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Attorney: Vertex Pharmaceuticals Incorporated


Number of patents: 66
Last date: March 06, 2012

1    
NumberTitleIssue Date
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
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
7960415Caspase inhibitors and uses thereof
The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical composi...
06/14/2011
7951820Triazole compounds useful as protein kinase inhibitors
This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitr...
05/31/2011
7906650Caspase 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...
03/15/2011
7659283Pyrrolo [3,2-C] pyridines 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...
02/09/2010
7622463Dihydrodiazepines 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...
11/24/2009
7605174Indane derivatives as modulators of ion channels
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...
10/20/2009
7598412Modulators of ATP-binding cassette transporters
The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE...
10/06/2009
7592340Quinoxalines useful as inhibitors of protein kinases
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,...
09/22/2009
7205327Imidazole and benzimidazole caspase inhibitors and uses thereof
This invention provides caspase inhibitors having the formula: wherein R1 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R2 and R3 are ...
04/17/2007
7183307Pyrazole-derived kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R1, n, R3, Q and R4 are described in the specification. The compounds ar...
02/27/2007
7179826Compositions 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 said compounds and methods of using the compositions in the treatment of various disease, conditions, ...
02/20/2007
7169798Inhibitors of c-Jun N terminal kinases (JNK) and other protein kinases
The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described be...
01/30/2007
7169800Imidazole compositions useful as inhibitors of protein kinases
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods o...
01/30/2007
7157476Aminofurazan compounds useful as protein kinase inhibitors
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, ...
01/02/2007
7115746Processes 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...
10/03/2006
7115739Triazole compounds useful as protein kinase inhibitors
This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2
10/03/2006
7109172Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds of formula I or formula Ia or pharmaceutically acceptable salts thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the l...
09/19/2006
7109357Process and intermediates for making substituted aspartic acid acetals
Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula I: wherein R1 is an optionally substituted group selected from an aliphatic group, aralkyl group, he...
09/19/2006
7098330Pyrazolylamine substituted quinazoline compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula III: wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R...
08/29/2006
7091343Compositions useful as inhibitors of protein kinases
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, ...
08/15/2006
7087603Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IV: wherein Z1 or Z2 is nitrogen, Q is —S—, —O—, —N(R4)—, —C(R6′)2—, 1,2-cyclo...
08/08/2006
7087642Inhibitors of IMPDH enzyme
The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH e...
08/08/2006
7084159Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative o thereof, wherein A, B, Ra, R1, R2, R3, and R4 are as des...
08/01/2006
7078209CAK inhibitors and uses thereof
The present invention relates to compounds useful as inhibitors of CAK, compositions thereof. The present invention also relates to methods using the compositions for treating CAK-mediated diseases, such as fungal infections. ...
07/18/2006
7074782Carbamate caspase inhibitors and uses thereof
This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electron...
07/11/2006
7056944Pyrazole compositions useful as inhibitors of erk
Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease st...
06/06/2006
7053057Caspase inhibitors and uses thereof
This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2
05/30/2006
7041687Indazole compounds useful as protein kinase inhibitors
The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2, and V3 are as described i...
05/09/2006
6994868Compositions useful as inhibitors of ERK
This invention provides a method of treating a disease state in mammals that is alleviated by treatment with a protein kinase inhibitor, especially an ERK inhibitor, which method comprises administering a compound having the pharmacophoric features Grp 1, Grp 2 and ...
02/07/2006
6949655Acyclic piperidine derivatives
A compound having the formula (I): wherein: each R1, R2, R3 and R4 are independently selected from (C1-C10)-straight ...
09/27/2005
6949580Pyrazole compositions useful as inhibitors of ERK
Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating dis...
09/27/2005
6949544Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
The present invention provide a compound of formula I or II: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, R3, and R4 are as described in the specifica...
09/27/2005
6930116Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts ...
08/16/2005
6909000Bridged bicyclic serine protease inhibitors
The present invention relates to peptidomimetic compounds which 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 a...
06/21/2005
6884804Inhibitors of Src and other protein kinases
The present invention provides compounds of formula I: wherein A is N or CR, and G, R1, R2 and R3 are as described in the specification. These compounds are inhibitors of protein kinase...
04/26/2005
6846928Compositions 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 said compounds and methods of using the compositions in the treatment of various disease, conditions, ...
01/25/2005
6824769Optimal compositions and methods thereof for treating HCV infections
The present invention relates to optimal compositions useful in treating HCV infections in humans. These compositions comprise alpha-interferon or a derivative thereof and an IMPDH inhibitor, wherein the IMPDH inhibitor is present in an amount such that a ratio of C...
11/30/2004
6800619Caspase inhibitors and uses thereof
Described herein are compounds that are useful as caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrog...
10/05/2004
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