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AstraZeneca AB

AstraZeneca AB Patent applications
Patent application numberTitlePublished
20120130097PROCESS FOR THE PREPARATION OF CYCLOPROPYL CARBOXYLIC ACID ESTERS AND DERIVATIVES - The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.05-24-2012
20120122892CHEMICAL COMPOUNDS - This invention relates to novel compounds having the formula (I):05-17-2012
20120122843Compounds and Their Use for Treatment of Amyloid Beta-Related Diseases - 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 Aβ-related diseases.05-17-2012
20120122817HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF - 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.05-17-2012
20120114750PHARMACEUTICAL COMPOSITION 271 - The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.05-10-2012
20120108814PROCESS 738 - 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.05-03-2012
201201086102-PYRAZINONE DERIVATIVES FOR THE TREATMENT OF DISEASE OR CONDITION IN WHICH INHIBITION OF NEUTROPHIL ELASTASE ACTIVITY IS BENEFICIAL - The invention provides compounds of formula05-03-2012
20120108602Carbamoyl Compounds as DGAT1 Inhibitors 190 - DGAT-1 inhibitor compounds of formula (1), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity05-03-2012
20120108577COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS - 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.05-03-2012
20120101274Process For Preparing [1S-[1-alpha, 2-alpha, 3-beta (1S*,2R*) 5-beta]]-3-[7-[2-(3,4-difluorophenyl)-cyclopropylamino]-5-(propylthio)-3H- -1,2,3-triazolo [4,5-d] pyrimidin-3-yl]-5-(2-hydroxyethoxy) cyclopentane-1,2-diol And To Its Intermediates - The present invention is directed to a process for preparing [1S-[1α,2α,3β(1S*,2R*),5β]]-3-[7-[2-(3,4-difluorophenyl)-cyclopropylamino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol and to intermediates useful in the process.04-26-2012
20120101109ETHANOLAMINE SALT OF N- (3-METHOXY-5-METHYLPYRAZIN-2YL) -2- (4-[1, 3, 4-OXADIAZOLE-2-YL] PHENYL) PYRIDINE-3- SULPHONAMIDE - N-(3-Methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide ethanolamine salt and its uses are described.04-26-2012
20120095011NOVEL COMPOUNDS - The invention provides compounds of formula04-19-2012
201200949952-AZA-BICYCLO[2.2.1]HEPTANE COMPOUNDS AND USES THEREOF - This invention relates to 2-aza-bicyclo[2.2.1]heptane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GlyT1) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, post-traumatic stress disorders and pain.04-19-2012
20120077813Imidazole Substituted Pyrimidines Useful in the Treatment of Glycogen Synthase Kinase-3 Related Disorders such as Alzheimer's Disease - The present invention relates to a new compound of formula (I) wherein R03-29-2012
20120065214COMPOUNDS AND THEIR USES 708 - The present invention relates to pyrazinone derivatives of formula (I):03-15-2012
20120046219MELANOCORTIN RECEPTOR-SPECIFIC PEPTIDES - The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I)02-23-2012
20120035363CRYSTALLINE 4-(3-CHLORO-2-FLUOROANILINO)-7 METHOXY-6-... - 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.02-09-2012
20120035219Compound for the Treatment of Tuberculosis - (5R)-3-[4-[1-[(2S)-2,3-dihydroxypropanoyl]-3,6-dihydro-2H-pyridin-4-yl]-3,5-difluoro-phenyl]-5-(isoxazol-3-yloxymethyl)oxazolidin-2-one, or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, for use in the treatment of 02-09-2012
201200351572-PYRIDONE DERIVATIVES AS NEUTROPHIL ELASTASE INHIBITORS AND THEIR USE - There are provided novel compounds of formula (I),02-09-2012
20120035134CHEMICAL COMPOUNDS - The present invention relates to compounds of Formula (I):02-09-2012
20120028924CHEMICAL COMPOUNDS - The present invention relates to compounds of Formula (I) and/or Formula (Ia):02-02-2012
20120022110PHARMACEUTICAL DEPOT FOR 5-FLUORO-2-[[(1S)-1-(5-FLUORO-2-PYRIDYL)ETHYL]AMINO]-6-[(5-ISOPROPOXY-1H-- PYRAZOL-3-YL)AMINO]PYRIDINE-3-CARBONITRILE - A pharmaceutical depot comprising (i) 5-fluoro-2-[[(1S)-1-(5-fluoro-2-pyridyl)ethyl]amino]-6-[(5-isopropoxy-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation.01-26-2012
201200221072-(PIPERIDIN-1-YL)-4-AZOLYL-THIAZOLE-5-CARBOXYLIC ACID DERIVATIVES AGAINST BACTERIAL INFECTIONS - 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.01-26-2012
20120022082PYRAZINE DERIVATIVES - The invention concerns pyrazine derivatives of the Formula I01-26-2012
20120010189(3-(4-(AMINOMETHYL)PHENOXY OR PHENYLTHIO)AZETIDIN-1-YL)(5-PHENYL-1,3,4-OXADIAZOL-2-YL)METHANONE COMPOUNDS - Disclosed herein are azetidinyl compounds of formula I,01-12-2012
20120004243AMIDE DERIVATIVES BEARING A CYCLOPROPYLAMINOACARBONYL SUBSTITUENT USEFUL AS CYTOKINE INHIBITORS - 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.01-05-2012
20110319426Substituted Isoindoles - 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.12-29-2011
20110319384Pharmaceutical Compositions - 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.12-29-2011
20110319383Extended Release Formulations Comprising Quetiapine and Methods for Their Manufacture - 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.12-29-2011
20110313172PROCESS FOR THE PREPARATION OF 1-[5-(3-CHLORO-PHENYL)-ISOOXAZOL-3-YL]-ETHANONE AND (R)-1-[5-(3-CHLORO-PHENYL)-ISOOXAZOL-3-YL]-ETHANOL - 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.12-22-2011
