CHEMICAL COMPOUNDS (Fri, 01 Aug 2014)
The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1 and R2 have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
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COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS (Fri, 01 Aug 2014)
Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
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Chemical Compounds - 759 (Fri, 06 Jun 2014)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="52.49mm" wi="62.65mm" file="US20140155394A1-20140605-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.</p>
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Novel Ticagrelor Co-Crystal (Fri, 30 May 2014)
<p id="p-0001" num="0000">The present invention relates to a novel co-crystal of the compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="58.59mm" wi="74.17mm" file="US20140148403A1-20140529-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein the co-former molecule is acetyl salicylic acid, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a such a co-crystal.</p>
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TRPA1 Receptor Antagonist (Fri, 30 May 2014)
<p id="p-0001" num="0000">A compound of Formula (I), pharmaceutically acceptable salts thereof, enantiomers, or mixtures thereof: pharmaceutical compositions containing said compounds, enantiomers or mixtures, processes for making said compounds, enantiomers or mixtures, the use of said compounds, enantiomers or mixtures, and medicaments containing the same for treatment of pain and other conditions, and methods of treating pain and other conditions with the same.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.10mm" wi="73.41mm" file="US20140148466A1-20140529-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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CHEMICAL COMPOUNDS 542 (Fri, 09 May 2014)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.36mm" wi="64.01mm" file="US20140128371A1-20140508-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.</p>
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(4-Tert-butylpiperazin-2-yl)(piperazin-1-yl)methanone-N-carboxamide derivatives (Thu, 08 May 2014)
The present invention relates to compounds of formula (I) The compounds act via antagonism of the CCR2b receptor and may be used to treat inflammatory disease and/or neuropathic pain.
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ENGINEERED POLYPEPTIDES HAVING ENHANCED DURATION OF ACTION (Fri, 18 Apr 2014)
<p id="p-0001" num="0000">Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including oral administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including obesity and overweight, diabetes, dyslipidemia, hyperlipidemia, Alzheimer's disease, fatty liver disease, short bowel syndrome, Parkinson's disease, cardiovascular disease, and other and disorders of the central nervous system.</p>
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Methods For Affecting Body Composition (Fri, 07 Mar 2014)
<p id="p-0001" num="0000">Methods for affecting body composition include the use of amylin or amylin agonist(s). Total body weight be reduced, maintained or even increased; however, the body fat is reduced or body fat gain is prevented, while lean body mass is maintained or increased.</p>
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NOVEL COMPOUNDS (Fri, 07 Mar 2014)
<p id="p-0001" num="0000">There is provided a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.78mm" wi="63.25mm" file="US20140066455A1-20140306-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.</p>
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IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-PHTHALAZIN-1-ONE (Fri, 07 Mar 2014)
<p id="p-0001" num="0000">The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.</p>
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COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS (Fri, 28 Feb 2014)
The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
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COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS (Fri, 28 Feb 2014)
The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist- induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
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9-Substituted 8-Oxoadenine Compound (Fri, 14 Feb 2014)
<p id="p-0001" num="0000">The present invention provides an 8-oxoadenine compound having immunomodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.54mm" wi="74.85mm" file="US20140045837A1-20140213-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">[wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z<sup>1 </sup>represents alkylene, X<sup>2 </sup>represents oxygen atom, sulfur atom, SO<sub>2</sub>, NR<sup>5</sup>, CO, CONR<sup>5</sup>, NR<sup>5</sup>CO and the like, Y<sup>1</sup>, Y<sup>2 </sup>and Y<sup>3 </sup>represent independently a single bond or an alkylene group, X<sup>1 </sup>represents oxygen atom, sulfur atom, NR<sup>4 </sup>(R<sup>4 </sup>is hydrogen atom or an alkyl group) or a single bond, R<sup>2 </sup>represents a substituted or unsubstituted alkyl group, R<sup>1 </sup>represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] <br/> or its pharmaceutically acceptable salt. </p>
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Chromenone Derivatives (Fri, 07 Feb 2014)
<p id="p-0001" num="0000">The invention concerns chromenone compounds of Formula I;</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.69mm" wi="68.92mm" file="US20140038937A1-20140206-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">or pharmaceutically-acceptable salts thereof, wherein each of R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, n and R<sup>6 </sup>has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.</li> </ul> </li> </ul> </p>
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Heterocyclic compounds as CCR2B antagonists (Fri, 07 Feb 2014)
<p id="p-0001" num="0000">Compounds of formula (I) <br/> <?in-line-formulae description="In-line Formulae" end="lead"?>Q-L-W—C(═X)—Z—P<?in-line-formulae description="In-line Formulae" end="tail"?> <br/> wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">Q is an amine of the formula —N(R<sup>1</sup>)(R<sup>2</sup>);</li> <li id="ul0002-0002" num="0000">L is an alkyl or heterocyclyl-alkyl linker;</li> <li id="ul0002-0003" num="0000">W is a 6- or 7-membered aliphatic ring comprising ring atoms Y<sup>1 </sup>and Y<sup>2 </sup>which are linked to groups L and C(X) respectively and Y<sup>1 </sup>and Y<sup>2 </sup>are independently selected from N and C;</li> <li id="ul0002-0004" num="0000">X is O, N, N—CN or S;</li> <li id="ul0002-0005" num="0000">Z is NR<sup>3</sup>;</li> <li id="ul0002-0006" num="0000">P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; <br/> and pharmaceutically acceptable salts or solvates thereof, <br/> are useful in the treatment of C—C chemokine mediated conditions. </li> </ul> </li> </ul> </p>
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Camsylate Salt (Fri, 31 Jan 2014)
<p id="p-0001" num="0000">A camsylate salt of (1r,1′R,4R)-4-methoxy-5″-methyl-6′-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3′H-dispiro[cyclohexane-1,2′-inden-1′2′-imidazole]-4″-amine, pharmaceutical compositions containing the salt and therapeutic uses of the salt for treating Aβ-related pathologies such as Alzheimer's Disease, Down's syndrome, β-amyloid angiopathy and conditions such as dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.</p>
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CHEMICAL COMPOUNDS (Fri, 17 Jan 2014)
<p id="p-0001" num="0000">There is provided pyrimidinyl compounds of Formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.01mm" wi="55.54mm" file="US20140018364A1-20140116-C00001.TIF" alt="embedded image" 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"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">R<sup>2 </sup>is</li> </ul> </li> </ul> </p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="68.16mm" wi="65.28mm" file="US20140018364A1-20140116-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.</p>
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CYCLOHEXANE-1,2'-NAPHTHALENE-1',2"-IMIDAZOLE COMPOUNDS AND THEIR USE AS BACE INHIBITORS (Sat, 28 Dec 2013)
Cyclohexane-1,2'-naphthalene-1',2''-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.
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CAMSYLATE SALT (Sat, 28 Dec 2013)
A camsylate salt of (1r,1 'R,4R)- 4-methoxy-5"-methyl-6'-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3'H-dispiro[cyclohexane-1,2'-inden-1'2'-imidazole]-4"-amine, pharmaceutical compositions containing the salt and therapeutic uses of the salt for treating Αβ-related pathologies such as Alzheimer's Disease, Down's syndrome, β-amyloid angiopathy and conditions such as dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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CYCLOHEXANE-1,2'-INDENE-1',2"-IMIDAZOL COMPOUNDS AND THEIR USE AS BACE INHIBITORS (Sat, 28 Dec 2013)
Cyclohexane-1,2'-indene-1',2''-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.
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CYCLOALKYL ETHER COMPOUNDS AND THEIR USE AS BACE INHIBITORS (Sat, 28 Dec 2013)
Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration and pharmaceutical compositions containing such compounds. Formula (I) wherein A is -O-, or -CH2-, n is 0 or 1.
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2H-IMIDAZOL-4-AMINE COMPOUNDS AND THEIR USE AS BACE INHIBITORS (Sat, 28 Dec 2013)
2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration methods of therapy, and pharmaceutical compositions containing such compounds. Formula (I) wherein A is -O- or -CH2-, n is 1 or 1.
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CARBOXYLIC ACID COMPOUNDS (Fri, 22 Nov 2013)
The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.
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PANCREATIC POLYPEPTIDE FAMILY MOTIFS, POLYPEPTIDES AND METHODS COMPRISING THE SAME (Fri, 15 Nov 2013)
<p id="p-0001" num="0000">The present invention provides novel Pancreatic Polypeptide Family (“PPF”) polypeptides and methods for their use.</p>
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2-Carboxamide-7-Piperazinyl-Benzofuran Derivatives (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.31mm" wi="35.31mm" file="US20130296296A1-20131107-C00001.TIF" alt="embedded image" 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">R<sup>1 </sup>is heteroaryl or heterocyclyl, optionally substituted;</li> <li id="ul0001-0002" num="0000">R<sup>2 </sup>is C<sub>1-4</sub>alkyl, heterocyclyl, C<sub>1-4</sub>alkylaryl, C<sub>1-4</sub>alkylheteroaryl, carbocyclyl, C<sub>1-4</sub>alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted;</li> <li id="ul0001-0003" num="0000">R<sup>3 </sup>is hydrogen or C<sub>1-4</sub>alkyl, or</li> <li id="ul0001-0004" num="0000">R<sup>2 </sup>and R<sup>3 </sup>may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted;</li> <li id="ul0001-0005" num="0000">R<sup>4 </sup>is hydrogen, halogen, methyl or methoxy; <br/> to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. </li> </ul> </p> <p id="p-0004" num="0000">The present invention further relates to new intermediates useful in the preparation thereof.</p>
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DPP-IV RESISTANT GIP HYBRID POLYPEPTIDES WITH SELECTABLE PROPERTIES (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and/or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.</p>
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HETEROBICYCLIC COMPOUNDS AS BETA-LACTAMASE INHIBITORS (Fri, 11 Oct 2013)
The present invention is directed to compounds which are beta-lactamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R 2, R 3 and R 4 are described herein.
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TRANSMUCOSAL DELIVERY OF ENGINEERED POLYPEPTIDES (Fri, 04 Oct 2013)
Formulations are provided that comprise compounds having inter alia good duration of action, high potency and/or convenient dosing regimens, and a permeation enhancer for transmucosal administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. The pharmaceutical compositions provided are suitable for methods of treatment for diseases and disorders including obesity and overweight, diabetes, dyslipidemia, hyperlipidemia, Alzheimer's disease, fatty liver disease, short bowel syndrome, Parkinson's disease, cardiovascular disease, and other and disorders of the central nervous system.
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3 -CYANO- 5 -ARYLAMINO-7 -CYCLOALKYLAMINOPYRROLO [1, 5 -A] PYRIMIDINE DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS (Fri, 04 Oct 2013)
The invention relates to chemical compounds of Formula (I): or a salt thereof. In some embodiments, the invention relates to inhibitors of CK2. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and treatment of CK2-related conditions and diseases, e.g., cancer.
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ENGINEERED POLYPEPTIDES (Fri, 04 Oct 2013)
Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens. The compounds are engineered polypeptides which incorporate an exendin domain in combination with a humanized chimeric seal leptin. Also provided are pharmaceutical compositions and methods of treatment for diseases including diabetes, overweight, obesity, Alzheimer's disease, short bowel syndrome, fatty liver disease, dyslipidemia, coronary artery disease, stroke, hyperlipidemia, NASH or Parkinson's disease.
