₆)-alkylene-NH—(C₁-C₆)-alkyl; R4 is H, (C₁-C₆)-alkyl or C(═O)—(C₁-C₆)-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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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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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="US20110301107A1-20111208-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">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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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 —CH₂, —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, —CH₂-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) —SO₂—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, —CH₂-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 —CH₂-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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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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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 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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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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STREPTOSPIROLE DERIVATIVES (Fri, 02 Dec 2011)
<p id="p-0001" num="0000">The invention relates to streptospirole derivatives of the general formula (I), wherein R₁, R₂, R₃, X₁, X₂, Y₁and Y₂are 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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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 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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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-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-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-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 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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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 R₁is 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 R₄are 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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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 R₁, R₂, R₃, 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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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 R₁, R₂, 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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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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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, R₁, R₇and R₈are 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, R₁, R₂, R₃, R₄a, R₄b, and R₅are 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, R₁, R₂, R₃, R₄a, R₄b, and R₅are 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-BETA-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="US20110224446A1-20110915-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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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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Annelated pyrrolidin sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals (Fri, 26 Aug 2011)
<p id="p-0001" num="0000">The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), 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> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.21mm" wi="75.27mm" file="US08329725-20121211-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Biomolecules having multiple attachment moieties for binding to a substrate surface (Fri, 19 Aug 2011)
<p id="p-0001" num="0000">Compounds relating to attachment chemistries for binding biomolecules to a substrate surface are described. These include compounds of the following structure:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.21mm" wi="65.19mm" file="US08067581-20111129-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> The biomolecule includes a single nucleic acid, oligonucleotides, polynucleotides, DNAs, RNAs, proteins, peptides, enzymes, antibodies, CNAs (cyclohexyl nucleic acids), p-MeNAs (methyl or methoxy phosphate nucleic acids), peptide nucleic acids (PNAs), and pyranosyl RNAs (p-RNAs). </p>
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[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-flouro-1-(2-methoxy-ethyl)-4-trifluorom as an inhibitor of mast cell tryptase (Fri, 19 Aug 2011)
<p id="p-0001" num="0000">The present invention is directed to an indole benzylamine compound of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="50.21mm" wi="72.14mm" file="US08217178-20120710-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier. </p>
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Crystallized form of dronedarone base (Thu, 11 Aug 2011)
The invention relates to a novel crystallized form of dronedarone base, to its process of preparation and to the pharmaceutical compositions containing said novel crystallized form.
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SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES AS RHO KINASE INHIBITORS (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">The invention relates to substituted isoquinoline and isoquinolinones 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.</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="US20110190341A1-20110804-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BI- AND POLYCYCLIC SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">The invention relates to bi- and polycyclic substituted isoquinoline and isoquinolinones of the formula (I) wherein R₁to R₁₂are as defined in the application 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> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="69.85mm" file="US20110190340A1-20110804-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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6-substituted isoquinolines and isoquinolinones (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">The invention relates to 6-substituted isoquinoline and isoquinolinone 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.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="70.10mm" file="US08399482-20130319-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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OXAZOLOPYRIMIDINES AS EDG-1 RECEPTOR AGONISTS (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">The present invention relates to oxazolopyrimidine compounds of the formula I in which A, R¹, R²and R³are 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> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.98mm" wi="57.83mm" file="US20110190490A1-20110804-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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METHOD FOR PREPARING THE ETHYL ESTER OF 4-[TRANS-4-[(PHENYLMETHYL)-AMINO]CYCLOHEXYL]BENZOIC ACID AND THE HEMIFUMARATE SALT THEREOF (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">The present invention relates to the compound of formula (I) and to the use thereof as an intermediate for the synthesis of the compound of formula (A) or pharmaceutically acceptable salts thereof: formulae (II).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="86.44mm" wi="74.42mm" file="US20110190529A1-20110804-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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OXYGEN-SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 05 Aug 2011)
The present invention relates to compounds of the formula I, wherein A, D, E, 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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Multivalent meningococcal derivatized polysaccharide-protein conjugates and vaccine (Thu, 04 Aug 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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AZETIDINE POLYSUBSTITUTED COMPOUNDS, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF (Fri, 29 Jul 2011)
<p id="p-0001" num="0000">The invention relates to compounds of the formula (I) where: R is a (C₁-C₆)alkyl group, a halo(C₁-C₆)alkyl group; R1 is a hydrogen atom; R2 is a heterocyclic group bound by a carbon atom, a heterocyclic-(C₁-C₄)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; X is a hydrogen atom, a halogen, a cyano, a (C₁-C₆)alkyl group, a halo(C₁-C₆)alkyl group, a (C₁-C₆)alkoxy group, a halo(C₁-C₆)alkoxy group or a (C₁-C₆)alkylS(0)_pgroup; and p is 0 to 2. 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="25.57mm" wi="66.97mm" file="US20110183961A1-20110728-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Thiophene-2-carboxamide derivatives, preparation thereof and therapeutic use thereof (Fri, 29 Jul 2011)
<p id="p-0001" num="0000">The subject matter of the invention is compounds corresponding to formula (I), in which: R₁and R₂, together with the nitrogen atom to which they are attached, constitute a saturated heterocyclic radical containing from 4 to 7 atoms, which is preferably substituted; one of the two substituents R₃and R₆is a group Y-A-R₉; Y is an oxygen atom or an —S(O)_n′—, or —OSO₂group; A is an unsubstituted (C₁-C₄) alkylene group; R₉is an —OR₁₉, —CH₃, —NR₁₉R₂₀, —CONR₁₉R₂₀, —NR₁₅COR₁₉, —S(O)_nR₂₁, or —NR₁₃SO₂R₂₁group; —R₁₀is a hydrogen atom or a (C₁-C₄) alkyl group. The present invention also relates to the methods of preparation and the therapeutic uses of the compounds of formula (I).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.81mm" wi="62.74mm" file="US08410137-20130402-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Derivatives of pyrroloindole which are inhibitors of Hsp90, compositions containing same, and use thereof (Fri, 29 Jul 2011)
<p id="p-0001" num="0000">Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R′1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1, 2 and m=0, 1; R1 and/or R′1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments.</p>
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ALKYL-HETEROCYCLE CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 29 Jul 2011)
The invention relates to compounds corresponding to the general formula (I) : in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or -NR8R9; 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 C1-6-alkylene or -O-C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 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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AZACARBOLINE DERIVATIVES, PREPARATION METHOD THEREOF AND THERAPEUTIC USE OF SAME (Fri, 22 Jul 2011)
<p id="p-0001" num="0000">The invention relates to novel azacarbonlines having formula (I), wherein: R3, R4 represent independently H; hal; CF₃; substituted oxy, optionally substituted alkoxy; optionally substituted amino; substituted carbonyl; optionally substituted carboxyl; optionally substituted amide; sulphur, such as optionally substituted sulphones, sulphoxides or sulphides; linear, branched or cyclic C₁-C₁₀alkyl optionally comprising an optionally substituted heteroatom; optionally substituted linear, branched or cyclic C₂-C₇alkenyl; optionally substituted linear or branched C₂-C₆alkynyl; optionally substituted aryl or heteroaryl; of which may be optionally substituted; in the form of a base or an acid addition salt. The invention also relates to the use of same in therapeutics for the treatment of cancer and to synthesis methods.</p>
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Novel phenyl-substituted imidazolidines, process for preparation thereof, medicaments comprising said compounds and use thereof (Fri, 22 Jul 2011)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I) wherein the groups have stated meanings, and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.</p>
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TROPINONE BENZYLAMINES AS BETA-TRYPTASE INHIBITORS (Fri, 22 Jul 2011)
The present invention discloses and claims a series of substituted tropinone benzylamines of formula (I). More specifically, the compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted tropinone benzylamines.
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Multivalent meningococcal derivatized polysaccharide-protein conjugates and vaccine (Thu, 21 Jul 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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PLATINUM-N-HETEROCYCLIC CARBENE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 15 Jul 2011)
<p id="p-0001" num="0000">The invention relates to the platinum N-heterocycle derivatives of general formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.14mm" wi="51.73mm" file="US20110172199A1-20110714-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which—R₁and/or R₂are, independently of one another, an aryl or aralkyl group, each optionally substituted, a linear or branched C1-C6 alkyl group, a monocyclic C3-C7 cycloalkyl group or a linear or branched C2-C6 alkenyl group, or else R′ is a hydrogen atom and R is a group selected from the following groups: cycloalkyl or heterocycloalkyl, which is monocyclic or bicyclic and has from 3 to 8 carbon atoms, or benzyl, which is optionally substituted, or else R and R′ form, together with NH, a C3-C8 monocyclic or bicyclic heterocycloalkyl, V is a nitrogen atom or a C—R₄radical, R₃and/or R₄are hydrogen or a phenyl group or R₃and R₄may also together form a C3-C6 alkylene radical or a C3-C6 heteroalkylene radical with one or more nitrogenous heteroatoms, it being possible for the carbon atoms of the heteroalkylene radical to be modified in the form of a carbonyl radical, and X is iodine, bromine, chlorine or a nitrato (—ONO₂) group.</p>
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TETRAHYDROCARBOLINE DERIVATIVES AS EG5 INHIBITORS (Fri, 15 Jul 2011)
The present invention relates to substituted tetrahydro-β-carbolines and substituted tetrahydro-γ-carbolines. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are inhibitors of Eg5 kinesin. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of diseases.
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NEW PROCESS FOR THE PREPARATION OF DRONEDARONE (Fri, 15 Jul 2011)
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) and the new intermediates of the reparation process.
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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, 15 Jul 2011)
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.
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HSP90 inhibitory carbazole derivatives, compositions containing same and use thereof (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="176.70mm" wi="53.59mm" file="US08309721-20121113-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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SPIROPIPERIDINE BENZYLAMINES AS BETA-TRYPTASE INHIBITORS (Fri, 01 Jul 2011)
The present invention discloses and claims a series of substituted spiropiperidine benzylamines of formula (I) wherein R is as described herein. More specifically, the compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents for treating joint inflammation, including arthritis, rheumatoid arthritisand other arthritic condition such as rheumatoid spondylitis, gouty arthπtis, traumatic arthritis, rubella arthritis, psoriatic arthritis, osteoarthritis or other chronic inflammatory joint disease, or diseases of joint cartilage destruction, ocular conjunctivitis, vernal conjunctivitis, inflammatory bowel disease, asthma, allergic rhinitis, interstitial lung diseases, fibrosis, sceleroderma, pulmonary fibrosis, liver cirrhosis, myocardial fibrosis, neurofibromas, hypertrophic scars, various dermatological conditions, for example, atopic dermatitis and psoriasis, myocardial infarction, stroke, angina or other consequences of atherosclerotic plaque rupture, as well as periodontal disease, diabetic retinopathy, macular degeneration, acute macular degeneration, wet macular degeneration, tumour growth, anaphylaxis, multiple sclerosis, peptic ulcers, or a syncytial viral infection.
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INDOLYL-PIPERIDINYL BENZYLAMINES AS BETA-TRYPTASE INHIBITORS (Fri, 01 Jul 2011)
The present invention discloses and claims a series of substituted indolyl-piperidinyl benzylamines of formula (I), wherein R1, R2 and R3 are as described herein. More specifically, the compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted indolyl-piperidinyl benzylamines. In one of the embodiments, there is provided the compounds of formula (I) wherein R3 is (II).
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PRODRUGS OF [4[4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL)-METHANONES AND SYNTHESIS THEREOF (Fri, 01 Jul 2011)
The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase including but not limited to for example asthma and other inflammatory diseases including acute macular degeneration.
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TREATMENT FOR INFLAMMATORY BOWEL DISEASE (Fri, 01 Jul 2011)
A treatment for inflammatory bowel disease 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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[4[4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL)-METHANONES AND SYNTHESIS THEREOF (Fri, 01 Jul 2011)
The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase including but not limited to for example asthma and other inflammatory diseases including age-related macular degeneration.
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AZETIDINE POLYSUBSTITUTED COMPOUNDS, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF (Fri, 24 Jun 2011)
<p id="p-0001" num="0000">The invention relates to compounds of the formula (I) where: R is a (C₁-C₆)alkyl group, a halo(C₁-C₆)alkyl group; R1 is a hydrogen atom; R2 is a heteroaromatic group or a heteroaromatic(C₁-C₄)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; Y is a hydrogen atom, a halogen, a cyano, a (C₁-C₆)alkyl group, a halo(C₁-C₆)alkyl group, a (C₁-C₆)alkoxy group, a halo(C₁-C₆)alkoxy group or a (C₁-C₆)alkylS(O)_pgroup; and p is 0 to 2. Said compounds can be in the form_—of a base or a salt for addition to an acid. 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="29.13mm" wi="64.77mm" file="US20110152236A1-20110623-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals (Fri, 24 Jun 2011)
<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="24.05mm" wi="70.10mm" file="US08362073-20130129-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, Y, Z, R³to R⁶, R²⁰to R²²and R⁵⁰have 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 LPA₁receptor, 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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PYRROLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 24 Jun 2011)
<p id="p-0001" num="0000">The subject of the invention is compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.81mm" wi="63.16mm" file="US20110152320A1-20110623-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which R₁-R₁₀are as defined within, the method of preparation and therapeutic application as cannabinoid CB1 receptor antagonists.</p>
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AZAINDOLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 24 Jun 2011)
The disclosure relates generally to compounds that inhibit Pim kinases. Provided herein are N-substituted azaindoles, or pharmaceutically acceptable salts thereof, which are useful as selective inhibitors of Pim kinases. The disclosure also relates to pharmaceutical compositions comprising these compounds, processes for their preparation, and methods of using the same.
