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Assignee: Vertex Pharmaceuticals Incorporated


Location: Cambridge, MA
No. of patents: 433

1                      
NumberTitleIssue Date
8173635Kinase 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, o...
05/08/2012
8168798Caspase inhibitor prodrugs
This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to ...
05/01/2012
8163917Azaindoles 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 treatm...
04/24/2012
8163772Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxypheny1]-1,4-dihydro-4-oxoquinoline-3-carboxamide
Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof. ...
04/24/2012
8163737CGRP receptor antagonists
The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions. ...
04/24/2012
8163732Tricyclic 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 treatm...
04/24/2012
8163720Pyrrolidinyl phenyl sulphonamides as modulators of ion channels
The present invention relates to 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 variou...
04/24/2012
8158637Quinazolines useful as modulators of voltage gated ion 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...
04/17/2012
8153668Polymorphic forms of (S)-1-tetrahydrofuran-3-yl-3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzylcarbamate
The present invention relates to polymorphic forms of (S)-tetrahydrofuran-3-yl 3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzylcarbamate, processes therein, pharmaceutical compositions thereof, and uses therewith. ...
04/10/2012
8153655Compositions 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...
04/10/2012
8153642Quinazolines useful as modulators of ion channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the composition...
04/10/2012
8143297Heterocyclic 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 v...
03/27/2012
8129546Derivatives for modulation of ion channels
Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions. ...
03/06/2012
8129399Aminopyrimidines useful as kinase inhibitors
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 diseas...
03/06/2012
8129387Substituted 5,6-dihydroimidazo[1,5-F]pteridines useful as protein kinase inhibitors
The present invention relates to substituted 5,6-dihydroimidazo[1,5-f]pteridines of formula I: which are useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprisin...
03/06/2012
8129381Caspase inhibitors and uses thereof
The present invention relates to compounds of formula I: useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the ...
03/06/2012
8124781Processes 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). ...
02/28/2012
8124392Crystal structure of Aurora-2 protein and binding pockets thereof
The present invention provides crystalline molecules or molecular complexes which comprise binding pockets of Aurora-2 or its homologues. The invention also provides crystals comprising Aurora-2. The present invention also relates to a computer comprising a data sto...
02/28/2012
8119631Inhibitors of interleukin-1β converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmace...
02/21/2012
8101770Pyridones 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, ...
01/24/2012
8101767Modulators 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 metho...
01/24/2012
8101378Dual expression vector system and screening methods
The present invention features vectors that contain a promoter effective for expression in bacterial cells and a promoter effective for expression in insect cells. The dual promoter system allows use of the same vector in both host cell systems so that construction ...
01/24/2012
8097636Heterocyclic 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 v...
01/17/2012
8093392Caspase inhibitors and uses thereof
This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R...
01/10/2012
8076357Compositions of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
Pharmaceutical compositions including N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods of using such compositions are described herein. ...
12/13/2011
8076343Benzimidazoles useful as inhibitors of protein kinases
The present invention relates to compounds useful as inhibitors of Aurora, FLT-3, or PDK1 protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various...
12/13/2011
8071618Caspase inhibitors and uses thereof
The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 ...
12/06/2011
8067606Gyrase inhibitors and uses thereof
The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods...
11/29/2011
8067417Imidazo[1,2-F]pteridines useful as inhibitors of protein kinases
The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. The invention also provides ...
11/29/2011
8058271Selective inhibitors of rock protein kinase and uses thereof
Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurologica...
11/15/2011
8039661Thiophene-carboxamides 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 compositions in the treatment of various diseas...
10/18/2011
8039623Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As ...
10/18/2011
8039491Modulators 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 p...
10/18/2011
8039475Co-crystals and pharmaceutical compositions comprising the same
The invention relates to compositions and co-crystals each comprising (1S,3aR,6aS)-2-[(2S)-2-[[(2S)-2-Cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c...
10/18/2011
8034950Processes for the facile synthesis of diaryl amines and analogues thereof
The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the proce...
10/11/2011
8034832Gyrase inhibitors and uses thereof
The present invention relates to compounds that 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 pr...
10/11/2011
8022202Dihydrodiazepines 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, o...
09/20/2011
8022041Prodrug of an ICE inhibitor
This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative...
09/20/2011
8017781Azaindazoles 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, o...
09/13/2011
8017619Compositions useful as inhibitors of protein kinases
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositi...
09/13/2011
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