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Injectable Emulsion of Sedative Hypnotic Agent (Fri, 13 Sep 2013)
<p id="p-0001" num="0000">The present invention provides novel pharmaceutical formulations of a substituted phenylacetic acid ester compound, which is useful as a short-acting sedative hypnotic agent for anesthesia and sedation. The pharmaceutical formulations are oil-in-water emulsions suitable for administration by injection. The invention further provides processes for the preparation of the formulation and the use of the formulation in medical treatment of a mammal.</p>
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Novel Amide Compounds (Fri, 13 Sep 2013)
<p id="p-0001" num="0000">The present invention provides compounds of formula (1)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.03mm" wi="70.19mm" file="US20130237507A1-20130912-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein n, R<sup>1</sup>, R<sup>2</sup>, X<sup>1</sup>, X<sup>2</sup>, X<sup>3</sup>, X<sup>4</sup>, X<sup>5</sup>, R<sup>3a</sup>, R<sup>3b</sup>, R<sup>4</sup>, R<sup>5 </sup>and R<sup>6 </sup>are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.</p>
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Compounds and Their Use as BACE Inhibitors (Fri, 16 Aug 2013)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.</p>
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Pyrimidine sulphonamide derivatives as chemokine receptor modulators (Fri, 09 Aug 2013)
<p id="p-0001" num="0000">A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.84mm" wi="58.25mm" file="US08722883-20140513-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PHARMACEUTICAL COMPOSITION 271 (Fri, 02 Aug 2013)
<p id="p-0001" num="0000">The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.</p>
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GIP ANALOG AND HYBRID POLYPEPTIDES WITH SELECTABLE PROPERTIES (Fri, 02 Aug 2013)
<p id="p-0001" num="0000">The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and/or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.</p>
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Phenyl and benzodioxinyl substituted indazole derivatives (Thu, 01 Aug 2013)
A compound of formula Ia : The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
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GLP-1 RECEPTOR AGONIST COMPOUNDS HAVING STABILIZED REGIONS (Fri, 19 Jul 2013)
<p id="p-0001" num="0000">The disclosure provides GLP-1 receptor agonist compounds having stabilized regions corresponding to alpha-helical regions of the natural peptide compounds. The disclosure also provides benzamide-containing exendin-4 analogs and alkene-constrained exendin-4 analogs, both of which have stabilized regions corresponding to alpha-helical regions of exendin-4.</p>
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Therapeutic agents (Fri, 19 Jul 2013)
<p id="p-0001" num="0000">Disclosed herein are azetidinyl compounds of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.16mm" wi="75.69mm" file="US08685958-20140401-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition. </p>
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PROCESSES FOR MAKING CYCLOPROPYL AMIDE DERIVATIVES AND INTERMEDIATES ASSOCIATED THEREWITH (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition.</p>
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Ethanamine compounds and methods of using the same (Thu, 04 Jul 2013)
The present invention is directed to 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and the use of same for treating depression.
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Azaquinolinone Derivatives and Uses Thereof (Fri, 28 Jun 2013)
<p id="p-0001" num="0000">The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.</p>
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Benzothiazoles as ghrelin receptor modulators (Thu, 27 Jun 2013)
A compound of formula I or a pharmaceutically acceptable salt thereof in which R 1 , R 2 , R 3 , R 4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.
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Chromenone derivatives (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">The invention concerns chromenone derivatives of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="58.76mm" wi="76.28mm" file="US08673906-20140318-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically-acceptable salts thereof, wherein each of R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, n and R<sup>9 </sup>has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders. </p>
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CHEMICAL COMPOUNDS (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use in the treatment of bacterial infections are also described.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.16mm" wi="71.54mm" file="US20130150366A1-20130613-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUNDS AND THEIR USE AS IKACH BLOCKERS (Fri, 07 Jun 2013)
<p id="p-0001" num="0000">The invention relates to compounds according to Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.83mm" wi="69.43mm" file="US20130143858A1-20130606-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt thereof, wherein m, n, R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, R<sub>5</sub>, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.</p>
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ETHANAMINE COMPOUNDS AND METHODS OF USING THE SAME (Fri, 31 May 2013)
<p id="p-0001" num="0000">The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treatingh depression by administering the ethanamine compound.</p>
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PYRAZINE DERIVATIVES (Fri, 17 May 2013)
<p id="p-0001" num="0000">The invention concerns pyrazine derivatives of the Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.48mm" wi="69.85mm" file="US20130123275A1-20130516-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or pharmaceutically-acceptable salts thereof; wherein each of n, m and R has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of bone-related disorders or conditions.</p>
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(Fri, 03 May 2013)

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MONO-FLUORO BETA-SECRETASE INHIBITORS (Fri, 19 Apr 2013)
Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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PYRAZOLYLAMINOPYRIDINE DERIVATIVES USEFUL AS KINASE INHIBITORS (Fri, 12 Apr 2013)
<p id="p-0001" num="0000">This invention relates to novel compounds having the formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.76mm" wi="58.17mm" file="US20130090358A1-20130411-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.</p>
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INJECTABLE EMULSION OF SEDATIVE HYPNOTIC AGENT (Thu, 28 Mar 2013)
The present invention provides novel pharmaceutical formulations of a substituted phenylacetic acid ester compound, which is useful as a short-acting sedative hypnotic agent for anesthesia and sedation. The pharmaceutical formulations are oil-in-water emulsions suitable for administration by injection. The invention further provides processes for the preparation of the formulation and the use of the formulation in medical treatment of a mammal.
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TRISUBSTITUTED TRIAZOLOPYRIMIDINES FOR USE IN PLATELET AGGREGATION INHIBITION (Fri, 22 Mar 2013)
<p id="p-0001" num="0000">The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.</p>
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Pyrimidline derivatives having immune modulating properties that act via TLR7 for the treatment of viral or allergic diseases and cancers (Fri, 22 Feb 2013)
<p id="p-0001" num="0000">The present invention provides compounds of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="52.92mm" file="US08765939-20140701-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3 </sup>and R<sup>4 </sup>are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy. </p>
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Compound (Fri, 15 Feb 2013)
<p id="p-0001" num="0000">There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.15mm" wi="69.85mm" file="US08735413-20140527-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.</p>
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Amide derivatives bearing a cyclopropylaminoacarbonyl substituent useful as cytokine inhibitors (Fri, 08 Feb 2013)
<p id="p-0001" num="0000">The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.</p>
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2 - (2, 4, 5 - SUBSTITUTED -ANILINO) PYRIMIDINE DERIVATIVES AS EGFR MODULATORS USEFUL FOR TREATING CANCER (Fri, 01 Feb 2013)
The present invention relates to certain 2-(2,4,5-substituted-anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
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AZETIDINE DERIVATIVES FOR TREATMENT OF MELANIN RELATED DISORDERS (Fri, 25 Jan 2013)
Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin- concentrating hormone related disease or condition.
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Compounds-801 (Fri, 18 Jan 2013)
<p id="p-0001" num="0000">Spirocyclic amide derivatives of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.25mm" wi="75.95mm" file="US08476265-20130702-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein <br/> ArCH<sub>2</sub>CH<sub>2</sub>NH— represents a β-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation. </p>
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ENGINEERED POLYPEPTIDES HAVING ENHANCED DURATION OF ACTION WITH REDUCED IMMUNOGENICITY (Fri, 18 Jan 2013)
Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including oral administration, and reduced immunogenicity. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including obesity and overweight, diabetes, dyslipidemia, hyperlipidemia, Alzheimer's disease, fatty liver disease, Short Bowel Syndrome, Parkinson's disease, and cardiovascular disease.
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N- (6- ( (2R,3S) -3,4-DIHYDROXYBUTAN-2-YLOXY) -2- (4 - FLUOROBENZYLTHIO) PYRIMIDIN- 4 - YL) -3- METHYLAZETIDINE- 1 - SULFONAMIDE AS CHEMOKINE RECEPTOR MODULATOR (Fri, 18 Jan 2013)
There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
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Chemical compounds (Fri, 04 Jan 2013)
<p id="p-0001" num="0000">There is provided pyrimidinyl compounds of Formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.01mm" wi="69.85mm" file="US08552004-20131008-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein: <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<sup>2 </sup>is</li> </ul> </li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="72.81mm" wi="69.85mm" file="US08552004-20131008-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. </p>
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CRYSTALLINE FORM OF INDAZOLYL AMIDE DERIVATIVES FOR THE TREATMENT GLUCOCORTICOID RECEPTOR MEDIATED DISORDERS (Fri, 04 Jan 2013)
Crystalline forms of 2,2,2-trifluoro-N-[(lR,2S)-l-[l-(4-fluorophenyl)in- dazol-5-yl]oxy-l-(3-methoxyphenyl)propan-2-yl]acetamide, processes for obtaining them, pharmaceutical intermediates used in their manu¬ facture, pharmaceutical compositions containing them, and their use in medical treatment.
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PROCESS FOR PREPARING INDOL-5-OXY-QUINAZOLINE DERIVATIVES AND INTERMEDIATES (Thu, 03 Jan 2013)
The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline.
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PROCESS FOR PREPARING INDOL-5-OXY-QUINAZOLINE DERIVATIVES AND INTERMEDIATES (Thu, 03 Jan 2013)
The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline.
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Compounds (Fri, 21 Dec 2012)
<p id="p-0001" num="0000">The present invention relates to spirocyclic amide derivatives of the formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.36mm" wi="69.85mm" file="US08629271-20140114-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing them, and their use in therapy. </p>
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PROCESS FOR PREPARING HETEROCYCLIC COMPOUNDS INCLUDING TRANS-7-OXO-6-(SULPHOOXY)-1,6-DIAZABICYCLO[3,2,1]OCTANE-2-CARBOXAMIDE AND SALTS THEREOF (Fri, 21 Dec 2012)
The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6- diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
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NOVEL TICAGRELOR CO - CRYSTAL (Fri, 07 Dec 2012)
The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is acetyl salicylic acid, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a such a co-crystal.
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PROCESS (Fri, 23 Nov 2012)
Processes for the preparation of the compound of formula (II) and intermediate compounds for use in the processes.
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Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof (Thu, 01 Nov 2012)
Methods and compounds for production of cycloproyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
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Chromenone derivatives (Fri, 19 Oct 2012)
<p id="p-0001" num="0000">The invention concerns chromenone compounds of Formula I;</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.69mm" wi="69.17mm" file="US08530470-20130910-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or pharmaceutically-acceptable salts thereof, wherein each of R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, n and R<sup>6 </sup>has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders. </p>
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Compounds suitable as precursors to compounds that are useful for imaging amyloid deposits (Fri, 19 Oct 2012)
<p id="p-0001" num="0000">The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.</p>
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CHROMENONE COMPOUNDS AS PI 3 -KINASE INHIBITORS FOR THE TREATMENT OF CANCER (Fri, 19 Oct 2012)
The invention concerns chromenone compounds of Formula I; or pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, n and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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Benzamide compounds useful as histone deacetylase inhibitors (Fri, 07 Sep 2012)
<p id="p-0001" num="0000">The invention concerns benzamide compounds of formula (I): compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.81mm" wi="69.85mm" file="US08735429-20140527-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C<sub>1-4</sub>alkyl, C<sub>3-4</sub>cycloalkyl, C<sub>1-4</sub>alkoxy and C<sub>3-4</sub>cycloalkoxy; <br/> or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC). </p>
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N-cyclopropyl-3-fluoro-5-[3-[[1-[2-[2- [(2-hydroxethyl)amino] ethoxy]phenyl] cyclopropyl] amino]-2-oxo-1 (2H)-pyrazinyl]-4-methyl-benzamide, or pharmaceutically acceptable salts thereof and their uses (Fri, 24 Aug 2012)
<p id="p-0001" num="0000">The present invention relates to pyrazinone derivatives of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.24mm" wi="62.91mm" file="US08299246-20121030-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6 </sup>and R<sup>7 </sup>are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy. </p>
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Dibenzothiazepine derivatives and uses thereof—424 (Fri, 10 Aug 2012)
<p id="p-0001" num="0000">Compounds the following formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.17mm" wi="57.49mm" file="US08653257-20140218-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds. </p>
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Quinazoline derivatives as angiogenesis inhibitors (Fri, 03 Aug 2012)
<p id="p-0001" num="0000">The invention relates to the use of compounds of formula (I) and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.98mm" wi="69.85mm" file="US08492560-20130723-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Biphenyloxyacetic acid derivatives for the treatment of respiratory disease (Fri, 13 Jul 2012)
<p id="p-0001" num="0000">The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.</p>
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Biphenyloxyacetic acid derivatives for the treatment of respiratory disease (Fri, 13 Jul 2012)
<p id="p-0001" num="0000">The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim <b>1</b>, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.</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="US08722741-20140513-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Compounds and their use as BACE inhibitors (Fri, 29 Jun 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.</p>
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COMPOUNDS AND THEIR USE AS BACE INHIBITORS (Fri, 29 Jun 2012)
The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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COMPOUNDS AND THEIR USE AS BACE INHIBITORS (Fri, 29 Jun 2012)
The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Αβ-related pathologies such as Down's syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.
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2-CARBOXAMIDE-4-PIPERAZINYL-BENZOFURAN DERIVATIVE (Fri, 29 Jun 2012)
The present invention relates to a compound of formula (I), and to pharmaceutical compositions containing said compound and to the use of said compound in therapy, for instance in treating cognitive disorders, as well as to intermediates useful in the preparation thereof.
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Pyrimidine sulphonamide derivatives as chemokine receptor modulators (Fri, 22 Jun 2012)
<p id="p-0001" num="0000">A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.84mm" wi="58.17mm" file="US08410123-20130402-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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IMIDAZO [4, 5 -C] QUINOLIN- 1 -YL DERIVATIVE USEFUL IN THERAPY (Fri, 22 Jun 2012)
The invention provides the compound of formula (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy.
