Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 546/120)
-
Patent number: 7265128Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: January 13, 2004Date of Patent: September 4, 2007Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Charles G. Caldwell, Robert J. Mathvink, Hyun O. Ok, Leah Bitalac Reigle, Ann E. Weber
-
Patent number: 7166596Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: GrantFiled: September 2, 2003Date of Patent: January 23, 2007Assignee: Bristol-Myers Squibb Co.Inventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
-
Patent number: 7148235Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.Type: GrantFiled: June 22, 2005Date of Patent: December 12, 2006Assignee: WyethInventors: Aranapakam Mudumbai Venkatesan, Jamie M. Davis, Yansong Gu
-
Patent number: 7135469Abstract: The present application describes linear chain substituted monocyclic and bicyclic compounds and derivatives thereof of Formula I: P4-P-M-M4I or pharmaceutically acceptable salt forms thereof, P-M are rings substituted by a linear group. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: March 16, 2004Date of Patent: November 14, 2006Assignee: Bristol Myers Squibb, Co.Inventor: Donald J. Pinto
-
Patent number: 7122557Abstract: The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula I: P4-P-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a ring, P is an optional ring, and P4 and M4 are as defined below. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: March 16, 2004Date of Patent: October 17, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. Pinto, Jennifer X. Qiao, Timur Gungor, Patrick Y. S. Lam, Yun-Long Li
-
Patent number: 7115627Abstract: The present application describes glycinamidic compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: November 25, 2002Date of Patent: October 3, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. P. Pinto, Wei Han, Zilun Hu, Jennifer Qiao
-
Patent number: 7074928Abstract: Provided are new crystalline Forms III, IV, V and VI of clopidogrel hydrogensulfate and the amorphous form of clopidogrel hydrogensulfate, as well as their pharmaceutical compositions, and method of treatments with such compositions. Also provided are novel processes for preparation of clopidogrel hydrogensulfate Form I, Form II, Form III, Form IV, Form V, Form VI and amorphous form.Type: GrantFiled: January 8, 2003Date of Patent: July 11, 2006Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Revital Lifshitz-Liron, Eti Kovalevski-Ishai, Shlomit Wizel, Sharon Avhar-Maydan, Rami Lidor-Hadas
-
Patent number: 7041675Abstract: The invention relates to compounds of the formula I and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors.Type: GrantFiled: January 25, 2001Date of Patent: May 9, 2006Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Reinhold Mueller, Sabine Schult
-
Patent number: 6992086Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: November 17, 2003Date of Patent: January 31, 2006Assignee: Telik, Inc.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
-
Patent number: 6989391Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: May 20, 2004Date of Patent: January 24, 2006Assignee: Bristol-Myers-Squibb Pharma CompanyInventors: Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L. Koch
-
Patent number: 6977262Abstract: The present invention provides dihydropyrazolopyridine compounds represented by the formula (I): wherein each symbol is as defined in the specification, optically active forms thereof, and pharmaceutically acceptable salts thereof and hydrates thereof. The compounds of the present invention show a selective and strong inhibitory activity on glycogen synthase kinase-3 beta (GSK-3?), and are useful as medicaments for prevention and/or treatment of diabetes, diabetic complications and neurodegenerative diseases or as immunopotentiators.Type: GrantFiled: August 1, 2003Date of Patent: December 20, 2005Assignee: Mitsubishi Pharma CorporationInventors: Toshiyuki Kohara, Kenji Fukunaga, Masatake Fujimura, Tokushi Hanano, Hirotaka Okabe
