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AstraZeneca AB

AstraZeneca AB Patent applications
Patent application numberTitlePublished
20160137634Chemical Compounds - The invention concerns compounds of Formula (I)05-19-2016
20160136140Chemical Compounds - The invention concerns compounds of Formula (I)05-19-2016
20160130249Quinazoline Derivatives as VEGF Inhibitors - The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R05-12-2016
20160113953METHOD OF TREATMENT - A method for treating NAFLD and/or NASH and suitable compositions for carrying out the method are claimed.04-28-2016
20160074412Chemical Compounds - There is provided pyrimidinyl compounds of Formula (I),03-17-2016
20160060240CHROMENONE DERIVATIVES - The invention concerns chromenone derivatives of Formula I03-03-2016
20160022690COMBINATION TREATMENT - The present invention relates to the use of combinations comprising 8-[(1R)-1-(3,5-difluorophenylamino)ethyl]-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide or a pharmaceutically acceptable salt thereof and a taxane in the treatment or prophylaxis of cancer; pharmaceutical compositions comprising Compound [I] (or a pharmaceutically acceptable salt thereof) and a taxane; kits comprising Compound [I] or a pharmaceutically acceptable salt thereof and a taxane, optionally with instructions for use; and methods of treatment comprising the simultaneous, sequential or separate administration of Compound [I] or a pharmaceutically acceptable salt thereof and a taxane to warm-blooded animal, such as man.01-28-2016
20150376170BENZOXAZINONE AMIDES AS MINERALOCORTICOID RECEPTOR MODULATORS - Disclosed are certain derivatives of benzoxazinone amides of formula (I), or pharmaceutically acceptable salts thereof,12-31-2015
20150374673Combination Therapy for the Treatment of Nosocomial Pneumonia - The present invention relates to a method of treatment of nosocomial pneumonia using a combination of ceftazidime (a third generation cephalosporin) and avibactam (a novel β-lactamase inhibitor), optionally with one or more additional therapeutic agents.12-31-2015
20150336952Imidazo[4,5-c]quinolin-2-one Compounds and Their Use in Treating Cancer - The specification generally relates to compounds of Formula (I):11-26-2015
20150328239Chemical Compounds - The present invention relates to compounds of Formula (I):11-19-2015
20150320751Quinazoline Inhibitors of activating mutant forms of Epidermal Growth Factor Receptor - The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof:11-12-2015
20150307534CHEMICAL COMPOUNDS - Quinazoline derivatives of formula (I):10-29-2015
20150299134NOVEL COMPOUNDS - There is provided a compound of formula (I):10-22-2015
20150252077Melanocortin Receptor-Specific Peptides - The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I)09-10-2015
20150210655CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS - The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),07-30-2015
20150203513COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS - Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.07-23-2015
20150182531Novel Protein Kinase B Inhibitors - 060 - The invention relates to a novel group of compounds of Formula (I) or salts thereof:07-02-2015
20150140104THERAPEUTIC POLYMERIC NANOPARTICLES AND METHODS OF MAKING AND USING SAME - Described herein are polymeric nanoparticles that include a therapeutic agent which is 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide (also known as AZD1152 hqpa) or a pharmaceutically acceptable salt thereof, and methods of making and using such therapeutic nanoparticles.05-21-2015
20150122249INHALER 624 - The present invention relates to an Breath actuated inhaler (BAI) actuator, comprising: a loading element capable of being loaded with an actuation force, a breath actuated trigger mechanism arranged to counteract the actuation force of the loading element, and to fire the actuator by releasing the actuation force of the loading element in response to an inhalation breath, and actuation locking means moveable between a locked position wherein it relieves the actuation force from the trigger mechanism setting the trigger mechanism in a neutral position, and an armed position wherein the trigger mechanism is set in an armed position.05-07-2015
201501193792-(2,4,5-SUBSTITUTED-ANILINO)PYRIMIDINE COMPOUNDS - 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 Exon19 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.04-30-2015
20150087661Crystalline Forms of (s)-4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo[2,3-d]py- rimidin-4-yl) piperidine-4-carboxamide - The present invention discloses certain new solid state forms of (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy.03-26-2015
20150080396Novel Pyrimidine Derivatives and Their Use in the Treatment of Cancer and Further Diseases - The invention concerns compounds of Formula (I): wherein L03-19-2015
20150073011Beta-Lactamase Inhibitor Compounds - The present invention is directed to compounds which are beta-lacatamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia):03-12-2015