20110306768PROCESSES FOR THE MANUFACTURE OF 3--PYRIDINE, 4-METHYL-3-METHYLTHIO-5-(3-PYRIDYL)-L,2,4-TRIAZOLE, AND (1R)-1-[2-(3-METHYLPHENYL)-2H-TETRAZOL-5-YL]ETHANOL - The present invention provides a process for the manufacture of the compound 3-{4-methyl-5-[(1R)-1-(2-(3-methylphenyl-2H-tetrazol-5-yl)-ethoxy]-4H-[1,2,4]triazol-3-yl}-pyridine of formula 14 wherein a) the compound 3-(5-methane-sulfonyl-4-methyl-4H-1,2,4-triazol-3-yl)-pyridine of formula 6 and the compound (1R)-[2-(3-methylphenyl)-2H-tetrazol-5-yl]ethanol of formula 13 are dissolved in an aprotic solvent, whereafter an alkoxide base is added, providing the compound of formula 14. The invention also provides methods for manufacturing 3-(5-methanesulfonyl-4-methyl-4H-1,2,4-triazol-3-yl)-pyridine and (1R)-1-[2-(3-methylphenyl)-2H-tetrazol-5-yl]ethanol.12-15-2011
20110306613CHEMICAL COMPOUNDS - There is provided pyrimidinyl compounds of Formula (I),12-15-2011
20110295016A NEW PROCESS FOR PREPARING 4-[4-METHYL-5-(CL-10ALKYLTHIO/C5-10ARYL-CL-6ALKYLTHIO)-4H-1,2,4-TRIAZOL-3- -YL]PYRIDINES - The invention relates to a method of manufacturing a compound according to formula (I) wherein R is C12-01-2011
2011029476616 Alpha, 17 Alpha-Acetal Glucocorticosteroidal Derivatives and their Use - The present invention provides compounds of formula (I) wherein R12-01-2011
20110288084[4-( 1-AMINO-ETHYL) - CYCLOHEXYL ] - METHYL - AMINES AS ANTIBACTERIALS - 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.11-24-2011
20110281894HEMIFUMARATE SALT - 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.11-17-2011
20110277762PACKAGE - A package for a dispensing device, comprising a protection pouch arranged to enclose the dispensing device. The protection pouch comprises a base section that is arranged to support the dispensing device in the general vertical direction, and the package comprises a support member arranged to essentially elevate the base section of the pouch from a support surface.11-17-2011
20110257395Chemical Process - 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.10-20-2011
20110253138INHALER WITH AUDIBLE INDICATOR MEANS - The disclosure relates to an inhaler comprising an outlet through which doses of medicament may be dispensed. The inhaler also comprises a dispensing mechanism having a primed state, in which it is ready for dispensing a dose, and a fired state, in which it has dispensed a dose. In one aspect, the inhaler also comprises a disabler which, after the final dose has been dispensed, is activated to disable the dispensing mechanism from generating a sound which has been audible when the dispensing mechanism has moved from its primed state to its fired state. In a second aspect, the disabler prevents the dispensing mechanism from being in its primed state when an outlet cover is in an open position, whereby a not ready indication is presented to the user.10-20-2011
20110251173CHEMICAL COMPOUNDS - 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 obesity10-13-2011
20110245293PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST - 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 β10-06-2011
201102452922-HYDROXY-ETHANESULFONATE SALT - 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.10-06-2011
20110237610Quinazoline Derivatives as Antiproliferative Agents - The invention concerns quinazoline derivatives of Formula I09-29-2011
20110224273Pyrazole Derivatives as 11-Beta-HSD1 Inhibitors - A compound of formula (I):09-15-2011
20110224261CRYSTALLINE FORM OF 4-(5--4-METHYL-4H-1,2,4-TRIAZOL-3-YL)PYRIDINE - The present invention relates to a novel crystalline form of 4-(5-{(IR)-1-[5-(3-chlorophenyl)isoxazol-3-yl]ethoxy}-4-methyl-4H-1,2,4-triazol-3-yl)pyridine. Further, the present invention also relates to the use of the novel crystalline form for the treatment of gastrointestinal disorders, pharmaceutical compositions containing it.09-15-2011
20110224229Novel Crystalline Form - 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.09-15-2011
20110218330Novel triazolo pyrimidine compounds - 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.09-08-2011
20110218182CHEMICAL COMPOUNDS 251 - 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.09-08-2011
20110212978Combination of ZD6474 and Pemetrexed - 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 the administration of ZD6474 in combination with pemetrexed; to a pharmaceutical composition comprising ZD6474 and pemetrexed; to a combination product comprising ZD6474 and pemetrexed for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and pemetrexed; to the use of ZD6474 and pemetrexed 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.09-01-2011
20110212084BINDING MEMBERS FOR IGE MOLECULES - 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.09-01-2011
20110207770PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A SECOND ACTIVE INGREDIENT - 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.08-25-2011
20110207755USE OF MYELOPEROXIDASE (MPO) INHIBITORS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF TO TREAT MULTIPLE SYSYEM ATROPHY (MSA) 938 - The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection.08-25-2011
20110207745SOLID FORMS OF 4--N,N-DIETHYLBENZAMIDE, COMPOSITIONS THEREOF, AND USES THEREWITH - 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.08-25-2011
20110190520Process for the preparation of cyclopropyl carboxylic acid esters and derivatives - The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.08-04-2011
20110190272CHEMICAL COMPOUNDS - 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.08-04-2011