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PURINE DERIVATIVES (Fri, 22 Jun 2012)
The invention provides the compound of formula. (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy.
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Compounds and their use as IKACh blockers (Fri, 08 Jun 2012)
<p id="p-0001" num="0000">The invention relates to compounds according to Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.64mm" wi="69.60mm" file="US08361998-20130129-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof, wherein m, n, R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, R<sub>5</sub>, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter. </p>
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NEW IKACH BLOCKERS (Fri, 08 Jun 2012)
The invention relates to compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula (I) are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.
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N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl]-4-(3,4-dimethylpiperazin-1-yl)benzamide and salts thereof (Fri, 25 May 2012)
<p id="p-0001" num="0000">There is provided a compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.22mm" wi="69.85mm" file="US08604022-20131210-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer. </p>
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AMINOALKOXYPHENYL COMPOUNDS AND THEIR USE IN THE TREATMENT OF DISEASE (Fri, 25 May 2012)
The invention concerns compounds of Formula (I): (I) wherein n, m, p, R1 and R2 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, novel intermediates useful in the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.
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BENZYLAMINE COMPOUNDS AS TOLL -LIKE RECEPTOR 7 AGONISTS (Fri, 25 May 2012)
The invention concerns compounds of Formula (I), and pharmaceutically acceptable salts thereof: where such compounds act as TLR7 agonists and at the same time show advantageous selectivity over TLR8 and hERG, wherein the variable groups R1, R2 and n are as defined herein. The invention also relates to methods for the preparation of such compounds and intermediates useful in the preparation thereof, to pharmaceutical compositions containing such compounds, to the use of such compounds in the preparation of medicaments, and to the use of such compounds in the treatment of conditions mediated by TLR7, such as allergic diseases, autoimmune diseases, viral diseases and, in particular, cancer.
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PHENOL COMPOUNDS ALS TOLL -LIKE RECEPTOR 7 AGONISTS (Fri, 25 May 2012)
The invention concerns compounds of Formula (I): wherein R1, R2, R3 and Q are as defined in the description. The present invention also relates to processes for the preparation of such compounds, novel intermediates useful in the preparation of such compounds, pharmaceutical compositions containing them and their use as toll-like receptor 7 agonists.
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CYCLIC AMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF DISEASE (Fri, 25 May 2012)
The invention concerns compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein n, R1 and R2 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, novel intermediates useful in the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.
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COMPOUNDS AND THEIR USE FOR TREATMENT OF Αβ-RELATED DISEASES (Sat, 19 May 2012)
The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of Αβ-related diseases.
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INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF 4-(ACETYLAMINO))-3-[(4-CHLORO-PHENYL)THIO]-2-METHYL-1H-INDOLE-1-ACETIC ACID (Thu, 17 May 2012)
The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound of formula (I): X is =0, =N-0H or =N-OC(O)Me; Y is hydrogen, PhS- or <i>p</i>-chlorophenylsulfanyl; Z is hydrogen or -CH<sb>2</sb>COOR<sp>1</sp> wherein R<sb>1</sb> is selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.
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2-CARBOXAMIDE-7-PIPERAZINYL-BENZOFURAN DERIVATIVES (Thu, 10 May 2012)
The present invention relates to compounds of formula (I), wherein R<sp>1</sp> is heteroaryl or heterocyclyl, optionally substituted R<sp>2</sp> is C<sb>1-4</sb>alkyl, heterocyclyl, C<sb>1-4</sb>alkylaryl, C<sb>1-4</sb>alkylheteroaryl, carbocyclyl, C<sb>1-</sb> <sb>4</sb>alkylheterocyclyl, heterocyclylheteroaryl, arylheterocyclyl, carbocyclylheteroaryl, heterocyclylaryl, optionally substituted R<sp>3 </sp>is hydrogen or C<sb>1-4</sb>alkyl, or R<sp>2</sp> and R<sp>3</sp> may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted R<sp>4</sp> is hydrogen, halogen, methyl or methoxy to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.
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2-pyrazinone derivatives for the treatment of disease or condition in which inhibition of neutrophil elastase activity is beneficial (Fri, 04 May 2012)
<p id="p-0001" num="0000">The invention provides compounds of formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="62.06mm" file="US08410114-20130402-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>14</sup>, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase. </p>
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Process for the preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-([1-(N-methylcarbamoymethyl)piperidin-4-yl]oxy)quinazoline (Fri, 04 May 2012)
<p id="p-0001" num="0000">Processes for the preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline, salts thereof, and the intermediates used in the process are described.</p>
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Process for preparing [1<i>S</i>-[1-α, 2-α, 3-β(1<i>S</i>*,2<i>R</i>*) 5-β]]-3-[7-[2-(3,4-difluorophenyl)-cyclopropylamino]-5-(propylthio)-3<i>H</i>-1,2,3-triazolo [4,5-<i>d</i>] pyrimidin-3-yl]-5-(2-hydroxyethoxy) cyclopentane-1,2-diol and to its intermediates (Fri, 27 Apr 2012)
<p id="p-0001" num="0000">The present invention is directed to a process for preparing [1S-[1α,2α,3β(1S*,2R*),5β]]-3-[7-[2-(3,4-difluorophenyl)-cyclopropylamino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol and to intermediates useful in the process.</p>
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IMIDAZOLE SUBSTITUTED PYRIMIDINE HAVING A HIGH GSK3 INHIBITING POTENCY AS WELL AS PAN-KINASE SELECTIVITY (Fri, 20 Apr 2012)
The present invention relates to a new compound of formula (I) as a free base or a pharmaceutically acceptable salt thereof, in an essentially pure and isolated form, a pharmaceutical composition containing a compound of formula (I), to the use of said active compound in therapy, to the use for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as for the method of treatment of said disorders, comprising administering to a mammal, including human in need of such treatment, a therapeutically effective amount of said compound.
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ENGINEERED POLYPEPTIDES HAVING ENHANCED DURATION OF ACTION (Fri, 20 Apr 2012)
Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including oral administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including obesity and overweight, diabetes, dyslipidemia, hyperlipidemia, Alzheimer's disease, fatty liver disease, short bowel syndrome, Parkinson's disease, cardiovascular disease, and other and disorders of the central nervous system.
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TRPA1 RECEPTOR ANTAGONIST (Fri, 20 Apr 2012)
A compound of Formula (I), pharmaceutically acceptable salts thereof, enantiomers, or mixtures thereof: pharmaceutical compositions containing said compounds, enantiomers or mixtures, processes for making said compounds, enantiomers or mixtures, the use of said compounds, enantiomers or mixtures, and medicaments containing the same for treatment of pain and other conditions, and methods of treating pain and other conditions with the same.
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ISOXAZOL-3(2H)-ONE ANALOGS AS PLASMINOGEN INHIBITORS AND THEIR USE IN THE TREATMENT OF FIBRINOLYSIS RELATED DISEASES (Fri, 13 Apr 2012)
A compound of formula (I): wherein R1 is hydrogen; R2 is C1-C10 alkyl, which C1-C10 alkyl comprises 0, 1, 2, 3 or 4 heteroatoms, selected from O and N, or 0, 1 or 2 acid, ester or amide functionalities, and said C1-C10 alkyl is substituted by 0, 1, 2, 3 or 4 CH3, halogen or CF3, or -XR20, wherein X is a bond or _-CH2-, and R20 is a 4 to 10 membered, monocyclic or bicyclic heterocyclic aromatic or non-aromatic ring containing 1, 2, 3 or 4 heteroatoms selected from O and N, and R20 is substituted by 0, 1, 2, 3 or 4 CH3, halogen or CF3, pharmaceutical compositions, medical uses and treatment or prophylaxis of a disease or condition in which modulation of fibrinolysisis is beneficial.
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NOVEL COMBINATIONS (Fri, 13 Apr 2012)
The invention provides a pharmaceutical product comprising, in combination, (1) a named glucocorticosteroid receptor agonist and (2) a β2 adrenoreceptor agonist, a dual β2 adrenoreceptor agonist/M3 receptor antagonist, a muscarinic antagonist, a p38 kinase inhibitor, a neutrophil elastase inhibitor, a phosphodiesterase PDE4 inhibitor, an IKK2 kinase inhibitor or a non-steroidal glucocorticoid receptor agonist, and the use of said product in treating respiratory diseases.
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CRYSTALLINE NALOXOL-PEG CONJUGATE (Fri, 06 Apr 2012)
Naloxol-polyethlyene glycol conjugates of the formula:are provided in oxalate or phosphate salt forms including crystalline forms. Methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms are also provided.
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NOVEL CHROMANE COMPOUND FOR THE TREATMENT OF PAIN DISORDERS (Fri, 30 Mar 2012)
The present invention relates to the compound N-[(3S)-5-(5-methoxypyrazin-2-yl)-3,4- dihydro-2H-chromen-3-yl]-6-[(2,2,2-trifluoroethoxy)methyl]pyridine-3-carboxamide, or a pharmaceutical composition comprising said compound and to the use of said compounds in therapy.
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Compounds and their uses 708 (Fri, 16 Mar 2012)
<p id="p-0001" num="0000">The present invention relates to pyrazinone derivatives of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.15mm" wi="62.91mm" file="US08163905-20120424-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6 </sup>and R<sup>7 </sup>are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy. </p>
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Chemical compounds (Fri, 09 Mar 2012)
<p id="p-0001" num="0000">Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.</p>
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Methods for affecting body composition using amylin agonists (Fri, 02 Mar 2012)
<p id="p-0001" num="0000">Methods for affecting body composition include the use of amylin agonists, such as pramlintide or davalintide. Total body weight may be reduced, maintained or even increased; however, the body fat is reduced or body fat gain is prevented, while lean body mass is maintained or increased.</p>
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N-terminus conformationally constrained GLP-1 receptor agonist compounds (Fri, 24 Feb 2012)
<p id="p-0001" num="0000">The disclosure provides N-terminus conformationally constrained compounds, which may comprise peptide mimetics and/or amino acid substitutions, which may be used in peptides, such as GLP-1 receptor agonist compounds, to induce a β-turn secondary structure at the N-terminus. The N-terminus conformationally constrained compounds may be used for research purposes; to produce GLP-1 receptor agonist compounds having improved GLP-1 receptor binding activity, enzymatic stability, or in vivo glucose lowering activity; and to develop GLP-1 receptor agonist compounds which have fewer amino acid residues. The disclosure also provides GLP-1 receptor agonist compounds, such as exendins, exendin analogs, GLP-1 (7-37), GLP-1 (7-37) analogs, comprising the N-terminus conformationally constrained compounds. The compounds are useful for treating various diseases, such as diabetes and obesity. The disclosure also provides methods for chemically synthesizing the N-terminus conformationally constrained compounds.</p>
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Crystalline 4-(3-chloro-2-fluoroanilino)-7 methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy} quinazoline difumarate Form A (Fri, 10 Feb 2012)
<p id="p-0001" num="0000">4-(3-chloro-2-fluoroanilino)-7 methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.11mm" wi="55.37mm" file="US08404839-20130326-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">difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.</li> </ul> </li> </ul> </p>
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2-pyridone derivatives as neutrophil elastase inhibitors and their use (Fri, 10 Feb 2012)
<p id="p-0001" num="0000">There are provided novel compounds 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="58.00mm" file="US08501784-20130806-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>4</sup>, G<sup>1</sup>, G<sup>2</sup>, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase. </p>
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N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS (Fri, 10 Feb 2012)
The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
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4-(1H-INDOL-3-YL) -PYRIMIDINES AS ALK INHIBITORS (Fri, 10 Feb 2012)
The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the treatment of cancer.
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CHEMICAL COMPOUNDS (Fri, 10 Feb 2012)
The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the treatment of cancer.</p>
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N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS (Fri, 10 Feb 2012)
The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.</p>
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Chemical compounds (Fri, 03 Feb 2012)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I) and/or Formula (Ia):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="94.06mm" wi="69.51mm" file="US08461170-20130611-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the treatment of cancer. </p>
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GLP-1 RECEPTOR AGONIST COMPOUNDS HAVING STABILIZED REGIONS (Fri, 03 Feb 2012)
The disclosure provides GLP-1 receptor agonist compounds having stabilized regions corresponding to alpha-helical regions of the natural peptide compounds. The disclosure also provides benzamide-containing exendin-4 analogs and alkene-constrained exendin-4 analogs, both of which have stabilized regions corresponding to alpha-helical regions of exendin-4.</p>
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Pyrazine derivatives (Fri, 27 Jan 2012)
<p id="p-0001" num="0000">The invention concerns pyrazine derivatives of the Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.56mm" wi="69.85mm" file="US08198285-20120612-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or pharmaceutically-acceptable salts thereof; wherein each of n, m and R has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of bone-related disorders or conditions. </p>
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PROCESS FOR PREPARING ADENINE COMPOUNDS AND INTERMEDIATES THEREOF (Fri, 27 Jan 2012)
The present invention relates to a process for preparing a compound of Formula (III), or a salt thereof; wherein R1 is C1-6 alkyl; R2 and R3 are each independently hydrogen or C1-4 alkyl, or R2 and R3 combine together with the nitrogen atom to which they are attached to form a pyrrolidine ring, a morpholine ring, a piperidine ring, or a piperazine ring; and n is 1, 2 or 3.
