VERTEX PHARMACEUTICALS INCORPORATED Patent applications |
Patent application number | Title | Published |
20160096807 | CO-CRYSTALS OF MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present disclosure relates to co-crystals comprising N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and a co-former and methods for their preparation. The present disclosure further relates to pharmaceutical compositions comprising the co-crystal forms, as well as methods of treatment therewith and kits. | 04-07-2016 |
20160095858 | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention features a compound of formula I: | 04-07-2016 |
20160052916 | SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL)CYCLOPROPANECARBOXAMIDO)-3-- METHYLPYRIDIN-2-YL) BENZOIC ACID - The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith. | 02-25-2016 |
20160030424 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE AND COMBINATION THERAPIES THEREOF - The present invention relates to compounds useful as inhibitors of ATR protein kinase and combination therapies thereof. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 02-04-2016 |
20150336945 | QUINOLINE AND QUINAZOLINE AMIDES AS MODULATORS OF SODIUM CHANNELS - The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: | 11-26-2015 |
20150328196 | AMIDES AS MODULATORS OF SODIUM CHANNELS - The invention relates to amide compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: | 11-19-2015 |
20150246028 | PYRIDONE AMIDES AS MODULATORS OF SODIUM CHANNELS - The invention relates to pyridone amide compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: | 09-03-2015 |
20150140094 | PHARMACEUTICAL COMPOSITIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID AND ADMINISTRATION THEREOF - A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient. | 05-21-2015 |
20150111871 | DNA-PK INHIBITORS - The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 04-23-2015 |
20150065500 | Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 03-05-2015 |
20150065439 | PHARMACEUTICAL COMPOSITIONS - Described herein are compositions that can include Compound 1 or Form J of Compound 1, or a pharmaceutically acceptable salt of the aforementioned compounds. Also, described herein is a method of treating a HCV infection in a subject that can include administering to the subject a composition that includes Compound 1 or Form J of Compound 1, or a pharmaceutically acceptable salt of the aforementioned compounds. | 03-05-2015 |
20150031720 | ISOTHIAZOLOPYRIDINONES USEFUL FOR THE TREATMENT OF (INTER ALIA) CYSTIC FIBROSIS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-29-2015 |
20150031661 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 01-29-2015 |
20140343098 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 11-20-2014 |
20140323521 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 10-30-2014 |
20140315931 | DEAZAPURINES USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 10-23-2014 |
20140309413 | METHODS OF STEREOSELECTIVE SYNTHESIS OF SUBSTITUTED NUCLEOSIDE ANALOGS - The present invention relates to the novel diastereoselective syntheses for generating phosphorothioate compounds. Examples include nucleoside phosphorothioate analogs that are useful in treating diseases and/or conditions such as viral infections. | 10-16-2014 |
20140308242 | BIOMARKERS FOR HCV INFECTED PATIENTS - The invention relates to biomarkers measurable in a human subject that have prognostic value with respect to efficacy of therapeutic treatments for Hepatitis C viral infection. The markers also are believed to have value for diagnosis liver health/liver damage. | 10-16-2014 |
20140303204 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. | 10-09-2014 |
20140288347 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 09-25-2014 |
20140275059 | DNA-PK INHIBITORS - The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 09-18-2014 |
20140275024 | DNA-PK INHIBITORS - The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 09-18-2014 |
20140274930 | MANNOSE DERIVATIVES FOR TREATING BACTERIAL INFECTIONS - The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: | 09-18-2014 |
20140256770 | PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1, | 09-11-2014 |
20140255483 | PHARMACEUTICAL COMPOSITION AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition. | 09-11-2014 |
20140249138 | AZAINDOLES USEFUL AS INHIBITORS OF JAK AND OTHER PROTEIN KINASES - The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 09-04-2014 |
20140249137 | PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS - The present invention relates to compounds useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the inventions and | 09-04-2014 |
20140243289 | PRODRUGS OF MODULATORS OF ABC TRANSPORTERS - The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 08-28-2014 |