20110186451PREFILLED CONTAINER INSERT FOR MIXING TWO OR MORE INGREDIENTS FOR USE IN A PHARMACEUTICAL CONTAINER SYSTEM - The present invention relates to pharmaceutical container systems, and to prefilled container inserts for use therein, for mixing two or more ingredients of a pharmaceutical product. The prefilled container insert of one embodiment comprises a molded container casing having walls, a bottom and an open top for receiving a solid component, a resilient stopper for sealing the open top of the molded container casing, and a bottom disc formed by a weakening rim in the bottom periphery of the molded container casing. The bottom disc is openable to allow mixing of the prefilled solid component with a diluents fluid of the pharmaceutical container system by introducing a spike through the resilient stopper applying a pushing force on the bottom disc, by which force the weakening rim is broken and the container is opened. The prefilled container insert of a further embodiment comprises a molded container casing having walls, a bottom and an open top for receiving an inner open cylinder and a solid component, a resilient stopper for sealing the open top of the molded container casing, and a bottom disc formed by a weakening rim in the bottom periphery of the molded container casing. The bottom disc is openable to allow mixing of the prefilled solid component with a diluents fluid of the pharmaceutical container system by applying a pushing force onto the top of the molded container compressing the casing and forcing the inner cylinder to push on the bottom disc, by which force the weakening rim is broken and the container insert is opened.08-04-2011
20110183954TRICYCLIC 2,4-DIAMINO-L,3,5-TRIAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF CANCER AND MYELOPROLIFERATIVE DISORDERS - 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.07-28-2011
20110166139PYRIDINE COMPOUNDS - 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.07-07-2011
20110160184Dibenzothiazepine Derivatives and Use Thereof - 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.06-30-2011
20110160180Cannabinoid Receptor Ligands - Compounds of Formulae (I), or pharmaceutically acceptable salts thereof: wherein R06-30-2011
20110160167Steroid Derivatives Acting As Glucocorticosteroid Receptor Agonists - The present invention provides compounds of formula (I) wherein n, p, R06-30-2011
20110144331Cinnoline Compounds for the Treatment of Anxiety, Cognitive and Mood Disorders - This invention relates to novel compounds having the structural formula I below:06-16-2011
20110144089METHOD OF TREATING SCHIZOPHRENIA AND OTHER DISORDERS - 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 I06-16-2011
20110137056Chemical Process For Preparation Of Intermediates - 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.06-09-2011
20110137045BENZIMIDAZOLE DERIVATIVES - Provided herein are compounds in accord with Formula I:06-09-2011
20110136820Heterocyclic Compounds as CCR2 Antagonists - Compounds of formula (I)06-09-2011
20110136804Nicotinic Acetylcholine Receptor Ligands 101 - Nicotinic acetylcholine receptor ligands of Formula I06-09-2011
20110136801Novel Compounds - The present invention provides compounds of formula (I):06-09-2011
20110136784Method of Treating Anxiety Disorders - 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 I06-09-2011
20110130432Heterocyclic Carboxamides For Use As Thrombin Inhibitors - 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)06-02-2011
20110130428Sublingual Compositions Comprising (2S) - (4E) -N-Methyl-5- (3- (5-Isopropoxypyridin) YL)-4-Penten-2-Amine - The present invention relates to sublingual compositions comprising (2S)-(4E)-N-methyl-5-(3-(5-iso-propoxypyridin)yl)-4-penten-2-amine or pharmaceutically acceptable salts thereof, to the preparation of said compositions and the use of thereof in therapy.06-02-2011
20110130426Novel Sulphonamide Derivatives as Glucocorticoid Receptor Modulators for the Treatment of Inflammatory Diseases - 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).06-02-2011
20110124672Thienyl Compounds - Compounds of formula I:05-26-2011
20110118275OXAZOLO[4,5-c]PYRIDINE SUBSTITUTED PYRAZINE - The present invention relates to a compound of formula (I)05-19-2011
201101182382-ANILINOPURIN-8-ONES AS INHIBITORS OF TTK/MPS1 FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - 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.05-19-2011
20110112144METHODS OF PREPARING SUBSTITUTED HETEROCYCLES - 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.05-12-2011
201101055375,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES FOR THE SELECTIVE INHIBITION OF CHEMOKINE RECEPTORS - There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I)05-05-2011
20110098292New Compounds Useful for Treating CNS Disorders - 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.04-28-2011
20110098271CHROMENONE DERIVATIVES - The invention concerns chromenone derivatives of Formula I04-28-2011
20110097321COMBINATION OF ANGIOPOIETIN-2 ANTAGONIST AND OF VEGF-A, KDR AND/OR FLT1 ANTAGONIST FOR TREATING CANCER - The invention relates to agents which possess anti-angiogenic activity and are accordingly useful in methods of treatment of disease states associated with angiogenesis in the animal or human body. More specifically the invention concerns a combination of an antagonist of the biological activity of Angiopoietin-2 and an antagonist of the biological activity of VEGF-A, and/or KDR, and/or Flt1, and uses of such antagonists.04-28-2011
20110092526Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1 826 - A compound of formula (I):04-21-2011
201100925195,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES AS CHEMOKINE INHIBITORS - There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R04-21-2011
