Astrazeneca - organic-reaction.com

PYRAZINE DERIVATIVES (Fri, 17 May 2013)
The invention concerns pyrazine derivatives of the Formula I <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> 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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(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)
This invention relates to novel compounds having the formula (I): <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> and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
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TRISUBSTITUTED TRIAZOLOPYRIMIDINES FOR USE IN PLATELET AGGREGATION INHIBITION (Fri, 22 Mar 2013)
The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
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AMIDE DERIVATIVES BEARING A CYCLOPROPYLAMINOACARBONYL SUBSTITUENT USEFUL AS CYTOKINE INHIBITORS (Fri, 08 Feb 2013)
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.
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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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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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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 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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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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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)
The present invention relates to pyrazinone derivatives of formula (I): <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> wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy. 
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Biphenyloxyacetic acid derivatives for the treatment of respiratory disease (Fri, 13 Jul 2012)
The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
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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 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.
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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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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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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)
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. <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> 
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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)
The invention relates to compounds according to Formula I: <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> 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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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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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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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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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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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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2-pyrazinone derivatives for the treatment of disease or condition in which inhibition of neutrophil elastase activity is beneficial (Fri, 04 May 2012)
The invention provides compounds of formula <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> wherein R1, R3, R4, R5, R14, 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. 
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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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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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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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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)
The present invention relates to pyrazinone derivatives of formula (I): <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> wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy. 
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Chemical compounds (Fri, 09 Mar 2012)
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.
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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)
4-(3-chloro-2-fluoroanilino)-7 methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline <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> 
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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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Pyrazine derivatives (Fri, 27 Jan 2012)
The invention concerns pyrazine derivatives of the Formula I <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> 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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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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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-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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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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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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Extended Release Formulations Comprising Quetiapine and Methods for Their Manufacture (Fri, 30 Dec 2011)
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.
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Pharmaceutical Compositions (Fri, 30 Dec 2011)
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.
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Substituted Isoindoles (Fri, 30 Dec 2011)
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. <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> 
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Process for preparing benzimidazole compounds (Fri, 30 Dec 2011)
Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: <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> wherein Z, X1, X2, X5, R2b and R10 are as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives. 
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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)
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. <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> 
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Chemical compounds (Fri, 16 Dec 2011)
There is provided pyrimidinyl compounds of Formula (I), <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> 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">R2 is</li> </ul> </li> </ul> <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> or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. 
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9-SUBSTITUTED 8-OXOADENINE COMPOUND (Fri, 16 Dec 2011)
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): <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.71mm" wi="73.91mm" file="US20110306610A1-20111215-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> [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, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt. 
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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.
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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)
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) <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> 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) <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> is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.
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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)
The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy. <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> 
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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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[4-( 1-AMINO-ETHYL) - CYCLOHEXYL ] - METHYL - AMINES AS ANTIBACTERIALS (Fri, 25 Nov 2011)
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. <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> 
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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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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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HEMIFUMARATE SALT (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 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.
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Phenoxiacetic acid derivatives (Fri, 18 Nov 2011)
The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
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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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Chemical Process (Fri, 21 Oct 2011)
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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CHEMICAL COMPOUNDS (Fri, 14 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 <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> wherein, R1, R2, R3, R4, X2, q, Y1, Y2, n, Q and Z are as defined in the description.
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PROCESS FOR THE PREPARATION OF 2-(6-SUBSTITUTED-1,-3-DIOXANE-4-YL) ACETIC ACID DERIVATIVES (Fri, 14 Oct 2011)
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 R1, R2, and R3 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 OR3 group in formula (1) being replaced by an OY group, where X, R1 and R2 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.
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FUSED, SPIROCYCLIC HETEROAROMATIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS (Fri, 07 Oct 2011)
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. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.26mm" wi="59.52mm" file="US20110245224A1-20111006-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST (Fri, 07 Oct 2011)
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 β2-adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.
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2-HYDROXY-ETHANESULFONATE SALT (Fri, 07 Oct 2011)
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.
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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)
The invention concerns quinazoline derivatives of Formula I <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> wherein each of R1a, R1b, R2, R3 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.
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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)
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.
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Pyrazole derivatives as 11-beta-HSD1 inhibitors (Fri, 16 Sep 2011)
A compound of formula (I): <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> 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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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)
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. <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> 
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Triazolo pyrimidine compounds (Fri, 09 Sep 2011)
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. <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> 
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BINDING MEMBERS FOR IGE MOLECULES (Fri, 02 Sep 2011)
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.
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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)
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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PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A SECOND ACTIVE INGREDIENT (Fri, 26 Aug 2011)
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.
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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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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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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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HETEROCYCLIC JAK KINASE INHIBITORS (Fri, 19 Aug 2011)
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. <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> 
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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)
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. <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> 
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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)
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. <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> 
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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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SPIRO CONDENSED BARBITURIC ACID DERIVATIVES FOR USE AS ANTIBACTERIAL (Fri, 22 Jul 2011)
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. <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> 
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Quinuclidine derivatives as muscarinic M3 receptor antagonists (Fri, 15 Jul 2011)
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. <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> 
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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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PYRIDINE COMPOUNDS (Fri, 08 Jul 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. <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> 
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Steroid Derivatives Acting As Glucocorticosteroid Receptor Agonists (Fri, 01 Jul 2011)
The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy. <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> 
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Dibenzothiazepine Derivatives and Use Thereof (Fri, 01 Jul 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. <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> 
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Cannabinoid Receptor Ligands (Fri, 01 Jul 2011)
Compounds of Formulae (I), or pharmaceutically acceptable salts thereof: wherein R1, R2 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. <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> 
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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)
The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
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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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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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METHOD OF TREATING SCHIZOPHRENIA AND OTHER DISORDERS (Fri, 17 Jun 2011)
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 <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> 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.