20140243283 | MANNOSE DERIVATIVES FOR TREATING BACTERIAL INFECTIONS - The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: | 08-28-2014 |
20140243273 | METHODS FOR TREATING INFLAMMATORY DISEASES AND PHARMACEUTICAL COMBINATIONS USEFUL THEREFOR - The present invention provides method of treating or lessening the severity of a disease selected from spondyloarthropathy, systemic lupus erythematosus, rheumatoid arthritis, or any combination thereof comprising the administration of a compound of Formula I and an optional co-therapy (e.g., chemotherapy agent, DMARD, or any combination thereof). The present invention also provides a pharmaceutical composition comprising a compound of Formula I, a method of manufacturing a pharmaceutical composition comprising a compound of Formula I, and a method of administering a pharmaceutical composition comprising a solid form of a compound of Formula I. | 08-28-2014 |
20140243257 | BENZIMIDAZOLE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I: | 08-28-2014 |
20140242172 | Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 08-28-2014 |
20140235705 | FORMULATIONS OF THIOPHENE COMPOUNDS - A pharmaceutical composition comprises: a) polymorphic form M or tromethamine salt of Compound (1) represented by the following structural formula: | 08-21-2014 |
20140235704 | THIOPHENE COMPOUNDS - A co-crystal of Compound (1) includes Compound (1) and a co-crystal former selected from the group consisting of urea, nicotinamide, and isonicotinamide, wherein Compound (1) is characterized by the following structural formula: | 08-21-2014 |
20140235703 | THIOPHENE COMPOUNDS - Polymorph Forms M, H, P, X, and ZA of Compound (1) represented by the following structural formula: | 08-21-2014 |
20140235668 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR VPI - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 08-21-2014 |
20140235625 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators. | 08-21-2014 |
20140221435 | AMIDES AS MODULATORS OF SODIUM CHANNELS - The invention relates to amide compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: | 08-07-2014 |
20140221430 | Solid Forms of 3-(6-(1-(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)Cyclopropanecarboxamido)-3-- Methylpyridin-2-yl)Benzoic Acid - The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith. | 08-07-2014 |
20140221336 | COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 08-07-2014 |
20140221334 | KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 08-07-2014 |
20140213616 | PYRIDONE AMIDES AS MODULATORS OF SODIUM CHANNELS - The invention relates to pyridone amide compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: | 07-31-2014 |
20140206888 | METHODS FOR PREPARATION OF THIOPHENE COMPOUNDS - A method of preparing Compound (1): | 07-24-2014 |
20140206720 | DOSAGE UNITS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D] [1,3] DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in Form I, pharmaceutical packs or kits thereof, and methods of treatment therewith. | 07-24-2014 |
20140206689 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 07-24-2014 |
20140206671 | TRICYCLIC HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASE - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 07-24-2014 |
20140199684 | METHODS FOR AMPLIFYING HEPATITIS C VIRUS NUCLEIC ACIDS - A method of amplifying an HCV nucleic acid in an HCV infected sample comprises amplifying a segment of a DNA template that is complementary to a genome of HCV RNA from the sample by a two-stage PCR, wherein a first stage PCR employs a first outer primer and a second outer primer, and a second stage PCR employs a first inner primer and a second inner primer. The nucleotide sequence of the first outer primer comprises a nucleotide sequence as set forth in SEQ ID NO: 2; or SEQ ID NO:9, wherein optionally 1, 2 or 3 nucleotides are other nucleotides than those of SEQ ID NO: 9. The nucleotide sequence of the second outer primer comprises a nucleotide sequence set forth in SEQ ID NO: 3 or 4; or a nucleotide sequence as set forth in SEQ ID NO: 10 or 11, wherein optionally 1, 2 or 3 nucleotides are other nucleotides than those of SEQ ID NO: 10 and 11. The nucleotide sequence of the first inner primer comprises a nucleotide sequence as set forth in SEQ ID NO: 5; or SEQ ID NO:12, wherein optionally 1, 2 or 3 nucleotides are other nucleotides than those of SEQ ID NO: 12. The nucleotide sequence of the second inner primer comprises a nucleotide sequence as set forth in SEQ ID NO: 6 or 7; or a nucleotide sequence as set forth in SEQ ID NO: 13 or 14, wherein optionally 1, 2 or 3 nucleotides are other nucleotides than those of SEQ ID NO: 13 and 14. | 07-17-2014 |
20140187787 | PROCESS FOR PREPARING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith. | 07-03-2014 |
20140187781 | AMINOPYRIDINES AND AMINOPYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 07-03-2014 |
