Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 546/120)
  • Patent number: 7265128
    Abstract: 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: Grant
    Filed: January 13, 2004
    Date of Patent: September 4, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Robert J. Mathvink, Hyun O. Ok, Leah Bitalac Reigle, Ann E. Weber
  • Patent number: 7166596
    Abstract: 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: Grant
    Filed: September 2, 2003
    Date of Patent: January 23, 2007
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
  • Patent number: 7148235
    Abstract: 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: Grant
    Filed: June 22, 2005
    Date of Patent: December 12, 2006
    Assignee: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Jamie M. Davis, Yansong Gu
  • Patent number: 7135469
    Abstract: 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: Grant
    Filed: March 16, 2004
    Date of Patent: November 14, 2006
    Assignee: Bristol Myers Squibb, Co.
    Inventor: Donald J. Pinto
  • Patent number: 7122557
    Abstract: 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: Grant
    Filed: March 16, 2004
    Date of Patent: October 17, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Donald J. Pinto, Jennifer X. Qiao, Timur Gungor, Patrick Y. S. Lam, Yun-Long Li
  • Patent number: 7115627
    Abstract: The present application describes glycinamidic compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: November 25, 2002
    Date of Patent: October 3, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Donald J. P. Pinto, Wei Han, Zilun Hu, Jennifer Qiao
  • Patent number: 7074928
    Abstract: 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: Grant
    Filed: January 8, 2003
    Date of Patent: July 11, 2006
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Revital Lifshitz-Liron, Eti Kovalevski-Ishai, Shlomit Wizel, Sharon Avhar-Maydan, Rami Lidor-Hadas
  • Patent number: 7041675
    Abstract: 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: Grant
    Filed: January 25, 2001
    Date of Patent: May 9, 2006
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Reinhold Mueller, Sabine Schult
  • Patent number: 6992086
    Abstract: 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: Grant
    Filed: November 17, 2003
    Date of Patent: January 31, 2006
    Assignee: 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: 6989391
    Abstract: 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: Grant
    Filed: May 20, 2004
    Date of Patent: January 24, 2006
    Assignee: Bristol-Myers-Squibb Pharma Company
    Inventors: 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: 6977262
    Abstract: 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: Grant
    Filed: August 1, 2003
    Date of Patent: December 20, 2005
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Toshiyuki Kohara, Kenji Fukunaga, Masatake Fujimura, Tokushi Hanano, Hirotaka Okabe
  • Patent number: 6967208
    Abstract: 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: Grant
    Filed: September 17, 2002
    Date of Patent: November 22, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: 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: 6962926
    Abstract: 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: Grant
    Filed: August 8, 2003
    Date of Patent: November 8, 2005
    Assignees: 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: 6946473
    Abstract: 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: Grant
    Filed: March 17, 2003
    Date of Patent: September 20, 2005
    Assignee: Wyeth Holdings Corporation
    Inventors: Jeremy I. Levin, James M. Chen, Xue-Mei Du, Jay D. Albright, Arie Zask
  • Patent number: 6939870
    Abstract: 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: Grant
    Filed: August 29, 2003
    Date of Patent: September 6, 2005
    Assignee: Wyeth
    Inventors: Aranapakam M. Venkatesan, Jamie M. Davis, Yansong Gu
  • Patent number: 6919451
    Abstract: 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: Grant
    Filed: December 3, 2002
    Date of Patent: July 19, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jiacheng Zhou, Lynette M. Oh, Philip Ma, Hui-Yin Li, Pasquale Confalone
  • Patent number: 6867208
    Abstract: 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: Grant
    Filed: May 13, 2002
    Date of Patent: March 15, 2005
    Assignees: 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: 6867202
    Abstract: 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: Grant
    Filed: July 22, 2003
    Date of Patent: March 15, 2005
    Assignee: Pfizer Inc.
    Inventors: Philip Albert Carpino, Charles Kwok-Fung Chiu, Lydia Codetta Pan, Bruce Allen Lefker, Judith Lee Treadway, Michael Paul Zawistoski
  • Patent number: 6855708
    Abstract: 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: Grant
    Filed: March 13, 2002
    Date of Patent: February 15, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Linus S. Lin, George Doherty, Shrenik K. Shah, Linda L. Chang, William K. Hagmann, Richard A. Mumford
  • Patent number: 6852734
    Abstract: 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: Grant
    Filed: May 1, 2001
    Date of Patent: February 8, 2005
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Yasuo Yamamoto, Kenzo Hariyama, Yumiko Yanagisawa, Sojiro Shiokawa, Takumi Takeyasu, Osami Takenouchi, Hidenori Kasai
  • Patent number: 6849620
    Abstract: 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: Grant
    Filed: October 17, 2002
    Date of Patent: February 1, 2005
    Assignee: Pfizer Inc
    Inventors: 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: 6706730
    Abstract: 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: Grant
    Filed: April 17, 2002
    Date of Patent: March 16, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Donald Joseph Philip Pinto
  • Patent number: 6693116
    Abstract: 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: Grant
    Filed: September 18, 2002
    Date of Patent: February 17, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Heinrich Nettekoven, Sebastien Schmitt
  • Patent number: 6689790
    Abstract: 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: Grant
    Filed: October 7, 2002
    Date of Patent: February 10, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Heinrich Nettekoven, Sebastien Schmitt
  • Patent number: 6686359
    Abstract: 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: Grant
    Filed: December 6, 2002
    Date of Patent: February 3, 2004
    Assignee: Pfizer Inc.