20110092495COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS - 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.04-21-2011
20110086870Combination Therapy - 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.04-14-2011
20110083667DISPENSER AND METHOD FOR ENTRAINING POWDER IN AN AIRFLOW 537 - The invention relates to a method for entraining in an airflow a medicament powder contained in a cavity having a cavity opening. Large airflow vortices are provided, for instance, by means of an obstacle in a flow passage. The airflow with large vortices is arranged to by-pass the cavity opening, thereby generating an eddy in the cavity which contributes to entraining the powder in said airflow. The invention also relates to a medical dispenser, for instance an inhaler, in which said method may be performed.04-14-2011
20110082173DIARYLMETHYLIDENE PIPERIDINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF - Compounds of formula: (I) wherein R04-07-2011
20110082155Novel 2-Pyridone Compounds - The invention provides compounds of formula04-07-2011
20110071290Process And Catalyst - 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.03-24-2011
20110065736QUINAZOLINE DERIVATIVES AS VEGF INHIBITORS - The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R03-17-2011
20110065706Therapeutic Agents 812 - A compound of formula I03-17-2011
201100600224-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic Acid - 465 - 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.03-10-2011
20110059992New Compounds - This invention relates to novel compounds having the structural formula I below:03-10-2011
20110059981New Pyridine Analogues V - The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y03-10-2011
20110059969PIPERAZINES AS ANTI-OBESITY AGENTS - The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.03-10-2011
20110054931Diagnostic System and Method - A diagnostic system and method. In one embodiment, the invention is a diagnostic system comprising: a form comprising one or more diagnostic questions and one or more possible answers to each diagnostic question; a first overlay comprising one or more windows and one or more diagnostic fields, wherein when the first overlay is positioned over the form, the answers to the diagnostic questions that are indicative of the user having a first medical condition are visible through the windows of the first overlay; and wherein the one or more diagnostic fields contain criteria for diagnosing the user with the first medical condition based on the user's selection of answers on the form that are visible through the windows of the first overlay. In other embodiments, the invention is a computer-based version of the diagnostic system and a diagnostic method.03-03-2011
20110053969NOVEL DIAZASIPIROAKANES AND THEIR USE FOR TREATMENT OF CCR8 MEDIATED DISEASES - The invention provides compounds of general formula. (II) wherein R and 03-03-2011
20110046191COMBINATION OF A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST - 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 β02-24-2011
20110046119THERAPEUTIC TREATMENT - A combination comprising candesartan and rosuvastatin for the prevention or treatment of atherosclerosis and for the prevention of cardiovascular events is described.02-24-2011
20110046108PYRIMIDINE DERIVATIVES - The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R02-24-2011
20110040573Diagnostic System and Method - A diagnostic system and method. In one embodiment, the invention is a diagnostic system comprising: a form comprising one or more diagnostic questions and one or more possible answers to each diagnostic question; a first overlay comprising one or more windows and one or more diagnostic fields, wherein when the first overlay is positioned over the form, the answers to the diagnostic questions that are indicative of the user having a first medical condition are visible through the windows of the first overlay; and wherein the one or more diagnostic fields contain criteria for diagnosing the user with the first medical condition based on the user's selection of answers on the form that are visible through the windows of the first overlay. In other embodiments, the invention is a computer-based version of the diagnostic system and a diagnostic method.02-17-2011
20110039858Novel Compounds - The invention relates to at least one compound of general formula I02-17-2011
20110034432BENZAMIDE DERIVATIVES AND THEIR USE AS GLUCOKINASE ACTIVATING AGENTS - Compounds of Formula (I):02-10-2011
20110028530NOVEL CRYSTALLINE FORMS OF 4-[4-(2-ADAMANTYLCARBAMOYL)-5-TERT-BUTYL-PYRAZOL-1-YL]BENZOIC ACID 471 - 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.02-03-2011
20110028529NOVEL CRYSTALLINE FORMS OF 4-[4-(2-ADAMANTYLCARBAMOYL)-5-TERT-BUTYL-PYRAZOL-1-YL]BENZOIC ACID 471 - 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.02-03-2011
20110028488COMBINATION PRODUCT COMPRISING SRC KINASE INHIBITOR AZDO530 AND AN ANTIOESTROGEN OR EGFR-TK-INHIBITOR - The invention relates to a combination for use in the synergistic treatment of breast cancer comprising an antioestrogen and the Src kinase inhibitor AZD0530, a combination for the synergistic treatment of cancer comprising an EGFR TKI and the Src kinase inhibitor AZD0530 and a triple combination for the synergistic treatment of breast cancer comprising an antioestrogen, an EGFR TKI and the Src kinase inhibitor AZD0530.02-03-2011
20110028471COMBINATION THERAPY 238 - 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.02-03-2011