20140187770 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 07-03-2014 |
20140183768 | PHARMACEUTICAL COMPOSITIONS - Methods of spray drying are described. | 07-03-2014 |
20140171454 | Substituted Pyrrolo[2,3-d]pyrimidines as Inhibitors of Protein Kinases - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 06-19-2014 |
20140171427 | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels - The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 06-19-2014 |
20140163068 | Pharmaceutical Compositions for the Treatment of CFTR Mediated Diseases - Pharmaceutical compositions comprising 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1) in Form I and a solid dispersion comprising substantially amorphous N-(5-hydroxy-2,4-ditert-butyl-phenyl)-4-oxo-1H-quinoline-3-carboxamide (Compound 2), methods of treating, lessening the severity of, or symptomatically treating CFTR mediated diseases, such as cystic fibrosis, methods of manufacturing, methods of administering, and kits thereof are disclosed. | 06-12-2014 |
20140163011 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 06-12-2014 |
20140155626 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 06-05-2014 |
20140155431 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 06-05-2014 |
20140154151 | AUTOMATED DEVELOPER FOR IMMUNO-STAINED BIOLOGICAL SAMPLES - Disclosed herein are systems and methods for the developing of immuno-stained biological samples. The systems disclosed herein are automated and are configured to control one or more steps of the developing procedure. Reagents may be added using automatic syringe dispensing. Reagent temperature, reagent stirring, and wash procedures are programmable and can be separately controlled for separate immuno-staining procedures that are performed at the same time. | 06-05-2014 |
20140148434 | PYRAZOLOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 05-29-2014 |
20140142312 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith. | 05-22-2014 |
20140142138 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 05-22-2014 |
20140142119 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 05-22-2014 |
20140127160 | TREATMENT OF HEPATITIS C VIRUS WITH TELAPREVIR (VX-950) IN PATIENTS NON-RESPONSIVE TO TREATMENT WITH PEGYLATED INTERFERON-ALPHA 2A/2B AND RIBAVIRIN - The present invention relates to antiviral therapies and compositions for treating or preventing Hepatitis C infections in patients and relates to other methods disclosed herein. The invention also relates to kits and pharmaceutical packs comprising compositions and dosage forms. The invention also relates to processes for preparing these compositions, dosages, kits, and packs. | 05-08-2014 |
20140121381 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators. | 05-01-2014 |
20140121379 | PROCESSES FOR PRODUCING CYCLOALKYLCARBOXAMIDO-PYRIDINE BENZOIC ACIDS - The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1). | 05-01-2014 |
20140121208 | Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases - The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions. | 05-01-2014 |
20140113933 | Solid Forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-- (trifluoromethyl)-1,4-dihyroquinoline-3-carboxamide - The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith. | 04-24-2014 |
20140113005 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present disclosure relates to pyrazine compounds of formula I: | 04-24-2014 |
20140112988 | Pharmaceutical Composition and Administrations Thereof - The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention. | 04-24-2014 |
20140107318 | PROCESSES AND INTERMEDIATES - The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections. | 04-17-2014 |
20140107093 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 04-17-2014 |
20140107049 | MANNOSE DERIVATIVES FOR TREATING BACTERIAL INFECTIONS - The present invention relates to compounds useful for the treatment or prevention of bacteria infections. The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. The invention also provides processes for making the compounds of the invention. | 04-17-2014 |
20140094499 | FORMULATIONS OF (R)-1-(2,2-DIFLUOROBENZO[D] [1,3] DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METHYLPRO- PAN-2-YL)-1H-INDOL-5-YL)CYCLOPROPANECARBOXAMIDE - The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith. | 04-03-2014 |
20140094473 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 04-03-2014 |
20140088160 | Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6- -fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarbox- amide and administration thereof - A pharmaceutical composition comprising Compound 1, (R)-1-(2,2-difluorobenzo[d][1,3]dioxo-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed. | 03-27-2014 |
20140088142 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - This invention relates to a compound of Formula I: | 03-27-2014 |
