Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/212.07)
  • Patent number: 6943169
    Abstract: The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R1, R4, R5, R6, R7, R8, R9 and are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: September 13, 2005
    Assignee: Roche Palo Alto LLC
    Inventors: David Bruce Repke, Russell Stephen Stabler, Ralph New Harris, III
  • Patent number: 6906056
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: March 20, 2003
    Date of Patent: June 14, 2005
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. Vanmeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Patent number: 6906059
    Abstract: The use of benzazepin-N-acetic acid derivatives which contain an oxo group in the a position to the nitrogen atom and are substituted in the 3 position by a 1-(carboxyalkyl)-cyclopentyl-carbonyl-amino radical, and of their salts and biolabile esters, for the prophylaxis and/or treatment of heart damage caused by cardiotoxic doses of medicaments or chemicals, in larger mammals and in particular humans. The invention is particularly applicable to the prophylaxis and/or treatment of heart damage, in particular to the myocardium, which may occur during cytostatic chemotherapy. The invention also includes the use of the afore-mentioned benzazepin-N-acetic acid derivatives for adjuvant treatment in therapies in which medicaments having oxidative-toxic side-effects are used, and the preparation of medicaments suitable for this prophylaxis and/or treatment or adjuvant treatment.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: June 14, 2005
    Assignee: Solvay Pharmaceuticals
    Inventors: Zsuzsanna Lonovics, Julius Gy. Papp, Dirk Thormaehlen, Harald Waldeck, Zsuzsanna Rozsa
  • Publication number: 20040248878
    Abstract: The present invention provides crystalline (N)—((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-4,5,6,7-tetrahydro-2H-3-benzazepin-2-one dihydrate, compositions thereof, and methods for using the same, processes for making the same, and processes for making intermediates thereof.
    Type: Application
    Filed: April 28, 2003
    Publication date: December 9, 2004
    Inventors: Thomas Mitchell Koenig, James Edmund Audia, David Mitchell, Stacey Leigh McDaniel, Lynne Ann Buccilli, Gary Lowell Engel, James Abraham Aikins
  • Patent number: 6825188
    Abstract: Compounds having a benzodiazepinyl core structure are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis, angiogenesis, tumor growth and metastasis, atherosclerosis, restenosis and inflammation.
    Type: Grant
    Filed: October 22, 2003
    Date of Patent: November 30, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: James Francis Callahan, Russell Donovan Cousins, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Irene Nijole Uzinskas
  • Publication number: 20040224938
    Abstract: The invention relates to substituted benzo[b]azepin-2-one compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.
    Type: Application
    Filed: April 14, 2004
    Publication date: November 11, 2004
    Inventors: Michael Sattlegger, Helmut Buschmann, Michael Przewosny, Werner Englberger, Babette-Yvonne Koegel, Hans Schick
  • Patent number: 6767905
    Abstract: The invention relates to the use of an angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of acute MI and for the secondary prevention of acute MI.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: July 27, 2004
    Assignee: Novartis, AG
    Inventors: Jessica M. Mann, Pascale Oddou, Eric Michel Neuhart
  • Publication number: 20040142918
    Abstract: This invention relates to the use of a vitronectin receptor antagonist to inhibit adhesion formation.
    Type: Application
    Filed: October 9, 2003
    Publication date: July 22, 2004
    Inventor: Robert N. Willette
  • Publication number: 20040142919
    Abstract: The present invention relates to novel benzazepinone derivatives, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and are therefore useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
    Type: Application
    Filed: October 21, 2003
    Publication date: July 22, 2004
    Inventors: Robert S. Meissner, Paul J. Coleman, Mark E. Duggan, George D. Hartman, Jiabing Wang, John H. Hutchinson
  • Patent number: 6737419
    Abstract: Stable tablets comprising benazepril hydrochloride are prepared by employing zinc stearate as the lubricant.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: May 18, 2004
    Inventor: Bernard Charles Sherman
  • Publication number: 20040077627
    Abstract: The present invention provides ctystalline (N)-((S)-2-hydroxy-3-methyl-butyryl-1-(L-alaninyl)-(S)-1-amino-3-methyl-4,5,6,7-tetrahydro-2H-3-benzazcepin-2-one anhydrate, compositions thereof, and methods for using the same, processes for making the same, and processes for making intermediate thereof.
    Type: Application
    Filed: September 3, 2003
    Publication date: April 22, 2004
    Inventors: Thomas Mitchell Koenig, David Mitchell, Jeffrey Scott Nissen
  • Publication number: 20040058900
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Application
    Filed: January 6, 2003
    Publication date: March 25, 2004
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. Mcdaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Publication number: 20040043977
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Application
    Filed: January 6, 2003
    Publication date: March 4, 2004
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Publication number: 20040029862
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Application
    Filed: February 5, 2003
    Publication date: February 12, 2004
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Publication number: 20030216377
    Abstract: A compound of the formula (I) is disclosed which is a vitronectin receptor antagonist and is useful in the treatment of osteoporosis: 1
    Type: Application
    Filed: May 5, 2003
    Publication date: November 20, 2003
    Applicant: SmithKline Beecham Corporation
    Inventor: Dirk Heerding
  • Patent number: 6635632
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: October 21, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Publication number: 20030162768
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Application
    Filed: December 12, 2002
    Publication date: August 28, 2003
    Inventors: James E. Audia, Bruce A. Dressman, Qing Shi
  • Patent number: 6602864
    Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: August 5, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
  • Publication number: 20030129188
    Abstract: The present invention is directed to integrin targeting compounds comprising an integrin targeting component linked to a functional component such as a therapeutic agent or antibody. Structures of various integrin targeting compounds are provided. Additionally provided are methods of delivering a functional component to integrin associated with cells or tissue of an individual using the integrin targeting compounds. Also provided are methods of treating or preventing a disease or condition in an individual using the wherein said disease or condition involves an integrin using the integrin targeting compounds.
    Type: Application
    Filed: October 22, 2002
    Publication date: July 10, 2003
    Applicant: The Scripps Research Institute
    Inventors: Carlos F. Barbas, Christoph Rader, Subhash C. Sinha
  • Publication number: 20030125317
    Abstract: Compounds having a benzodiazepinyl core structure are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis, angiogenesis, tumor growth and metastasis, atherosclerosis, restenosis and inflammation.
    Type: Application
    Filed: December 16, 2002
    Publication date: July 3, 2003
    Applicant: SmithKline Beecham Corporation
    Inventors: James Francis Callahan, Russell Donovan Cousins, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Irene Nijole Uzinskas
  • Publication number: 20030114438
    Abstract: Lactam derivatives of the formula 1
    Type: Application
    Filed: October 9, 2002
    Publication date: June 19, 2003
    Inventors: Karnail S. Atwal, Saleem Ahmad, Francis N. Ferrara
  • Patent number: 6579867
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: June 17, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, James J. Droste, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Publication number: 20030105075
    Abstract: The invention relates to the use of hymenialdisine or derivatives thereof of formula (I) in which R1 and R2, identical or different, represent H or Br, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in inhibiting acceptable salt thereof, in the manufacture of a medicament for use in inhibiting cycline dependent kineases, GSK-3&bgr; and casein kinase 1. Application for preventing and treating neurodegenerative disorders, diabetes, inflammatory pathologies and cancers.
    Type: Application
    Filed: October 4, 2002
    Publication date: June 5, 2003
    Inventor: Laurent Meijer
  • Publication number: 20030096804
    Abstract: This invention relates generally to a novel class of bicyclic heterocyclic compounds of the Formula (I): 1
    Type: Application
    Filed: May 22, 2002
    Publication date: May 22, 2003
    Inventors: Irina C. Jacobson, Mimi L. Quan, Yun-Long Li, Ruth R. Wexler, Patrick Y.S. Lam
  • Publication number: 20030087894
    Abstract: A compound of the formula (I) is disclosed which is a vitronectin receptor antagonist and is useful in the treatment of osteoporosis: 1
    Type: Application
    Filed: October 22, 2002
    Publication date: May 8, 2003
    Applicant: SmithKline Beecham Corporation
    Inventor: Dirk Heerding
  • Patent number: 6559141
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: May 6, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Patent number: 6552013
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: April 22, 2003
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and Company
    Inventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
  • Patent number: 6544978
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: April 8, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Patent number: 6544980
    Abstract: The present invention provides a method of inhibiting matrix metallo-proteinases (MMPs) in a patient in need thereof comprising administering to the patient an effective matrix metalloproteinase inhibiting amount of the N-carboxymethyl substituted benzolactams of formula (1): wherein A is —OH or —NRR′. Such inhibitors are useful in treating neoplasms, atherosclorosis, and chronic inflammatory diseases. The present invention also provides novel N-carboxymethyl substituted benzolactams of formula (1a): wherein A is —NRR′.
