Abstract: The present application de gibes novel cyclic hydroxamic acids of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
June 17, 1999
Date of Patent:
August 6, 2002
Inventors:
Chu-Biao Xue, Carl P. Decicco, Xiaohua He
Abstract: The present application describes 6-membered aromatics of formula I:
or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(═NH)NH2, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
February 15, 2000
Date of Patent:
July 30, 2002
Assignee:
Bristol - Myers Squibb Pharma Company
Inventors:
James Russell Pruitt, Donald Joseph Phillip Pinto, Mimi Lifen Ouan, Ruth Richmond Wexler
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
Abstract: The present application describes inhibitors of factor Xa which are cyano-pyrazole, cyano-triazole, cyano-imidazole, and cyano-pyrrole compounds of Formulae Ia, Ib, Ic, and Id:
or pharmaceutically acceptable salt forms thereof.
Abstract: The present invention provides novel radiopharmaceuticals useful for imaging the heart, brain, lungs, liver or kidneys, kits useful for preparing the radiopharmaceuticals, and methods of imaging the heart, brain, lungs, liver or kidneys in a patient in need of such imaging. The radiopharmaceuticals are comprised of technetium or rhenium radionuclide complexes of a ternary ligand system: one hydrazido or diazenido ligand, one aminoalcohol ligand, and one pi-acid ligand selected from phosphines, arsines, and imine nitrogen-containing heterocycles. The radiopharmaceuticals have the formula, ML1L2L3, wherein the variables are as defined herein.
Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
June 11, 2002
Inventors:
Patrick Y. S. Lam, Charles G. Clark, John M. Fevig, Robert A. Galemmo, Qi Han, Irina C. Jacobson, Renhau Li, Donald J. P. Pinto, Ruth R. Wexler
Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I:
or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
Type:
Grant
Filed:
September 10, 1999
Date of Patent:
June 11, 2002
Inventors:
Robert A. Galemmo, Jr., Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
Abstract: The present application describes novel lactams and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
March 1, 2000
Date of Patent:
June 11, 2002
Inventors:
Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie, Jr.
Abstract: The present application describes aryl sulfonyls of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein D, E, and M are defined below, are effective factor Xa inhibitors.
Abstract: The present application describes novel amides and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein these compounds are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
April 23, 2002
Inventors:
Jingwu Duan, Carl P. Decicco, David J. Nelson, Chu-Biao Xue
Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
April 9, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Patrick Y. S. Lam, Charles G. Clark, Renhau Li, Donald J. P. Pinto
Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
May 13, 1999
Date of Patent:
April 2, 2002
Inventors:
Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I:
or pharmaceutically acceptable salt forms thereof, wherein rings D—E represent guanidine mimics, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
June 18, 1998
Date of Patent:
January 15, 2002
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
Abstract: A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described.
These compounds are useful as factor Xa inhibitors.
Type:
Grant
Filed:
October 10, 2000
Date of Patent:
December 11, 2001
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Jiacheng Zhou, Lynette May Oh, Pasquale N. Confalone, Hui-yin Li, Philip Ma
Abstract: The present application describes nitrogen containing heteroaromatics with ortho-substituted P1's and derivatives thereof of formula I:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D is substituted ortho to G on E and may be CH2NH2, which are useful as inhibitors of factor Xa.
Type:
Grant
Filed:
December 21, 1998
Date of Patent:
August 7, 2001
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Robert A. Galemmo, Jr., Lori L. Bostrom, Donald J. P. Pinto, Karen A. Rossi
Abstract: A palatable oral liquid pharmaceutical composition of benzoxazinone compounds useful as HIV reverse transcriptase inhibitors comprising the benzoxazinone active ingredient in a liquid vehicle comprising medium chain fatty acid triglycerides. Other formulating agents such as sweetening agents, lecithin suspending agents, etc. may be optionally added.
Abstract: The present invention relates to compounds of formula I:
or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as inhibitors of HIV protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Type:
Grant
Filed:
November 7, 1997
Date of Patent:
April 17, 2001
Assignee:
Dupont Pharmaceuticals
Inventors:
James David Rodgers, Patrick Yuk-Sun Lam
Abstract: The present application describes inhibitors of factor Xa of formula I:
or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.
Type:
Grant
Filed:
September 8, 1998
Date of Patent:
March 27, 2001
Assignee:
DuPont Pharmaceuticals Company
Inventors:
Qi Han, Celia Dominguez, Eugene C. Amparo, Jeongsook M. Park, Mimi L. Quan, Karen A. Rossi
Abstract: The present invention relates to 1,3-benzodiazepin-2-ones and 1,3-benzoxazepin-2-ones of formula I:
or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Type:
Grant
Filed:
June 29, 1999
Date of Patent:
March 20, 2001
Assignee:
DuPont Pharmaceuticals Company
Inventors:
James D. Rodgers, Anthony J. Cocuzza, Donna M. Bilder
Abstract: The present invention relates to benzoxazinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.
Type:
Grant
Filed:
October 21, 1998
Date of Patent:
October 31, 2000
Assignee:
DuPont Pharmaceutical Company
Inventors:
Joseph Marian Fortunak, Rodney Lawrence Parsons, Jr.