20110021540Bis-(Sulfonylamino) Derivatives in Therapy 066 - The invention provides compounds of formula wherein R01-27-2011
20110020360TARGETED BINDING AGENTS DIRECTED TO PDGRF-ALPHA AND USES THEREOF - Targeted binding agents directed to the antigen PDGFR-alpha and uses of such agents are disclosed herein. More specifically the invention relates to fully human monoclonal antibodies directed to the antigen PDGFR-alpha and uses of these antibodies. Aspects of the invention also relate to hybridomas or other cell lines expressing such antibodies. The described targeted binding agents and antibodies are useful as diagnostics and for the treatment of diseases associated with the activity and/or overexpression of PDGFR-alpha.01-27-2011
20110015393PHTHALAZINONE COMPOUND - 4-(4-Fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one as crystalline Form C.01-20-2011
20110009647Process 054 - 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)01-13-2011
20110009373COMPOSITION COMPRISING A COMBINATION OF AN AROMATASE INHIBITOR, A PROGESTIN AND AN OESTROGEN AND ITS USE FOR THE TREATMENT OF ENDOMETRIOSIS - The invention relates to a method of treating endometriosis using a combination of an aromatase inhibitor, a progestin and an oestrogen. The invention also relates to pharmaceutical formulations comprising said combination.01-13-2011
20110003831N-(-3-METHOXY-5-METHYLPYRAZIN-2-YL)-2-(4-'1,3,4-OXADIAZOL-2-YL!PHENYL)PYRI- DINE-3 SULPHONAMIDE AS AN ANTICANCER AGENT - The use of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, in the treatment of cancer and/or pain in a warm blooded animal such as man is described.01-06-2011
20100331575Processes For The Preparation Of Optically Active Intermediates - This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl)cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1α,2α,3β(1S*,2R*),5β)]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.12-30-2010
201003313412-CARBOXAMIDE-7-PIPERAZINYL-BENZOFURAN DERIVATIVES 774 - The present invention relates to compounds of formula (I),12-30-2010
20100331329BENZAMIDE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS - The invention concerns a compound of the formula (I)12-30-2010
20100331321Bis-(Sulfonylamino) derivatives for use in therapy - The invention provides compounds of formula (I) wherein R12-30-2010
20100330179Method for Treating a Patient at Risk for Developing an NSAID-associated Ulcer - The present disclosure is directed to a method for treating a disease or disorder in a patient at risk of developing an NSAID-associated ulcer by administering to said patient in need thereof a pharmaceutical composition in unit dose form comprising naproxen, or pharmaceutically acceptable salt thereof, and esomeprazole, or pharmaceutically acceptable salt thereof to said at risk patient and thereby decreasing the patient's risk of developing an ulcer.12-30-2010
20100330103Antibodies Directed to Alpha V Beta 6 And Uses Thereof - Targeted binding agents, such antibodies directed to the antigen αVβ6 and uses of such agents are described. In particular, fully human monoclonal antibodies directed to the antigen αVβ6 are disclosed. Nucleotide sequences encoding, and amino acid sequences comprising, heavy and light chain immunoglobulin molecules, particularly sequences corresponding to contiguous heavy and light chain sequences spanning the framework regions and/or complementarity determining regions (CDR's), specifically from FR1 through FR4 or CDR1 through CDR3 are disclosed. Hybridomas or other cell lines expressing such immunoglobulin molecules and monoclonal antibodies are also disclosed.12-30-2010
20100324328Process For Isolating Mono-Carboxy Substituted Probucol Derivatives - A process for isolating a compound of formula (I)12-23-2010
20100324289Chemical Process - The present invention provides a process for the preparation of a compound of formula (I); wherein X is halogen; Y is ZR12-23-2010
20100324072PYRROLOPYRIDINE DERIVATIVES AND THEIR USE AS BACE INHIBITORS - 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.12-23-2010
20100324068CHEMICAL COMPOUNDS 785 - 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, obesity12-23-2010
201003240409-(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 - 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.12-23-2010
20100317653OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS - Compounds of formula (I), and salts and pro-drugs thereof:12-16-2010
20100317626The Use Of (3-Amino-2-Fluoropropyl) Phosphinic Acid For Treatment Of NERD - The present invention is directed to the use of (3-Amino-2-fluoropropyl)phosphinic acid or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, for the treatment or prevention of non-erosive reflux disease (NERD).12-16-2010
201003175932,3-DIHYDRO-1H-INDENE COMPOUNDS - 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.12-16-2010
20100311737PYRIMIDO [4,5-B] -OXAZINES FOR USE AS DGAT INHIBITORS - Compounds of formula (I) or salts thereof, wherein A, and R12-09-2010
20100311648MELANOCORTIN RECEPTOR-SPECIFIC PEPTIDES - The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I)12-09-2010
20100305140BENZIMIDAZOLE DERIVATIVES WHICH ARE TO BE USED AS ANTAGONIST FOR THE CB1-RECEPTOR - Compounds of formula I or pharmaceutically acceptable salts thereof: wherein X, A, R12-02-2010
20100298392Isoindoline Derivatives For The Treatment Of Arrhythmias - There is provided compounds of formula I, wherein R11-25-2010
20100298364 SALTS 756 - 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.11-25-2010