20150057317GABR-A2 DIAGNOSTIC - The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sites known as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence at these GABR-A2 SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs.02-26-2015
20150051185Chemical Compounds 251 - The invention relates to chemical compounds of formula I,02-19-2015
20150038516Inhibitors of Protein Kinases - Compounds of general Formula I:02-05-2015
20150025091Maleate 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.01-22-2015
20150011545Chemical Compounds - 759 - The present invention relates to compounds of Formula (I):01-08-2015
20140378684Chemical Process for the Synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)qu- inazoline - 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-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.12-25-2014
20140364601PROCESS - Processes for the preparation of the compound of formula (II) and intermediate compounds for use in the processes.12-11-2014
20140357661CHEMICAL COMPOUNDS - The invention concerns compounds of Formula (I)12-04-2014
201403298302-CARBOXAMIDE-4-PIPERAZINYL-BENZOFURAN DERIVATIVE - 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.11-06-2014
20140329786COMBINATION TREATMENT OF CANCER - The present invention relates to a combination comprising AZD5363, or a pharmaceutically acceptable salt thereof, and at least one androgen receptor signalling modulator selected from MDV-3100 (also known as enzalutamide), AZD3514, abiraterone (or an ester prodrug thereof: e.g. abiraterone acetate), and bicalutamide; or a pharmaceutically acceptable salt thereof. Each of these combinations may be useful in the treatment of cancer. The invention also relates to pharmaceutical compositions comprising such combinations, and further relates to methods of treatment comprising the simultaneous, sequential or separate administration of AZD5363, or a pharmaceutically acceptable salt thereof, with at least one androgen receptor signalling modulator as described above, to warm-blooded animal, such as a human for the treatment of cancer. The invention also relates to a kit comprising such combinations.11-06-2014
20140296534COMPOUNDS SUITABLE AS PRECURSORS TO COMPOUNDS THAT ARE USEFUL FOR IMAGING AMYLOID DEPOSITS - The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.10-02-2014
20140288091MONO-FLUORO BETA-SECRETASE INHIBITORS - 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 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.09-25-2014
20140286878COMPOSITION FOR INHALATION - The invention relates to a formulation comprising formoterol and budesonide for use in the treatment of respiratory diseases. The composition further contains HFA 227, PVP and PEG, preferably PVP K25 and PEG 1000.09-25-2014
20140255486Coated Tablet Formulation and Method - A coated tablet formulation is provided which includes a medicament such as the DPP4-inhibitor, saxaglipitin09-11-2014
20140255428Quinazoline Inhibitors of activating mutant forms of Epidermal Growth Factor Receptor - The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof:09-11-2014
20140243517METHODS OF PRODUCING C-ARYL GLUCOSIDE SGLT2 INHIBITORS - Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.08-28-2014
20140243262PHARMACEUTICAL FORMULATIONS CONTAINING AN SGLT2 INHIBITOR - Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate08-28-2014
20140235606CRYSTALLINE FORMS OF N-[2-[[(2,3-DIFLUOROPHENYL)METHYL]THIO]-6--4-PYRIMIDINYL]-1-AZETIDINESULF- ONAMIDE - 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.08-21-2014
20140221443NOVEL HYDROGEN SULFATE SALT - The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation.08-07-2014
20140221400USE 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.08-07-2014
20140206700CHEMICAL COMPOUNDS - The invention concerns compounds of Formula (I)07-24-2014
20140206677COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS - Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.07-24-2014
20140194419CHROMENONE DERIVATIVES - The invention concerns chromenone derivatives of Formula I07-10-2014
20140179712PHARMACEUTICAL FORMULATION OF N-[5-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-2H-PYRAZOL-3-YL]-4-[(3R,5S)-3,5-DIMET- HYLPIPERAZIN-1-YL]BENZAMIDE - There are provided pharmaceutical compositions comprising a compound of Formula (I) as defined herein and an amount of an alkaline effervescent agent that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.06-26-2014
20140162984PHOSPHONOXY QUINAZOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE - Quinazoline derivatives of formula (I):06-12-2014
20140155394Chemical Compounds - 759 - The present invention relates to compounds of Formula (I):06-05-2014
20140135509Process for the Preparation of Benzyl [(3aS,4R,6S,6aR)-6-hydroxy-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]d- ioxol]-4-yl]carbamate and Intermediates in the Process - The present invention is directed to a process for the preparation of benzyl [(3aS,4R,6S,6aR)-6-hydroxy-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl]carbamate (VI),05-15-2014
20140128371CHEMICAL COMPOUNDS 542 - The present invention relates to compounds of Formula (I):05-08-2014
