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Vertex Pharmaceuticals Incorporated Patents
Assignee:
Vertex Pharmaceuticals Incorporated
Address:
Cambridge, MA
No. of patents:
289
Patents:


1 2 3 4 5 6


Patent Number Title Of Patent Date Issued
RE40245 Gyrase inhibitors and uses thereof April 15, 2008
The present invention relates to compounds of the formula I: ##STR00001## or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infect
7618974 Gyrase inhibitors and uses thereof November 17, 2009
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 present invention also
7612091 Caspase inhibitors and uses thereof November 3, 2009
The present invention provides a compound of formula I: ##STR00001## wherein: X is --OR.sup.1 or --N(R.sup.5).sub.2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R.sup.1 is: C.sub.1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or al
7612065 Inhibitors of c-JUN N-terminal kinases (JNK) November 3, 2009
The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions
7608632 Sulfonamide inhibitors of aspartyl protease October 27, 2009
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also
7605270 Polymorphic forms of (S).-tetrahydrofuran-3-yl-3-(3-(3-methoxy-4-(oxazol-5-yl) phenyl) ureido) October 20, 2009
The present invention relates to polymorphic forms of (S)-tetrahydrofuran-3-yl 3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzylcarbamate (Compound 1): ##STR00001## and pharmaceutical compositions thereof. The present invention also relates to processes to prepare compound 1 and
7605174 Indane derivatives as modulators of ion channels October 20, 2009
The present invention relates to indane 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.
7601718 Compositions useful as inhibitors of protein kinases October 13, 2009
The present invention provides a compound of formula I: ##STR00001## or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors of GSK-3 mam
7598412 Modulators of ATP-binding cassette transporters October 6, 2009
The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R.sup.B, n, B, R.sup.C, R.sup.D, R.sup.E, A, and Z are described generally and in classes and subclasses below.
7598277 Inhibitors of p38 October 6, 2009
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The i
7598245 Aminotriazole compounds useful as inhibitors of protein kinases October 6, 2009
The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.
7592368 Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors September 22, 2009
The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability
7592340 Quinoxalines useful as inhibitors of protein kinases September 22, 2009
The present invention relates to compounds of formula I 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 di
7589214 Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases September 15, 2009
The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds, to methods of using the compounds and to the compositions in the treatment of various disease, conditions,
7582641 Gyrase inhibitors and uses thereof September 1, 2009
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 of using compounds
7569604 Heterocyclic derivatives for modulation of calcium channels August 4, 2009
Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
7569591 Gyrase inhibitors and uses thereof August 4, 2009
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 present invention also
7563795 Phenyl-piperazine derivatives as modulators of muscarinic receptors July 21, 2009
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
7558717 Crystal structure of human JAK3 kinase domain complex and binding pockets thereof July 7, 2009
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 s
7557106 Substituted pyrimidines useful as protein kinase inhibitors July 7, 2009
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-med
7553855 Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline- -3 June 30, 2009
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.
7553852 Caspase inhibitors and uses thereof June 30, 2009
The present invention relates to compounds of formula I: ##STR00001## useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the compounds, and methods of using the compounds an
7547794 Compositions useful as inhibitors of protein kinases June 16, 2009
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.
7544810 Processes for preparing biaryl ureas and analogs thereof June 9, 2009
The present invention relates to processes for preparing biaryl ureas derivatives and analogs thereof. The invention also provides compounds useful as intermediates in the processes of the present invention. The process is useful for preparing compounds that inhibit IMPDH.
7531570 Treatment of diseases using ICE inhibitors May 12, 2009
This invention relates to methods and compositions for treating autoinflammatory diseases. The invention also assays for evaluating the ability of an ICE inhibitor to treat autoinflammatory diseases.
7531556 Compositions useful as inhibitors of rock and other protein kinases May 12, 2009
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.
7531536 Pyrazole compounds useful as protein kinase inhibitors May 12, 2009
This invention describes novel pyrazole compounds of formula IIIa: ##STR00001## wherein R.sup.1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R.sup.x, R.sup.y, R.sup.2; and R.
7531523 Sodium channel protein type III alpha-subunit splice variant May 12, 2009
The present invention is directed to a splice variant of a human sodium channel alpha subunit and methods and compositions for making and using the same.
7528142 Aminopyrimidines useful as kinase inhibitors May 5, 2009
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
7528138 Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases May 5, 2009
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
7527952 Crystals of inosine monophosphate dehydrogenase/oxidized inosine monophosphate thiomidate interm May 5, 2009
The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site binding pockets of IMPDH. Such data storage material is capable of displaying such molecules and molecular c
7514448 Azaindoles useful as inhibitors of rock and other protein kinases April 7, 2009
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.
7507826 Azaindoles useful as inhibitors of JAK and other protein kinases March 24, 2009
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.
7504515 Polymorphic forms of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4- (oxazol-5-yl)phenyl) ureido March 17, 2009
The present invention relates to polymorphic forms of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate (Compound 1): ##STR00001## pharmaceutical compositions thereof. The present invention also relates to processes to prepare compound 1
7501415 Selective inhibitors of ERK protein kinase and uses thereof March 10, 2009
Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferative disorders such as cancer.
7498166 Dual expression vector system and screening methods March 3, 2009
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 of only a single vecto
7495103 Modulators of ATP-binding cassette transporters February 24, 2009
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 tra
7495014 Gyrase inhibitors and uses thereof February 24, 2009
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
7494988 Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease February 24, 2009
The present invention relates to compounds that are useful as protease inhibitors, particularly as serine protease inhibitors, and more particularly as hepatitis C NS3 protease inhibitors. As such, they act by interfering with the life cycle of the hepatitis C virus and are also usef
7494660 HCV NS3-NS4A protease resistance mutants February 24, 2009
The present invention is directed to mutants of HCV NS3/4A protease. More particularly, the present invention identifies mutant of HCV NS3/4A protease that are resistant to drug treatment.
7491730 Compositions useful as inhibitors of GSK-3 February 17, 2009
The present invention provides a compound of formula I: ##STR00001## or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3 mammalian protein kinase. The invention also provides pharmaceutically acceptable
7488727 Thiazole compounds useful as inhibitors of protein kinase February 10, 2009
The present invention provides a compound of formula I: ##STR00001## or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3, Aurora2, and Syk mammalian protein kinases. The invention also provides pharm
7485664 Inhibitors of TACE February 3, 2009
The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.
7473691 Pyrazole compounds useful as protein kinase inhibitors January 6, 2009
This invention describes novel protein kinase inhibitors of formula VII: ##STR00001## wherein G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents indep
7465738 Compounds useful as promoters of SMN2 December 16, 2008
The present invention relates to compounds useful as promoters of the SMN2 gene. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of Spinal Muscular Atrophy.
7462612 Pyridine inhibitors of ERK2 and uses thereof December 9, 2008
The present invention relates to compounds useful of 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.
7456190 Compositions useful as protein kinase inhibitors November 25, 2008
The present invention relates to compounds useful of 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.
7452873 Inhibitors of GSK-3 and uses thereof November 18, 2008
The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provide
7446199 Compositions useful as inhibitors of protein kinases November 4, 2008
The present invention relates to compounds useful of 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.
7446112 Modulators of muscarinic receptors November 4, 2008
The modulator compounds described herein modulate muscarinic receptors and are useful for treating muscarinic receptor mediated diseases.
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