20100298357MALEATE SALTS OF A QUINAZOLINE DERIVATIVE USEFUL AS AN ANTIANGIOGENIC AGENT - 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.11-25-2010
20100298350Triazolo[4,5-D]Pyrimidine Compounds For Treatment Of Abdominal Aortic Aneurysms - The invention provides triazolo [4,5-d]pyrimidine compounds, acting as P11-25-2010
20100298340Thiazol-Guanidine Derivatives Useful As A (Beta)-Related Pathologies - 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.11-25-2010
20100292279Bis-(Sulfonylamino) Derivatives in Therapy - The invention provides compounds of formula11-18-2010
20100292222CHEMICAL COMPOUNDS 751 - The invention concerns bicyclic compounds of Formula (I)11-18-2010
20100292210Novel Compounds for A-Beta-Related Pathologies - 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.11-18-2010
20100286202New Compounds - The present invention relates to new compounds11-11-2010
20100286181PYRROLE DERIVATIVES WITH ANTIBACTERIAL ACTIVITY - 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.11-11-2010
20100280082Metabotropic Glutamate Receptor Oxadiazole Ligands and Their Use as Potentiators - Compounds of Formula (I) wherein R11-04-2010
20100280000THERAPEUTIC AGENTS 713 - Disclosed herein are compounds of formula I11-04-2010
20100273805SULPHIDE BRIDGED DERIVATIVES AS MODULATORS OF MGLUR5 733 - 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.10-28-2010
20100267740Oxadiazole Derivatives and Their Use as Metabotropic Glutamate Receptor Potentiators - 842 - Compounds of Formula (I) wherein R10-21-2010
20100267723Imidazole Substituted Pyrimidines - A compound of formula (I)10-21-2010
20100267720 Crystalline Forms of 2-Hydroxy-3- [5- (Morpholin- 4- Ylmethyl) Pyridin-2-YL] IH- Indole- 5 -Carbonitrile Citrate - 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.10-21-2010
20100261755ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS - or a pharmaceutically suitable salt thereof, wherein, 10-14-2010
20100261733THERAPEUTIC AGENTS 927 - (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.10-14-2010
20100261723TRISUBSTITUTED PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES - 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.10-14-2010
20100261704THERAPEUTIC AGENTS 928 - 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.10-14-2010
20100260765TARGETED BINDING AGENTS DIRECTED TO KDR AND USES THEREOF - 035 - The invention relates to targeted binding agents against KDR and uses of such agents. More specifically, the invention relates to fully human monoclonal antibodies directed to KDR. The described targeted binding agents are useful in the treatment of diseases associated with the activity and/or overproduction of KDR and as diagnostics.10-14-2010
20100249196Novel Salt Forms Of (2S)-(4E)-N-Methyl-5-[3-(5-Isopropoxypyridin)yl]-4-Penten 2-Amine - 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.09-30-2010
20100249131MORPHOLINO PYRIMIDINE DERIVATIVES USED IN DISEASES LINKED TO MTOR KINASE AND/OR PI3K - A compound of formula (I) or a pharamaceutically 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.09-30-2010
20100247617Transdermal Administration Of (2S)-(4E)-N-Methyl-5-(3-(5-Isopropoxypyridin)yl)-4-Penten-2-Amine - The present invention generally relates to the transdermal administration of (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, or pharmaceutically acceptable salts thereof. The transdermal administration can be effected using transdermal drug delivery devices, semi-solid dosage forms, or iontophoresis. The drug delivery devices and/or semi-solid dosage forms can provide instantaneous release, sustained release, or combinations thereof, and can include permeation enhancers and other components to assist in drug transport across the dermis, especially the epidermis. The compositions can be used to treat and/or prevent any indication which the active ingredients are capable of treating and preventing, but deliver (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, or pharmaceutically acceptable salts thereof, in an efficacious manner. Disorders that can be treated and/or prevented include central nervous system disorders, addictions, pain, and inflammation.09-30-2010
20100240645COMBINATION OF CHECKPONIT KINASE (CHK) AND TELANGIECTASIA MUTATED (ATM) INHIBITORS FOR THE TREATMENT OF CANCER - A combination, comprising a checkpoint kinase (CHK) inhibitor, or a pharmaceutically acceptable salt thereof, and an ataxia telangiectasia mutated (ATM) inhibitor, or a pharmaceutically acceptable salt thereof is described.09-23-2010
20100234593 Imidazo[4,5-B]Pyridine-7-Carboxamides 704 - 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.09-16-2010
20100227858TRISUBSTITUTED PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES - 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.09-09-2010
20100227847Non-Anilinic Derivatives Of Isothiazol-3(2H)-one 1,1-Dioxides As Liver X Receptor Modulators - 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.09-09-2010
20100226917METHODS FOR THE TREATMENT OF HEMATOLOGIC MALIGNANCIES - The present invention discloses, in part, therapies for treating hematologic malignancies, including B cell lymphomas and leukemias or B cell related tumors comprising the administration of a CHK1 inhibitor in combination with a B cell depleting antibody. The present invention further includes treating hematologic malignancies, including B cell lymphomas and leukemias, or B cell related tumors, which are resistant to cancer treatment comprising the administration of a CHK1 inhibitor.09-09-2010
