Title:
NOVEL INHIBITORS OF CHYMASE
Document Type and Number:
WIPO Patent Application WO2005073214
Kind Code:
A3
Abstract:
The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
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Inventors:
HAWKINS MICHAEL J (US)
GRECO MICHAEL N (US)
POWELL EUGENE (US)
DE GARAVILLA LAWRENCE (US)
MARYANOFF BRUCE E (US)
GRECO MICHAEL N (US)
POWELL EUGENE (US)
DE GARAVILLA LAWRENCE (US)
MARYANOFF BRUCE E (US)
Application Number:
PCT/US2005/001659
Publication Date:
October 20, 2005
Filing Date:
January 18, 2005
Export Citation:
Assignee:
JANSSEN PHARMACEUTICA NV (BE)
HAWKINS MICHAEL J (US)
GRECO MICHAEL N (US)
POWELL EUGENE (US)
DE GARAVILLA LAWRENCE (US)
MARYANOFF BRUCE E (US)
HAWKINS MICHAEL J (US)
GRECO MICHAEL N (US)
POWELL EUGENE (US)
DE GARAVILLA LAWRENCE (US)
MARYANOFF BRUCE E (US)
International Classes:
A61K31/165; A61K31/381; A61K31/4436; A61K31/453; A61K31/662; C07F9/30; C07F9/32; C07F9/38; C07F9/40; C07F9/572; C07F9/59; C07F9/60; C07F9/62; C07F9/655; C07F9/6553; C07F9/6558; C07F9/6561; C07F9/6571; (IPC1-7): C07F9/30; C07F9/32; C07F9/38; C07F9/40; A61K31/662
Foreign References:
| EP0661260A1 | 1995-07-05 |
Other References:
P.TEMPEST ET AL.: "MCC/SnAr methodology. Part1", TETRAHEDRON LETT., vol. 42, 2001, pages 4963 - 4968, XP002336083
M.N.GRECO ET AL.: "Nonpeptide inhibitors of Cathepsin G: Optimization of a novel beta-Ketophosphonic acid Lead by Structure-based Drug Design", J.AM.CHEM.SOC., vol. 124, 2002, pages 3810 - 3811, XP002336084
FUKAMI H ET AL: "CHYMASE: ITS PATHOPHYSIOLOGICAL ROLES AND INHIBITORS", CURRENT PHARMACEUTICAL DESIGN, BENTHAM SCIENCE PUBLISHERS, SCHIPHOL, NL, vol. 4, no. 6, 1998, pages 439 - 453, XP000885575, ISSN: 1381-6128
J.A.BERTRAND ET AL.: "Inhibition of Trypsin and Thrombin by Amino(4-amidinophenyl)methanephosphonate Diphenyl Ester Derivatives", BIOCHEM., vol. 35, 1996, pages 3147 - 3155, XP002336085
J.OLEKSYSZYN ET AL.: "Irreversible Inhibition of Serine Proteases by Peptide Derivatives of (alpha-Aminoalkyl)- phosphonate Diphenyl Esters", BIOCHEM., vol. 30, 1991, pages 485 - 493, XP002336086
Y.AOYAMA ET AL.: "Synthesis and Structure-Activity Relationships of a new class of 1-Oxacephem-based Human Chymase Inhibitors", BIOORG.MED.CHEM.LETT., vol. 10, 2000, pages 2397 - 2401, XP002336087
V.LACHKOVA ET AL.: "Interaction between Phenylmethanephosphonic acid Diethyl Ester and Isothiocyanates", PHOSPHORUS, SULFUR AND SILICON, vol. 48, 1990, pages 227 - 233, XP009050625
M.N.GRECO ET AL.: "Nonpeptide inhibitors of Cathepsin G: Optimization of a novel beta-Ketophosphonic acid Lead by Structure-based Drug Design", J.AM.CHEM.SOC., vol. 124, 2002, pages 3810 - 3811, XP002336084
FUKAMI H ET AL: "CHYMASE: ITS PATHOPHYSIOLOGICAL ROLES AND INHIBITORS", CURRENT PHARMACEUTICAL DESIGN, BENTHAM SCIENCE PUBLISHERS, SCHIPHOL, NL, vol. 4, no. 6, 1998, pages 439 - 453, XP000885575, ISSN: 1381-6128
J.A.BERTRAND ET AL.: "Inhibition of Trypsin and Thrombin by Amino(4-amidinophenyl)methanephosphonate Diphenyl Ester Derivatives", BIOCHEM., vol. 35, 1996, pages 3147 - 3155, XP002336085
J.OLEKSYSZYN ET AL.: "Irreversible Inhibition of Serine Proteases by Peptide Derivatives of (alpha-Aminoalkyl)- phosphonate Diphenyl Esters", BIOCHEM., vol. 30, 1991, pages 485 - 493, XP002336086
Y.AOYAMA ET AL.: "Synthesis and Structure-Activity Relationships of a new class of 1-Oxacephem-based Human Chymase Inhibitors", BIOORG.MED.CHEM.LETT., vol. 10, 2000, pages 2397 - 2401, XP002336087
V.LACHKOVA ET AL.: "Interaction between Phenylmethanephosphonic acid Diethyl Ester and Isothiocyanates", PHOSPHORUS, SULFUR AND SILICON, vol. 48, 1990, pages 227 - 233, XP009050625
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