20140121228Quinazoline Derivatives as VEGF Inhibitors - The invention relates to quinazoline derivatives of formula (I),05-01-2014
20140121227THERAPEUTIC TREATMENT - The present invention relates to a combination comprising (5)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, or a pharmaceutically acceptable salt thereof, hereafter “Compound (I)”, and a taxane. Taxanes include established cancer drugs such as docetaxel (Taxotere™) and paclitaxel (Taxol™). Such combinations may be useful in the treatment or prophylaxis of cancer. The invention also relates to a pharmaceutical composition comprising such Compound (I) and a taxane. The invention further relates to a method of treatment comprising the simultaneous, sequential or separate administration of Compound (I) and a taxane, to warm-blooded animal, such as man. The invention also relates to a kit comprising Compound (I) and a taxane, optionally with instructions for use.05-01-2014
20140096771ENTRAINING POWDER IN AN AIRFLOW - A device for inhalation of at least one air stream carrying a dose of medicament powder. The device comprises a powder-containing cavity which opens into a flow passage. The flow passage is arranged to direct an inhalation air flow across the cavity opening. A circulating flow is thereby induced in the cavity by the phenomenon of shear driven cavity flow. Powder is entrained in the circulating flow and deaggregated before exiting the cavity and becoming entrained in the flow of air along the flow passage.04-10-2014
20140083422INHALER - A dry powder inhaler comprises a disc-shaped assembly (03-27-2014
20140066455NOVEL COMPOUNDS - There is provided a compound of formula (I):03-06-2014
20140045895PHARMACEUTICAL 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.02-13-2014
20140038978HETEROCYCLIC COMPOUNDS AS CCR2B ANTAGONISTS - Compounds of formula (I)02-06-2014
20140038937Chromenone Derivatives - The invention concerns chromenone compounds of Formula I;02-06-2014
20140031379Camsylate Salt - A camsylate salt of (1r,1′R,4R)-4-methoxy-5″-methyl-6′-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3′H-dispiro[cyclohexane-1,2′-inden-1′2′-imidazole]-4″-amine, pharmaceutical compositions containing the salt and therapeutic uses of the salt for treating Aβ-related pathologies such as Alzheimer's Disease, Down's syndrome, β-amyloid angiopathy and conditions such as dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.01-30-2014
20140018364CHEMICAL COMPOUNDS - There is provided pyrimidinyl compounds of Formula (I),01-16-2014
20140000601INHALER01-02-2014
20130345272Cycloalkyl Ether Compounds and Their Use as Bace Inhibitors - Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration and pharmaceutical compositions containing such compounds.12-26-2013
20130345248Cyclohexane-1,2'-Naphthalene-1',2"-Imidazol Compounds and Their Use as Bace - Cyclohexane-1,2′-naphthalene-1′,2″-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.12-26-2013
20130345247Cyclohexane-1,2'-Indene-1',2"-Imidazol Compounds and Their Use as Bace Inhibitors - Cyclohexane-1,2′-indene-1′,2″-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.12-26-2013
201303452462H-Imidazol-4-Amine Compounds and Their Use as Bace Inhibitors - 2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. methods of therapy, and pharmaceutical compositions containing such compounds.12-26-2013
20130310344N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS - 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-X11-21-2013
20130289043(4-TERT-BUTYLPIPERAZIN-2-YL)(PIPERAZIN-1-YL)METHANONE-N-CARBOXAMIDE DERIVATIVES - The present invention relates to compounds of formula (I)10-31-2013
20130237548INJECTABLE EMULSION OF SEDATIVE HYPNOTIC AGENT - Polymorphs of 7-methyl-5-(3-piperazin-1-ylmethyl-[1,2,4]oxadiazol-5-yl)-2-(4-trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one mesylate salt, methods of making these polymorphs and uses thereof.09-12-2013
20130237473Melanocortin Receptor-Specific Peptides - The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I)09-12-2013
20130236501Injectable Emulsion of Sedative Hypnotic Agent - 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.09-12-2013
20130225827New Process for the Preparation of Aryl Substituted Olefinic Amines - 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.08-29-2013
20130225555Imidazoquinolines with Immuno-Modulating Properties - The present invention provides compounds of formula (I)08-29-2013
20130220320Inhaler Comprising A Base Having A Plurality of Medicament Containing Sealed Cavities - An inhaler which comprises a base having a plurality of consecutive sealed cavities containing medicament. Foil portions are on one side attached to the base for sealing the medicament within respective associated cavities. A plurality of separating elements are attached to the other side of the foil portions, each separating element being associated with a respective cavity for separating a foil portion from that cavity. Each separating element can be moved-away from its associated cavity so that the sealing foil portion is separated from the cavity which is thereby uncovered so that medicament contained therein is enabled to become entrained in a fluid flow, and then returned with the attached foil portion to cover its associated cavity. A method of operating an inhaler is also disclosed.08-29-2013