20140088141 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. | 03-27-2014 |
20140080826 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 03-20-2014 |
20140080825 | Modulators of ATP-binding cassette transporters - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 03-20-2014 |
20140073653 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to compounds of formula IVA, formula IVB, or formula IVC, useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators. | 03-13-2014 |
20140072995 | Modulators of ATP-Binding Cassette Transporters - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 03-13-2014 |
20140065103 | COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRIDAE VIRAL INFECTIONS - A compound is selected from the structural formulae depicted in FIG. | 03-06-2014 |
20140057906 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 02-27-2014 |
20140056847 | INHIBITORS OF SERINE PROTEASES - This invention relates to compounds of formula I: | 02-27-2014 |
20140051724 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 02-20-2014 |
20140050697 | ANALYSIS OF HCV GENOTYPES - A method for predicting response of a patient infected with HCV-1a to interferon treatment. | 02-20-2014 |
20140044802 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASEAND COMBINATION THERAPIES THEREOF - The present invention relates to compounds useful as inhibitors of ATR protein kinase and combination therapies thereof. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 02-13-2014 |
20140038935 | DIHYDRODIAZEPINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 02-06-2014 |
20140037754 | AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 02-06-2014 |
20140031277 | INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE - The present invention relates to compounds of formula I: | 01-30-2014 |
20140024672 | AZAINDOLE DERIVATIVES AS CFTR MODULATORS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-23-2014 |
20140023706 | PHARMACEUTICAL COMPOSITIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID AND ADMINISTRATION THEREOF - A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient. | 01-23-2014 |
20140018352 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 01-16-2014 |
20140012003 | PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1, | 01-09-2014 |
20140011846 | Solid Forms of 3-(6-(1-(2,2-Difluorobenzo[D][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-- methylpyridin-2-yl) Benzoic Acid - The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith. | 01-09-2014 |
20140010784 | INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE - The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. | 01-09-2014 |
20140005197 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION | 01-02-2014 |
20140005192 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION | 01-02-2014 |
20130345208 | ION CHANNEL MODULATORS AND METHODS OF USE - In general, the invention relates to novel 4-phenylpyrimidine compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels for the treatment of pain. | 12-26-2013 |
20130345197 | AZAINDOLES USEFUL AS INHIBITORS OF JAK AND OTHER PROTEIN KINASES - The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 12-26-2013 |
20130338188 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 12-19-2013 |
20130338119 | Pyrrolidinone Benzenesulfonamide Derivatives as Modulators of Ion Channels - The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 12-19-2013 |
20130331567 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 12-12-2013 |
20130331412 | Pharmaceutical Compositions and Administrations Thereof - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 12-12-2013 |
20130324743 | PROCESS OF PRODUCING CYCLOALKYLCARBOXAMIDO-INDOLE COMPOUNDS - The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis. | 12-05-2013 |
20130317060 | Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to solid state forms of N—[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 11-28-2013 |
20130317020 | Pyridyl Derivatives as CFTR Modulators - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 11-28-2013 |
20130316945 | INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE - The present invention relates to compounds of formula I: | 11-28-2013 |
20130310418 | Azaindazoles useful as inhibitors of kinases - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 11-21-2013 |
20130296364 | MODULATORS OF ATP-BINDING CASSETTE-TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 11-07-2013 |
20130296306 | Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 11-07-2013 |
20130281487 | Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith. | 10-24-2013 |
20130274477 | PROCESSES FOR PRODUCING CYCLOALKYLCARBOXAMIDO-PYRIDINE BENZOIC ACIDS - The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1). | 10-17-2013 |