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Cinnoline Compounds for the Treatment of Anxiety, Cognitive and Mood Disorders (Fri, 17 Jun 2011)
This invention relates to novel compounds having the structural formula I below: <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> 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.
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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)
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 <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> 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.
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Nicotinic Acetylcholine Receptor Ligands 101 (Fri, 10 Jun 2011)
Nicotinic acetylcholine receptor ligands of Formula I <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> wherein X, n, R1 and R2 are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing, and methods for using the same.
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Novel Compounds (Fri, 10 Jun 2011)
The present invention provides compounds of formula (I): <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 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. </li> </ul> </li> </ul> 
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Heterocyclic Compounds as CCR2 Antagonists (Fri, 10 Jun 2011)
Compounds of formula (I) <?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"?> wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C—C chemokine mediated conditions. 
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Chemical Process For Preparation Of Intermediates (Fri, 10 Jun 2011)
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.
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Benzimidazole derivatives (Fri, 10 Jun 2011)
Provided herein are compounds in accord with Formula I: <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> that are useful in the treatment of pain. 
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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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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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Heterocyclic Carboxamides For Use As Thrombin Inhibitors (Fri, 03 Jun 2011)
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) <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> 
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Novel Sulphonamide Derivatives as Glucocorticoid Receptor Modulators for the Treatment of Inflammatory Diseases (Fri, 03 Jun 2011)
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). <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> 
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Pyrimidine sulphonamide derivatives as chemokine receptor modulators (Fri, 27 May 2011)
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. <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> 
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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.
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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)
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. <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> 
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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) <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> 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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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)
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.
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Quinazoline derivatives and pharmaceutical compositions containing them (Wed, 11 May 2011)
The invention relates to quinazoline derivatives of formula (1) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.17mm" wi="69.85mm" file="USRE042353-20110510-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, 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 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. 
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5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES FOR THE SELECTIVE INHIBITION OF CHEMOKINE RECEPTORS (Fri, 06 May 2011)
There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) <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> wherein R1, R2, R3, R4 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 CX3CR1 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.
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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 (Fri, 29 Apr 2011)
The invention concerns chromenone derivatives of Formula I <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> 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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New Compounds Useful for Treating CNS Disorders (Fri, 29 Apr 2011)
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. <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> 
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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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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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Compounds for the treatment of multi-drug resistant bacterial infections (Fri, 22 Apr 2011)
The present invention relates to compounds of Formula V(A): <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> 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. 
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Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1 826 (Fri, 22 Apr 2011)
A compound of formula (I): <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> 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.
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5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES AS CHEMOKINE INHIBITORS (Fri, 22 Apr 2011)
There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 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 CX3CR1 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.
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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)
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.
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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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DIARYLMETHYLIDENE PIPERIDINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF (Fri, 08 Apr 2011)
Compounds of formula: (I) wherein R1, R2, R3, R4 and R7 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. <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> 
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2-pyridone compounds (Fri, 08 Apr 2011)
The invention provides compounds of formula <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> 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.
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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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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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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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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)
Compounds of formula (I): <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> 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. 
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Process and catalyst (Fri, 25 Mar 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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Therapeutic Agents 812 (Fri, 18 Mar 2011)
A compound of formula I <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> 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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QUINAZOLINE DERIVATIVES AS VEGF INHIBITORS (Fri, 18 Mar 2011)
The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 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. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.17mm" wi="69.85mm" file="US20110065736A1-20110317-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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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)
This invention relates to novel compounds having the structural formula I below: <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> 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.
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4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic Acid - 465 (Fri, 11 Mar 2011)
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.
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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)
There is provided pyrimidinyl indole compounds of Formula (I), <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> or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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NOVEL DIAZASIPIROAKANES AND THEIR USE FOR TREATMENT OF CCR8 MEDIATED DISEASES (Fri, 04 Mar 2011)
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. <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> 
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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)
The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, ring A, n, R3, and R4 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. <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> 
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COMBINATION OF A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST (Fri, 25 Feb 2011)
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 β2-adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.
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METHOD FOR PREPARING ADENINE COMPOUND (Fri, 25 Feb 2011)
A method for producing adenine compound (1): <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> wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): <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> and compound (3): <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> in the presence of a boron-containing reducing agent.
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Pharmaceutical process and intermediates 714 (Fri, 25 Feb 2011)
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): <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> X is ═O, ═N—OH or ═N—OC(O)Me; Y is hydrogen, PhS- or p-chlorophenylsulfanyl; Z is hydrogen or —CH2COOR1 wherein R1 is selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.
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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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4-(phenyl-piperazinyl-methyl)benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders (Fri, 18 Feb 2011)
The invention relates to at least one compound of general formula I <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> wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 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. 
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BENZAMIDE DERIVATIVES AND THEIR USE AS GLUCOKINASE ACTIVATING AGENTS (Fri, 11 Feb 2011)
Compounds of Formula (I): <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> wherein: R1 is methoxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; 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. 