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Crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]THIO]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfonamide (Fri, 20 Jan 2012)
<p id="p-0001" num="0000">There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.</p>
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NEW CRYSTALLINE FORMS OF N-[2-[[(2,3-DIFLUOROPHENY)METHYL)THIO]-6-{[(1R,2S)-2,3-DIHYDROXY-1- METHYLPROPYL]OXY}-4-PYRIMIDINYL]-1-AZETIDINESULFONAMIDE (Fri, 20 Jan 2012)
There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6- {[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
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PHARMACEUTICAL FORMULATIONS (Fri, 20 Jan 2012)
The present invention relates to processes for reducing the particle size of active pharmaceutical ingredients and to pharmaceutical compositions and pharmaceutical formulations prepared by these processes.
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NEW CRYSTALLINE FORMS OF N-[2-[[(2,3-DIFLUOROPHENYL)METHYL]THIO]-6-{[(1R,2S)-2,3-DIHYDROXY-1-METHYLPROPYL]OXY}-4-PYRIMIDINYL}-1-AZETIDINESULFONAMIDE (Fri, 20 Jan 2012)
There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6- {[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfon-amide 5 anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.</p>
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(3-(4-(aminomethyl)phenoxy or phenylthio)azetidin-1-yl)(5-phenyl-1,3,4-oxadiazol-2-yl)methanone compounds (Fri, 13 Jan 2012)
<p id="p-0001" num="0000">Disclosed herein are azetidinyl compounds of formula I,</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.69mm" wi="74.68mm" file="US08546375-20131001-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition. </p>
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THERAPEUTIC AGENTS 976 (Fri, 13 Jan 2012)
Disclosed herein are azetidinyl compounds of formula (I), as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
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THERAPEUTIC AGENTS 976 (Fri, 13 Jan 2012)
Disclosed herein are azetidinyl compounds of formula (I), as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.</p>
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Piperidine derivatives (Thu, 05 Jan 2012)
The present invention provides the compound (S)-{4-[4-(3,4-dichloro-2-methyl-phenoxy)-piperidin-1-ylmethyl]-piperidin-1-yl}-3-(4-ftuoro-phenyl)-propionic acid, or a pharmaceutically acceptable salt thereof; to composition comprising such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state (such as asthma or rhinitis).
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Pharmaceutical Compositions (Fri, 30 Dec 2011)
<p id="p-0001" num="0000">The present invention provides methods of treatment with a pharmaceutical composition, more particularly a sustained release pharmaceutical composition, comprising 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo-[b,f][1,4]thiazepine or a pharmaceutically acceptable salt thereof, as well as new and improved methods for treating a variety of psychological disorders and conditions including, but not limited to, Mood Disorders and Anxiety Disorders and for treating one or more of the symptoms of these disorders.</p>
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Extended Release Formulations Comprising Quetiapine and Methods for Their Manufacture (Fri, 30 Dec 2011)
<p id="p-0001" num="0000">The present invention relates to extended release formulations of quetiapine and its pharmaceutically acceptable salts. The formulations comprise polymers, preferably hydroxypropyl methylcellulose of different viscosities, selected to cause the formulations to conform to preselected quetiapine release profiles. A process for the manufacture of said formulations is also disclosed.</p>
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Substituted Isoindoles (Fri, 30 Dec 2011)
<p id="p-0001" num="0000">The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.18mm" wi="55.29mm" file="US20110319426A1-20111229-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Process for preparing benzimidazole compounds (Fri, 30 Dec 2011)
<p id="p-0001" num="0000">Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.77mm" wi="61.21mm" file="US08383832-20130226-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein Z, X<sup>1</sup>, X<sup>2</sup>, X<sup>5</sup>, R<sup>2b </sup>and R<sup>10 </sup>are as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives. </p>
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Benzimidazole compounds (Fri, 30 Dec 2011)
<p id="p-0001" num="0000">Provided are compounds having Formula VIIIa-1:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.26mm" wi="58.17mm" file="US08501956-20130806-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein Z, X<sup>5</sup>, R<sup>2</sup>, R<sup>2a </sup>and R<sup>10 </sup>are as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives. </p>
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CYCLOPROPYL AMIDE DERIVATIVES TARGETING THE HISTAMINE H3 RECEPTOR (Thu, 29 Dec 2011)
Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
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PROCESS FOR THE PREPARATION OF 1-[5-(3-CHLORO-PHENYL)-ISOOXAZOL-3-YL]-ETHANONE AND (R)-1-[5-(3-CHLORO-PHENYL)-ISOOXAZOL-3-YL]-ETHANOL (Fri, 23 Dec 2011)
<p id="p-0001" num="0000">The present invention provides a process for the preparation of the compound 1-[5-(3-chloro-phenyl)-isooxazol-3-yl]-ethanone: Wherein the compound 5-(3-chlorophenyl)-isooxazol-3-carboxylate is reacted with CH3MgX. The present invention also provides a process for the preparation of (R)-1-[5-(3-chloro-phenyl)-isooxazol-3-yl]-ethanol: Wherein 1-[5-(3-chloro-phenyl)-isooxazol-3-yl]-ethanone is reduced to (R)-1-[5-(3-chloro-phenyl)-isooxazol-3-yl]-ethanol.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="79.76mm" wi="54.02mm" file="US20110313172A1-20111222-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TRIAZOLO[4,3-B]PYRIDAZINE DERIVATIVES AND THEIR USES FOR PROSTATE CANCER (Thu, 22 Dec 2011)
The invention concerns bicyclic compounds of Formula (I) wherein Formula (II), R<sp>1</sp>, R<sp>2</sp>, L<sp>1</sp>, L<sp>2</sp>, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.
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Chemical compounds (Fri, 16 Dec 2011)
<p id="p-0001" num="0000">There is provided pyrimidinyl compounds of Formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.01mm" wi="55.54mm" file="US08252802-20120828-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein: <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<sup>2 </sup>is</li> </ul> </li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="75.61mm" wi="63.58mm" file="US08252802-20120828-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. </p>
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9-substituted 8-oxoadenine compound (Fri, 16 Dec 2011)
<p id="p-0001" num="0000">The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.71mm" wi="73.91mm" file="US08575180-20131105-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z<sup>1 </sup>represents alkylene, X<sup>2 </sup>represents oxygen atom, sulfur atom, SO<sub>2</sub>, NR<sup>5</sup>, CO, CONR<sup>5</sup>, NR<sup>5</sup>CO and the like, Y<sup>1</sup>, Y<sup>2 </sup>and Y<sup>3 </sup>represent independently a single bond or an alkylene group, X<sup>1 </sup>represents oxygen atom, sulfur atom, NR<sup>4 </sup>(R<sup>4 </sup>is hydrogen atom or an alkyl group) or a single bond, R<sup>2 </sup>represents a substituted or unsubstituted alkyl group, R<sup>1 </sup>represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] <br/> or its pharmaceutically acceptable salt. </p>
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MORPHOLINO PYRIMIDINES AND THEIR USE IN THERAPY (Fri, 16 Dec 2011)
There is provided pyrimidinyl compounds of Formula (I), wherein R2 is (1) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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COMPOUNDS (Fri, 16 Dec 2011)
Compounds of formula (I), having activities at muscarinic and β2-receptors (MABAs) for use in therapy.
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SUBSTITUTED N-[1-CYANO-2-(PHENYL)ETHYL] 1-AMINOCYCLOALK-1-YLCARBOXAMIDE COMPOUNDS - 760 (Fri, 16 Dec 2011)
The present invention provides compounds of formula (I) in which, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
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MORPHOLINO PYRIMIDINES AND THEIR USE IN THERAPY (Fri, 16 Dec 2011)
There is provided pyrimidinyl compounds of Formula (I), wherein R2 is (1) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.</p>
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Process for the Manufacture of the Calcium Salt of Rosuvastatin (E)-7-[4-(4-Fluorophenyl)-6-Isopropyl-2-[Methyl(Methylsulfonyl)Amino]-Pyrimidin-5-yl](3R,5S)-3,5-Dihydroxyhept-6-Enoic Acid and Crystalline Intermediates Thereof (Fri, 09 Dec 2011)
<p id="p-0001" num="0000">A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.35mm" wi="71.88mm" file="US20110301348A1-20111208-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A is an acetal or ketal protecting group and R is alkyl, via isolated crystalline compounds of the formula (8) or of formula (10)</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="99.14mm" wi="71.88mm" file="US20110301348A1-20111208-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.</p>
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BENZODIAZEPINE COMPOUNDS USEFUL FOR THE TREATMENT OF HEPATITIS C (Fri, 09 Dec 2011)
The invention concerns benzodiazepine derivatives of Formula (I) wherein A, X, L1, L2, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
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16 Alpha, 17 Alpha-Acetal Glucocorticosteroidal Derivatives and their Use (Fri, 02 Dec 2011)
<p id="p-0001" num="0000">The present invention provides compounds of formula (I) wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5 </sup>and R<sup>6 </sup>are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.37mm" wi="62.74mm" file="US20110294766A1-20111201-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Pharmaceutically acceptable salts of methyl (3-{ [[3-(6-amino- 2-butoxy-8-oxo-7,8-dihydro-9H-purin-9-yl) propyl] (3-morpholin-4-ylpropyl) amino] methyl }phenyl) acetate and their use in therapy (Fri, 02 Dec 2011)
<p id="p-0001" num="0000">The present invention concerns hydrochloric acid, hydrobromic acid and maleic acid salts of methyl (3-{[[3-(6-amino-2-butoxy-8-oxo-7,8-dihydro-9H-purin-9-yl)propyl](3-morpholin-4-ylpropyl)amino]methyl}phenyl)acetate, compositions comprising them and their use in therapy.</p>
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INJECTABLE EMULSION OF SEDATIVE HYPNOTIC AGENT (Fri, 02 Dec 2011)
The present invention provides novel pharmaceutical formulations of a substituted phenylacetic acid ester compound, which is useful as a short-acting sedative hypnotic agent for anesthesia and sedation. The pharmaceutical formulations are oil-in-water emulsions suitable for administration by injection. The invention further provides processes for the preparation of the formulation and the use of the formulation in medical treatment of a mammal.
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INJECTABLE EMULSION OF SEDATIVE HYPNOTIC AGENT (Fri, 02 Dec 2011)
The present invention provides novel pharmaceutical formulations of a substituted phenylacetic acid ester compound, which is useful as a short-acting sedative hypnotic agent for anesthesia and sedation. The pharmaceutical formulations are oil-in-water emulsions suitable for administration by injection. The invention further provides processes for the preparation of the formulation and the use of the formulation in medical treatment of a mammal.</p>
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[4-( 1-AMINO-ETHYL) - CYCLOHEXYL ] - METHYL - AMINES AS ANTIBACTERIALS (Fri, 25 Nov 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.93mm" wi="75.44mm" file="US20110288084A1-20111124-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NEW PROCESS FOR THE PREPARATION OF ARYL SUBSTITUTED OLEFINIC AMINES (Fri, 25 Nov 2011)
An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N- methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.