20130273003 | Therapies for Treating Hepatitis C Virus Infection - The present invention provides a treatment for Hepatitis C virus infection patients of different IL28B gentoypes. The invention therefore provides for the prevention of the clinical sequelae of Hepatitis C viral infections. The present invention also provides a treatment for liver damage and liver inflammation. In one embodiment the invention provides a therapeutic regimen comprising administering to a patient having IL28B genotype CC, CT or TT, VX-222, or a pharmaceutically acceptable salt thereof. | 10-17-2013 |
20130267540 | SOLID FORMS OF GYRASE INHIBITOR (R)-1-ETHYL-3-[6-FLUORO-5-[2-(1-HYDROXY-1-METHYL-ETHYL)PYRIMIDIN-5-YL]-7-- (TETRAHYDROFURAN-2-YL)-1H-BENZIMIDAZOL-2-YL]UREA - The present application is directed to solid forms of compounds of formula I: | 10-10-2013 |
20130261077 | MANNOSE DERIVATIVES FOR TREATING BACTERIAL INFECTIONS - The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: | 10-03-2013 |
20130252939 | TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 09-26-2013 |
20130245273 | AMINOPYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 09-19-2013 |
20130237516 | AZAINDOLES USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 09-12-2013 |
20130231370 | AMIDES USEFUL AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 09-05-2013 |
20130231368 | Solid Forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluorormethyl)phenyl)-4-oxo-5- -(trifluoromethyl)-1,4-dihyroquinoline-3-carboxamide - The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith. | 09-05-2013 |
20130231364 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 09-05-2013 |
20130224293 | PHARMACEUTICAL COMPOSITION AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions containing a solid dispersion of N—[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition. | 08-29-2013 |
20130203706 | COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - A compound is represented by Structural Formula (I): | 08-08-2013 |
20130196983 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators. | 08-01-2013 |
20130195797 | HIGH POTENCY FORMULATIONS OF VX-950 - High potency pharmaceutical compositions comprising VX-950, sodium lauryl sulfate and a polymer selected from the group consisting of hypromellose acetate succinate-M, hypromellose acetate succinate-L and hypromellose acetate succinate-H. | 08-01-2013 |
20130190289 | COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - A compound is represented by Structural Formula (I): | 07-25-2013 |
20130186801 | FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a disintegrant, a surfactant, a binder, and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Processes of preparing pharmaceutical compositions comprising Compound 1 are also disclosed. | 07-25-2013 |
20130184292 | Processes for Making Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. | 07-18-2013 |
20130184276 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 07-18-2013 |
20130184259 | PYRIDONES USEFUL AS INHIBITORS OF KINASES - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes. | 07-18-2013 |
20130184258 | Compositions Useful as Inhibitors of Voltage-Gated Sodium Channels - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 07-18-2013 |
20130183266 | COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - A compound is represented by Structural Formula (I): | 07-18-2013 |
20130177531 | Inhibitors of Serine Proteases - This invention relates to compounds of formula I: | 07-11-2013 |
20130172276 | PROCESSES AND INTERMEDIATES - The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections. | 07-04-2013 |
20130165442 | Modulators of ATP-Binding Cassette Transporters - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 06-27-2013 |
20130158071 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 06-20-2013 |
20130157997 | BENZIMIDAZOLE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I: | 06-20-2013 |
20130157258 | HCV NS5B PROTEASE MUTANTS - The invention provides polypeptides comprising an amino acid sequence comprising at least one variation from wild-type HCV NS5B polymerase, the at least one variation selected from the group consisting of cysteine, isoleucine, valine, or proline at amino acid position 419; alanine, valine, or asparagine at amino acid position 482; valine, isoleucine, threonine, or serine at amino acid position 486; and isoleucine at amino acid position 494, as the amino acid positions are defined in SEQ ID NO: 1, and having Hepatitis C Virus (HCV) NS5B polymerase activity. Polynucleotides encoding the polypeptide, antibodies, host cells, compositions, and methods for detecting an HCV NS5B polymerase having resistance to a polymerase inhibitor also are provided. | 06-20-2013 |
20130143919 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 06-06-2013 |