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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)
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.
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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)
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.
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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)
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.
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NOVEL ADENINE COMPOUND (Fri, 04 Feb 2011)
A novel adenine compound represented by the formula (1): <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> wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straightened or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 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 R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof. The compound and salt are useful as a medicine.
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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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Bis-(Sulfonylamino) Derivatives in Therapy 066 (Fri, 28 Jan 2011)
The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, 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. <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> 
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METHOD FOR TREATING CANCERS HAVING HIGH GLUCOSE REQUIREMENTS EMPLOYING AN SGLT2 INHIBITOR AND COMPOSITIONS THEREOF (Fri, 21 Jan 2011)
Methods are provided for treating cancers that have high glucose requirements and that express SGLT2 at levels higher than normal cells, such as metastatic cancers, for example, metastatic lung cancers, employing an SGLT2 inhibitor alone or in combination with a cytotoxic agent and to a composition containing a combination of an SGLT2 inhibitor and a cytotoxic agent.
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PHTHALAZINONE COMPOUND (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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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)
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) <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> and to products of said process.
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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 (Fri, 14 Jan 2011)
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 p-chlorophenylsulfanyl; Z is hydrogen or -CH2COOR1 wherein R1 is selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.
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Benzoyl amino heterocyclyl compounds as glucokinase (GLK) activators (Thu, 13 Jan 2011)
The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R 1 , R 2 , R 3 , n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).
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Process for the manufacture of the calcium salt of rosuvastatin and crystalline intermediates thereof (Thu, 13 Jan 2011)
A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3 R ,5 S )-3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7) 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) is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.
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NOVEL COMPOUNDS FOR TREATMENT OF NEURODEGENERATION ASSOCIATED WITH DISEASES, SUCH AS ALZHEIMER'S DISEASE OR DEMENTIA (Fri, 07 Jan 2011)
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.
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NOVEL COMPOUNDS FOR TREATMENT OF NEURODEGENERATION ASSOCIATED WITH DISEASES, SUCH AS ALZHEIMER'S DISEASE OR DEMENTIA (Fri, 07 Jan 2011)
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.
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2-CARBOXAMIDE-7-PIPERAZINYL-BENZOFURAN DERIVATIVES 774 (Fri, 07 Jan 2011)
The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1- 4alkylheterocyclyl, heterocyclylheteroaryl, arylheterocyclyl, carbocyclylheteroaryl, heterocyclylaryl, optionally substituted R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted R4 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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5H-PYRROLO[3,4-£>]PYRAZIN-7-AMINE DERIVATIVES INHIBITORS OF BETA-SECRETASE (Fri, 07 Jan 2011)
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.
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Bis-(Sulfonylamino) derivatives for use in therapy (Fri, 31 Dec 2010)
The invention provides compounds of formula (I) wherein R1,R3,L1,L2,G1,G2, 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. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="22.44mm" wi="65.45mm" file="US20100331321A1-20101230-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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2-carboxamide-7-piperazinyl-benzofuran derivatives 774 (Fri, 31 Dec 2010)
The present invention relates to compounds of formula (I), <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="46.31mm" wi="35.31mm" file="US08367676-20130205-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">R1 is heteroaryl or heterocyclyl, optionally substituted;</li> <li id="ul0001-0002" num="0000">R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted;</li> <li id="ul0001-0003" num="0000">R3 is hydrogen or C1-4alkyl, or</li> <li id="ul0001-0004" num="0000">R2 and R3 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">R4 is hydrogen, halogen, methyl or methoxy;</li> <li id="ul0001-0006" num="0000">to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders.</li> </ul> The present invention further relates to new intermediates useful in the preparation thereof.
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Benzamide derivatives useful as histone deacetylase inhibitors (Fri, 31 Dec 2010)
The invention concerns a compound of the formula (I) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.02mm" wi="67.65mm" file="US08247562-20120821-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by histone deacetylase. 
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9-(PYRAZOL-3-YL)-9H-PURINE-2-AMINE AND 3-(PYRAZOL-3-YL) -3H-IMIDAZO[4,5-B] PYRIDIN-5- AMINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER (Fri, 24 Dec 2010)
The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="52.15mm" wi="62.40mm" file="US20100324040A1-20101223-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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PYRROLOPYRIDINE DERIVATIVES AND THEIR USE AS BACE INHIBITORS (Fri, 24 Dec 2010)
This invention relates to novel compounds having the structural formula I below: (I) 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. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="29.46mm" wi="50.04mm" file="US20100324072A1-20101223-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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Substituted pyrazines as DGAT-1 inhibitors (Fri, 24 Dec 2010)
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, obesity <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.86mm" wi="70.87mm" file="US08188092-20120529-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl;</li> <li id="ul0001-0002" num="0000">q is 0 or 1 and X2 is fluoro, chloro or (1-3C)alkyl;</li> <li id="ul0001-0003" num="0000">Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy;</li> <li id="ul0001-0004" num="0000">n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl;</li> <li id="ul0001-0005" num="0000">p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring;</li> <li id="ul0001-0006" num="0000">Z is carboxy or —CONHSO2Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.</li> </ul> 
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Metabotropic glutamate receptor isoxazole ligands and their use as potentiators (Fri, 24 Dec 2010)
Compounds in accord with Formula I: <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.55mm" wi="67.39mm" file="US07888353-20110215-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same. 