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NEW PROCESS FOR THE PREPARATION OF ARYL SUBSTITUTED OLEFINIC AMINES (Fri, 25 Nov 2011)
An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N- methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.</p>
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4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer (Thu, 24 Nov 2011)
This invention relates to novel compounds having the formula (I) : and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
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Phenoxiacetic acid derivatives (Fri, 18 Nov 2011)
<p id="p-0001" num="0000">The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.</p>
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HEMIFUMARATE SALT (Fri, 18 Nov 2011)
<p id="p-0001" num="0000">The present invention relates to a hemifumarate salt of the compound (1S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine, Form A thereof and its pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.</p>
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NOVEL HEMIFUMARATE SALT OF ISOINDOLE COMPOUND ACTING AS BACE INHIBITOR (Fri, 18 Nov 2011)
The present invention relates to a hemifumarate salt of the compound (1S)-1-(2- (difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine, Form A thereof and its pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Αβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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Pyrazolylaminopyridine derivatives useful as kinase inhibitors (Thu, 03 Nov 2011)
This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
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Process for the manufacture of 4-fluoro-2-methyl-1H-indol-5-ol (Fri, 21 Oct 2011)
<p id="p-0001" num="0000">The present invention relates to a chemical process for the manufacture of a compound of Formula II</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.35mm" wi="54.78mm" file="US08754240-20140617-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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CHEMICAL COMPOUNDS (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, diabetes and obesity</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.40mm" wi="73.15mm" file="US20110251173A1-20111013-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, X<sub>2</sub>, q, Y<sub>1</sub>, Y<sub>2</sub>, n, Q and Z are as defined in the description.</p>
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PROCESS FOR THE PREPARATION OF 2-(6-SUBSTITUTED-1,-3-DIOXANE-4-YL) ACETIC ACID DERIVATIVES (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">The invention relates to the preparation of 2-(6-substituted-1,3-dioxane-4-yl)acetic acid derivatives of formula (1), where X stands for a leaving group, and R<sub>1</sub>, R<sub>2</sub>, and R<sub>3 </sub>each independently stand for an alkyl group with 1-3 carbon atoms from 4-hydroxy-6-X-substituted-methyl-tetrahydropyran-2-one compounds, where X is as defined above, with the aid of an acetalization agent, in the presence of an acid catalyst. The invention also relates to the novel compounds of formula (1) as well as salts and acids to be prepared from these, with the OR<sub>3 </sub>group in formula (1) being replaced by an OY group, where X, R<sub>1 </sub>and R<sub>2 </sub>have the meanings defined above and where Y stands for an alkaline (earth) metal or a substituted or unsubstituted ammonium group or stands for hydrogen, and to the novel compounds of formula (2). The products concerned are, after conversion into the t-butyl ester of 2-(6-hydroxymethyl-1,3-dioxane-4-yl)acetic acid, important as intermediary products in the preparation of statins.</p>
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PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST (Fri, 07 Oct 2011)
<p id="p-0001" num="0000">The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist selected, and a second active ingredient which is a β<sub>2</sub>-adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.</p>
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2-HYDROXY-ETHANESULFONATE SALT (Fri, 07 Oct 2011)
<p id="p-0001" num="0000">The invention provides (R)-1-[3-(R)-cyclohexyl-hydroxy-phenyl-methyl)-isoxazol-5-ylmethyl]-3-(3-fluoro-phenoxy)-1-azonia-bicyclo[2.2.2]octane 2-hydroxy ethanesulfonate, pharmaceutical compositions containing the compound and its use as a muscarinic antagonists, for the treatment of chronic obstructive pulmonary disease.</p>
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Fused, spirocyclic heteroaromatic compounds for the treatment of bacterial infections (Fri, 07 Oct 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.26mm" wi="59.52mm" file="US08658641-20140225-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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4 -AMINO -7,8- DIHYDROPYRIMIDO [5, 4 - F] [1, 4] OXAZEPIN- 5 ( 6H) - ONE BASED DGAT1 INHIBITORS (Fri, 07 Oct 2011)
DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro- drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, diabetes and obesity wherein, R1, R2, R3, R4, X2, q, Y1, Y2, n, Q and Z are as defined in the description.
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Quinazoline Derivatives as Antiproliferative Agents (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">The invention concerns quinazoline derivatives of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.17mm" wi="69.85mm" file="US20110237610A1-20110929-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein each of R<sup>1a</sup>, R<sup>1b</sup>, R<sup>2</sup>, R<sup>3 </sup>and a have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.</p>
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4H- [1, 2, 4] TRIAZOLO [5, 1 -B] PYRIMIDIN-7 -ONE DERIVATIVES AS CCR2B RECEPTOR ANTAGONISTS (Fri, 23 Sep 2011)
The present invention relates to novel compounds for use in the compositions, to processes for their preparation, to intermediates useful in their preparation and to their use as therapeutic agents. The present invention also relates to pharmaceutical compositions, which comprise compounds that act via antagonism of the CCR2b receptor for which MCP-1 is one of the known ligands and so may be used to treat inflammatory disease, atherosclerosis, diabetes, obesity, cancer, chronic obstructive pulmonary disease (COPD) rheumatoid arthritis and/or neuropathic pain, which is mediated by these receptors.
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Novel Crystalline Form (Fri, 16 Sep 2011)
<p id="p-0001" num="0000">Crystalline Forms of 6-[2-(4-cyano-phenyl)-2H-pyrazol-3-yl]-5-methyl-3-oxo-4-(3-trifluoromethyl-phenyl)-3,4-dihydro-pyrazine-2-carboxylic acid ethylamide are disclosed together with processes for preparing the Forms, pharmaceutical compositions comprising the Forms, and the use of the Forms in therapy.</p>
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Pyrazole derivatives as 11-beta-HSD1 inhibitors (Fri, 16 Sep 2011)
<p id="p-0001" num="0000">A compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.91mm" wi="59.44mm" file="US08344016-20130101-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described. </p>
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POLYMORPHIC FORMS OF 6- [2- (4 -CYANOPHENYL) - 2H - PYRAZOL - 3 - YL] - 5 -METHYL - 3 - OXO - 4 - (TRIFLUOROMETHYL - PHENYL) 3,4-DIHYDROPYRAZINE-2-CARBOXYLIC ACID ETHYLAMIDE (Fri, 16 Sep 2011)
Crystalline Forms of 6- [2- (4 - cyano -phenyl) - 2H -pyrazol - 3 -yl] - 5 -methyl - 3 - oxo - 4 - (3- trifluoromethyl -phenyl) - 3, 4 - dihydro -pyrazine - 2 - carboxylic acid ethylamide are disclosed together with processes for preparing the Forms, pharmaceutical compositions comprising the Forms, and the use of the Forms in therapy as neutrophil elastase inhibitors for the treatment of inflammatory diseases.
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Combination of beta-adrenoceptor agonist and corticosteroid (Thu, 15 Sep 2011)
The invention provides a pharmaceutical product comprising a first active ingredient which is N -[2-(Diethylamino)ethyl]- N -(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-naphthyl)ethoxy]propanamide or a salt thereof, and a second active ingredient which is a corticosteroid.
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HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF (Thu, 15 Sep 2011)
This invention relates to a series of novel heterocyclic compounds that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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CHEMICAL COMPOUNDS 251 (Fri, 09 Sep 2011)
<p id="p-0001" num="0000">The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.35mm" wi="50.29mm" file="US20110218182A1-20110908-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Triazolo pyrimidine compounds (Fri, 09 Sep 2011)
<p id="p-0001" num="0000">The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.59mm" wi="71.63mm" file="US08273879-20120925-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BINDING MEMBERS FOR IGE MOLECULES (Fri, 02 Sep 2011)
<p id="p-0001" num="0000">This invention relates to binding members, especially antibody molecules, for IgE. The binding members are useful for, inter alia, treatment of disorders mediated by IgE including allergies and asthma.</p>
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Process for preparing rosuvastatin (Thu, 01 Sep 2011)
A process for formation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, via a Heck reaction is described. Intermediates useful in the process and processes for making said intermediates are also described.
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Heterocyclic Inhibitors of MEK and methods of use thereof (Thu, 01 Sep 2011)
This invention relates to a series of novel heterocyclic compounds that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. This invention also relates to a method of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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SOLID FORMS OF 4--N,N-DIETHYLBENZAMIDE, COMPOSITIONS THEREOF, AND USES THEREWITH (Fri, 26 Aug 2011)
<p id="p-0001" num="0000">Solid forms comprising salts of 4-{(R)-(3-aminophenyl)[4-(4-fluorobenzyl)piperazin-1-yl]methyl}-N,N-diethylbenzamide, compositions comprising the solid forms, methods of making the solid forms, and methods of their use for the treatment of various diseases and/or disorders are provided herein.</p>
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PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A SECOND ACTIVE INGREDIENT (Fri, 26 Aug 2011)
<p id="p-0001" num="0000">The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist, and a second active ingredient which is selected from a phosphodiesterase inhibitor, a modulator of chemokine receptor function, an inhibitor of kinase function, a protease inhibitor, a steroidal glucocorticoid receptor agonist, a non-steroidal glucocorticoid receptor agonist and a purinoceptor antagonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.</p>
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SOLID FORMS COMPRISING A CYCLOPROPYL AMIDE DERIVATIVE (Fri, 26 Aug 2011)
This disclosure relates to at least one solid form of 4-{(1S, 2S)-2-[((R)-4- cyclobutyl-2-methylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide. This disclosure also relates to at least one pharmaceutical composition comprising at least one solid form described herein, methods of using the solid forms and pharmaceutical compositions comprised thereof, and processes of manufacturing the solid forms.
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PROCESSES FOR MAKING CYCLOPROPYL AMIDE DERIVATIVES AND INTERMEDIATES ASSOCIATED THEREWITH (Fri, 26 Aug 2011)
Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition.
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NEW CRYSTALLINE FORM OF A CYCLOPROPYL BENZAMIDE DERIVATIVE (Fri, 26 Aug 2011)
The present invention relates to a crystalline form of compound (I), 4-{(1S, 2S)-2-[(4-cyclobutylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide, (I) pharmaceutical formulations containing said compound and to the use of said active compound in therapy.
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NEW CRYSTALLINE FORM OF A CYCLOPROPYL BENZAMIDE DERIVATIVE (Fri, 26 Aug 2011)
The present invention relates to a crystalline form of compound (I), 4-{(1S, 2S)-2-[(4-cyclobutylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide, (I) pharmaceutical formulations containing said compound and to the use of said active compound in therapy.</p>
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SOLID FORMS COMPRISING A CYCLOPROPYL AMIDE DERIVATIVE (Fri, 26 Aug 2011)
This disclosure relates to at least one solid form of 4-{(1S, 2S)-2-[((R)-4- cyclobutyl-2-methylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide. This disclosure also relates to at least one pharmaceutical composition comprising at least one solid form described herein, methods of using the solid forms and pharmaceutical compositions comprised thereof, and processes of manufacturing the solid forms.</p>
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PROCESSES FOR MAKING CYCLOPROPYL AMIDE DERIVATIVES AND INTERMEDIATES ASSOCIATED THEREWITH (Fri, 26 Aug 2011)
Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition.</p>
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HETEROCYCLIC JAK KINASE INHIBITORS (Fri, 19 Aug 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.01mm" wi="56.56mm" file="US20110201628A1-20110818-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Salt forms of (2S)-(4E)-N-Methyl-5-[(5-Isopropoxy)pyridin-3-yl]-4-penten-2-amine (Thu, 18 Aug 2011)
Phosphoric acid, edisylic acid (1,2-ethanedisulfonic acid), citric acid, orotic acid (uracil-6-carboxylic acid), R-mandelic acid, sulfuric acid, 1,5-naphthalenedisulfonic acid, D-aspartic acid, and lysine monohydrochloride salts of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine, and methods for their preparation, pharmaceutical compositions comprising said salts, and use, are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
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Isoindolone compounds and their use as metabotropic glutamate receptor potentiators (Thu, 18 Aug 2011)
The present invention is directed to compounds of formula I: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
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COMBINATIONS OF MEK AND HH INHIBITORS (Fri, 12 Aug 2011)
The present invention relates to a therapeutic combination comprising a MEK inhibitor and an HH- pathway inhibitor, and to methods for the production of an anti- cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to: a therapeutic combination comprising a MEK inhibitor and an HH- pathway inhibitor; a combination product comprising a MEK inhibitor and an HH- pathway inhibitor, a kit of parts comprising a MEK inhibitor and an HH- pathway inhibitor; use of a therapeutic combination, combination product or kit of parts in the treatment of cancer; a method of treating cancer comprising administering the therapeutic combination, combination product or kit of parts to a patient. The therapeutic combination and methods of the invention are also useful in the treatment of conditions in which the inhibition of MEK and/or the HH-pathway is beneficial.
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CHEMICAL COMPOUNDS (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-IR kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.64mm" wi="69.85mm" file="US20110190272A1-20110804-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TRICYCLIC 2,4-DIAMINO-L,3,5-TRIAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF CANCER AND MYELOPROLIFERATIVE DISORDERS (Fri, 29 Jul 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula (I): (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.11mm" wi="64.35mm" file="US20110183954A1-20110728-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PYRAZINE DERIVATIVES (Fri, 29 Jul 2011)
The invention concerns pyrazine derivatives of the Formula (I) or pharmaceutically-acceptable salts thereof; wherein each of n, m and R has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of bone-related disorders or conditions.