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Polysaccharides with antithrombotic activity comprising at least one covalent bond with biotin or a biotin derivative (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to novel synthetic polysaccharides with antithrombotic activity exhibiting at least one covalent bond with biotin or a biotin derivative and to a process employing avidin or streptavidin which makes it possible to neutralize these polysaccharides.</p>
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SUBSTITUTED ALKYL PYRIMIDIN-4-ONE DERIVATIVES (Fri, 17 Jun 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="30.06mm" wi="54.10mm" file="US20110144092A1-20110616-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein X, R1, R2, R3, R4, and m are defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.</p>
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Derivatives of (bridged piperazinyl)-1-alkanone and use thereof as p75 inhibitors (Fri, 17 Jun 2011)
<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="20.15mm" wi="69.85mm" file="US08193190-20120605-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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Substituted 1-benzyl-cinnolin-4(1<i>H</i>)-one derivatives, preparation thereof, and therapeutic use thereof (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention is related to novel substituted 1-benzylcinnolin-4(1H)-one derivatives having affinity for cannabinoid CB₂receptors, their preparation and their therapeutic application.</p>
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SUBSTITUTED PYRIMIDIN-4-ONE DERIVATIVES (Fri, 17 Jun 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="29.38mm" wi="61.04mm" file="US20110144132A1-20110616-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Y, R1, R2, R3, and R4 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.</p>
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Derivatives of 2-oxoalkyl-1-piperazin-2-one, preparation method thereof and therapeutic use of same (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to derivatives of 4-{2-[phenyl-3,6-dihydropyridin-1-yl]-2-oxoalkyl}-1-piperazin-2-one and 4-{2-[phenyl-2,5-dihydropyrrol-1-yl]-2-oxoalkyl}-1-piperazin-2-one having general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.94mm" wi="67.39mm" file="US08247404-20120821-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which A, B, m, R3 and n are as defined herein. The invention also relates to the preparation thereof and to the therapeutic use thereof. </p>
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Phenyl-alkyl piperazines having TNF-modulating activity, preparation method, and therapeutic use thereof (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to phenyl-alkyl piperazines of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.56mm" wi="73.74mm" file="US08153637-20120410-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which A, R1, R2 and R3 are as defined herein, having TNF-modulating activity. The invention also relates to the preparation thereof, pharmaceutical compositions thereof, and to the therapeutic use thereof. </p>
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Pyrrole derivatives, preparation of same and therapeutic application thereof (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The subject of the invention is Compound of Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.05mm" wi="61.64mm" file="US08383666-20130226-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which R1-R8 and R10 are defined within, its method of preparation, and its therapeutic application. </p>
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Pyrrolidinyl-alkyl-amide derivatives, their preparation, and their therapeutic application as CCR3 receptor ligands (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="86.70mm" wi="53.51mm" file="US08420636-20130416-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein the variables are as defined herein, to their preparation and to their therapeutic use as CCR3 receptor ligands. </p>
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NEW PROCESS FOR THE PREPARATION OF DRONEDARONE (Fri, 17 Jun 2011)
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) and the new intermediates of the preparation process.
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COMBINATION OF A NICOTINIC RECEPTOR PARTIAL AGONIST AND OF AN ACETYLCHOLINESTERASE INHIBITOR, PHARMACEUTICAL COMPOSITION CONTAINING SAME AND USE THEREOF IN THE TREATMENT OF COGNITIVE DISORDERS (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">The combination of an alpha-7 nicotinic receptor agonist and of an acetylcholinesterase inhibitor, pharmaceutical composition comprising the combination and the use thereof in the treatment of cognitive disorders.</p>
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Novel imidazo[1,5-a]pyridine derivatives, method for preparing same and pharmaceutical compositions containing same (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">The invention concerns compounds of formula I, a method for preparing said compounds, pharmaceutical compositions containing same and the theraprutic uses thereof.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.67mm" wi="69.85mm" file="US20110136856A1-20110609-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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FUMARATE SALT OF 4-BROMOPHENYL 1,4-DIAZABICYCLO[3.2.2]NONANE-4-CARBOXYLATE, CRYSTALLINE FORMS THEREOF, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 03 Jun 2011)
<p id="p-0001" num="0000">Fumarate salt of 4-bromophenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate, crystalline forms thereof, methods of preparation thereof, and therapeutic use thereof.</p>
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Pyridinopyridinone derivatives, preparation thereof and therapeutic use thereof (Fri, 27 May 2011)
<p id="p-0001" num="0000">The present invention relates to pyridopyridone derivatives of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.25mm" wi="75.01mm" file="US08436011-20130507-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which the variables are as defined herein, to their preparation and to their therapeutic use as inhibitors of the kinase activity of PDGF (platelet-derived growth factor) ligand receptors and possibly of FLT3 (fms-like tyrosine kinase receptor) ligand receptors. </p>
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Indol-2-one derivatives disubstituted in the 3-position, preparation thereof and therapeutic use thereof (Fri, 20 May 2011)
<p id="p-0001" num="0000">The present application discloses compounds of the formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.20mm" wi="69.85mm" file="US08202871-20120619-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and pharmaceutical compositions containing same and their use for treating and preventing various pathologies, including obesity, appetite disorders, excess weight and diabetes. </p>
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CARBAMOYLBENZOTRIAZOLE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES (Fri, 20 May 2011)
<p id="p-0001" num="0000">The invention relates to carbamoylbenzotriazole derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.31mm" wi="57.23mm" file="US20110118321A1-20110519-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Method for preparing azetidine derivatives (Fri, 20 May 2011)
<p id="p-0001" num="0000">This invention discloses and claims an industrial method for the production of azetidine derivatives, such as, N-(1-benzhydrylazetidin-3-yl)-N-phenylmethylsulphonamide.</p>
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STREPTOSPIROLE DERIVATIVES (Thu, 19 May 2011)
The invention relates to streptospirole derivatives of the general formula (I), wherein R<sb>1</sb>, R<sb>2</sb>, R<sb>3</sb>, X<sb>1</sb>, X<sb>2</sb>, Y<sb>1</sb> and Y<sb>2</sb> are as defined herein, a process for the preparation of said compounds by fermenting the microorganism <i>Streptomyces sp</i>. 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.