20100222335Process For The Preparation Of N,N'-Disubstituted Oxabispidines - 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 C09-02-2010
20100216812Cyclopropyl Amide Derivatives - 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.08-26-2010
20100216759Novel 2-Azetidinone Derivatives And Their Use As Cholesterol Absorption Inhibitors For The Treatment Of Hyperlipidaemia - 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.08-26-2010
20100215773Use of Quinazoline Derivative ZD6474 Combined With Platinum Compounds and Optionally Ionising Radiation in the Treatment of Diseases Associated With Angiogenesis and/or Increased Vascular Permeability - 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 the administration of ZD6474 in combination with a platinum anti-tumour agent; to a pharmaceutical composition comprising ZD6474 and a platinum anti-tumour agent; to a combination product comprising ZD6474 and a platinum anti-tumour agent for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and a platinum anti-tumour agent; to the use of ZD6474 and a platinum anti-tumour agent in the manufacture of a medicament for use in the production of all antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.08-26-2010
20100210841CHEMICAL PROCESS 632 - A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof08-19-2010
20100210621CRYSTALLINE POLYMORPHIC FORM 631 - A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described.08-19-2010
201002042465-AMINOPYRAZOL-3-YL-3H-IMIDAZO (4,5-B) PYRIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER - The present invention relates to compounds of Formula (I) and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.08-12-2010
20100204231AMINO-THIAZOLYL-PYRIMIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER - 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.08-12-2010
20100203565Peptide Fingerprint from the Degradation of Elastin by HNE - Methods for producing and using protein/peptide fingerprints, derived from elastin degraded by the enzyme human Neutrophil Elastase (HNE), allowing identification and investigation of disease-associated proteins/peptides that can be linked to specific drug targets, or to specific drug target combinations. The methods are particularly useful for studies relating to Chronic Obstructive Pulmonary Disease (COPD).08-12-2010
20100197749CHEMICAL COMPOUNDS - The invention relates to chemical compounds of formula (I) and (II):08-05-2010
20100193536 BLISTER PACK DEVICE AND A METHOD OF EJECTING A UNIT DOSAGE FROM A BLISTER PACK USING THE DEVICE - The present invention relates to a blister pack device for dispensing a dosage unit from a blister pack. The blister pack has at least one blister and a lid foil. The device comprises a first arm and a second lever arm hingedly connected to each other, the first arm comprises an aperture through which the dosage unit can be ejected. The lever arm comprises a protruding member for pressing out a dosage unit from the blister when the lever arm is lowered down onto the blister positioned on the first arm. The protruding member comprises a first section for applying a pressing force on the dosage unit inside the blister to initiate the breaking of the lid foil of the blister pack and a second section for distributing the pressing force over the dosage unit and for ejecting the dosage unit.08-05-2010
20100190745HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF - 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.07-29-2010
20100184813CHEMICAL COMPOUNDS 553 - DGAT-1 inhibitor compounds of formula (I) and pharmaceutically-acceptable salts thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity07-22-2010
20100184738Uses of cinnoline compounds to treat schizophrenia - This invention relates to the use of compounds having the structural formula I below:07-22-2010
20100183729Novel Process - The invention relates to a stable pharmaceutical composition useful in the treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease (COPD) and a novel micronisation process for manufacturing a stable formulation for formoterol or its enantiomers and a carrier/diluent comprising a carbohydrate such as lactose.07-22-2010
20100179199Ethanamine Compounds and Methods of Using the Same 545 - The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treating depression by administering the ethanamine compound.07-15-2010
20100179161PYRAZOLINE DERIVATIVES FOR THE TREATMENT OF TURBERCULOSIS - Compounds of the formula (I) and pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, useful in the treatment of 07-15-2010
20100179150ANTIBACTERIAL PIPERDINE DERIVATIVES - 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.07-15-2010
20100173941Muscarinic Receptor Agonists that are Effective in the Treatment of Pain, Alzheimer's Disease and Schizophrenia - Compounds of Formulae I, or pharmaceutically acceptable salts thereof: wherein R07-08-2010
20100173935Muscarinic Receptor Agonists that are Effective in the Treatment of Pain, Alzheimer's Disease and Schizophrenia - Compounds of Formula IA, or pharmaceutically acceptable salts thereof: IA wherein G07-08-2010
20100173909PIPERIDINE COMPOUNDS AND USES THEREOF - 596 - 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.07-08-2010
20100173890Compounds, Process for their Preparation, Intermediates, Pharmaceutical Compositions and their use in the Treatment of 5-HT6 Mediated Disorders such as Alzheimer's Disease, Cognitive Disorders, Cognitive Impairment Associated with Schizophrenia, Obesity and Parkinson's Disease - The present invention relates to new compounds of formula I, or salts, solvates or solvated salts thereof, process 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 the treatment of 5-HT6 mediated disorders such as Alzheimer's disease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and Parkinson's disease.07-08-2010