20130143918 | Solid Forms of (R)-1(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)-N-(1-(2,3-Dihydroxypropyl-6-F- luoro-2-(1-Hydroxy-2-Methylpropan-2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxa- mide - The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith. | 06-06-2013 |
20130137722 | SOLID FORMS OF N-(4-(7-AZABICYCLO[2.2.1]HEPTAN-7-YL)-2-TRIFLUOROMETHYL)PHENYL)-4-OXO-5-(- TRIFLUOROMETHYL)-1,4-DIHYDROQUINOLINE-3-CARBOXAMIDE - The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith. | 05-30-2013 |
20130137703 | AMINOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 05-30-2013 |
20130137125 | CRYSTAL STRUCTURE OF HUMAN JAK3 KINASE DOMAIN COMPLEX AND BINDING POCKETS THEREOF - The present invention relates to human Janus Kinase 3 (JAK3) and JAK3-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to JAK3 protein or JAK3 protein homologues, or complexes thereof. The invention also relates to crystallizable compositions and crystals comprising JAK3 kinase domain and JAK3 kinase domain complexes with AMP-PNP. | 05-30-2013 |
20130136719 | COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I: | 05-30-2013 |
20130131359 | PROCESSES AND INTERMEDIATES FOR PREPARING STERIC COMPOUNDS - This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 | 05-23-2013 |
20130131109 | BICYCLIC DERIVATIVES AS MODULATORS OF VOLTAGE GATED ION CHANNELS - Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions. | 05-23-2013 |
20130131107 | PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF - The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. | 05-23-2013 |
20130116238 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 05-09-2013 |
20130116228 | THIAZOLES AND PYRAZOLES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 05-09-2013 |
20130116169 | INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE - The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds. | 05-09-2013 |
20130115314 | Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 05-09-2013 |
20130115313 | Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 05-09-2013 |
20130115312 | Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 05-09-2013 |
20130115311 | Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 05-09-2013 |
20130115310 | Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 05-09-2013 |
20130109717 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE | 05-02-2013 |
20130102782 | PROCESSES AND INTERMEDIATES FOR PRODUCING AZAINDOLES - The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK). | 04-25-2013 |
20130102629 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula (I) | 04-25-2013 |
20130096277 | PROCESSES AND INTERMEDIATES - A process for preparing enantioselectively a compound of formula I-1a or I-1b: | 04-18-2013 |
20130096139 | Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 04-18-2013 |
20130095500 | AUTOMATED DEVELOPER FOR IMMUNO-STAINED BIOLOGICAL SAMPLES - Disclosed herein are systems and methods for the developing of immuno-stained biological samples. The systems disclosed herein are automated and are configured to control one or more steps of the developing procedure. Reagents may be added using automatic syringe dispensing. Reagent temperature, reagent stirring, and wash procedures are programmable and can be separately controlled for separate immuno-staining procedures that are performed at the same time. | 04-18-2013 |
20130095193 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 04-18-2013 |
20130095181 | PHARMACEUTICAL COMPOSITIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIODIN-2-YL)BENZOIC ACID AND ADMINISTRATION THEREOF - A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient. | 04-18-2013 |
20130090479 | THIAZOLES, IMIDAZOLES, AND PYRAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions. | 04-11-2013 |
20130090364 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I | 04-11-2013 |
20130090354 | Pharmaceutical Compositions and Administrations Thereof - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of CFTR mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. | 04-11-2013 |
20130090351 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I | 04-11-2013 |
20130090331 | TRICYCLIC HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASE - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 04-11-2013 |
20130089626 | Treating Cancer with ATR Inhibitors - This invention relates to methods and compositions for treating pancreatic cancer. More specifically, this invention relates to treating pancreatic cancer with certain ATR inhibitors in combination with gemcitabine and/or radiation therapy. This invention also relates to methods and compositions for treating non-small cell lung cancer. More specifically, this invention relates to treating non-small cell lung cancer with an ATR inhibitor in combination with cisplatin or carboplatin, etoposide, and ionizing radiation. | 04-11-2013 |
20130089625 | Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; solid forms of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 04-11-2013 |