-
Patent number: 6967208Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: September 17, 2002Date of Patent: November 22, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L. Koch
-
Patent number: 6962926Abstract: Compounds of formula A and formula B: and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The compounds are antagonists of MCP-1 function, and are useful in the prevention and treatment of chronic or acute inflammatory or autoimmune diseases, such as multiple sclerosis, and in the prevention and treatment of allergic hypersensitivity disorders.Type: GrantFiled: August 8, 2003Date of Patent: November 8, 2005Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Wenli Ma, Yukiharu Matsumoto, Kunihisa Baba, Hideaki Inagaki, Katsumasa Tanaka, Yoshiro Ishiwata, Shoji Yokochi, Masayuki Okamoto, Takashi Nakamura, Atsushi Miyachi, Mitsuaki Takeuchi, Kouji Matsushima
-
Patent number: 6946473Abstract: Compounds of the formula which are useful in disease conditions mediated by TNF-?, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: March 17, 2003Date of Patent: September 20, 2005Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, James M. Chen, Xue-Mei Du, Jay D. Albright, Arie Zask
-
Patent number: 6939870Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.Type: GrantFiled: August 29, 2003Date of Patent: September 6, 2005Assignee: WyethInventors: Aranapakam M. Venkatesan, Jamie M. Davis, Yansong Gu
-
Patent number: 6919451Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.Type: GrantFiled: December 3, 2002Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Jiacheng Zhou, Lynette M. Oh, Philip Ma, Hui-Yin Li, Pasquale Confalone
-
Patent number: 6867208Abstract: The present invention relates to compounds of the formula I A—B—D—E—F—G??(I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: May 13, 2002Date of Patent: March 15, 2005Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
-
Patent number: 6867202Abstract: This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.Type: GrantFiled: July 22, 2003Date of Patent: March 15, 2005Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, Charles Kwok-Fung Chiu, Lydia Codetta Pan, Bruce Allen Lefker, Judith Lee Treadway, Michael Paul Zawistoski
-
Patent number: 6855708Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: March 13, 2002Date of Patent: February 15, 2005Assignee: Merck & Co., Inc.Inventors: Linus S. Lin, George Doherty, Shrenik K. Shah, Linda L. Chang, William K. Hagmann, Richard A. Mumford
-
Patent number: 6852734Abstract: According to this invention, there is provided an indole derivative having the general formula (I) wherein A is an oxygen atom or a nitrogen atom which nitrogen atom is optionally substituted with an alkyl group, and (i) R1 and R2 each stand for a hydrogen atom or an alkyl group, independently, or (ii) R1 and R2 as taken together form a cycloalkyl group or an aromatic ring, or (iii) R1 and R2 as taken together form a heterocyclic ring, and R3 is a hydrogen atom, a (C1-C10)alkyl group or others, R4 is a substituted alkyl group and R5 is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group and so on, as novel compounds by a novel chemical synthetic process. The indole derivative of formula (I) exhibits a useful chymase inhibitory activity.Type: GrantFiled: May 1, 2001Date of Patent: February 8, 2005Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yasuo Yamamoto, Kenzo Hariyama, Yumiko Yanagisawa, Sojiro Shiokawa, Takumi Takeyasu, Osami Takenouchi, Hidenori Kasai
-
Patent number: 6849620Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 17, 2002Date of Patent: February 1, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, Eric Jon Jacobsen, David W. Piotrowski, Brad A. Acker, Donn G. Wishka, Jeffrey W. Corbett, Mark R. Rauckhorst, Vincent E. Groppi, Jr.
