Patents Represented by Attorney, Agent or Law Firm David A. Muthard
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Patent number: 8222269Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives of formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: July 6, 2007Date of Patent: July 17, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Matthew H. Katcher, Alan B. Northrup
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Patent number: 8207186Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 22, 2006Date of Patent: June 26, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: James P. Jewell, Jason D. Katz
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Patent number: 8101603Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: July 9, 2007Date of Patent: January 24, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Matthew H. Katcher, Alan B. Northrup
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Patent number: 7893081Abstract: This invention relates to salt forms of the compound N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N?-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide, an inhibitor of tyrosine kinases, in particular the receptor tyrosine kinase MET, that are useful in the treatment of cellular proliferative diseases, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. In particular, the invention relates to the sodium salt of N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N?-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide.Type: GrantFiled: December 17, 2008Date of Patent: February 22, 2011Assignee: Merck & Co., Inc.Inventors: Paolo Avalle, Jennifer R. Foley, Peter Mullens, Yaling Wang, Peter Yehl
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Patent number: 7790739Abstract: The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: October 18, 2006Date of Patent: September 7, 2010Assignee: Merck & Co., Inc. and Merck Sharp & Dohme Corp.Inventors: Jongwon Lim, Ana Esther Gabarda Ortega
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Patent number: 7737184Abstract: This invention relates to hydroxamic acid derivatives having a urea linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.Type: GrantFiled: July 8, 2005Date of Patent: June 15, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Sandro Belvedere, Christopher Laurence Hamblett, Thomas A. Miller, David J. Witter, Jiaming Yan
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Patent number: 7709475Abstract: The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: May 19, 2005Date of Patent: May 4, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Jun Shibata, Tadashi Shimamura, Hideki Kurihara, Takashi Mita, Nobuhiko Kawanishi, Takashi Hashihayata, Mikako Kawamura, Takeshi Sagara, Sachie Arai, Hiroshi Hirai
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Patent number: 7592392Abstract: The present invention relates to a novel process for the preparation of solid-supported scavenging reagents and solid-supported functional polymers. The invention further relates to novel solid-supported functional polymers and to their use in organic synthesis and combinatorial chemistry.Type: GrantFiled: March 31, 2004Date of Patent: September 22, 2009Assignee: Merck & Co. Inc.Inventors: Craig W. Lindsley, David D. Wisnoski
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Patent number: 7550478Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 22, 2006Date of Patent: June 23, 2009Assignee: Merck & Co. Inc.Inventors: Christopher J. Dinsmore, Ana Esther Gabarda Ortega, David J. Guerin, James P. Jewell, Jason D. Katz, Jongwon Lim, Michelle R. Machacek, Ryan D. Otte, Jonathan R. Young
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Patent number: 7262169Abstract: The present invention is directed to the improved synthesis of compounds of formula (I) an intermediate compound which is useful in the synthesis of the anticancer agents known as PSA conjugates.Type: GrantFiled: October 18, 2000Date of Patent: August 28, 2007Assignees: Merck & Co., Inc., Merck Sharp & Dohme LimitedInventors: Michael Stewart Ashwood, Brian Christopher Bishop, Ian Frank Cottrell, Khateeta Moneek Emerson, David Hands, Guo Jie Ho, Joseph Edward Lynch, Yao Jun Shi, Robert Darrin Wilson
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Patent number: 7192949Abstract: The present invention relates to cycloalkylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: April 24, 2006Date of Patent: March 20, 2007Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, Robert M. Garbaccio
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Patent number: 7060705Abstract: The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: November 1, 2002Date of Patent: June 13, 2006Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, William F. Hoffman
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Patent number: 6979676Abstract: The present invention is directed to a pharmaceutical composition comprising a compound of Formula I dissolved in propylene glycol and water. The present invention also relates to a pharmaceutical composition containing a compound of Formula I dissolved in propylene glycol and a buffer that has a pH between about 3 and about 5.Type: GrantFiled: September 26, 2002Date of Patent: December 27, 2005Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Yuichi Sato, David T. Breslin, Shyam B. Karki
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Patent number: 6875767Abstract: The present invention relates to compounds having the formula I: which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions. The compounds of the present invention are useful in treating angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: June 19, 2002Date of Patent: April 5, 2005Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, George D. Hartman
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Patent number: 6872724Abstract: The present invention relates to active polymorphs of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, retinal ischemia, macular edema, inflammatory diseases, and the like in mammals.Type: GrantFiled: June 26, 2003Date of Patent: March 29, 2005Assignee: Merck & Co., Inc.Inventors: Matthew M. Zhao, Mark T. Bilodeau
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Patent number: 6610722Abstract: The present invention is directed to peptidomimetic macrocyclic compounds that inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: April 6, 2001Date of Patent: August 26, 2003Assignee: Merck & Co., Inc.Inventors: Craig A. Stump, Theresa M. Williams
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Patent number: 6552166Abstract: The present invention is directed to the improved synthesis of compounds of formula I: which may be useful in the treatment of prostate cancer. Such compounds are synthesized in the presence of a carboxyl activating agent, an additive and a base for the preparation of a PSA conjugate which comprises an anthracycline antibiotic and an oligopeptide.Type: GrantFiled: October 18, 2000Date of Patent: April 22, 2003Assignee: Merck & Co., Inc.Inventors: Joseph E. Lynch, Michael A. Robbins, Yao-Jun Shi, David R. Lieberman
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Patent number: 6500841Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.Type: GrantFiled: September 12, 1996Date of Patent: December 31, 2002Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel L. Graham
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Patent number: 6413964Abstract: The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1 is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: January 9, 2001Date of Patent: July 2, 2002Inventors: S. Jane deSolms, Suzanne C. MacTough, Anthony W. Shaw
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Patent number: 6410534Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: June 29, 1999Date of Patent: June 25, 2002Assignee: Merck & Co., Inc.Inventors: Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams