Patents Represented by Attorney, Agent or Law Firm Karoline K.M. Shair
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Patent number: 6693108Abstract: 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 below. These compounds are inhibitors of protein kinase, particularly 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 comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: February 12, 2002Date of Patent: February 17, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Guy Bemis, Anne-Laure Grillot, Mark Ledeboer, Francesco G. Salituro, Edmund Harrington, Huai Gao, Christopher Baker, Jingrong Cao, Michael Hale
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Patent number: 6656939Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 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; 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: December 20, 2001Date of Patent: December 2, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier
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Patent number: 6613776Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided 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; and R1, R2, R2′, R3, and T 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: September 2, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, David Bebbington, Hayley Binch, Julian Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
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Patent number: 6448443Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.Type: GrantFiled: July 25, 1998Date of Patent: September 10, 2002Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Matthew D. Shair, Derek S. Tan, Michael A. Foley, Brent R. Stockwell
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Patent number: 6420384Abstract: Compounds and methods of treating or preventing bone disorders including osteoporosis, rheumatoid arthritis, and metastatic bone disease are provided. The inventive compounds comprise a bone targeting moiety and a payload. The payload portion of these inventive compounds inhibit the proton pump of osteoclasts, thereby, reducing bone resorption.Type: GrantFiled: December 18, 2000Date of Patent: July 16, 2002Assignee: Ariad Pharmaceuticals, Inc.Inventors: Manfred Weigele, David C. Dalgarno, John Iuliucci, Terence P. Keenan, Tomi K. Sawyer
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Patent number: 6369234Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.Type: GrantFiled: October 11, 2000Date of Patent: April 9, 2002Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dang Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
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Patent number: 6355639Abstract: The present invention provides a method for treating a subject in need of immunosuppression, comprising administering to the subject an effective amount of a compound having structure (I) wherein R1, R6 and R7 are independently hydrogen, OH, NH2, SH, halogen, C1-C9 linear or branched chain alkyl, alkylmercapto, alkylamino, etc.; wherein R0 and R2 are independently hydrogen, OH, C1-C9 linear or branched chain alkyl, —CR3R3—CH(O)CH2, —CR3R3—CH═CHR4, etc.; wherein R3 and R4 are independently hydrogen halogen C1-C9 linear or branched chain alkyl, etc.; wherein R5 is hydrogen, C1-C9 linear or branched chain alkyl, phenyl, alkylphenyl, dialkylphenyl, alkylmercapto, etc.; and wherein R8 is hydrogen, C1-C9 linear or branched chain acyl, benzoyl, alkylbenzoyl, etc. Also provided are methods of treating autoimmune disease and preventing organ graft rejection using N-acetylardeemin and related compounds.Type: GrantFiled: February 16, 2000Date of Patent: March 12, 2002Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Ting-Chao Chou, Joseph R. Bertino, Samuel J. Danishefsky, Barry D. Kahan
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Patent number: 6316630Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.Type: GrantFiled: June 6, 2000Date of Patent: November 13, 2001Assignee: Sloan Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
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Patent number: 6300355Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.Type: GrantFiled: September 13, 2000Date of Patent: October 9, 2001Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dang Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
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Patent number: 6284781Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.Type: GrantFiled: October 18, 2000Date of Patent: September 4, 2001Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dand Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
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Patent number: 6254890Abstract: The present invention provides biodegradable polymer nanospheres capable of transporting and releasing therapeutic agents, specifically nucleic acids. In preferred embodiments, a sub-150 nm nanosphere is formed containing nucleic acids. Thereafter, the agent is released from the nanosphere. In one embodiment a biodegradable polymer nanosphere surface has attached to it a targeting moiety. In another embodiment, the biodegradable polymer nanosphere surface has attached to it a masking moiety. In yet another embodiment both targeting and masking moieties are attached to the nanosphere surface.Type: GrantFiled: December 10, 1998Date of Patent: July 3, 2001Assignee: Massachusetts Institute of TechnologyInventors: Sachiko Hirosue, Bernhard G. Mueller, Robert S. Langer, Richard C. Mulligan
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Patent number: 6242469Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.Type: GrantFiled: December 3, 1997Date of Patent: June 5, 2001Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dang Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
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Patent number: 6238668Abstract: The present invention provides processes for the preparation of the KH-1 and N3 antigens, as well as related analgoues thereof, which are useful as anticancer therapeutics. The present invention also provides various intermediates useful in the preparation of KH-1 and N3 and analogues thereof. Additionally, the invention provides various compositions comprising any of the analogues of KH-1 and N3 available through the methods of the invention and pharmaceutical carriers useful in the treatment of subjects suffering from various forms of epithelial cancer.Type: GrantFiled: January 13, 1998Date of Patent: May 29, 2001Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Prashant P. Deshpande, In Jong Kim, Philip Livingston, Hyun Jin Kim, Ragupathi Govindaswami, Tae Kyo Park