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Chlorothiophene-amides as inhibitors of coagulation factors Xa and thrombin (Fri, 13 May 2011)
<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="46.57mm" wi="70.19mm" file="US08378092-20130219-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. 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 preparations comprising them. </p>
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CHLOROTHIOPHENE-ISOXAZOLES AS INHIBITORS OF COAGULATION FACTORS XA AND THROMBIN (Fri, 13 May 2011)
<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="48.26mm" wi="69.85mm" file="US20110112074A1-20110512-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. 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 preparations comprising them.</p>
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Substituted imidazoline-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof (Fri, 13 May 2011)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.98mm" wi="63.84mm" file="US20110112097A1-20110512-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Aminoquinoline derivatives and their use as adenosine A3 ligands (Fri, 13 May 2011)
<p id="p-0001" num="0000">The present invention relates to an adenosine A₃receptor ligand of the general formula (I).</p>
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OXAZOLOPYRIMIDINES AS EDG-1 RECEPTOR AGONISTS (Thu, 12 May 2011)
The present invention relates to oxazolopyrimidine compounds of the formula I in which A, R<sp>1</sp>, R<sp>2</sp> and R<sp>3 </sp>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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ACYLAMINO-SUBSTITUTED CYCLIC CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS (Fri, 06 May 2011)
The present invention relates to compounds of the formula (I) wherein A, Y, Z, R20 to R22 and R50 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 LPA1 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.
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PHENYLOXADIAZOLE DERIVATIVES AS PGDS INHIBITORS (Fri, 15 Apr 2011)
This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
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2,3,6-trisubstituted-4-pyrimidone derivatives (Thu, 14 Apr 2011)
A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (1) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein Q represents CH or nitrogen atom; R represents a C 1 -C 12 alkyl group; the ring of: represents piperazine ring or piperidine ring.
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NEW MAYTANSINOIDS AND THE USE OF SAID MAYTANSINOIDS TO PREPARE CONJUGATES WITH AN ANTIBODY (Fri, 08 Apr 2011)
The invention relates to a compound of formula (I): wherein : • ALK is a (C1-C6)alkylene group; • X1 et X2 are each independently one of the following groups : -CH=CH-, -CO-, -CONR-, - NRCO-. -COO-. -OCO-. -OCONR-. -NRCOO-. -NRCONR'-. -NR-. -S(O)n (n=0,1 or 2) or O-; • R and R' are independently H or a (C1-C6)alkyl group; • I is an integer of from 1 to 40, preferably from 1 to 20, and more preferably from 1 to 10; • j is an integer corresponding to 1 when X2 is -CH=CH- and 2 when X2 is not -CH=CH-; • Zb is a simple bond, -O- or -NH- and Rb is H or a (C1-C6)alkyl, (C3-C7)cycloalkyl, aryl, heteroaryl or (C3-C7)heterocycloalkyl group; or Zb is a single bond and Rb is Hal. The invention relates to the use of said maytansinoids to prepare conjugates with an antibody having an affinity for tumor cells.
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ANTIBODIES THAT SPECIFICALLY BIND TO THE EPHA2 RECEPTOR (Fri, 08 Apr 2011)
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.
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2,3,6-trisubstituted-4-pyrimidone derivatives (Thu, 07 Apr 2011)
A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein Q represents CH or nitrogen atom; R represents a C 1 -C 12 alkyl group; the ring of: represents piperazine ring or piperidine ring.
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Substituted dihydro, trihydro and tetrahydro cycloalkyloxazolopyrimidinones, preparation and use thereof (Fri, 01 Apr 2011)
<p id="p-0001" num="0000">The present disclosure relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.38mm" wi="68.24mm" file="US08207181-20120626-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein p, n, A, B, X, Y, R₁, R₂, R₃, R₄, R₅, R₆, R₇and R₈are 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, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis. </p>
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DERIVATIVES OF 5-PYRIDINYL-1-AZABICYCLO[3.2.1]OCTANE, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS (Fri, 01 Apr 2011)
<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="31.92mm" wi="52.24mm" file="US20110077264A1-20110331-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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SYNTHESIS OF (4-FLUORO-3-PIPERIDIN-4-YL-BENZYL)-CARBAMIC ACID TERT-BUTYL ESTER AND INTERMEDIATES THEREOF (Fri, 01 Apr 2011)
The present invention is an improved method for the preparation of 4-fluoro-3-piperidin-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-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).
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Tetravalent meningococcal vaccine with enhanced immunogenicity (Thu, 31 Mar 2011)
The present invention is a method of enhancing immunogenicity against Neisseria meningitidis serogroups A, C, W-135, and Y.
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TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES AND TRIAZOLOPYRIMIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 25 Mar 2011)
<p id="p-0001" num="0000">The disclosure relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.42mm" wi="61.30mm" file="US20110071162A1-20110324-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein X, A, R₁and R₂are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.</p>
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TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 25 Mar 2011)
<p id="p-0001" num="0000">The invention relates to the triazolopyridine carboxamide derivatives of general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="45.30mm" wi="70.02mm" file="US20110071161A1-20110324-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">Wherein X, A, R₁and R₂are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.</p>
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1,3-dihydro-2<i>H</i>-pyrrolo[3,2-<i>b</i>pyridin-2-one derivatives, preparation thereof and therapeutic uses thereof (Fri, 25 Mar 2011)
<p id="p-0001" num="0000">The subject matter of the present invention are compounds corresponding to formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="56.64mm" wi="69.85mm" file="US08324214-20121204-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">in which: X is an unsubstituted or substituted divalent (C₁-C₅)alkylene radical; R_Iis an —NR₈R₉group; or an unsubstituted or substituted piperidin-3-yl or piperidin-4-yl radical; R₂is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R₃is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R₄is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group; and R₅is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group.</p>
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SUBSTITUTED DIHYDRO BENZOCYCLOALKYLOXYMETHYL OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF (Fri, 25 Mar 2011)
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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SUBSTITUTED PARA-BIPHENYLOXYMETHYL DIHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF (Fri, 25 Mar 2011)
The present invention relates to a series of substituted para-biphenyloxymethyl dihydro 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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SUBSTITUTED PHENOXYMETHYL DIHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF (Fri, 25 Mar 2011)
The present invention relates to a series of substituted phenoxymethyl dihydro oxazolopyrimidinones of formula (I) 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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Method for producing pyrazole glycoside derivatives (Thu, 24 Mar 2011)
A process for preparing pyrazole-glycoside derivatives of the general formula (I) in which the meanings are R1 H and R2 F; or R1 F and R2 H; or R1 F and R2 F; R3 (C 1 -C 8 )-alkyl, where one, more than one or all hydrogen(s) may be replaced by fluorine; X (C 1 -C 3 )-alkylene, (C 2 -G 3 )-alkenylone.
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Polysubstituted derivatives of 2-aryl-6-phenyl-imidazo[1,2-a]pyridines, and preparation and therapeutic use thereof (Fri, 18 Mar 2011)
<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="22.94mm" wi="69.85mm" file="US08148370-20120403-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R₁, R₂, R₃, R₄and 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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Polysubstituted derivatives of 6-heteroarylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof (Fri, 18 Mar 2011)
<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="24.47mm" wi="65.79mm" file="US08088765-20120103-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R₁, R₂, R₃, R₄, 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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Polysubstituted derivatives of 2-heteroaryl-6-phenylimidazo[1,2-<i>a</i>]pyridines, and preparation and therapeutic use thereof (Fri, 18 Mar 2011)
<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="US08338451-20121225-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R, R₁, R₂, R₃, R₄and 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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POLYSUBSTITUTED 2-ARYL-6-PHENYLIMIDAZO[1,2-A]PYRIDINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 18 Mar 2011)
<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="25.40mm" wi="69.85mm" file="US20110065745A1-20110317-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R, R₁, R₂, R₃, R₄, 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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PROCESS FOR THE PRODUCTION OF ARTEMISININ INTERMEDIATES (Fri, 18 Mar 2011)
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.
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3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, preparation thereof and therapeutic use thereof (Fri, 11 Mar 2011)
<p id="p-0001" num="0000">The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application.</p> <p id="p-0002" num="0000">The compounds of the present invention correspond to the formula (I):</p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="61.47mm" wi="70.19mm" file="US08362067-20130129-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which the variables are as set forth in the specification. </p> <p id="p-0004" num="0000">These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V_1areceptors and some compounds additionally exhibit a strong affinity for AVP V_1breceptors.</p>
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PYRAZOLE DERIVATIVES AND USE THEREOF AS OREXIN RECEPTOR ANTAGONISTS (Fri, 11 Mar 2011)
<p id="p-0001" num="0000">The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.</p>
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PHOTOCHEMICAL PROCESS FOR PRODUCING ARTEMISININ (Fri, 11 Mar 2011)
Provided is a new photochemical process for preparing artemisinin. Also provided are certain dihydroartemisinic acid derivatives useful for preparing artemisinin.
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Type 5 and type 8 capsular polysaccharides of overproducing <i>S. aureus </i>strains (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">The invention relates to the type 5 and type 8 capsular polysaccharides produced by overproducing <i>S. aureus </i>strains, and also to the immunogenic compositions and the vaccines comprising said capsular polysaccharides.</p>
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AZETIDINE-DERIVED COMPOUNDS, PREPARATION METHOD THEREFOR AND THERAPEUTIC USE OF SAME (Fri, 04 Mar 2011)
<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="25.57mm" wi="67.31mm" file="US20110053908A1-20110303-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R, R1, R2, R3, R4 and Y are as defined in the disclosure, or an acid addition salt thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.</p>
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Arylchalcogenoarylalkyl-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.98mm" wi="64.52mm" file="US20110053947A1-20110303-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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METHOD FOR PRODUCING PYRAZOLE GLYCOSIDE DERIVATIVES (Fri, 04 Mar 2011)
A process for preparing pyrazole-glycoside derivatives of the general Formula (I) in which the meanings are R1 H and R2 F; or R1 F and R2 H; or R1 F and R2 F; R3 (C1-C8)-alkyl, where one, more than one or all hydrogen(s) may be replaced by fluorine; X (C1-C3)-alkylene, (C2-C3)-alkenylene.
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Photochemical process for producing artemisinin (Thu, 03 Mar 2011)
Provided is a new photochemical process for preparing artemisinin. Also provided are certain dihydroartemisinic acid derivatives useful for preparing artemisinin.
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Heterocycle-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising them and use thereof (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.64mm" wi="63.84mm" file="US20110046105A1-20110224-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Arylchalcogenoarylalkyl-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">The invention relates to compounds of formula (I) wherein the groups R and R′ A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.56mm" wi="62.99mm" file="US20110046185A1-20110224-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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DISUBSTITUTED [4-(5-AMINOMETHYL-PHENYL)-PIPERIDIN-1-YL]-1H-INDOL-3-YL]-METHANONES (Fri, 25 Feb 2011)
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 ARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES (Fri, 18 Feb 2011)
<p id="p-0001" num="0000">The disclosure relates to a series pyrimidone derivatives 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="35.81mm" wi="63.67mm" file="US20110039835A1-20110217-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein: <br/> Y, Z, R1, R2, R3, R4, R5 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions. </p>
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Cyclic indole-3-carboxamides, their preparation and their use as pharmaceuticals (Fri, 18 Feb 2011)
<p id="p-0001" num="0000">The present invention relates to cyclic indole-3-carboxamides of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.58mm" wi="64.18mm" file="US08211885-20120703-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, R, R¹⁰, R²⁰, R³⁰, R⁴⁰, 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 formula I, their use and pharmaceutical compositions comprising them. </p>
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CYCLIC AZAINDOLE-3-CARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS (Fri, 18 Feb 2011)
<p id="p-0001" num="0000">The present invention relates to cyclic azaindole-3-carboxamides of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.58mm" wi="63.33mm" file="US20110039861A1-20110217-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A, R, R¹⁰, R²⁰, R³⁰, R⁴⁰, Y¹, Y², Y³, Y⁴, 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 formula I, their use and pharmaceutical compositions comprising them.</p>
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PYRIMIDONE DERIVATIVES USED AS TAU PROTEIN KINASE 1 INHIBITORS (Fri, 18 Feb 2011)
A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C-X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted,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).
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PROCESS FOR PREPARING 4-METHYL-3-THIENYLAMINE HYDROCHLORIDE (Fri, 18 Feb 2011)
This invention is related to a process for preparing 3-amino-4-methylthiophene hydrochloride.
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PROCESS FOR PREPARING 2-CHLORO-3N-(2-BENZIMIDAZOLYL)-4-METHYL-3-THIENYLAMINE USEFUL AS A SODIUM/PROTON EXCHANGER TYPE 3 INHIBITOR (Fri, 18 Feb 2011)
The present invention is related to an improved process for preparing 2-chloro-3N-(2-benzimidazolyl)-4-methyl-3-thienylamine as an NHE-3 inhibitor which is useful for treating respiratory disorders, disorders of the central nervous system, etc. (Formula I )
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PROCESS FOR PREPARING 2-ARYLAMINO OR HETEROARYLAMINO SUBSTITUTED BENZIMIDAZOLE COMPOUNDS (Fri, 18 Feb 2011)
The present invention is related to a process for preparing 2-arylamino or heteroarylamino substituted benzimidazole compounds.
