Patents by Inventor Julian M. C. Golec
Julian M. C. Golec has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 7790713Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.Type: GrantFiled: January 18, 2007Date of Patent: September 7, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Publication number: 20100222367Abstract: 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 inventions.Type: ApplicationFiled: May 5, 2010Publication date: September 2, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Julian M.C. Golec
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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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Publication number: 20100215772Abstract: 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.Type: ApplicationFiled: October 30, 2009Publication date: August 26, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Julian M.C. Golec, Daniel David Robinson, John Studley
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Patent number: 7737151Abstract: The present invention relates to compounds useful as inhibitors of protein kinases of the following formula: or a pharmaceutically acceptable salt thereof. 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 inventions.Type: GrantFiled: August 17, 2006Date of Patent: June 15, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian M. C. Golec
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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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Publication number: 20090131456Abstract: 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: ApplicationFiled: January 26, 2009Publication date: May 21, 2009Inventors: Julian M.C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
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Patent number: 7517987Abstract: 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: June 10, 2002Date of Patent: April 14, 2009Assignee: Vertex Pharmaceutical IncorporatedInventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
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Publication number: 20080199454Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.Type: ApplicationFiled: December 21, 2007Publication date: August 21, 2008Inventors: Michael Mortimore, Julian M.C. Golec
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Patent number: 7410956Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.Type: GrantFiled: February 11, 2003Date of Patent: August 12, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian M. C. Golec
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Patent number: 7288624Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: June 21, 2001Date of Patent: October 30, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W Bemis, Julian M C. Golec, David J Lauffer, Michael D Mullican, Mark A Murcko, David J Livingston
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Patent number: 7205327Abstract: This invention provides caspase inhibitors having the formula: wherein R1 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R2 and R3 are each independently selected from hydrogen or an optionally substituted C1–C6 aliphatic group; and R4 and R5 are each independently selected from hydrogen, an optionally substituted C1–C6 aliphatic group, or R4 and R5 taken together with the ring to which they are attached form an optionally substituted bicyclic ring. The caspase inhibitors are useful for treating a number of diseases such as cancer, acute inflammatory and autoimmune disorders, ischemic diseases and certain neurodegenerative disorders.Type: GrantFiled: November 19, 2001Date of Patent: April 17, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Kay, Julian M. C. Golec
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Patent number: 7179826Abstract: 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.Type: GrantFiled: March 14, 2003Date of Patent: February 20, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Patent number: 7115739Abstract: 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 nitrogen; 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 independently selected from —R1; 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 Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: October 3, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian M. C. Golec, Pan Li, Jean-Damien Charier
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Patent number: 7098330Abstract: 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; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–8 membered carbocyclo ring; and R2 and R2? 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: September 14, 2001Date of Patent: August 29, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian M. C. Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert J. Davies
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Patent number: 7091343Abstract: 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.Type: GrantFiled: March 14, 2003Date of Patent: August 15, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Patent number: 7074782Abstract: 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 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 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: August 21, 2003Date of Patent: July 11, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M. C. Golec
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Patent number: 7053057Abstract: This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2, R, or —CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3 is hydrogen, an optionally substituted C1-6 alkyl, F2, CN, aryl or R3 is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0–2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.Type: GrantFiled: May 23, 2001Date of Patent: May 30, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, David Bebbington, Guy Brenchley, Ronald Knegtel, Michael Mortimore
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Patent number: 7041687Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2, and V3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT, PKA, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.Type: GrantFiled: January 23, 2003Date of Patent: May 9, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Guy Brenchley, Julian M. C. Golec, Ronald Knegtel, Michael Mortimore, Sanjay Patel, Alistair Rutherford
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Patent number: 6974809Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), interferon-?-(“IFN-?”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis- and interferon-?-mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: April 25, 2003Date of Patent: December 13, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, David J. Lauffer, David J. Livingston, Michael D. Mullican, Mark A. Murcko, Philip L. Nyce, Andrea L. C. Robidoux, Marion W. Wannamaker