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PYRAZINE CARBOXAMIDES AS INHIBITORS OF DGAT1 (Fri, 24 Dec 2010)
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, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X1 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or - CONHSO2 Me or CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.
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Raman spectroscopic method for determining the ratio of 5-methoxy and 6-methoxy isomers of omeprazole (Wed, 22 Dec 2010)
The present invention relates to a novel method to determine the ratio of 5-methoxy and 6-methoxy isomers of omeprazole present in a mixture thereof. The method uses different Raman scattering efficiency values for the 5-methoxy and 6-methoxy isomers. This is of importance since the two isomers have different stability in the solid state in bulk form and in admixture with pharmaceutical excipients.
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2,3-DIHYDRO-1H-INDENE COMPOUNDS (Fri, 17 Dec 2010)
Provided herein are 2,3-dihydro-1H-indene compounds, methods for making the compounds, pharmaceutical compositions containing the compounds. The described compounds inhibit IAP proteins and can be used to treat various cancers.
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HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF (Fri, 17 Dec 2010)
Compounds of formula (IA) 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. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="41.40mm" wi="71.46mm" file="US20100317624A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS (Fri, 17 Dec 2010)
Compounds of formula (I), and salts and pro-drugs thereof: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="18.54mm" wi="69.85mm" file="US20100317653A1-20101216-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001-en" list-style="none"> <li>wherein for example R1 is optionally substituted aryl or heteroaryl;</li> <li>Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain;</li> <li>R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group;</li> <li>are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.</li> </ul> 
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Metabotropic glutamate-receptor-potentiating isoindolones (Fri, 17 Dec 2010)
Compounds of formula I: <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.43mm" wi="57.07mm" file="US08153638-20120410-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy. 
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Metabotropic glutamate receptor isoxazole ligands and their use as potentiators—286 (Fri, 17 Dec 2010)
Compounds in accord with Formula I: <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.55mm" wi="67.39mm" file="US08148372-20120403-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same. 
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A NOVEL 4-METHYLBENZENESULPHONATE SALT AND A PROCESS FOR PREPARING A PHARMACEUTICAL COMPOSITION COMPRISING THE SALT (Fri, 17 Dec 2010)
The invention provides a 4-methylbenzenesulphonate salt of the muscarinic antagonist (R)- 1-(4-fluorophenethyl)-3-((S)-2-phenyl-2-(piperidin-1 -yl)propanoyloxy)-1- azoniabicyclo[2.2.2]octane and its use in therapy,as well as a process for preparing a pharmaceutical composition comprising the salt and its use in therapy.
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2, 3-DIHYDRO-1H-INDENE COMPOUNDS AND THEIR USE TO TREAT CANCER (Fri, 17 Dec 2010)
Provided herein are 2,3-dihydro-1H-indene compounds, methods for making the compounds, pharmaceutical compositions containing the compounds. The described compounds inhibit IAP proteins and can be used to treat various cancers.
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HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF (Fri, 17 Dec 2010)
Compounds of formula (IA) 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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SUBSTITUTED N-[1-CYANO-2-(PHENYL)ETHYL]PIPERIDIN-2-YLCARBOXMIDE COMPOUNDS 761 (Fri, 17 Dec 2010)
The present invention provides a compound: (S)-N-((S)-1-Cyano-2-(4-(1-methyl-2-oxoindolin-6-yl)phenyl)ethyl)piperidine-2- carboxamide; (S)-N-((S)-1-Cyano-2-(4-(3-(3-methoxypropyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-5- yl)phenyl)ethyl)piperidine-2-carboxamide; (S)-N-((S)-1-Cyano-2-(4'-(ethylsulfonyl)biphenyl-4-yl)ethyl)piperidine-2-carboxamide; 4'-((S)-2-Cyano-2-((S)-piperidine-2-carboxamido)ethyl)biphenyl-4-yl methanesulfonate; or, (S)-N-((S)-1-Cyano-2-(4-(1-oxoisoindolin-5-yl)phenyl)ethyl)piperidine-2-carboxamide; or a pharmaceutically acceptable salt thereof; a process for its preparation, pharmaceutical compositions containing it and its use in therapy.
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HETEROCYCLIC AMIDES USEFUL FOR THE TREATMENT OF CANCER AND PSORIASIS (Fri, 10 Dec 2010)
The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z). <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="71.20mm" wi="73.41mm" file="US20100311748A1-20101209-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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Pyrimido [4,5-B]-oxazines for use as DGAT inhibitors (Fri, 10 Dec 2010)
Compounds of formula (I) or salts thereof, wherein A, and R1 to R5 are as defined in the specification, are DGAT-1 inhibitors and are thereby useful in the treatment of, for example, obesity. Processes to make compounds of formula (I) are also described. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.66mm" wi="70.95mm" file="US08017603-20110913-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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BENZIMIDAZOLE DERIVATIVES WHICH ARE TO BE USED AS ANTAGONIST FOR THE CB1-RECEPTOR (Fri, 03 Dec 2010)
Compounds of formula I or pharmaceutically acceptable salts thereof: wherein X, A, R1, R2, R3 and R4 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.