    Type: Grant
    Filed: February 20, 2002
    Date of Patent: April 8, 2003
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Alan M. Warshawsky, Michael J. Janusz, Gary A. Flynn
  • Patent number: 6541466
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: April 1, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Patent number: 6534496
    Abstract: The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.
    Type: Grant
    Filed: October 7, 1999
    Date of Patent: March 18, 2003
    Assignee: Takeda Chemical Industries, Inc.
    Inventors: Yuji Ishihara, Yukio Fujisawa, Naoki Furuyama
  • Publication number: 20030050302
    Abstract: A method for increasing the generation of non-amyloidogenic soluble APP comprising activation of protein kinase C (PKC) by administering an effective amount of at least one PKC activator. Also provided is a method for altering conditions associated with amyloid processing in order to enhance an &agr;-secretase pathway to generate soluble &agr;-amyloid precursor protein (&agr;-APP) so as to prevent &bgr;-amyloid aggregation comprising administering an effective amount of a benzolactam.
    Type: Application
    Filed: September 26, 2002
    Publication date: March 13, 2003
    Applicant: Neurologic, Inc.
    Inventors: Rene Etcheberrigaray, Lixin Qiao, Alan P. Kozikowski
  • Patent number: 6528505
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: March 4, 2003
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Bruce A. Dressman, Qing Shi
  • Publication number: 20030040512
    Abstract: The use of benzazepin-N-acetic acid derivatives which contain an oxo group in the a position to the nitrogen atom and are substituted in the 3 position by a 1-(carboxyalkyl)-cyclopentyl-carbonyl-amino radical, and of their salts and biolabile esters, for the prophylaxis and/or treatment of heart damage caused by cardiotoxic doses of medicaments or chemicals, in larger mammals and in particular humans. The invention is particularly applicable to the prophylaxis and/or treatment of heart damage, in particular to the myocardium, which may occur during cytostatic chemotherapy. The invention also includes the use of the afore-mentioned benzazepin-N-acetic acid derivatives for adjuvant treatment in therapies in which medicaments having oxidative-toxic side-effects are used, and the preparation of medicaments suitable for this prophylaxis and/or treatment or adjuvant treatment.
    Type: Application
    Filed: January 14, 2002
    Publication date: February 27, 2003
    Inventors: Zsuzsanna Rozsa, Julius Gy. Papp, Dirk Thormaehlen, Harald Waldeck, Zsuzsanna Lonovics
  • Patent number: 6514965
    Abstract: This invention relates to substituted 1-benzazepines and derivatives thereof useful as antibacterial agents, to compositions, including pharmaceutical compositions, comprising such compounds, to processes for making these compounds and to methods of using these compounds for killing bacteria or inhibiting bacterial growth.
    Type: Grant
    Filed: November 7, 2000
    Date of Patent: February 4, 2003
    Assignee: Antex Pharma Inc.
    Inventors: Alenka Tomazic, Liren Huang, Kenneth D. Tucker
  • Patent number: 6514964
    Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as &agr;v&bgr;3, &agr;v&bgr;5, &agr;v&bgr;6 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: September 26, 2000
    Date of Patent: February 4, 2003
    Assignee: Amgen Inc.
    Inventors: Zhidong Chen, Celia Dominguez, Ellen Grenzer-Laber, Nianhe Han, Longbing Liu, Ofir A. Moreno, Melvin C. Rutledge, Andrew S. Tasker
  • Patent number: 6509331
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: January 21, 2003
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
  • Patent number: 6500819
    Abstract: A bicyclolactam compound of the formula (1) is disclosed, which has an excellent anxiolytic effect, is high in safety, and is useful as an effective component of medicinals which are greatly diminished in side effects such as hypnotic, muscle relaxant and sedative effects A bicyclolactam derivative represented by the following formula (1) is also disclosed, and is useful as an effective component of an anxiolytic agent
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: December 31, 2002
    Assignee: Taiho Pharmaceutical Company Limited
    Inventors: Junji Yamamoto, Takashi Arima, Nobuo Kasahara, Masato Nanri, Kazuo Ogawa, Ichiro Yamawaki, Manabu Kaneda
  • Publication number: 20020183308
    Abstract: Stable tablets comprising benazepril hydrochloride are prepared by employing zinc stearate as the lubricant.
