Patents Represented by Attorney Jennifer G. Che
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Patent number: 8329662Abstract: 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 colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.Type: GrantFiled: August 16, 2011Date of Patent: December 11, 2012Assignee: Vertexd Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Robert J. Davies
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Patent number: 8288537Abstract: 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 R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: GrantFiled: December 1, 2011Date of Patent: October 16, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Marie Binch
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Patent number: 8168798Abstract: 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 the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.Type: GrantFiled: December 17, 2010Date of Patent: May 1, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Steven Durrant, Jean-Damien Charrier, John Studley
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Patent number: 8093392Abstract: 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 R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: GrantFiled: February 8, 2011Date of Patent: January 10, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Marie Binch
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Patent number: 8071618Abstract: The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 is: C1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF3, CI, F, OMe, OEt, OCF3, CN, or NMe2; C1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with —O— or —NR5—; R2 is C1-6 straight chained or branched alkyl; Art Unit 1625 R3 is hydrogen, halo, OCF3, CN, or CF3; R4 is hydrogen, halo, OCF3, CN, or CF3; and each R5 is independently H, C1-6 straight chained or branched alkyl, aryl, —O—C1-6 straight chained or branched alkyl, or —O-aryl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated disease, particularly in the central nervous system.Type: GrantFiled: September 18, 2009Date of Patent: December 6, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean Damien Charrier, Michael Mortimore, John Studley
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Patent number: 8022041Abstract: 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 colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.Type: GrantFiled: July 1, 2008Date of Patent: September 20, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Robert J. Davies
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Patent number: 7968716Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: GrantFiled: September 16, 2010Date of Patent: June 28, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 7879891Abstract: 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 the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.Type: GrantFiled: July 20, 2006Date of Patent: February 1, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Steven Durrant, Jean-Damien Charrier, John Studley
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Patent number: 7875712Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; ?between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: September 23, 2008Date of Patent: January 25, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Patent number: 7872129Abstract: The present invention provides a compound of formula I: 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 compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: December 18, 2008Date of Patent: January 18, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Cornelia J. Forster, Larry C. Park, Marion W. Wannamaker, Yung-Mae M. Yao
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Patent number: 7855214Abstract: The present invention relates to compounds useful as inhibitors of Tec family protein kinases. These compounds have the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, G, Cy1, and X are as defined herein. 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.Type: GrantFiled: January 26, 2005Date of Patent: December 21, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Sanjay Patel, David Kay, Ronald Knegtel, Oliver Philps
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Patent number: 7842712Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.Type: GrantFiled: August 20, 2007Date of Patent: November 30, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, David J. Lauffer, Huan Qiu Li, Ronald Charles Tomlinson, Pan Li
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Patent number: 7829561Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: GrantFiled: July 1, 2008Date of Patent: November 9, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 7786130Abstract: 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.Type: GrantFiled: August 28, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Guy Brenchley, Ronald Knegtel, Michael Mortimore
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Patent number: 7786120Abstract: 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.Type: GrantFiled: August 25, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Julian M. C. Golec, Michael Mortimore
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Patent number: 7691885Abstract: 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.Type: GrantFiled: August 29, 2006Date of Patent: April 6, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant
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Patent number: 7691853Abstract: This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2?, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: March 6, 2006Date of Patent: April 6, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian M. C. Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert J. Davies, Pan Li, Marion W. Wannamaker, Cornelia J. Forster, Albert C. Pierce
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Patent number: 7652153Abstract: The present invention provides a compound of formula I: wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula I, and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.Type: GrantFiled: February 28, 2005Date of Patent: January 26, 2010Inventors: Jean Damien Charrier, Steven Durrant, Michael Mortimore, Michael O'Donnell, Alistair Rutherford, Sharn Ramaya, John Studley, Martin Trudeau, Adam Looker
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Patent number: 7652135Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein A, B, Q, R1, and R2 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT or PDK1 kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds, and methods of utilizing those compositions in the treatment of various disorders.Type: GrantFiled: September 23, 2004Date of Patent: January 26, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Simon Everitt, Francesca Mazzei, Daniel Robinson
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Patent number: 7612091Abstract: The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 is: C1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF3, Cl, F, OMe, OEt, OCF3, CN, or NMe2; C1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with —O— or —NR5—; R2 is C1-6 straight chained or branched alkyl; R3 is hydrogen, halo, OCF3, CN, or CF3; R4 is hydrogen, halo, OCF3, CN, or CF3; and each R5 is independently H, C1-6 straight chained or branched alkyl, aryl, —O—C1-6 straight chained or branched alkyl, or —O-aryl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated disease, particularly in the central nervous system.Type: GrantFiled: December 22, 2003Date of Patent: November 3, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Michael Mortimore, John R. Studley