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METHODS FOR TREATING TYPE 2 DIABETES IN PATIENTS RESISTANT TO PREVIOUS TREATMENT WITH OTHER ANTI-DIABETIC DRUGS EMPLOYING AN SGLT2 INHIBITOR AND COMPOSITIONS THEREOF (Fri, 03 Dec 2010)
The invention provides methods for treating a patient having type 2 diabetes who has failed on previous regimens of one or more oral and/or injectable anti-diabetic agents, which include the step of administering a therapeutically effective amount of an SGLT2 inhibitor alone or in combination with another anti-diabetic agent and/or other therapeutic agent to such patient. A pharmaceutical composition containing dapagliflozin or dapagliflozin-S-propylene glycol solvate and one or more diabetic agents and/or other therapeutic agents for use in the methods of the invention is also provided.
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HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF (Fri, 03 Dec 2010)
Compounds of formula (IA) 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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Quiniclidine derivatives of (hetero) arylcycloheptanecarboxylic acid as muscarinic receptor antagonists (Thu, 02 Dec 2010)
The invention provides compounds of formula (I) wherein R 4 is a group of formula (II) or (IIIa) or (IIIb) and R 1 , R 2 , R 3 , R 5 , a, b and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation
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PTERIDINE COMPOUNDS FOR THE TREATMENT OF PSORIASIS (Wed, 01 Dec 2010)

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Thiazol-Guanidine Derivatives Useful As A (Beta)-Related Pathologies (Fri, 26 Nov 2010)
This invention relates to novel compounds having the structural formula I below: 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. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="19.39mm" wi="58.50mm" file="US20100298340A1-20101125-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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SALTS 756 (Fri, 26 Nov 2010)
The invention provides salts of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate, pharmaceutical compositions containing them and their use in therapy.
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MALEATE SALTS OF A QUINAZOLINE DERIVATIVE USEFUL AS AN ANTIANGIOGENIC AGENT (Fri, 26 Nov 2010)
The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.
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Isoindoline Derivatives For The Treatment Of Arrhythmias (Fri, 26 Nov 2010)
There is provided compounds of formula I, wherein R1 to R7 have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="27.43mm" wi="69.85mm" file="US20100298392A1-20101125-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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DISACCHARIN, DIFUMARIC ACID, DI-L-HYDROXY-2-NAPHTHOIC ACID AND MONO-BENZOIC ACID SALTS OF 4- (DIMETHYLAMIN0)BUTYL 2- (4- ( (2-AMINO-4-METHYL-6- (PENTYLAMINO) PYRIMIDIN- 5 -YL) METHYL) PHENYL)ACETATE (Fri, 26 Nov 2010)
The invention provides salts of 4- (dimethylamino) butyl 2- (4- ( (2-amino-4-methyl-6- (pentylamino) pyrimidin-5-yl ) methyl ) phenyl ) acetate (compound (I)), pharmaceutical compositions containing them and their use in therapy.
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NOVEL PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND FURTHER DISEASES (Fri, 26 Nov 2010)
The invention concerns compounds of Formula (I): wherein L1, R1, R2, R3, R4 and X 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 disease, for example cancer.
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Cyclopropyl amide derivatives (Thu, 25 Nov 2010)
Disclosed herein is at least one cyclopropyl amide derivative of formula (I), 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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Novel Compounds for A-Beta-Related Pathologies (Fri, 19 Nov 2010)
The present invention relates to novel compounds of formulae I and II and therapeutically acceptable salts thereof, their pharmaceutical compositions processes for making them and their use in therapeutic methods for treatment and/or prevention of various diseases. In particular, the invention relates to compounds which interfere with γ-secretase and/or its substrate and hence modulate the formation of Aβ peptides. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="64.26mm" wi="65.45mm" file="US20100292210A1-20101118-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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CHEMICAL COMPOUNDS 751 (Fri, 19 Nov 2010)
The invention concerns bicyclic compounds of Formula (I) <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="47.50mm" wi="72.73mm" file="US20100292222A1-20101118-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p 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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Bis-(Sulfonylamino) Derivatives in Therapy (Fri, 19 Nov 2010)
The invention provides compounds of formula <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="26.75mm" wi="58.00mm" file="US20100292279A1-20101118-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> wherein R1, R2, R3, 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.
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NEW COMPOUNDS MODULATING GAMMA-SECRETASE AND THEIR USE IN THE TREATMENT OF ALPHA BETA RELATED PATHOLOGIES, SUCH AS ALZHEIMER'S DISEASE (Fri, 19 Nov 2010)
The present invention relates to novel compounds of formulae (I) and (II) and therapeutically acceptable salts thereof, their pharmaceutical compositions processes for making them and their use in therapeutic methods for treatment and/or prevention of various diseases. In particular, the invention relates to compounds which interfere with γ-secretase and/or its substrate and hence modulate the formation of Aβ peptides.
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BIS-(SULFONYLAMINO) DERIVATIVES FOR TREATMENT OF PAIN AND INFLAMMATION (Fri, 19 Nov 2010)
The invention provides compounds of formula (I) wherein R1, R2, R3, 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.
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[1,2,4] TRIAZOLO [4,3-B] PYRIDAZINES AS LIGANDS OF THE ANDROGEN RECEPTOR (Fri, 19 Nov 2010)
The invention concerns bicyclic compounds of Formula (I): wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p 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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PYRROLE DERIVATIVES WITH ANTIBACTERIAL ACTIVITY (Fri, 12 Nov 2010)
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. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="24.89mm" wi="71.29mm" file="US20100286181A1-20101111-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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Substituted 1-cyanoethylheterocyclylcarboxamide compounds (Fri, 12 Nov 2010)
The present invention provides compounds of formula (I) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="38.78mm" wi="69.85mm" file="US08193239-20120605-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> in which y, m, 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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Compounds (Fri, 12 Nov 2010)
The present invention relates to new compounds <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.08mm" wi="61.38mm" file="US08168668-20120501-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy. 
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Process for the manufacturing of the compound 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile 701 (Fri, 12 Nov 2010)
The present invention relates to a new process for the manufacture of the compound 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, particularly the 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, and to new intermediates prepared in said process suitable for large scale manufacturing of said compound.
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SUBSTITUTED 1-CYANOETHYLHETEROCYCLYLCARBOXAMIDE COMPOUNDS 750 (Fri, 12 Nov 2010)
The present invention provides compounds of formula (I), in which y, m, 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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Compositions and methods for the control, prevention, and treatment of obesity and eating disorders (Thu, 11 Nov 2010)
Compositions and methods for preventing, treating or controlling conditions or disorders associated with obesity, diet, and nutrition are provided. The methods provided generally involve the administration of an amylin or an amylin agonist to a subject in order to prevent, treat or controlling conditions or disorders associated with obesity, diet, and nutrition.
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NOVEL COMPOUNDS 660 (Fri, 05 Nov 2010)
The invention provides compounds of formula (I) <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="36.41mm" wi="65.28mm" file="US20100278835A1-20101104-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 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 useful in the treatment of respiratory syncytial virus (RSV).
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Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase (Fri, 05 Nov 2010)
The invention provides certain novel 6-heteroaryl-5-methyl-3-oxo-4-[3(trifluoromethyl)phenyl]-3,4-dihydropyrazine-2-carboxamide derivatives and pharmaceutically acceptable salts thereof and particular Forms thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.
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Metabotropic Glutamate Receptor Oxadiazole Ligands and Their Use as Potentiators (Fri, 05 Nov 2010)
Compounds of Formula (I) wherein R1, R2, R3 R4 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="35.73mm" wi="69.43mm" file="US20100280082A1-20101104-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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Therapeutic agents 713 (Fri, 05 Nov 2010)
Disclosed herein are compounds of formula I <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.35mm" wi="75.86mm" file="US08110566-20120207-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> in which R1, R2, R3, R4, R5, A, X, Y are as described in the specification, their use in pharmaceutical compositions and in methods of treatment or prophylaxis of a melanin-concentrating hormone related disease or condition. 
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Imidazoquinolines with immuno-modulating properties (Fri, 05 Nov 2010)
The present invention provides compounds of formula (I) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.15mm" wi="69.85mm" file="US08436178-20130507-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein Ra, 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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THERAPEUTIC AGENTS 713 (Fri, 05 Nov 2010)
Disclosed herein are compounds of Formula (I) in which R1, R2, R3, R4, R5, A, X, Y are as described in the specification, their use in pharmaceutical compositions and in methods of treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
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METHOD FOR PRODUCING ADENINE COMPOUND (Thu, 04 Nov 2010)
A method for producing adenine compound (1): , wherein m and n are independently an integer of 2 to 5, R 1 is C 1-6 alkyl group, R 2 and R 3 are the same or different, and hydrogen atom, or C 1-6 alkyl group, or R 2 and R 3 are combined with the adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R 4 is C 1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.
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MANDELIC ACID DERIVATIVES (Mon, 01 Nov 2010)

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SULPHIDE BRIDGED DERIVATIVES AS MODULATORS OF MGLUR5 733 (Fri, 29 Oct 2010)
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Metalloproteinase inhibitors (Fri, 29 Oct 2010)
Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.79mm" wi="69.85mm" file="US08153673-20120410-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> useful as metalloproteinase inhibitors, especially as inhibitors of MMP12. 
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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, 29 Oct 2010)
There is provided a compound of formula (I): <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.68mm" wi="64.01mm" file="US08129391-20120306-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 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. 
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PROCESS FOR THE PREPARATION OF 4-(3-CHLORO-2-FLUORO-ANILINO)-7-METHOXY-6-{[1-(N-METHYLCARBAMOYLMETHYL)-PIPERIDIN-4-YL] OXY} QUINAZOLINE (Fri, 29 Oct 2010)
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.
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CRYSTALLINE FORM OF 4-AMINO-8-(2-FLUORO-6-METHOXY-PHENYL)-N-PROPYLCINNOLINE-3- CARBOXAMIDE HYDROGEN SULPHATE, FOR TREATMENT OF ANXIETY DISORDERS (Fri, 29 Oct 2010)
4-Amino-8-(2-fluoro-6-methoxy-phenyl)-N-propylcinnoline-3-carboxamide hydrogen sulphate, polymorphs thereof, pharmaceutical compositions contain them, methods of making them are described. They are useful in treating anxiety disorders.
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SULPHIDE BRIDGED DERIVATIVES AS MODULATORS OF MGLUR5 (Fri, 29 Oct 2010)
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Crystalline Forms of 2-Hydroxy-3- [5- (Morpholin- 4- Ylmethyl) Pyridin-2-YL] IH- Indole- 5 -Carbonitrile Citrate (Fri, 22 Oct 2010)
The present invention relates to new crystalline forms of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, a Form D and a Form E, respectively, a process for their preparations, pharmaceutical formulations containing said compounds and to the use of said active compounds in therapy, and particularly to GSK3 related conditions and disorders.