    Type: Application
    Filed: April 12, 2002
    Publication date: December 5, 2002
    Inventor: Bernard Charles Sherman
  • Publication number: 20020128257
    Abstract: A compound of the formula (I) is disclosed which is a vitronectin receptor antagonist and is useful in the treatment of osteoporosis: 1
    Type: Application
    Filed: May 8, 2002
    Publication date: September 12, 2002
    Applicant: SmithKline Beecham Corporation
    Inventor: Dirk Heerding
  • Publication number: 20020123487
    Abstract: A compound of the formula (I) is disclosed which is a vitronectin receptor antagonist and is useful in the treatment of osteoporosis: 1
    Type: Application
    Filed: April 29, 2002
    Publication date: September 5, 2002
    Applicant: SmithKline Beecham Corporation
    Inventor: William E. Bondinell
  • Publication number: 20020099048
    Abstract: A bicyclolactam compound of the formula (1) is disclosed, which has an excellent anxiolytic effect, is high in safety, and is useful as an effective component of medicinals which are greatly diminished in side effects such as hypnotic, muscle relaxant and sedative effects 1
    Type: Application
    Filed: January 10, 2002
    Publication date: July 25, 2002
    Applicant: Taiho Pharmaceutical Company Limited
    Inventors: Junji Yamamoto, Takashi Arima, Nobuo Kasahara, Masato Nanri, Kazuo Ogawa, Ichiro Yamawaki, Manabu Kaneda
  • Publication number: 20020095035
    Abstract: The present invention provides a method of inhibiting matrix metallo-proteinases (MMPs) in a patient in need thereof comprising administering to the patient an effective matrix metalloproteinase inhibiting amount of the N-carboxymethyl substituted benzolactams of formula (1): 1
    Type: Application
    Filed: February 20, 2002
    Publication date: July 18, 2002
    Inventors: Alan M. Warshawsky, Michael J. Janusz, Gary A. Flynn
  • Publication number: 20020061874
    Abstract: This invention relates to novel lactams having the Formula (I): 1
    Type: Application
    Filed: April 3, 2001
    Publication date: May 23, 2002
    Inventors: Michael G. Yang, Hong Liu
  • Patent number: 6387894
    Abstract: The present invention relates to compositions and methods of achieving a therapeutic effect including, but not limited to, the treatment of congestive heart failure or hypertension in an animal, preferably a mammal including a human subject or a companion animal, using a corticotropin releasing factor (CRF) antagonist and a renin-angiotensin system (RAS) inhibitor.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: May 14, 2002
    Assignee: Pfizer Inc.
    Inventor: Anthony A. Fossa
  • Publication number: 20020055499
    Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1
    Type: Application
    Filed: December 12, 2001
    Publication date: May 9, 2002
    Inventors: Dirk Heerding, James Martin Samanen
  • Publication number: 20020052361
    Abstract: The present invention relates to the use of benzazepine-N-acetic acid derivatives which contain an oxo-group in the &agr;-position to the nitrogen atom and are substituted in position 3 by a 1-(carboxyalkyl)cyclo-entylcarbonylamino radical, and their salts and biolabile esters for the treatment of hypertension, particularly for the treatment of certain forms of secondary hypertension, in larger mammals and particularly humans, and for the production of pharmaceutical compositions suitable for this treatment. The cause of the hypertension to be treated may have a wide variety of origins. The invention particularly relates to the treatment of those forms of secondary hypertension which may occur as a result of various non-cardiac diseases.
    Type: Application
    Filed: August 16, 2001
    Publication date: May 2, 2002
    Inventors: Martin R. Wilkins, Dirk Thormaehlen, Harald Waldeck
  • Publication number: 20020040047
    Abstract: The invention relates to the use of 4-aryl-4-hydroxy-tetrahydropyrans and 3-aryl-3-hydroxy-tetrahydrofurans for the treatment or prevention of chronic obstructive pulmonary disease.
    Type: Application
    Filed: December 6, 2000
    Publication date: April 4, 2002
    Inventors: Edward Raymond Halstead Walker, Roger Metcalf, Stephen John Foster
  • Publication number: 20020040136
    Abstract: A compound of the formula (I) is disclosed which is a vitronectin receptor antagonist and is useful in the treatment of osteoporosis: 1
    Type: Application
    Filed: November 28, 2001
    Publication date: April 4, 2002
    Applicant: SmithKline Beecham Corporation
    Inventor: Dirk Heerding
  • Publication number: 20020032187
    Abstract: A method for stimulating bone formation by administering integrin binding compounds which cause the release of osteocalcin from osteoblasts is disclosed.
    Type: Application
    Filed: September 20, 2001
    Publication date: March 14, 2002
    Applicant: SmithKline Beecham Corporation
    Inventor: Fred H. Drake