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PYRAZINE DERIVATIVES (Fri, 29 Jul 2011)
The invention concerns pyrazine derivatives of the Formula (I) or pharmaceutically-acceptable salts thereof; wherein each of n, m and R has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of bone-related disorders or conditions.</p>
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SPIRO CONDENSED BARBITURIC ACID DERIVATIVES FOR USE AS ANTIBACTERIAL (Fri, 22 Jul 2011)
<p id="p-0001" num="0000">In one aspect, the present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to method for their preparation.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.21mm" wi="59.86mm" file="US20110178064A1-20110721-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Quinuclidine derivatives as muscarinic M3 receptor antagonists (Fri, 15 Jul 2011)
<p id="p-0001" num="0000">The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.59mm" wi="69.85mm" file="US08329729-20121211-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PROCESS FOR MAKING A METABOTROPIC GLUTAMATE RECEPTOR POSITIVE ALLOSTERIC MODULATOR - 874 (Fri, 15 Jul 2011)
Processes for making 7-methyl-5-(3piperazin-1-ylmethyl-[1,2,4]oxadiazol-5-yl)-2-(4- trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one
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PROCESS FOR MAKING A METABOTROPIC GLUTAMATE RECEPTOR POSITIVE ALLOSTERIC MODULATOR - 874 (Fri, 15 Jul 2011)
Processes for making 7-methyl-5-(3piperazin-1-ylmethyl-[1,2,4]oxadiazol-5-yl)-2-(4- trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one</p>
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PYRIDINE COMPOUNDS (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.95mm" wi="69.85mm" file="US20110166139A1-20110707-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Steroid Derivatives Acting As Glucocorticosteroid Receptor Agonists (Fri, 01 Jul 2011)
<p id="p-0001" num="0000">The present invention provides compounds of formula (I) wherein n, p, R<sup>1</sup>, R<sup>2</sup>, X<sup>1</sup>, X<sup>2</sup>, X<sup>3</sup>, R<sup>3a</sup>, R<sup>3b</sup>, R<sup>4</sup>, R<sup>5 </sup>and R<sup>6 </sup>are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.03mm" wi="70.19mm" file="US20110160167A1-20110630-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Dibenzothiazepine Derivatives and Use Thereof (Fri, 01 Jul 2011)
<p id="p-0001" num="0000">Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.17mm" wi="57.57mm" file="US20110160184A1-20110630-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Cannabinoid Receptor Ligands (Fri, 01 Jul 2011)
<p id="p-0001" num="0000">Compounds of Formulae (I), or pharmaceutically acceptable salts thereof: wherein R<sup>1</sup>, R<sup>2 </sup>and Y are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.40mm" wi="69.85mm" file="US20110160180A1-20110630-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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PRODUCTION OF ROSUVASTATIN CALCIUM SALT (Fri, 01 Jul 2011)

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Biphenyloxyacetic acid derivatives for the treatment of respiratory disease (Fri, 24 Jun 2011)
<p id="p-0001" num="0000">The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.</p>
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Quinazoline derivatives as tyrosine kinase inhibitors (Fri, 24 Jun 2011)
<p id="p-0001" num="0000">The invention concerns quinazoline derivatives of the Formula I, or pharmaceutically acceptable salts thereof:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.62mm" wi="74.93mm" file="US08735410-20140527-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein each of R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and m are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, and, for example, EGFR tyrosine kinase. </p>
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COMBINATION OF A BENZOXAZINONE AND A FURTHER AGENT FOR TREATING RESPIRATORY DISEASES (Fri, 24 Jun 2011)
The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclohexyl-N-(2-(2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethylamino)ethyl)-3-(3-(1-methyl-1H-pyrazol-4- yl)phenethoxy)propanamide or a pharmaceutically acceptable salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist; a p38 inhibitor; a PDE inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease (for example chronic obstructive pulmonary disease (COPD) or asthma).
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QUATERNARY PIPERIDINE COMPOUNDS AND USES THEREOF (Fri, 24 Jun 2011)
This invention generally relates to quaternary piperidine compounds, particularly (S)-N-(2-(3-(4-chlorophenyl)piperidin-3-yl)etriyl)- l,l,l-trifluoro-2-methylpropan-2- amine and salts thereof. This invention also relates to pharmaceutical compositions comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), and processes for making such a compound.
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METHOD OF TREATING SCHIZOPHRENIA AND OTHER DISORDERS (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">A method of treating at least one symptom or condition associated with but not limited to: 1) Schizophrenia and other Psychotic Disorders including but not limited to Psychotic Disorder, Schizophreniform Disorder, Schizoaffective Disorder, Delusional Disorder, Brief Psychotic Disorder, Shared Psychotic Disorder, and Psychotic Disorder Due to a General Medical Condition and 2) Dementia and other Cognitive Disorders comprising administering an effective amount of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.33mm" wi="57.91mm" file="US20110144089A1-20110616-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or its pharmaceutically acceptable salt. In another aspect of the invention a pharmaceutical composition is provided comprising an effective amount of Formula I or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier or diluent.</p>
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Cinnoline Compounds for the Treatment of Anxiety, Cognitive and Mood Disorders (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">This invention relates to novel compounds having the structural formula I below:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.36mm" wi="42.25mm" file="US20110144331A1-20110616-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of anxiety disorders, cognitive disorders, and/or mood disorders.</p>
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Use of thioxanthine derivatives as MPO inhibitors (Thu, 16 Jun 2011)
A compound of formula (Ia) or (Ib) wherein X is S; Y is O; R 2 is C1 to 6 alkyl substituted by C1 to 6 alkoxy; and R 1 R 3 and R 4 are all hydrogen, or a pharmaceutically acceptable salt thereof, the preparation of such compounds, compositions comprising such compounds, and the use of such compounds in the treatment of MPO mediated disease states.
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Method of Treating Anxiety Disorders (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">A method of treating at least one symptom or condition associated with but not limited to: Anxiety Disorders including but not limited to Panic Disorder Without Agoraphobia, Panic Disorder With Agoraphobia, Agoraphobia Without History of Panic Disorder, Specific Phobia, Social Phobia, Obsessive-Compulsive Disorder, Postaumatic Stress Disorder, Acute Stress Disorder, Generalized Anxiety Disorder and Generalized Anxiety Disorder Due to a General Medical Condition comprising administering an effective amount of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.48mm" wi="57.74mm" file="US20110136784A1-20110609-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or its pharmaceutically acceptable salt. In another aspect of the invention a pharmaceutical composition is provided comprising an effective amount of Formula I or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier or diluent.</p>
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Nicotinic Acetylcholine Receptor Ligands 101 (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">Nicotinic acetylcholine receptor ligands of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="21.00mm" wi="69.85mm" file="US20110136804A1-20110609-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein X, n, R<sup>1 </sup>and R<sup>2 </sup>are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing, and methods for using the same.</p>
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Novel Compounds (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">The present invention provides compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.37mm" wi="69.85mm" file="US20110136801A1-20110609-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein R<sup>a</sup>, R<sup>b</sup>, R<sup>c</sup>, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, X<sup>1</sup>, Y<sup>1</sup>, Z<sup>1</sup>, A, n and m are as defined in the specification, <br/> and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy. </li> </ul> </li> </ul> </p>
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Heterocyclic Compounds as CCR2 Antagonists (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">Compounds of formula (I)</p> <p id="p-0002" num="0000"> <br/> <?in-line-formulae description="In-line Formulae" end="lead"?>Q-L-W—C(═X)—Z—P<?in-line-formulae description="In-line Formulae" end="tail"?> </p> <p id="p-0003" num="0000">wherein <br/> Q is an amine of the formula —N(R<sup>1</sup>)(R<sup>2</sup>); <br/> L is an alkyl or heterocyclyl-alkyl linker; <br/> W is a 6- or 7-membered aliphatic ring comprising ring atoms Y<sup>1 </sup>and Y<sup>2 </sup>which are linked to groups L and C(X) respectively and Y<sup>1 </sup>and Y<sup>2 </sup>are independently selected from N and C; <br/> X is O, N, N—CN or S; <br/> Z is NR<sup>3</sup>; <br/> P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; <br/> and pharmaceutically acceptable salts or solvates thereof, <br/> are useful in the treatment of C—C chemokine mediated conditions. </p>
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Benzimidazole derivatives (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">Provided herein are compounds in accord with Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.82mm" wi="70.02mm" file="US08093402-20120110-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> that are useful in the treatment of pain. </p>
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Chemical Process For Preparation Of Intermediates (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure trans-cyclopropane carboxylic acid derivatives, processes for preparing the carboxylic acid derivatives and their use in preparing pharmaceuticals.</p>
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DPP-IV resistant GIP hybrid polypeptides with selectable properties (Fri, 10 Jun 2011)
<p id="p-0001" num="0000">The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and/or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.</p>
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CO - CRYSTALS OF A TRIAZOLO [4,5 - D] PYRIMIDINE PLATELET AGGREGATION INHIBITOR (Fri, 10 Jun 2011)
The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4- hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2- methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).
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IMIDAZOQUINOLINES WHICH ACT VIA TOLL - LIKE RECEPTORS (TLR) (Fri, 10 Jun 2011)
The present invention provides compounds of formula (I): wherein Ra, Rb, Rc, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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CO - CRYSTALS OF A TRIAZOLO [4,5 - D] PYRIMIDINE PLATELET AGGREGATION INHIBITOR (Fri, 10 Jun 2011)
The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4- hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2- methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).</p>
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SOLID FORMS OF 4-{(R)-(3-AMINOPHENYL)[4-(4-FLUOROBENZYL)-PIPERAZIN-1-YL]METHYL}-N,N-DIETHYLBENZAMIDE, COMPOSITIONS THEREOF, AND USES THEREWITH (Sat, 04 Jun 2011)
Solid forms comprising salts of 4-{(R)-(3-aminophenyl)[4-(4-fluorobenzyl)piperazin-1- yl]methyl}-N,N-diethylbenzamide, compositions comprising the solid forms, methods of making the solid forms, and methods of their use for the treatment of various diseases and/or disorders are provided herein.
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Novel Sulphonamide Derivatives as Glucocorticoid Receptor Modulators for the Treatment of Inflammatory Diseases (Fri, 03 Jun 2011)
<p id="p-0001" num="0000">A compound of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="16.51mm" wi="60.62mm" file="US20110130426A1-20110602-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Heterocyclic Carboxamides For Use As Thrombin Inhibitors (Fri, 03 Jun 2011)
<p id="p-0001" num="0000">This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production. Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.88mm" wi="69.85mm" file="US20110130432A1-20110602-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Pyrimidine sulphonamide derivatives as chemokine receptor modulators (Fri, 27 May 2011)
<p id="p-0001" num="0000">A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.84mm" wi="58.00mm" file="US08269002-20120918-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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BENZOIMIDAZOLE COMPOUNDS AND USES THEREOF (Fri, 27 May 2011)
This invention generally relates to substituted benzoimidazole compounds, particularly methyl 2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-5-methyl-1H- benzo[d]imidazol-1-yl)methyl)morpholine-4-carboxylate and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.
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COMBINATIONS COMPRISING A GLUCOCORTICOID RECEPTOR MODULATOR FOR THE TREATMENT OF RESPIRATORY DISEASES (Fri, 27 May 2011)
The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a glucocorticoid receptor modulator and a second active ingredient selected from an Adenosine A2A receptor antagonist, an anti-infective, an antioxidant, a β2 adrenoceptor agonist, a CCR1 antagonist, a chemokine antagonist, a muscarinic antagonist, a glucocorticosteroid, a CRTh2 antagonist, a DP1 antagonist, a formyl peptide receptor antagonist, a Histone Deacetylase activator, a chloride channel hCLCA1 blocker, an Epithelial sodium channel blocker, an Inter-cellular adhesion molecule 1 blocker, an IKK2 kinase inhibitor, a JNK kinase inhibitor, a COX inhibitor, a lipoxygenase inhibitor, a leukotriene receptor antagonist, a MEK-1 kinase inhibitor, a MPO inhibitor, a PDE4, inhibitor, a PI 3 kinase γ inhibitor, a PPARγ agonist, a protease inhibitor, a p38 inhibitor, a RARγ modulator, a statin, a thromboxane antagonist and a vasodilator; and its use in the treatment of respiratory disease.