20130203995Process for Making a Metabotropic Glutamate Receptor Positive Allosteric Modulator - 874 - Processes for making 7-methyl-5-(3piperazin-1-ylmethyl-[1,2,4]oxadiazol-5-yl)-2-(4-trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one08-08-2013
20130203730BENZOTHIAZOLES AS GHRELIN RECEPTOR MODULATORS - A compound of formula I08-08-2013
20130199525INHALER CAP STRAP - An inhaler for dispensing doses of medicament from a container under user activation said inhaling which comprises a body which includes a mouthpiece through which the medicament is dispensed and a cap which can be place in a position to substantially occlude the mouthpiece. The cap is attached to said body by a strap which pivots from said body, said cap being arranged to slide on the strap such that the cap must translate away from the mouthpiece prior to the pivoting of the strap.08-08-2013
20130197041GABR-A2 DIAGNOSTIC - The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sites known as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence at these GABR-A2 SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs.08-01-2013
20130195971PHARMACEUTICAL 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.08-01-2013
20130184250Therapeutic Agents - Disclosed herein are azetidinyl compounds of formula I,07-18-2013
20130172560PROCESSES FOR MAKING CYCLOPROPYL AMIDE DERIVATIVES AND INTERMEDIATES ASSOCIATED THEREWITH - 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.07-04-2013
20130165473Azaquinolinone Derivatives and Uses Thereof - The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.06-27-2013
20130143858COMPOUNDS AND THEIR USE AS IKACH BLOCKERS - The invention relates to compounds according to Formula I:06-06-2013
20130137731ETHANAMINE COMPOUNDS AND METHODS OF USING THE SAME - The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treatingh depression by administering the ethanamine compound.05-30-2013
20130133643Inhalation Device - An actuator for an inhaler for delivering medicament by inhalation, comprising: a main body comprising a tubular member for receiving a canister containing medicament and having a valve stem extending therefrom; and an outlet assembly, as a part formed separately of the main body, comprising a mouthpiece for guiding medicament to the mouth of a user and a nozzle block for receiving the valve stem of the canister and delivering medicament from the canister into the mouthpiece; wherein the main body is provided with an outlet opening for receiving the outlet assembly in a position wherein the mouthpiece extends outside the outlet opening and the nozzle block is inserted through the outlet opening and arranged in position for receiving the valve stem of the canister. There is also disclosed an inhaler comprising the above-described actuator and a canister containing medicament, a main body and an outlet assembly.05-30-2013
20130131087Pharmaceutical Compositions - The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing 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.05-23-2013
20130123275PYRAZINE DERIVATIVES - The invention concerns pyrazine derivatives of the Formula I05-16-2013
20130109702TRISUBSTITUTED TRIAZOLOPYRIMIDINES FOR USE IN PLATELET AGGREGATION INHIBITION05-02-2013
20130090358PYRAZOLYLAMINOPYRIDINE DERIVATIVES USEFUL AS KINASE INHIBITORS - This invention relates to novel compounds having the formula (I):04-11-2013
20130061850INHALER 624 - The present invention relates to an Breath actuated inhaler (BAI) actuator, comprising: a loading element capable of being loaded with an actuation force, a breath actuated trigger mechanism arranged to counteract the actuation force of the loading element, and to fire the actuator by releasing the actuation force of the loading element in response to an inhalation breath, and actuation locking means moveable between a locked position wherein it relieves the actuation force from the trigger mechanism setting the trigger mechanism in a neutral position, and an armed position wherein the trigger mechanism is set in an armed position.03-14-2013
20130059870USE 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.03-07-2013
20130058876(TRIMETHOXYPHENYLAMINO) PYRIMIDINYL FORMULATIONS - There are provided pharmaceutical compositions comprising greater than 15% w/w of a compound of Formula (I) as defined herein and/or hydrate thereof and an amount of one or more effervescent agents that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.03-07-2013
201300534092-(2,4,5-SUBSTITUTED-ANILINO) PYRIMIDINE COMPOUNDS - 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 Exon19 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.02-28-2013
20130040970Co-Crystals Of A Triazolo [4,5-D] Pyrimide Platelet Aggregation Inhibitor - 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).02-14-2013
20130035346AMIDE 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.02-07-2013
20130030001QUINUCLIDINE DERIVATIVES AS MUSCARINIC M3 RECEPTOR ANTAGONISTS - The invention provides named compounds of formula (I),01-31-2013