-
Patent number: 6706730Abstract: The present application describes 1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-ones of Formula I or pharmaceutically acceptable salt forms thereof: wherein ring R is 3-amido or 4-methoxy, R1 is trifluoromethyl or amido, and R2 is aminomethyl, N-methylaminomethyl, and N,N-dimethylaminomethyl. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: April 17, 2002Date of Patent: March 16, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Donald Joseph Philip Pinto
-
Patent number: 6693116Abstract: The present application relates to compounds of the formula wherein R1 is hydrogen, halogen or lower alkoxy; R2 is hydrogen or is —C(O)-lower alkyl or —C(O)-phenyl, wherein the phenyl ring is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy and trifluoromethyl, or is —C(O)-furanyl or —C(O)-thiophenyl, wherein the rings are unsubstituted or substituted by halogen; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases associated with the adenosine A2 receptor.Type: GrantFiled: September 18, 2002Date of Patent: February 17, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Sebastien Schmitt
-
Patent number: 6689790Abstract: A compound of formula wherein R1 is —NR′R″, wherein R′ and R″ are independently selected from the group consisting of lower alkyl, —(CH2)n—C(O)NRaRb, —(CH2)n,-heteroaryl, —(CH2)n-aryl, —(CH2)n—CN, —(CH2)n—O-lower alkyl or —(CH2)n-cycloalkyl, or R′ and R″ form together with the N-atom a five or six-membered non-aromatic ring, containing no or one additional heteroatom selected from the group consiting of O and S, and said ring being unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, —C(O)NRaRb and —(CH2)n—O-lower alkyl, and RaRb are independently from each other hydrogen or lower alkyl; R2 is aryl or heteroaryl, unsubstituted or substituted by lower alkyl or halogen; and n is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 7, 2002Date of Patent: February 10, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Sebastien Schmitt
-
Patent number: 6686359Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintanence of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: December 6, 2002Date of Patent: February 3, 2004Assignee: Pfizer Inc.Inventor: Philip A. Carpino
-
Patent number: 6677365Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.Type: GrantFiled: March 25, 2002Date of Patent: January 13, 2004Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
-
Patent number: 6673929Abstract: This invention relates to improved processes for preparing compounds of Formula II, and compounds of Formula III, wherein R1, R2, R3 and Prt are defined as set forth in the specification.Type: GrantFiled: October 30, 2002Date of Patent: January 6, 2004Assignee: Pfizer Inc.Inventors: Frank R. Busch, Charles K. Chiu, Clifford N. Meltz, Ronald J. Post, Peter R. Rose
-
Patent number: 6673810Abstract: The present application describes imidazo-heterobicycles of formulas I and III: or pharmaceutically acceptable salt or prodrug forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: July 3, 2001Date of Patent: January 6, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Qi Han, Thomas E. Richardson
-
Patent number: 6670364Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: January 29, 2002Date of Patent: December 30, 2003Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
-
Patent number: 6653320Abstract: The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.Type: GrantFiled: March 1, 2002Date of Patent: November 25, 2003Assignees: Yamanouchi Pharmaceutical Co. Ltd., Ludwig Institute for Cancer Research, Imperial Cancer Research Technology Ltd.Inventors: Masahiko Hayakawa, Hiroyuki Kaizawa, Ken-Ichi Kawaguchi, Koyo Matsuda, Noriko Ishikawa, Tomonobu Koizumi, Mayumi Yamano, Minoru Okada, Mitsuaki Ohta
-
Patent number: 6630487Abstract: This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and the compounds of formula I.Type: GrantFiled: May 29, 2002Date of Patent: October 7, 2003Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, Charles Kwok-Fung Chiu, Lydia Codetta Pan, Bruce Allen Lefker, Judith Lee Treadway, Michael Paul Zawistoski
-