20130089624 | Compounds Useful as Inhibitors of ATR Kinase - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 04-11-2013 |
20130085158 | SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith. | 04-04-2013 |
20130085150 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I | 04-04-2013 |
20130084639 | Bicyclic Derivatives as Modulators of Ion Channels - The present invention relates to bicyclic compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 04-04-2013 |
20130079367 | SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE- -3-CARBOXAMIDE - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 03-28-2013 |
20130079289 | Pharmaceutical Compositions - Forms and formulations of VX-950 and uses thereof. | 03-28-2013 |
20130072687 | Process for Preparing Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith. | 03-21-2013 |
20130072523 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R1, R | 03-21-2013 |
20130072522 | Process for Making Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The invention provides a process for the preparation of a compound of Formula 1, | 03-21-2013 |
20130072440 | CO-CRYSTALS AND PHARMACEUTICAL FORMULATIONS COMPRISING THE SAME - The pharmaceutical composition including a co-crystal. The co-crystal includes a) a co-former; and b) an active pharmaceutical ingredient (API) with solubility in water is less than one part by weight of the API in ten parts by weight of water. Furthermore, the formulation includes a polymer, and a weight ratio of the co-crystal to the polymer is about 0.5:99.5 to about 99.5:0.5. The kinetic solubility of the co-crystal after being in contact with an environment of use is at a therapeutically acceptable level for a prolonged period of time. | 03-21-2013 |
20130071834 | COMPOSITIONS AND METHODS USEFUL FOR HCV INFECTION - The present invention provides compositions comprising cells that can effectively produce HCV after HCV infection, compositions for culturing the cells, methods for making the composition and methods for infecting the cells in the composition with HCV. The present invention also provides methods for assaying HCV production and methods for evaluating compounds that affect the production of HCV. | 03-21-2013 |
20130066083 | PROCESSES AND INTERMEDIATES - The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof. | 03-14-2013 |
20130066069 | PROCESSES FOR PREPARING SUBSTITUTED PYRIMIDINES - The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions. | 03-14-2013 |
20130053395 | PYRAZOLOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 02-28-2013 |
20130053394 | PYRAZOLOPYRIMIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 02-28-2013 |
20130053388 | PYRAZOLOPYRAZINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 02-28-2013 |
20130035310 | Piperidine and Piperazine Phenyl Sulfonamides as Modulators of Ion Channels - The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain. | 02-07-2013 |
20130034616 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 02-07-2013 |
20130034522 | THERAPIES FOR TREATING HEPATITIS C VIRUS INFECTION - A method of improving the pharmacokinetics of VX-222 in a patient infected with HCV comprises co-administering VX-222 and VX-950 to the patient. A method of treating a patient infected with HCV comprises administering VX-222 and VX-950 to the patient, wherein VX-222 is in an amount of about 20 mg to about 400 mg, and wherein VX-950 is in an amount of about 100 mg to about 1,500 mg. A method of treating a patient infected with HCV comprises administering a therapeutically effective amount of VX-222, wherein VX-222 is administered at an amount of about 20 mg to about 2,000 mg once a day. | 02-07-2013 |
20130023538 | Heteroaryl Derivatives as CFTR Modulators - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-24-2013 |
20130023525 | GYRASE INHIBITORS AND USES THEREOF - The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. | 01-24-2013 |
20130018072 | AMINOPYRAZOLE TRIAZOLOTHIADIAZOLE INHIBITORS OF C-MET PROTEIN KINASE - The present invention relates to compounds of formula I, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders. | 01-17-2013 |
20130018071 | Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3-carboxamide - The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. | 01-17-2013 |
20130018070 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-17-2013 |
20130018035 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 01-17-2013 |
20130017273 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 01-17-2013 |
20130012536 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, | 01-10-2013 |
20130012430 | INHIBITORS OF SERINE PROTEASES, PARTICULARLY HEPATITIS C VIRUS NS3 PROTEASE - The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus. | 01-10-2013 |
20130011923 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-10-2013 |