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IMIDAZOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS (Fri, 11 Feb 2011)
<p id="p-0001" num="0000">The invention relates to novel compounds of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.82mm" wi="68.75mm" file="US20110034456A1-20110210-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">where R1, R2, R3, R4, R5, R6, R7, R8, R9, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.</p>
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Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments (Fri, 11 Feb 2011)
<p id="p-0001" num="0000">The invention relates to novel compounds of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.78mm" wi="66.46mm" file="US08198272-20120612-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> where X, A⁻, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament. </p>
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Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments (Fri, 11 Feb 2011)
<p id="p-0001" num="0000">The invention relates to novel compounds of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.67mm" wi="68.75mm" file="US08076336-20111213-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament. </p>
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SF5 DERIVATIVES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS (Fri, 11 Feb 2011)
<p id="p-0001" num="0000">The invention relates to novel compounds of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.23mm" wi="69.93mm" file="US20110034461A1-20110210-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.</p>
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Tetrahydroisoquinoline sulfonamide derivatives, the preparation thereof, and the use of the same in therapeutics (Fri, 04 Feb 2011)
<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="20.07mm" wi="62.15mm" file="US08273733-20120925-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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CYCLIC (AZA)INDOLIZINECARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS (Fri, 04 Feb 2011)
The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, (Ia) (Ib) wherein R, Ra, R10, R20, R30, R40, 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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INDAZOLECARBOXAMIDE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF MALARIA (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.</p>
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SUBSTITUTED TETRAHYDRO-2H-ISOQUINOLIN-1-ONE DERIVATIVES, AND METHODS FOR THE PRODUCTION AND USE THEREOF (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their physiologically tolerated salts, methods for the preparation of these compounds and their use as medicaments.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.06mm" wi="52.66mm" file="US20110021462A1-20110127-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">These compounds are poly(ADP-ribose) polymerase (PARP) inhibitors.</p>
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6-pyrimidinyl-pyrimid-4-one derivative (Fri, 28 Jan 2011)
<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="40.56mm" wi="72.81mm" file="US08198437-20120612-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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SUBSTITUTED ARYLAMIDE OXAZEPINOPYRIMIDONE DERIVATIVES (Fri, 21 Jan 2011)
<p id="p-0001" num="0000">The disclosure relates to a series pyrimidone derivatives 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="31.24mm" wi="64.01mm" file="US20110015177A1-20110120-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein: <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.</li> </ul> </p>
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SUBSTITUTED HETEROARYLAMIDE OXAZEPINOPYRIMIDONE DERIVATIVES (Fri, 21 Jan 2011)
<p id="p-0001" num="0000">The disclosure relates to a series pyrimidone derivatives 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="30.99mm" wi="63.75mm" file="US20110015176A1-20110120-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein: <br/> Y, Z, R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions. </p>
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SUBSTITUTED HETEROARYLAMIDE DIAZEPINOPYRIMIDONE DERIVATIVES (Fri, 21 Jan 2011)
<p id="p-0001" num="0000">The disclosure relates to a series pyrimidone derivatives 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="35.48mm" wi="63.67mm" file="US20110015187A1-20110120-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">wherein:</li> <li id="ul0001-0002" num="0000">Y, Z, R1, R2, R3, R4, R5 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.</li> </ul> </p>
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PROCESS FOR THE PREPARATION OF TRYPTASE INHIBITORS (Fri, 21 Jan 2011)
<p id="p-0001" num="0000">This invention is directed to processes for the preparation of a compound of the formula I or salt thereof,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.64mm" wi="75.18mm" file="US20110015400A1-20110120-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">that is useful as a tryptase inhibitor, to intermediates useful in the preparation of such a compound, to processes for the preparation of such intermediates, and to the use of such intermediates for the preparation of such a compound.</p>
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Derivatives of indole-2-carboxamides and of azaindole-2-carboxamides substituted with a silanyl group, preparation thereof and therapeutic use thereof (Fri, 14 Jan 2011)
<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="28.70mm" wi="65.36mm" file="US08399491-20130319-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein G₁, G₂, G₃, G₄, n, Y, Z, Z₁, Z₂, Z₃, and Z₄are 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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AZABICYCLIC CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 14 Jan 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="33.27mm" wi="64.26mm" file="US20110009364A1-20110113-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein X₁, X₂, X₃, X₄, Z₁, Z₂, Z₃, Z₄, Ra, Rb, n, Y, 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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Tetrahydroquinoxaline urea derivatives (Fri, 14 Jan 2011)
<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="32.26mm" wi="76.03mm" file="US08211892-20120703-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as disclosed herein, to their preparation and to their therapeutic application. </p>
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AZETIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY (Fri, 14 Jan 2011)
<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="28.28mm" wi="75.69mm" file="US20110009377A1-20110113-C00001.TIF" 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′, 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.</li> </ul> </li> </ul> </p>
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Bicyclic derivatives of azabicyclic carboxamides, preparation thereof and therapeutic use thereof (Fri, 14 Jan 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="28.79mm" wi="56.81mm" file="US08299114-20121030-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein X₁, X₂, X₃, X₄, 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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5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS UROTENSIN II RECEPTOR ANTAGONISTS (Fri, 14 Jan 2011)
<p id="p-0001" num="0000">The present 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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N-azabicyclic carboxamide derivatives, preparation thereof and therapeutic use thereof (Fri, 14 Jan 2011)
<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="28.70mm" wi="56.81mm" file="US08394820-20130312-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein X₁, X₂, X₃, X₄, n, Y, W, and A 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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AMINOQUINOLINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS (Fri, 14 Jan 2011)
<p id="p-0001" num="0000">The present invention relates to an adenosine A₃receptor ligand of the general formula (VI″), (VII″) and (VIII″) and their preparation.</p>
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LEPTOMYCIN DERIVATIVES (Fri, 07 Jan 2011)
<p id="p-0001" num="0000">Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion.</p>
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3-methyl-2- ( (2S) -2- (4- (3-methyl-L, 2, 4-oxadiazol-5-YL) phenyl) morpholino) -6- (pyrim-idin-4-yl) pyrimidin-4 (3H) -one as tau protein kinase inhibitor (Fri, 07 Jan 2011)
<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="40.56mm" wi="72.90mm" file="US08288383-20121016-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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EXTRACELLULAR ALLOSTERIC INHIBITOR BINDING DOMAIN FROM A TYROSINE KINASE RECEPTOR (Fri, 07 Jan 2011)
The present invention relates to an extracellular binding domain for an allosteric inhibitor, whereby said binding domain is derived from a single membrane span tyrosine kinase receptor. More specifically, the invention relates to an extracellular domain derived from a Fibroblast Growth Factor Receptor (FGFR). It further relates to the use of this domain for the identification of similar domains in the extracellular part of other tyrosine kinase receptors, and to a screening method for identification of a small compound allosteric inhibitor.