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BENZOIMIDAZOLE COMPOUNDS AND USES THEREOF (Fri, 27 May 2011)
This invention generally relates to substituted benzoimidazole compounds, particularly methyl 2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-5-methyl-1H- benzo[d]imidazol-1-yl)methyl)morpholine-4-carboxylate and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.</p>
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Chemical coupling process with a phenyl boronic acid derivative (Thu, 26 May 2011)
Processes for preparing compounds of Formula I and IV are described.
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2-ANILINOPURIN-8-ONES AS INHIBITORS OF TTK/MPS1 FOR THE TREATMENT OF PROLIFERATIVE DISORDERS (Fri, 20 May 2011)
<p id="p-0001" num="0000">This invention relates to chemical compounds of the formula (I), or a pharmaceutically acceptable salt thereof, which possess inhibitory activity against the spindle checkpoint kinase: Tyrosine Threonine Kinase (TTK)/monopolar spindle 1 (Mps1) and are accordingly useful for their anti-cancer effect in a warm-blooded animal such as man. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them, and to their use in the manufacture of a medicament for the treatment of conditions mediated by TTK/Mps1, for use either alone or in combination with other anti-pro liferative agents.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.96mm" wi="64.94mm" file="US20110118238A1-20110519-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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OXAZOLO[4,5-c]PYRIDINE SUBSTITUTED PYRAZINE (Fri, 20 May 2011)
<p id="p-0001" num="0000">The present invention 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="33.27mm" wi="75.01mm" file="US20110118275A1-20110519-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein <br/> R<sup>1 </sup>is hydrogen or methyl, or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, to the use of said active compound in therapy, as well as intermediates. </p>
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OXAZOLO[4,5-C]PYRIDINE SUBSTITUTED PYRAZINE (Fri, 20 May 2011)
The present invention relates to a compound of formula (I), wherein R1 is hydrogen or methyl, or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, to the use of said active compound in therapy, as well as intermediates.
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Intermediates (Thu, 19 May 2011)
The invention provides compounds for the preparation of new triazolo[4,5 -d ]pyrimidine compounds of formula (I),
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METHODS OF PREPARING SUBSTITUTED HETEROCYCLES (Fri, 13 May 2011)
<p id="p-0001" num="0000">The present disclosure relates to methods of preparing substituted thiophenes, which are useful for the treatment and prevention of cancers. Also disclosed are substituted thiophenes made by the methods disclosed herein.</p>
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5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES FOR THE SELECTIVE INHIBITION OF CHEMOKINE RECEPTORS (Fri, 06 May 2011)
<p id="p-0001" num="0000">There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.50mm" wi="67.31mm" file="US20110105537A1-20110505-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX<sub>3</sub>CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.</p>
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CHROMENONE DERIVATIVES WITH ANTI-TUMOUR ACTIVITY (Fri, 06 May 2011)
The invention concerns chromenone derivatives of Formula (I) or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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CHROMENONE DERIVATIVES WITH ANTI-TUMOUR ACTIVITY (Fri, 06 May 2011)
The invention concerns chromenone derivatives of Formula (I) or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.</p>
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Chromenone derivatives (Fri, 29 Apr 2011)
<p id="p-0001" num="0000">The invention concerns chromenone derivatives of Formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="68.92mm" wi="76.20mm" file="US08399460-20130319-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically-acceptable salts thereof, wherein each of R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, n and R<sup>9 </sup>has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders. </p>
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New Compounds Useful for Treating CNS Disorders (Fri, 29 Apr 2011)
<p id="p-0001" num="0000">The present invention provides new compounds of formula (I) as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.06mm" wi="67.73mm" file="US20110098292A1-20110428-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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CYCLIC AMINE DERIVATIVES HAVING BETA2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY (Fri, 29 Apr 2011)
Compounds of formula (I) having activities at muscarinic and β2-receptors (MABAs) for use in therapy.
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ADAMANTYL IMINOCARBONYL-SUBSTITUTED PYRIMIDINES AS INHIBITORS OF 1 1 BETAHSD1 (Fri, 29 Apr 2011)
A compound of formula (I): and pharmaceutically acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.
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Compounds for the treatment of multi-drug resistant bacterial infections (Fri, 22 Apr 2011)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula V(A):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.76mm" wi="69.34mm" file="US08124602-20120228-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds of Formula V(A) useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. </p>
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5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES AS CHEMOKINE INHIBITORS (Fri, 22 Apr 2011)
<p id="p-0001" num="0000">There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>5 </sup>are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX<sub>3</sub>CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.</p>
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Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1 826 (Fri, 22 Apr 2011)
<p id="p-0001" num="0000">A compound of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="42.33mm" wi="62.23mm" file="US20110092526A1-20110421-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and pharmaceutically-acceptable salts thereof, wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described herein.</p>
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Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists (Thu, 21 Apr 2011)
The present invention relates to new compounds of formula 1, to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
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Thiopyrimidine derivative, useful as an intermediate for chemokine receptor modulators. (Thu, 21 Apr 2011)
The compound 4-chloro-2-[(2,3-difluorobenzyl)thio]-6-{(1R)-I-[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]ethoxy}pyrimidine.
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Combination Therapy (Fri, 15 Apr 2011)
<p id="p-0001" num="0000">The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human, which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises one of: the administration of ZD6474 in combination with 5-FU; the administration of ZD6474 in combination with CPT-11; and the administration of ZD6474 in combination with 5-FU and CPT-11; to a pharmaceutical composition comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11; to a combination product comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11, for use in a method of treatment of a human or animal body by therapy; to a kit comprising one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11; to the use of one of: ZD6474 and 5-FU; ZD6474 and CPT-11; and ZD6474 and 5-FU and CPT-11, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.</p>
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DIBENZOTHIAZEPINE DERIVATIVE AND USE THEREOF (Thu, 14 Apr 2011)
Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.
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2-pyridone compounds (Fri, 08 Apr 2011)
<p id="p-0001" num="0000">The invention provides compounds of formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.34mm" wi="69.85mm" file="US08436024-20130507-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, L, X and Y are as defined in the specification; together with processes and intermediates for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase. </p>
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DIARYLMETHYLIDENE PIPERIDINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF (Fri, 08 Apr 2011)
<p id="p-0001" num="0000">Compounds of formula: (I) wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4 </sup>and R<sup>7 </sup>are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="44.20mm" wi="63.58mm" file="US20110082173A1-20110407-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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2-PYRIDONE COMPOUNDS USED AS INHIBITORS OF NEUTROPHIL ELASTASE (Fri, 08 Apr 2011)
The invention provides compounds of formula (I) wherein R1, R3, R4, R5, R6, R7, L, X and Y are as defined in the specification; together with processes and intermediates for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.
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2-PYRIDONE COMPOUNDS USED AS INHIBITORS OF NEUTROPHIL ELASTASE (Fri, 08 Apr 2011)
The invention provides compounds of formula (I) wherein R1, R3, R4, R5, R6, R7, L, X and Y are as defined in the specification; together with processes and intermediates for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.</p>
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Substituted diphenyl-ethers, -amines, -sulfides and -methanes for the treatment of respiratory diseases (Thu, 07 Apr 2011)
The invention relates to substituted aromatic compounds as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
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Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes (Thu, 07 Apr 2011)
Compounds of formula (I) wherein R 1 , HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
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Thiophene and thiazole derivatives as CHK1 inhibitors (Thu, 07 Apr 2011)
This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
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FUMARATE SALT OF 4-(3-CHLORO-2-FLUOROANILINO)-7-METHOXY-6-{[1-(N-METHYLCARBAMOYLMETHYL)PIPERIDIN-4-YL]OXY}QUINAZOLINE (Thu, 07 Apr 2011)
4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.
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COMPOSITIONS WITH AND PROCESS FOR METHYLMORPHOLIN-SUBSITUTED PYRIDO[2,3-D]PYRIMIDINES (Thu, 07 Apr 2011)
There is provided a process for the preparation of a compound of Formula 1,the use of said process in the preparation of a compound of Formula 5 or a phosphate, suolphate, hydrogensulphate, malate, citrate, tartrate or fumarate salt thereof, and the use of the fumarate salt in a composition for use in therapy.
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PYRIDINE COMPOUNDS (Thu, 07 Apr 2011)
The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.
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PROCESS AND CATALYST (Fri, 01 Apr 2011)
Aromatic or heteroaromatic nitro compounds are catalytically hydrogenated to the corresponding amines in the presence of a platinum catalyst comprising elemental platinum on a support; the platinum catalyst is modified with a molybdenum compound and a phosphorus compound wherein the phosphorus has an oxidation state of less than +5, e.g. hypophosphorous acid; the catalyst is particularly useful in the hydrogenation of nitro compounds with halogen and/or sulfur-containing substituents.
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PROCESS AND CATALYST (Fri, 01 Apr 2011)
Aromatic or heteroaromatic nitro compounds are catalytically hydrogenated to the corresponding amines in the presence of a platinum catalyst comprising elemental platinum on a support; the platinum catalyst is modified with a molybdenum compound and a phosphorus compound wherein the phosphorus has an oxidation state of less than +5, e.g. hypophosphorous acid; the catalyst is particularly useful in the hydrogenation of nitro compounds with halogen and/or sulfur-containing substituents.</p>
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Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes (Thu, 31 Mar 2011)
The compound 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1-methylethyl)oxy]- N -1 H- pyrazol-3-ylbenzamide or a salt thereof, pharmaceutical compositions containing it and its use in the treatment of diabetes or obesity.
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Thiopyrimidine derivative, useful as an intermediate for chemokine receptor modulators (Thu, 31 Mar 2011)
The compound N -[2-[[(2,3-difluorophenyl)methyl]thio]-6-[(1 R )-1-[(4 S )-2,2-dimethyl-1,3-dioxolan-4-yl]ethoxy]-4-pyrimidinyl]-1-azetidinesulfonamide.
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Imidazolyl-pyrimidine compounds for use in the treatment of proliferative disorders (Thu, 31 Mar 2011)
Compounds of formula ( I ): which possess cell-cycle inhibitory activity are described.
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Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes (Thu, 31 Mar 2011)
The compound 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1 S )-2-hydroxy-1-methylethyl]oxy}- N -(5-methylpyrazin-2-yl)benzamide or a salt thereof, pharmaceutical compositions containing it and its use in the treatment of diabetes or obesity.
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Chemical compounds 572 (Fri, 25 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="25.91mm" wi="67.39mm" file="US08143290-20120327-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments. </p>
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Process and catalyst (Fri, 25 Mar 2011)
<p id="p-0001" num="0000">Aromatic or heteroaromatic nitro compounds are catalytically hydrogenated to the corresponding amines in the presence of a platinum catalyst comprising elemental platinum on a support; the platinum catalyst is modified with a molybdenum compound and a phosphorus compound wherein the phosphorus has an oxidation state of less than +5, e.g. hypophosphorous acid; the catalyst is particularly useful in the hydrogenation of nitro compounds with halogen and/or sulfur-containing substituents.</p>
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PHENOXYPYRIDINYLAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PDE4 MEDIATED DISEASE STATES (Thu, 24 Mar 2011)
The present invention provides a compound of a formula (I), wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.
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Therapeutic Agents 812 (Fri, 18 Mar 2011)
<p id="p-0001" num="0000">A compound 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="70.19mm" file="US20110065706A1-20110317-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.</p>
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Quinazoline derivatives as VEGF inhibitors (Fri, 18 Mar 2011)
<p id="p-0001" num="0000">The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R<sup>1 </sup>represents halogeno or C<sub>1-3</sub>alkyl; X<sup>1 </sup>represents —O—; R<sup>2 </sup>is selected from one of the following three groups: 1) C<sub>1</sub>-5alkylR<sup>3 </sup>(wherein R<sup>3 </sup>is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C<sub>1-4</sub>alkyl, C<sub>1-4</sub>hydroxyalkyl and C<sub>1-4</sub>alkoxy; 2) C<sub>2-5</sub>alkenylR<sup>3 </sup>(wherein R<sup>3 </sup>is as defined hereinbefore); 3) C<sub>2-5</sub>alkynylR<sup>3 </sup>(wherein R<sup>3 </sup>is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.17mm" wi="69.85mm" file="US08642608-20140204-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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4- (PYRIMIDIN-2-YL) -PIPERAZINE AND 4- (PYRIMIDIN-2-YL) -PIPERIDINE DERIVATIVES AS GPR119 MODULATORS (Fri, 18 Mar 2011)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.