Patent number: 6559174Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: March 13, 2002Date of Patent: May 6, 2003Assignee: Merck & Co., Inc.Inventors: Linus S. Lin, Shrenik K. Shah, Linda L. Chang, William K. Hagmann, Richard A. Mumford
-
6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
Patent number: 6559152Abstract: The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: February 27, 2001Date of Patent: May 6, 2003Assignee: DuPont Pharmaceuticals CompanyInventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk -
Patent number: 6541484Abstract: A class of substituted and/or ring-fused pyrazolo[3,4-b]pyridine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent on the pyrazole nitrogen atom adjacent the pyridine nucleus, and an optionally substituted cycloalkyl-alkoxy, aryl-alkoxy or heteroaryl-alkoxy substituent on the carbon atom adjacent the pyridine ring nitrogen atom, are selective ligands for GABAA receptors, in particular having high affinity for the &bgr;2 and/or &bgr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse neurological disorders, including anxiety and convulsions.Type: GrantFiled: June 14, 2002Date of Patent: April 1, 2003Assignee: Merck Sharp & Dohme LimitedInventors: Ian James Collins, Linda Elizabeth Keown, Leslie Joseph Street
-
Patent number: 6531449Abstract: The invention provides metabolites of the compound 2-amino-N-[2-(3a(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo-[4,3-c]pyridin-5-yl)-1-(R)-benzyl-oxymethyl-2-oxo-ethyl]-isobutyramide, the racemic-diastereomeric mixtures and optical isomers thereof, the prodrugs thereof, and the pharmaceutically acceptable salts of the metabolites, racemic-diastereomeric mixtures, optical isomers, and prodrugs; to pharmaceutical compositions thereof; and to methods of using the metabolites and the compositions in the treatment of diseases associated with reduced levels of growth hormone.Type: GrantFiled: March 8, 2001Date of Patent: March 11, 2003Assignee: Pfizer Inc.Inventors: S. Cyrus Khojasteh, John P. O'Donnell
-
Patent number: 6531477Abstract: The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: October 12, 1999Date of Patent: March 11, 2003Assignee: DuPont Pharmaceuticals CompanyInventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk
-
Patent number: 6531474Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.Type: GrantFiled: September 19, 2000Date of Patent: March 11, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
-
Patent number: 6525197Abstract: The present invention relates to methods for preparing macrocyclic products having 9 or more ring atoms by ring-closing diyne metathesis of suitable diyne substrates. The diyne substrates can be converted into cycloalkynes or into cycloalkadiynes by cyclodimerization, depending on the particular reaction conditions. Any alkyne metathesis catalyst can be used as the catalyst, regardless of whether said catalysts are heterogeneously or homogeneously present in the reaction medium. The preferred catalysts or pre-catalysts are transition metal alkylidyne complexes, transition metal compounds which form alkylidyne complexes under the reaction conditions, and transition metal compounds with metal-metal triple bonds. The method can be carried out with numerous functional groups, solvents, and additives.Type: GrantFiled: August 4, 2000Date of Patent: February 25, 2003Assignee: Studiengesellschaft Kohle mbHInventors: Alois Fürstner, Günter Seidel, Antonio Rumbo, Christian Mathes
-
Patent number: 6506771Abstract: The present application describes heteroaryl-phenyl heterobicycles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: June 22, 2001Date of Patent: January 14, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Donald J. P. Pinto, Mimi L. Quan, Francis J. Woerner, Renhua Li
-
Patent number: 6506772Abstract: Substituted [1,2,4]triazolo[1,5a]pyridine derivatives and pharmaceutically active salts thereof with activity as adenosine receptor ligands are disclosed. These compounds are useful for treatment of diseases responsive to modulation of the adenosine receptor.Type: GrantFiled: November 30, 2001Date of Patent: January 14, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Brodbeck, Matthias Heinrich Nettekoven
-