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Imidazole substituted pyrimidines (Fri, 22 Oct 2010)
Imidazole substituted pyrimidines and pharmaceutically acceptable salts thereof; pharmaceutical formulations containing such pyrimidines; the use of such compounds in therapy; the use of such compounds for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as methods of treatment of such disorders comprising administering to subjects in need of such treatment therapeutically effective amounts of such compounds.
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Chemical compounds—643 (Fri, 22 Oct 2010)
The invention concerns bicyclic compounds of Formula I <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.11mm" wi="73.07mm" file="US08258140-20120904-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein <img id="CUSTOM-CHARACTER-00001" he="2.79mm" wi="6.35mm" file="US08258140-20120904-P00001.TIF" alt="custom character" img-content="character" img-format="tif"/>, R1, R2, L1, L2, 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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Oxadiazole derivatives and their use as metabotropic glutamate receptor potentiators—842 (Fri, 22 Oct 2010)
Compounds of Formula (I) wherein R1 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.29mm" wi="69.85mm" file="US08377940-20130219-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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IMIDAZOLE SUBSTITUTED PYRIMIDINES USEFUL IN THE TREATMENT OF GLYCOGEN SYNTHASE KINASE 3 RELATED DISORDERS SUCH AS ALZHEIMER'S DISEASE (Fri, 22 Oct 2010)
The present invention relates to a new compound of formula (I) wherein R1 is hydrogen or fluoro; R2 and R3 are independently selected from hydrogen or methyl; or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, 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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TRISUBSTITUTED PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES (Fri, 15 Oct 2010)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="32.60mm" wi="54.19mm" file="US20100261723A1-20101014-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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Therapeutic agents (Fri, 15 Oct 2010)
(2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a pharmaceutically acceptable salt thereof is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.
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Therapeutic agents (Fri, 15 Oct 2010)
A compound (2S)-2-[1-(2,6-dichlorophenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-(3-hydroxyazetidin-1-yl)-N-(5-methylpyrazin-2-yl)propanamide is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.
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Isoxazol-3(2H)-one analogs as therapeutic agents (Fri, 15 Oct 2010)
<chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.73mm" wi="49.36mm" file="US08415378-20130409-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> or a pharmaceutically suitable salt thereof, wherein, <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3,</li> <li id="ul0001-0002" num="0000">R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile,</li> <li id="ul0001-0003" num="0000">or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4;</li> <li id="ul0001-0004" num="0000">wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate;</li> <li id="ul0001-0005" num="0000">R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring;</li> <li id="ul0001-0006" num="0000">or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.</li> </ul> 
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ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS (Fri, 15 Oct 2010)
Formula I or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.
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A PYRAZOLO [4,5-E] PYRIMIDINE DERIVATIVE AND ITS USE TO TREAT DIABETES AND OBESITY (Fri, 15 Oct 2010)
(2S)-2-[1-(2,6-dichlorophenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-(3-hydroxyazetidin-1-yl)-N-(5-methylpyrazin-2-yl)propanamide is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.
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PYRAZOLO [4, 5-E] PYRIMIDINE DERIVATIVE AND ITS USE TO TREAT DIABETES AND OBESITY (Fri, 15 Oct 2010)
(2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a pharmaceutically acceptable salt thereof is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.
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NOVEL COMPOUNDS (Fri, 08 Oct 2010)
The present invention provides compounds of formula (I) <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="43.10mm" wi="70.61mm" file="US20100256105A1-20101007-C00001.TIF" img-content="photograph" img-format="png"/> </chemistry> wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
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NOVEL AMIDE COMPOUNDS (Fri, 08 Oct 2010)
The present invention provides compounds of formula (I) <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="45.97mm" wi="70.70mm" file="US20100256104A1-20101007-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> wherein n, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
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AMIDE DERIVATIVES (Fri, 08 Oct 2010)
The invention concerns a compound of the Formula I <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="24.64mm" wi="69.85mm" file="US20100256120A1-20101007-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen and R4 is, (1-6C)alkyl or (1-6C)alkoxy; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
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Compounds (Fri, 08 Oct 2010)
The present invention provides named compounds of formula (I) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.69mm" wi="70.19mm" file="US08338587-20121225-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and pharmaceutical compositions containing them and their use in therapy. 
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NOVEL AMIDE DERIVATIVES OF STEROIDAL[3,2-C]PYRAZOLE COMPOUNDS WITH GLUCOCORTICOID ACTIVITY (Fri, 08 Oct 2010)
The present invention provides compounds of formula (I) wherein n, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
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NOVEL STEROIDAL[3,2-C]PYRAZOL DERIVATIVES WITH GLUCOCORTICOID ACTIVITY (Fri, 08 Oct 2010)
The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5, R6, are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
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NOVEL DERIVATIVES OF STEROIDAL[3,2-C]PYRAZOLE COMPOUNDS WITH GLUCOCORTICOID ACTIVITY (Fri, 08 Oct 2010)
The present invention provides named compounds of formula (I), and pharmaceutical compositions containing them and their use in therapy.
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BIS- (SULF ONYLAMINO) DERIVATIVES FOR USE IN THERAPY (Thu, 07 Oct 2010)
The invention provides compounds of formula (I) wherein R<sp>1</sp>,R<sp>3</sp>,L<sp>1</sp>,L<sp>2</sp>,G<sp>1</sp>,G<sp>2</sp>, 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.
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Morpholino pyrimidine derivatives used in diseases linked to mTOR kinase and/or PI3K (Fri, 01 Oct 2010)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.60mm" wi="54.19mm" file="US08138183-20120320-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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Salt forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)y1]-4-penten 2-amine (Fri, 01 Oct 2010)
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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Chemical compounds (Thu, 30 Sep 2010)
2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanyl-pyridin-2-yl]-3-piperidyl] acetic acid or a pharmaceutically-acceptable salt thereof.
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8-oxoadenine derivatives acting as modulators of TLR7 (Fri, 24 Sep 2010)
The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.73mm" wi="73.58mm" file="US08138172-20120320-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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Imidazo[4,5-B]Pyridine-7-Carboxamides 704 (Fri, 17 Sep 2010)
The present invention relates to new compounds of formula (I) as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, 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. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="34.37mm" wi="63.67mm" file="US20100234593A1-20100916-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ANTIVARAL AGENTS (Fri, 17 Sep 2010)
The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 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 useful in the treatment of respiratory syncytial virus (RSV).
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HYDROXAMIC ACID DERIVATIVES AS GRAM-NEGATIVE ANTIBACTERIAL AGENTS (Sat, 11 Sep 2010)
The invention relates to chemical compounds of formula (IB): or a salt thereof. In some embodiments, the invention relates to inhibitors of UDP-3-0 — (R-S-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC). In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and/or treatment of Gram- negative bacterial infections.
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TRISUBSTITUTED PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES (Fri, 10 Sep 2010)
A compound of formula (I) or a pharamaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use intherapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="32.60mm" wi="53.09mm" file="US20100227858A1-20100909-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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Non-anilinic derivatives of isothiazol-3(2H)-one 1,1-dioxides as liver X receptor modulators (Fri, 10 Sep 2010)
The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="28.19mm" wi="69.93mm" file="US07960380-20110614-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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A QUINOLINE DERIVATIVE ACTING AS A P2X7-RECEPTOR ANTAGONIST (Thu, 09 Sep 2010)
The invention provides a compound of formula (I), a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharamaceutical composition, and its use in treatment of rheumatoid arthritis, inflammatory bowel disease or Crohn's disease.
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4-ANILINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS (Fri, 03 Sep 2010)
A quinazoline derivative of the Formula (I): <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="38.69mm" wi="69.85mm" file="US20100222344A1-20100902-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.</li> </ul> </li> </ul> 
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Process For The Preparation Of N,N'-Disubstituted Oxabispidines (Fri, 03 Sep 2010)
There is provided a process for the preparation of a sulfonic acid salt of formula I, or a solvate thereof, which process comprises hydrogenating a sulfonic acid salt of formula II, or a solvate thereof; in the presence of a solvent system consisting essentially of water, a C3-5 secondary alkyl alcohol and no more than 15% v/v of another organic solvent, wherein the sulfonic acid salt of formula I is optionally, without isolation, converted to a compound of formula IX, or a pharmaceutically-acceptable derivative thereof, wherein R1, R2, R3, R6, R7, R8, A, B and D have meanings given in the description. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="100.75mm" wi="69.85mm" file="US20100222335A1-20100902-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> 
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PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ASTHMA, COPD, ALLERGIC RHINITIS, ALLERGIC CONJUNCTIVITIS, ATOPIC DERMATITIS, CANCER, HEPATITIS B, HEPATITIS C, HIV, HPV, BACTERIAL INFECTIONS AND DERMATOSIS (Thu, 02 Sep 2010)
The present invention provides compounds of formula (I) wherein R <sp>1</sp>, R<sp>2</sp>, R<sp>3</sp> and R<sp>4</sp> 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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PYRIDINYLQUINAZOLINAMINE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS (Fri, 27 Aug 2010)
The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B-Raf 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. 
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Cyclopropyl Amide Derivatives (Fri, 27 Aug 2010)
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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2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia (Fri, 27 Aug 2010)
Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="69.77mm" wi="76.20mm" file="US07863265-20110104-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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Salt 628 (Fri, 27 Aug 2010)
6-Methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form.
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TOSYLATE SALT OF A 5-PYRAZOLYL-2-PYRIDONE DERIVATIVE, USEFUL IN THE TREATMENT OF COPD (Fri, 27 Aug 2010)
6-Methyl-5-(I -methyl-1H-pyrazol-5-yl)-N-{ [5-(methylsulfonyl)pyridin-2-yl]methyl }-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a form, and the use of such a salt and form in therapy.
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CYCLOPROPYL AMIDE DERIVATIVES TARGETING THE HISTAMINE H3 RECEPTOR (Fri, 27 Aug 2010)
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 dihydroxy esters and derivatives thereof (Fri, 20 Aug 2010)
A process is provided for the preparation of a compound of formula (1) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.46mm" wi="68.58mm" file="US07888083-20110215-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein R and R′ represent optionally substituted hydrocarbyl groups and X represents a hydrocarbyl linking group. The process comprises either the stereoselective reduction of the keto group in a dihydroxy keto precursor followed by selective esterification of a primary hydroxy, or selective esterification of a primary hydroxy of a dihydroxy keto precursor followed by stereoselective reduction of the keto group. 
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