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New Compounds (Fri, 11 Mar 2011)
<p id="p-0001" num="0000">This invention relates to novel compounds having the structural formula I below:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.92mm" wi="50.55mm" file="US20110059992A1-20110310-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.</p>
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4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic Acid - 465 (Fri, 11 Mar 2011)
<p id="p-0001" num="0000">4-[4-(2-Adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid and pharmaceutically-acceptable salts thereof and a particular crystalline form of the Agent (Form 1); their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.</p>
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Pyrazole derivatives as 11-beta-HSD1 inhibitors (Thu, 10 Mar 2011)
A compound of formula (I): and pharmaceutically -acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11²HSD1, processes for making them and pharmaceutical compositions comprising them are also described.
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New crystalline form of a triazolo(4,5-d)pyrimidine compound (Thu, 10 Mar 2011)
The invention provides new forms of a chemical compound, processes for their preparation, their use as medicaments, and compositions containing them.
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Quinazoline compounds (Thu, 10 Mar 2011)
The invention relates to compounds of the formula I: wherein ring C is as defined herein, for example indolyl, indazolyl or azaindolyl; Z is -O-, -NH- or -S-; n is 0-5; m is 0-3; R 1 and R 2 are defined herein including groups: (i) Q 1 X 1 wherein Q 1 and X 1 are as defined herein; (ii) Q15W 3 wherein Q 15 and W 3 are as defined herein, (iii) Q 21 W 4 C 1-5 alkylX 1 - wherein Q 21 , W 4 and X 1 are as defined herein, (iv) Q 28 C 1-5 alkylX 1 -, Q 28 C 2-5 alkenylX 1- or Q 28 C 2-5 alkynylX 1 - wherein Q 28 and X 1 are as defined herein and (v) Q 29 C 1-5 alkylX 1 -, Q 29 C 2-5 alkenylX 1 - or Q 29 C 2-5 alkynylx 1 - wherein Q 29 and X 1 are as defined herein; R 2 can also be 6,7-methylenedioxy or 6,7-ethylenedioxy; and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals; processes for the preparation of such compounds; intermediates used in such processes; processes for making such intermediates; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof. The compounds of formula I inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
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CHEMICAL COMPOUNDS 610 (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">There is provided pyrimidinyl indole compounds of Formula (I),</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.43mm" wi="60.28mm" file="US20110053923A1-20110303-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.</p>
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NOVEL DIAZASIPIROAKANES AND THEIR USE FOR TREATMENT OF CCR8 MEDIATED DISEASES (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">The invention provides compounds of general formula. (II) wherein R and <img id="CUSTOM-CHARACTER-00001" he="2.46mm" wi="1.78mm" file="US20110053969A1-20110303-P00001.TIF" alt="custom-character" img-content="character" img-format="tif"/> are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.85mm" wi="58.17mm" file="US20110053969A1-20110303-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Compounds—801 (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">Spirocyclic amide derivatives of formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="51.22mm" wi="76.20mm" file="US08455483-20130604-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein <br/> ArCH<sub>2</sub>CH<sub>2</sub>NH— represents a β-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation. </p>
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HETEROCYCLIC UREA DERIVATIVES USEFUL FOR TREATMENT OF BACTERIAL INFECTION (Fri, 04 Mar 2011)
Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
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Compounds for the treatment of multi-drug resistant bacterial infections (Thu, 03 Mar 2011)
The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
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PYRIMIDINE DERIVATIVES (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R<sup>1</sup>, ring A, n, R<sup>3</sup>, and R<sup>4 </sup>are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4, and/or EphA2 and/or Src kinases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.66mm" wi="70.19mm" file="US20110046108A1-20110224-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMBINATION OF A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist selected, and a second active ingredient which is a β<sub>2</sub>-adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.</p>
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METHOD FOR PREPARING ADENINE COMPOUND (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">A method for producing adenine compound (1):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.59mm" wi="71.80mm" file="US20110046369A1-20110224-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein m and n are independently an integer of 2 to 5, R<sup>1 </sup>is C<sub>1-6 </sub>alkyl group, R<sup>2 </sup>and R<sup>3 </sup>are the same or different, and hydrogen atom, or C<sub>1-6 </sub>alkyl group, or R<sup>2 </sup>and R<sup>3 </sup>are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R<sup>4 </sup>is C<sub>1-3 </sub>alkyl group, <br/> which comprises a step of reacting compound (2): </p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="26.42mm" wi="63.25mm" file="US20110046369A1-20110224-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">and compound (3):</p> <p id="p-0006" num="0000"><chemistry id="CHEM-US-00003" num="00003"> <img id="EMI-C00003" he="19.05mm" wi="56.64mm" file="US20110046369A1-20110224-C00003.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0007" num="0000">in the presence of a boron-containing reducing agent.</p>
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Pharmaceutical process and intermediates 714 (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="75.01mm" wi="62.82mm" file="US08227622-20120724-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">X is ═O, ═N—OH or ═N—OC(O)Me; Y is hydrogen, PhS- or p-chlorophenylsulfanyl; Z is hydrogen or —CH<sub>2</sub>COOR<sup>1 </sup>wherein R<sup>1 </sup>is selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.</p>
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CINNOLINE COMPOUNDS, THEIR PREPARATION, AND THEIR USE (Fri, 25 Feb 2011)
The present invention relates to cinnoline compounds, particularly 4-amino-N-cyclopropyl- 7-fluoro-8-(3,6-dimethoxypyridazin-4-yl)cinnoline-3-carboxamide and salts thereof. The claimed invention also relates to compositions comprising such a compound, as well as uses of and processes for production of said compounds. The claimed cinnoline compounds are GABAA modulators useful in the treatment of anxiety disorders, cognitive disorders, mood disorders, schizophrenia and pain.
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Treatment of obesity and related diseases (Thu, 24 Feb 2011)
Methods for treating obesity or obesity related disorders are disclosed. These methods include the use of anti-obesity agents directed to the forebrain in combination with anti-obesity agents directed to the hindbrain.
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Treatment of obesity and related diseases (Thu, 24 Feb 2011)
Methods for treating obesity or obesity related disorders are disclosed. These methods include the use of anti-obesity agents directed to the forebrain in combination with anti-obesity agents directed to the hindbrain.
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Treatment of obesity and related disorders (Thu, 24 Feb 2011)
Methods for treating obesity or obesity related disorders are disclosed. These methods include the use of anti-obesity agents directed to the forebrain in combination with anti-obesity agents directed to the hindbrain.
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Treatment of obesity and obesity related diseases (Thu, 24 Feb 2011)
Methods for treating obesity or obesity related disorders are disclosed. These methods include the use of anti-obesity agents directed to the forebrain in combination with anti-obesity agents directed to the hindbrain.
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4-(phenyl-piperazinyl-methyl)benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders (Fri, 18 Feb 2011)
<p id="p-0001" num="0000">The invention relates to at least one compound of general formula I</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.99mm" wi="69.85mm" file="US08022074-20110920-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R<sup>1 </sup>phenyl and R<sup>1 </sup>heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF<sub>3</sub>, methyl, iodo, bromo, fluoro, and chloro; R<sup>2 </sup>is independently selected from ethyl and isopropyl; <br/> R<sup>3 </sup>is hydrogen or fluoro; R<sup>4 </sup>is —NH<sub>2 </sub>or —NHSO<sub>2</sub>R<sup>5</sup>; and R<sup>5 </sup>is hydrogen, —CF<sub>3</sub>, or C<sub>1</sub>-C<sub>6 </sub>alkyl, or pharmaceutically acceptable salts thereof; at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one δ receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I. </p>
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BENZAMIDE DERIVATIVES AND THEIR USE AS GLUCOKINASE ACTIVATING AGENTS (Fri, 11 Feb 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="34.46mm" wi="67.90mm" file="US20110034432A1-20110210-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein: <br/> R<sup>1 </sup>is methoxymethyl; <br/> R<sup>2 </sup>is selected from —C(O)NR<sup>4</sup>R<sup>5</sup>, —SO<sub>2</sub>NR<sup>4</sup>R<sup>5</sup>, —S(O)<sub>p</sub>R<sup>4 </sup>and HET-2; <br/> HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; <br/> HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; <br/> R<sup>3 </sup>is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; <br/> R<sup>4 </sup>is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; <br/> R<sup>5 </sup>is hydrogen or (1-4C)alkyl; <br/> or R<sup>4 </sup>and R<sup>5 </sup>together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; <br/> HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; <br/> p is (independently at each occurrence) 0, 1 or 2; <br/> m is 0 or 1; <br/> n is 0, 1 or 2; <br/> provided that when m is 0, then n is 1 or 2; <br/> or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described. </p>
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4-(Acetylamino)-3-[(4-chlorophenyl)thio]-2-methyl-1H-indole-1-acetic acid ethyl ester intermediate compound (Thu, 10 Feb 2011)
The present invention relates to the compound 4-(acetylamino)-3-[(4-chlorophenyl)thio]-2- methyl-1 H -indole-acetic acid ethyl ester as intermediate for the preparation of 4-(acetylamino)-3-[(4-chlorophenyl)thio]-2-methyl-1 H -indole-acetic acid which is a modulator of the CRTh2 receptor activity useful for the treatment of respiratory disorders.
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COMBINATION THERAPY 238 (Fri, 04 Feb 2011)
<p id="p-0001" num="0000">There is provided a combination product comprising a VEGFR tyrosine kinase inhibitor and a m TOR-selective kinase inhibitor, and methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient.</p>
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NOVEL CRYSTALLINE FORMS OF 4-[4-(2-ADAMANTYLCARBAMOYL)-5-TERT-BUTYL-PYRAZOL-1-YL]BENZOIC ACID 471 (Fri, 04 Feb 2011)
<p id="p-0001" num="0000">New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.</p>
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NOVEL CRYSTALLINE FORMS OF 4-[4-(2-ADAMANTYLCARBAMOYL)-5-TERT-BUTYL-PYRAZOL-1-YL]BENZOIC ACID 471 (Fri, 04 Feb 2011)
<p id="p-0001" num="0000">New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.</p>
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NOVEL ADENINE COMPOUND (Fri, 04 Feb 2011)
<p id="p-0001" num="0000">A novel adenine compound represented by the formula (1):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.14mm" wi="63.42mm" file="US20110028715A1-20110203-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L<sup>1 </sup>and L<sup>2 </sup>each independently represents straightened or branched alkylene, etc.; R<sup>1 </sup>represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R<sup>2 </sup>and R<sup>3 </sup>each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R<sup>2 </sup>combines together with L<sup>2 </sup>or R<sup>3 </sup>to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO<sub>2</sub>, NR<sup>7</sup>, NR<sup>7</sup>CO wherein R<sup>7 </sup>is hydrogen or alkyl, or a single bond; provided that X is a single bond when R<sup>1 </sup>is halogen, or a pharmaceutically acceptable salt thereof. The compound and salt are useful as a medicine.</p>
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SPIROCYCLIC AMIDE DERIVATIVES (Fri, 04 Feb 2011)
Spirocyclic amide derivatives of formula (I) wherein ArCH2CH2NH- represents a β-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.
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NEW COMBINATIONS FOR THE TREATMENT OF ASTHMA (Fri, 04 Feb 2011)
The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is (R)-7-(2-(2-fluoro-5-((4-(2-isopropylthiazole-4-carbonyl)-1-oxa-4,9-diazaspiro[5.5]undecan-9-yl)methyl)phenethylamino)-1-hydroxyethyl)-4- hydroxybenzo[d]thiazol-2(3H)-one or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a PDE4 inhibitor; a PPARγ agonist; a protease inhibitor; a p38 inhibitor, a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
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COMPOUNDS - 801 (Fri, 04 Feb 2011)
Spirocyclic amide derivatives of formula (I) wherein ArCH2CH2NH- represents a ß-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.</p>
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Bis-(Sulfonylamino) Derivatives in Therapy 066 (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">The invention provides compounds of formula wherein R<sup>1</sup>, R<sup>3</sup>, L<sup>1</sup>, L<sup>2</sup>, G<sup>1</sup>, G<sup>2</sup>, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.16mm" wi="66.46mm" file="US20110021540A1-20110127-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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PHTHALAZINONE COMPOUND (Fri, 21 Jan 2011)
<p id="p-0001" num="0000">4-(4-Fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one as crystalline Form C.</p>
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PHTHALAZINONE COMPOUND AS PARP INHIBITOR (Fri, 21 Jan 2011)
4-(4-Fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one as crystalline Form C.
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Process 054 (Fri, 14 Jan 2011)
<p id="p-0001" num="0000">The present invention is directed to a process for the preparation of a diastereomerically pure dibenzoyl-L-tartrate salt of a compound of formula (III)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.33mm" wi="52.75mm" file="US20110009647A1-20110113-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and to products of said process.</p>
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