Patent number: 6444617Abstract: A fused heterocyclic dicarboxylic acid diamide derivative represented by formula (I): wherein R1 is H, (C1-C6) alkyl; R2 and R3 are H, (halo) (C1-C6) alkyl, (C3-C8) cycloalkyl, substituted amino (C1-C6) alkyl, (substituted) phenyl (C1-C6) alkyl, (substituted) phenyl (C1-C6) alkoxy or the like or R2 and R3, taken conjointly, represent a (substituted) 5- or 6-membered heterocycle having at least one of O, S and N; X is H, halogen, NO2, CN, (C1-C6) alkyl, (substituted) phenyl, (substituted) phenoxy or the like; is or the like wherein Y, R4 and R9 are H, halogen, NO2, CN, (C1-C6) alkyl or the like, and A, B, D, E, F, G, J and K are O, S, N, sulfinyl or the like; and a herbicide containing said derivative as active ingredient.Type: GrantFiled: January 26, 2001Date of Patent: September 3, 2002Assignee: Nihon Nohyaku Co., Ltd.Inventors: Hideo Takaishi, Takeshi Katsuhira, Hiroshi Yamaguchi, Youichi Kawabata, Hiroto Harayama, Yoshiki Oda, Masahiko Murai
-
Patent number: 6413980Abstract: The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: December 22, 1999Date of Patent: July 2, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John M. Fevig, Joseph Cacciola, Charles G. Clark, Qi Han, Patrick Yuk Sun Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan, Karen A. Rossi
-
Patent number: 6403588Abstract: The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.Type: GrantFiled: April 26, 2001Date of Patent: June 11, 2002Assignees: Yamanouchi Pharmaceutical Co., Ltd., Ludwig Institute for Cancer Research, Imperial Cancer Research Technology, Ltd.Inventors: Masahiko Hayakawa, Hiroyuki Kaizawa, Ken-Ichi Kawaguchi, Koyo Matsuda, Noriko Ishikawa, Tomonobu Koizumi, Mayumi Yamano, Minoru Okada, Mitsuaki Ohta
-
Publication number: 20020049196Abstract: This invention is directed to compounds of the formula 1Type: ApplicationFiled: December 11, 2000Publication date: April 25, 2002Inventors: Philip A. Carpino, Paul A. DaSilva-Jardine, Bruce A. Lefker, John A. Ragan
-
Patent number: 6376509Abstract: Certain novel compounds and derivatives thereof are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: May 29, 2001Date of Patent: April 23, 2002Assignee: Merck & Co., Inc.Inventors: Raman Kumar Bakshi, Ravi P. Nargund, Zhixiong Ye
-
Patent number: 6358951Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery, improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: August 18, 1999Date of Patent: March 19, 2002Assignee: Pfizer Inc.Inventor: Philip A. Carpino
-
Patent number: 6340772Abstract: Three processes are described for preparing (hetero)aromatic substituted benzene derivatives which comprise aromatization of cyclohexenone derivatives via (chloro)cyclohexadiene derivatives.Type: GrantFiled: April 24, 2001Date of Patent: January 22, 2002Assignee: Nippon Kayaku Co., Ltd.Inventors: Tetsuya Toya, Hidetoshi Shirakura, Junichi Kon
-
Patent number: 6333336Abstract: Pyrazolo[4,3-c]pyridin-3-one derivatives substituted at the 2-position by an optionally substituted aryl or heteroaryl moiety, and having pendant substituents at the 7-position and optionally also at the 6-position, are selective ligands for GABAA receptors, particularly having high affinity for the &agr;2 and/or &agr;3 subunit, and are useful in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.Type: GrantFiled: August 23, 2000Date of Patent: December 25, 2001Assignee: Merck Sharp & Dohme Ltd.Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Michael Geoffrey Neil Russell, Leslie Joseph Street
-
Patent number: 6326379Abstract: Compounds of the formulas are useful as inhibitors of cGMP PDE, especially type V.Type: GrantFiled: September 10, 1999Date of Patent: December 4, 2001Assignee: Bristol-Myers Squibb Co.Inventors: John E. Macor, Guixue Yu
-
Patent number: 6303625Abstract: The invention is directed to novel triazolopyridine derivatives which are useful as antagonists of GPIIb/IIIa. Pharmaceutical compositions comprising the triazolopyridine derivatives of the present invention, methods of treating conditions mediated by GPIIb/IIIa (e.g., methods for treating platelet-mediated thrombotic disorders) along with processes for making the compounds and novel intermediates are also disclosed.Type: GrantFiled: July 15, 1999Date of Patent: October 16, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: William J. Hoekstra, Edward C. Lawson, Bruce E. Maryanoff