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Extracellular allosteric inhibitor binding domain from a tyrosine kinase receptor (Thu, 06 Jan 2011)
The present invention relates to an extracellular binding domain for an allosteric inhibitor, whereby said binding domain is derived from a single membrane span tyrosine kinase receptor. More specifically, the invention relates to an extracellular domain derived from a Fibroblast Growth Factor Receptor (FGFR). It further relates to the use of this domain for the identification of similar domains in the extracellular part of other tyrosine kinase receptors, and to a screening method for identification of an allosteric inhibitor.
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Method for the Production of Overproducing Staphylococcus Aureus Strains (Fri, 31 Dec 2010)
<p id="p-0001-en" num="0000">The present invention relates to a method for the production of an overproducing <i>Staphylococcus aureus </i>strain comprising: <ul id="ul0001-en" list-style="none"><li><ul id="ul0002-en" list-style="none"><li>(a) culturing a <i>Staphylococcus aureus </i>strain on a culture medium M1, M2 or M3,</li><li>(b) optionally, recovering the strains thus produced from the culture medium, <br/> and also to the use of said strains for the production of polysaccharides. </li></ul></li></ul></p>
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NOVEL FUMARATE SALTS OF A HISTAMINE H3 RECEPTOR ANTAGONIST (Thu, 30 Dec 2010)
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.
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UREA DERIVATIVES OF TROPANE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 24 Dec 2010)
<p id="p-0001-en" num="0000">The present invention is related to a compound of formula (I)</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="28.87mm" wi="65.79mm" file="US20100324084A1-20101223-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein R_1a, R_1b, R_1c, R_1d, R_2a, R_2b, R₃, R₄, p, r and <img id="custom-character-00001" he="2.46mm" wi="4.91mm" file="US20100324084A1-20101223-P00001.TIF" img-content="character" img-format="tif"/>Clipped Image are as defined herein, its preparation, pharmaceutical composition and use as a modulator of the activity of the 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1).</p>
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N-PHENYLIMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE COMPOUNDS, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 17 Dec 2010)
<p id="p-0001-en" num="0000">Compounds of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.52mm" wi="59.01mm" file="US20100317620A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">in which <br/> X, R₁, R₂, R₃, and R₄are as defined in the disclosure, or an acid addition salt thereof; and therapeutic uses thereof. </p>
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IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS (Fri, 17 Dec 2010)
<p id="p-0001-en" num="0000">Compounds of Formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="25.06mm" wi="40.39mm" file="US20100317656A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein X, Y, R₁, R₂, R₃, and R₄are as defined in the disclosure, or a acid addition salt thereof; and therapeutic use thereof.</p>
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N-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 17 Dec 2010)
<p id="p-0001-en" num="0000">Compounds of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.52mm" wi="59.52mm" file="US20100317673A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">in which: <ul id="ul0001-en" list-style="none"><li>X, R₁, R₂, R₃, and R₄are as defined in the disclosure, in the form of the base or of an addition salt with an acid; and therapeutic uses thereof.</li></ul></p>
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2-HETEROAROYLIMIDAZOL[1,2-a]PYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 17 Dec 2010)
<p id="p-0001-en" num="0000">Compounds of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.52mm" wi="56.81mm" file="US20100317688A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">in which: <br/> X, R₁, R₂, R₃, and R₄are as defined in the disclosure, or an acid addition salt thereof; an therapeutic use thereof. </p>
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2-BENZOYLIMIDAZO[1,2-a]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 17 Dec 2010)
<p id="p-0001-en" num="0000">Compounds of formula (I)</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.52mm" wi="56.73mm" file="US20100317687A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">in which: <br/> X, R₁, R₂, R₃, and R₄are as defined in the disclosure, or an acid addition salt thereof; and therapeutic use thereof. </p>
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N-HETEROCYCLIC-6-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF (Fri, 17 Dec 2010)
<p id="p-0001-en" num="0000">Compounds of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.52mm" wi="59.61mm" file="US20100317686A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">in which: <ul id="ul0001-en" list-style="none"><li>X, R₁, R₂, R₃and R₄are as defined in the disclosure, or an acid addition salt thereof; and therapeutic use thereof.</li></ul></p>
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N-PHENYL-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION (Fri, 17 Dec 2010)
<p id="p-0001-en" num="0000">Compounds of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.52mm" wi="59.61mm" file="US20100317685A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein: <ul id="ul0001-en" list-style="none"><li>X, R₁, R₂, R₃, and R₄are as defined in the disclosure, and therapeutic uses thereof.</li></ul></p>
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Cytotoxic agents comprising new tomaymycin derivatives and their therapeutic use (Fri, 17 Dec 2010)
<p id="p-0001" num="0000">The invention relates to novel tomaymicine derivatives comprising a linker. It also relates to the conjugate molecules that comprise one or more of said tomaymicine derivatives covalently linked to a cell binding agent through a linking group that is present on the linker of the tomaymycin derivative. It also relates to the preparation of the tomaymicine derivatives and of the conjugate molecules.</p>
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6-heterocyclic-imidazo[1,2-α]pyridine-2-carboxamide derivatives, preparation and therapeutic use thereof (Fri, 17 Dec 2010)
<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="27.52mm" wi="59.52mm" file="US08314109-20121120-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which: <br/> X, R₁, R₂, R₃and R₄are as defined in the disclosure, or an acid addition salt thereof; and therapeutic use thereof. </p>
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METHOD FOR AMIDATING POLYPEPTIDES WITH BASIC AMINO ACID C-TERMINALS BY MEANS OF SPECIFIC ENDOPROTEASES (Fri, 10 Dec 2010)
<p id="p-0001-en" num="0000">The invention relates to a method for producing C-terminal amidated dibasic or polybasic peptides, consisting in reacting two peptides in the presence of trypsin biologically active enzymes and, if necessary, in purifying the thus obtainable compounds of formula (I) by means of protein chemistry.</p>
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CRYSTALLINE PHASES OF 2'-{[2-(4-METHOXY-PHENYL)-ACETYLAMINO]-METHYL}-BIPHENYL-2-CARBOXYLIC ACID (2-PYRIDIN-3-YL-ETHYL)-AMIDE (Fri, 10 Dec 2010)
The present invention relates to polymorphic forms and solvates of 2'-{[2-(4-methoxy-phenyl)-acetylamino]-methyl]}-biphenyl-2-carboxylic acid (2-pyhdin-3-yl-ethyl)-amide, processes for their preparation and their use, in particular for the preparation of medicaments.
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Inhibitors of the chemokine receptor CxCR3 (Fri, 03 Dec 2010)
<p id="p-0001" num="0000">This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.</p>
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PROCESS FOR THE PRODUCTION OF DRONEDARONE INTERMEDIATES (Fri, 03 Dec 2010)
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.
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PROCESS FOR THE PRODUCTION OF BENZOFURANS (Fri, 03 Dec 2010)
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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Novel sulfated heptasaccharide and its use as antithrombotic agent (Thu, 02 Dec 2010)
Summary 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 acylated 1,6-anhhydro decasaccharide and its use as antithrombotic agent (Thu, 02 Dec 2010)
Summary 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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Novel sulfated octasaccharide and its use as antithrombotic agent (Thu, 02 Dec 2010)
Summary 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 decasaccharides and their use as antithrombotic agents (Thu, 02 Dec 2010)
Summary 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 3 - , 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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ORTHO-SUBSTITUTED AND META-SUBSTITUTED BIS-ARYL COMPOUNDS, METHOD FOR THE PRODUCTION THEREOF, THEIR USE AS MEDICAMENTS AND PHARMACEUTICAL PREPARATIONS CONTAINING THESE COMPOUNDS (Wed, 01 Dec 2010)

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NOVEL 6-TRIAZOLOPYRIDAZINESULFANYL BENZOTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES, METHOD FOR PRODUCTION THEREOF AND APPLICATION AS MEDICAMENTS AND PHARMNACEUTICAL COMPOSITIONS AND NOVEL USE AS MET INHIBITORS (Fri, 26 Nov 2010)
<p id="p-0001-en" num="0000">The disclosure relates to compounds of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="25.91mm" wi="63.08mm" file="US20100298315A1-20101125-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein <img id="custom-character-00001-en" he="2.79mm" wi="6.01mm" file="US20100298315A1-20101125-P00001.TIF" 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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NOVEL SUBSTITUTED INDAZOLES, THE PREPARATION THEREOF AND USE OF SAME IN THERAPEUTICS (Fri, 26 Nov 2010)
<p id="p-0001-en" num="0000">This disclosure relates to compounds of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="32.00mm" wi="69.77mm" file="US20100298377A1-20101125-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein R₁, R₂, R₃, R₄, E, and n₁are as defined in the disclosure, to compositions containing them, to processes for preparing them, and the use thereof.</p>
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Quinazolinedione derivatives, preparation thereof and therapeutic uses thereof (Fri, 26 Nov 2010)
<p id="p-0001" num="0000">The invention relates to quinazolinedione derivatives of the general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.20mm" wi="65.45mm" file="US08242126-20120814-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, R₁, R₂, R₃, R₄, m, n, p, p′, and r are as defined herein, processes for the preparation thereof and their therapeutic applications. </p>
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PROCESS FOR THE PREPARATION OF A COMPOUND USEFUL AS AN INHIBITOR OF TAFIA (Fri, 19 Nov 2010)
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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N-(Aminoheteroaryl)-1H-indole-2-carboxamide derivatives, and preparation and therapeutic application thereof (Fri, 12 Nov 2010)
<p id="p-0001-en" num="0000">The invention concerns compounds of general formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="29.97mm" wi="67.90mm" file="US20100286119A1-20101111-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">Wherein n, X₁, X₂, X₃, X₄, Y, Z, Z₁, Z₂, Z₃and Z₄are as defined herein. The invention also concerns a process for the preparation of compounds of formula (I) and their therapeutic use.</p>
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NOVEL ACYLATED DECASACCHARIDES AND THEIR USE AS ANTITHROMBOTIC AGENTS (Fri, 12 Nov 2010)
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 3 -, 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 (Fri, 12 Nov 2010)
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 (Fri, 12 Nov 2010)
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 (Fri, 12 Nov 2010)
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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PIPERIDINYLALKYLCARBAMATE DERIVATIVES, METHODS FOR THEIR PREPARATION AND THE THERAPEUTIC USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS (Fri, 05 Nov 2010)
<p id="p-0001-en" num="0000">The present invention relates to piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.</p>
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Derivatives of dioxan-2-alkyl carbamates, preparation thereof and application thereof in therapeutics (Fri, 05 Nov 2010)
<p id="p-0001" num="0000">A compound corresponding to general formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.84mm" wi="63.42mm" file="US08119687-20120221-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> in which R₁represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C₁-C₃)alkyl, (C₁-C₃)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C₃-C₆)cycloalkyl-O— or (C₃-C₆)cycloalkyl(C₁-C₃)alkoxy groups; R₂represents either a group of general formula CHR₃CONHR₄in which R₃represents a hydrogen atom or a methyl group and R₄represents a hydrogen atom or a (C₁-C₃)alkyl, (C₃-C₅) cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C₁-C₃)alkyl, (C₁-C₃)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases. </p>
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PROCESS FOR THE PREPARATION OF [4-(2-CHLORO-4-METHOXY-5-METHYLPHENYL)-5-METHYL-THIAZOLO-2-YL]-[2-CYCLOPROPYL-1-(3-FLUORO-4-METHYLPHENYL)-ETHYL]-AMINE (Fri, 05 Nov 2010)
The subject of the present invention is a novel process for the preparation of the [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl]-amine of formula (I) and the new intermediates of the preparation process.
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6-aryl/heteroalkyloxy benzothiazole and benzimidazole derivatives, method for preparing same, application thereof as drugs, pharmaceutical compositions and novel use in particular as C-MET inhibitors (Fri, 29 Oct 2010)
<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="15.66mm" wi="61.72mm" file="US08188078-20120529-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein A, W, R, R₅, and R₆are as defined in the disclosure, or a salt thereof, and to their use as drugs, in particular as c-Met inhibitors. </p>
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DERIVATIVES OF PYRROLIZINE, INDOLIZINE AND QUINOLIZINE, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF (Fri, 22 Oct 2010)
<p id="p-0001-en" num="0000">The disclosure relates to a compound of formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="39.79mm" wi="69.85mm" file="US20100267766A1-20101021-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">wherein m, n, Ar, and R are as defined in the disclosure, to compositions containing them and to their therapeutic use. The disclosure also relates to processes for preparing these compounds and to certain intermediate compounds.</p>
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