20130029956NEW METHOD - The invention provides a novel method of treating respiratory diseases, e.g., pediatric asthma, in a continuing regimen with not more than one daily dose of the drug budesonide using a nebulizer.01-31-2013
20130023562NOVEL PIPERIDINE DERIVATIVES - The present invention provides a compound of a formula (I):01-24-2013
20130005727QUINAZOLINE DERIVATIVES - The invention concerns quinazoline derivatives of Formula I01-03-2013
20130005725CHEMICAL COMPOUNDS - There is provided pyrimidinyl compounds of Formula (I),01-03-2013
20130005695QUINICLIDINE DERIVATIVES OF (HETERO) ARYLCYCLOHEPTANECARBOXYLIC ACID AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula (I) wherein R01-03-2013
20120329795QUINAZOLINE DERIVATIVES - The invention concerns quinazoline derivatives of Formula I:12-27-2012
20120329766FORMULATION - The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7α-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17β-diol, more particularly to a formulation adapted for administration by injection containing the compound 7α-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17β-diol in solution in a ricinoleate vehicle which additionally comprises at least one alcohol and a non-aqueous ester solvent which is miscible in the ricinoleate vehicle.12-27-2012
20120289520CHEMICAL 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, obesity11-15-2012
20120289513(4-TERT-BUTYLPIPERAZIN-2-YL)(PIPERAZIN-1-YL)METHANONE-N-CARBOXAMIDE DERIVATIVES - The present invention relates to compounds of formula (I)11-15-2012
20120289510Benzyl Amines, A Process For Their Production And Their Use As Anti-Inflammtory Agents - The present invention relates to the compounds of formula I,11-15-2012
20120289504Benzoimidazole Compounds and Uses Thereof - 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.11-15-2012
20120277272Ethanamine Compounds and Methods of Using the Same - (S)-2-methyl-11-01-2012
20120269872NOVEL SALT 628 - 6-M ethyl-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.10-25-2012
20120264943Compounds Suitable As Precursors to Compounds that are Useful for Imaging Amyloid Deposits - The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.10-18-2012
20120264762Heterocyclic Compounds as CCR2 Antagonists - Compounds of formula (I)10-18-2012
20120264731CHROMENONE DERIVATIVES - The invention concerns chromenone compounds of Formula I;10-18-2012
20120252826Combination 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: the administration of ZD6474 in combination with 5-FU; ZD6474 in combination with CPT-11; or ZD6474 in combination with 5-FU and CPT-11.10-04-2012
20120225907BENZAMIDE COMPOUNDS USEFUL AS HISTONE DEACETYLASE INHIBITORS - The invention concerns benzamide compounds of formula (I): compound of formula (I):09-06-2012
20120216802COMPOSITION FOR INHALATION - The invention relates to a formulation comprising formoterol and budesonide for use in the treatment of respiratory diseases. The composition further contains HFA 227, PVP and PEG, preferably PVP K25 and PEG 1000.08-30-2012
20120214822N-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 - The present invention relates to pyrazinone derivatives of formula (I):08-23-2012
20120207679Novel Heteroaryl Substituted Benzothiazoles - The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below:08-16-2012
20120190679Novel Protein Kinase B Inhibitors - 060 - The invention relates to a novel group of compounds of Formula (I) or salts thereof:07-26-2012
20120178726NOVEL COMPOUNDS - The present invention provides compounds of formula (I)07-12-2012
20120177705COMPOSITION 064 - A pharmaceutical composition which comprises N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide with mannitol and/or microcrystalline cellulose is described.07-12-2012
20120165351QUINAZOLINE DERIVATIVES - The invention concerns quinazoline derivatives of Formula I06-28-2012
20120165348Novel compounds - The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.06-28-2012
20120165347Compounds and their use as BACE Inhibitors - 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.06-28-2012
20120165346Compounds and their use as BACE inhibitors - 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 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.06-28-2012
20120149740PHARMACEUTICAL DEPOT FOR N-{5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL)-3-FLUORO-4-(PYRIDIN-2-Y- LMETHOXY)BENZAMIDE - A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, 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.06-14-2012
20120149739PHARMACEUTICAL DEPOT FOR N-{5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL)-3-FLUORO-4-(PYRIDIN-2-Y- LMETHOXY)BENZAMIDE - A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, 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.06-14-2012
20120142659COMPOUNDS AND THEIR USE AS IKACH BLOCKERS - The invention relates to compounds according to Formula I:06-07-2012
20120136167Processes 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.05-31-2012
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

Patent applications by AstraZeneca AB

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