20100173825HETEROARYL BENZAMIDE DERIVATIVES - The invention relates to a novel group of compounds of Formula (I) or a salt thereof:07-08-2010
20100168143QUINAZOLINE DERIVATIVES - The invention provided a compound of formula (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient.07-01-2010
20100168130Diarylmethyl Piperazine Derivatives, Preparations Thereof and Uses Thereof - Compounds of general formula:07-01-2010
20100168075Novel 2-Azetidinone Derivatives As Cholesterol Absorption Inhibitors For The Treatment Of Hyperlipidaemic Conditions - The application relates to novel 2-azetidinone derivatives of formula (I) and pharmaceutically acceptable salts, solvates and prodrugs thereof. The compounds are cholesterol absorption inhibitors and are useful in the treatment of hyperlipidaemic conditions, including atherosclerosis, Alzheimers' disease and cholesterol associated tumours. The application also relates to pharmaceutical formulations comprising such compounds and to processes for their preparation.07-01-2010
20100168039Novel 2-Azetidinone Derivatives As Cholesterol Absorption Inhibitors For The Treatment Of Hyperlipidaemic Conditions - 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.07-01-2010
20100160627NOVEL LACTAMS AND USES THEREOF - Compounds having the formula (I)06-24-2010
20100160626Process For The Preparation Of 3,7-Dihydroxy-1,5-Diazacyclooctanes - There is provided processes for the preparation of various compounds, including compounds of formulae I, IV and VII,06-24-2010
20100160374N-(2-Hydroxyethyl)-N-Methyl-4-(Quinolin-8-yl(1-(Thiazol-4-ylmethyl)Piperid- in-4-ylidene)Methyl)Benzamide - N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide, pharmaceutically acceptable salts thereof, and/or mixtures thereof, as well as, pharmaceutical compositions thereof, methods of treatment therewith, and processes of making N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide and intermediates thereof.06-24-2010
201001603254-(3-AMINOPYRAZOLE) PYRIMIDINE DERIVATIVES FOR USE AS TYROSINE KINASE INHIBITORS IN THE TREATMENT OF CANCER - 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.06-24-2010
20100158926ANTIBODIES TO ERBB2 - The present invention relates to antibodies including human antibodies and antigen-binding portions thereof that specifically hind to ErbB2, preferably human ErbB2. In another embodiment, the antibodies or antigen-binding portions thereof inhibit ErbB2. The invention also relates to antibodies that are chimeric, bispecific, derivatized, single chain antibodies or portions of fusion proteins. The invention also relates to isolated heavy and light chain immunoglobulins or portions thereof derived from human anti-ErbB2 antibodies and nucleic acid molecules encoding such immunoglobulins. The present invention also relates to methods of using the antibodies and compositions for diagnosis and treatment. The invention also provides gene therapy methods using nucleic acid molecules encoding the heavy and/or light immunoglobulin molecules that comprise the human anti-ErbB2 antibodies. The invention also relates to transgenic animals or plants comprising nucleic acid molecules of the present invention.06-24-2010
20100152441COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS - 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.06-17-2010
20100152197(4-TERT-BUTYLPIPERAZIN-2-YL)(PIPERAZIN-1-YL)METHANONE-N-CARBOXAMIDE DERIVATIVES - The present invention relates to compounds of formula (I)06-17-2010
201001521694-OXOQUINAZOLIN-3-YL BENZAMIDE DERIVATIVES FOR THE TREATMENT OF CYTOKINE DISEASES - The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R06-17-2010
20100152156 2-Azetidinone Derivatives For The Treatment Of Hyperlipidaemic Diseases - The invention relates to novel 2-azetidinone derivatives of formula (I) and to pharmaceutically acceptable salts, solvates and prodrugs thereof. The compounds are cholesterol absorption inhibitors, useful in the treatment of hyperlipidaemic conditions. The invention also relates to processes for their manufacture and to pharmaceutical compositions containing them.06-17-2010
20100150904BINDING MEMBERS FOR IGE MOLECULES - 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.06-17-2010
20100144759NOVEL N-(FLUORO-PYRAZINYL)-PHENYLSULFONAMIDES AS MODULATORS OF CHEMOKINE RECEPTOR CCR4 - The invention provides N-(fluoro-pyrazinyl)-phenylsulfonamides of formula (I)06-10-2010
20100144710Piperazine and Piperidine MGLUR5 Potentiators - Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof, wherein A, B, D, Ar1, Ar2, R2, R3, R4, a, m and n are defined in the specification, methods for the use thereof, processes for making and pharmaceutical compositions containing the same.06-10-2010
20100144606COMBINATION 408 - The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclohexyl-N06-10-2010
20100137397Chemical Compounds - A compound of the formula (1) or a pharmaceutically-acceptable salt: possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity such as 2 diabetes. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.06-03-2010
20100137322NOVEL N-(8-HETEROARYLTETRAHYDRONAPHTALENE-2YL) OR N-(5-HETEROARYLCHROMANE-3-YL) CARBOXAMIDE DERIVATIVES FOR THE TREATMENT OF PAIN - The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.06-03-2010

Patent applications by AstraZeneca AB