    Inventor: Philip A. Carpino
  • Patent number: 6677365
    Abstract: 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: Grant
    Filed: March 25, 2002
    Date of Patent: January 13, 2004
    Assignees: 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: 6673929
    Abstract: 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: Grant
    Filed: October 30, 2002
    Date of Patent: January 6, 2004
    Assignee: Pfizer Inc.
    Inventors: Frank R. Busch, Charles K. Chiu, Clifford N. Meltz, Ronald J. Post, Peter R. Rose
  • Patent number: 6673810
    Abstract: 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: Grant
    Filed: July 3, 2001
    Date of Patent: January 6, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Patrick Y. Lam, Charles G. Clark, Qi Han, Thomas E. Richardson
  • Patent number: 6670364
    Abstract: 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: Grant
    Filed: January 29, 2002
    Date of Patent: December 30, 2003
    Assignees: 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: 6653320
    Abstract: 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: Grant
    Filed: March 1, 2002
    Date of Patent: November 25, 2003
    Assignees: 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: 6630487
    Abstract: 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: Grant
    Filed: May 29, 2002
    Date of Patent: October 7, 2003
    Assignee: Pfizer Inc.
    Inventors: Philip Albert Carpino, Charles Kwok-Fung Chiu, Lydia Codetta Pan, Bruce Allen Lefker, Judith Lee Treadway, Michael Paul Zawistoski
  • Patent number: 6559174
    Abstract: 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: Grant
    Filed: March 13, 2002
    Date of Patent: May 6, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Linus S. Lin, Shrenik K. Shah, Linda L. Chang, William K. Hagmann, Richard A. Mumford
  • Patent number: 6559152
    Abstract: 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: Grant
    Filed: February 27, 2001
    Date of Patent: May 6, 2003
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk
  • Patent number: 6541484
    Abstract: 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: Grant
    Filed: June 14, 2002
    Date of Patent: April 1, 2003
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian James Collins, Linda Elizabeth Keown, Leslie Joseph Street
  • Patent number: 6531449
    Abstract: 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: Grant
    Filed: March 8, 2001
    Date of Patent: March 11, 2003
    Assignee: Pfizer Inc.
    Inventors: S. Cyrus Khojasteh, John P. O'Donnell
  • Patent number: 6531477
    Abstract: 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: Grant
    Filed: October 12, 1999
    Date of Patent: March 11, 2003
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk
  • Patent number: 6531474
    Abstract: 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: Grant
    Filed: September 19, 2000
    Date of Patent: March 11, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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: 6525197
    Abstract: 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: Grant
    Filed: August 4, 2000
    Date of Patent: February 25, 2003
    Assignee: Studiengesellschaft Kohle mbH
    Inventors: Alois Fürstner, Günter Seidel, Antonio Rumbo, Christian Mathes
  • Patent number: 6506771
    Abstract: 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: Grant
    Filed: June 22, 2001
    Date of Patent: January 14, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Donald J. P. Pinto, Mimi L. Quan, Francis J. Woerner, Renhua Li
  • Patent number: 6506772
    Abstract: 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: Grant
    Filed: November 30, 2001
    Date of Patent: January 14, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Brodbeck, Matthias Heinrich Nettekoven
  • Patent number: 6444617
    Abstract: 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: Grant
    Filed: January 26, 2001
    Date of Patent: September 3, 2002
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Hideo Takaishi, Takeshi Katsuhira, Hiroshi Yamaguchi, Youichi Kawabata, Hiroto Harayama, Yoshiki Oda, Masahiko Murai
  • Patent number: 6413980
    Abstract: 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: Grant
    Filed: December 22, 1999
    Date of Patent: July 2, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: 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: 6403588
    Abstract: 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: Grant
    Filed: April 26, 2001
    Date of Patent: June 11, 2002
    Assignees: 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: 20020049196
    Abstract: This invention is directed to compounds of the formula 1
    Type: Application
    Filed: December 11, 2000
    Publication date: April 25, 2002
    Inventors: Philip A. Carpino, Paul A. DaSilva-Jardine, Bruce A. Lefker, John A. Ragan
  • Patent number: 6376509
    Abstract: 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: Grant
    Filed: May 29, 2001
    Date of Patent: April 23, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Raman Kumar Bakshi, Ravi P. Nargund, Zhixiong Ye
  • Patent number: 6358951
    Abstract: 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: Grant
    Filed: August 18, 1999
    Date of Patent: March 19, 2002
    Assignee: Pfizer Inc.
    Inventor: Philip A. Carpino
  • Patent number: 6340772
    Abstract: Three processes are described for preparing (hetero)aromatic substituted benzene derivatives which comprise aromatization of cyclohexenone derivatives via (chloro)cyclohexadiene derivatives.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: January 22, 2002
    Assignee: Nippon Kayaku Co., Ltd.
    Inventors: Tetsuya Toya, Hidetoshi Shirakura, Junichi Kon
  • Patent number: 6333336
    Abstract: 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: Grant
    Filed: August 23, 2000
    Date of Patent: December 25, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Michael Geoffrey Neil Russell, Leslie Joseph Street
  • Patent number: 6326379
    Abstract: Compounds of the formulas are useful as inhibitors of cGMP PDE, especially type V.
    Type: Grant
    Filed: September 10, 1999
    Date of Patent: December 4, 2001
    Assignee: Bristol-Myers Squibb Co.
    Inventors: John E. Macor, Guixue Yu
  • Patent number: 6303625
    Abstract: 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: Grant
    Filed: July 15, 1999
    Date of Patent: October 16, 2001
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: William J. Hoekstra, Edward C. Lawson, Bruce E. Maryanoff