Abstract: Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.
Type:
Grant
Filed:
August 27, 1998
Date of Patent:
February 4, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Richard P. Polniaszek, Xuebao Wang, Jeffrey S. DePue, Chennagiri R. Pandit, Kumar G. Gadamasetti, Yadagiri Pendri, Eduardo J. Martinez
Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure
where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.
Type:
Grant
Filed:
September 25, 2000
Date of Patent:
January 28, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
Abstract: A method is provided for inhibiting platelet aggregation and thrombus formation by administering to a patient an ADP-receptor blocking antiplatelet drug, such as clopidogrel, in combination with a thromboxane A2 receptor antagonist, such as ifetroban, and optionally a cholesterol lowering drug, such as an HMG CoA reductase inhibitor, for example, pravastatin.
Abstract: Hydroxamic acids are provided which are ACE and/or NEP inhibitors and have the structure
wherein R*, R and R1 are as defined herein and A is a dipeptide preferably derived from an amino acid, or is a conformationally restricted dipeptide mimic.
Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure
including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;
Rx is H, alkyl, aryl or halogen;
A is
(1) a bond;
(2) —O—; or
(3)
B is:
and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,
are as defined herein.
Type:
Grant
Filed:
May 18, 1999
Date of Patent:
October 29, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
Abstract: The (R)-enantiomer of 4-[[(cyanoimino)[(1,2,2-trimethylpropyl)amino]methyl]amino]benzonitrile as well as the corresponding (S)-enantiomer are useful for promoting hair growth such as in male pattern baldness.
Abstract: A method for inhibiting hair loss and/or promoting hair growth in chemotherapy and/or radiation therapy patients wherein the (R)-enantiomer of 4-[[(cyanoimino)-[(1,2,2-trimethylpropyl)amino]methyl]amino]benzonitrile is administered prior to, simultaneous with and/or after chemotherapy and/or radiation treatment.
Abstract: Compounds are provided having the formula
including pharmaceutically acceptable salts thereof, wherein
R1 is lower alkyl, aryl or arylalkyl;
A is hydrogen or
B is hydrogen, alkyl, alkenyl, or
but when A is hydrogen, B may only be
R2, R2′, R2″, R3 R3′ and R3″ are as defined herein;
m is 0−3. These compounds possess activity at the beta 3 adrenergic receptor in mammals and are useful in the treatment of diabetes, obesity, depression, achalasia and intestinal hypermotility disorders.
Type:
Grant
Filed:
July 25, 2001
Date of Patent:
August 20, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Philip M. Sher, William N. Washburn, Jollie D. Godfrey, Jr.
Abstract: Compounds are provided which have the structure
wherein Q is C or N, A is 0 or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
Type:
Grant
Filed:
March 20, 2001
Date of Patent:
July 2, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Peter T. Cheng, Pratik Devasthale, Yoon Jeon, Sean Chen, Hao Zhang
Abstract: Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula
where
x is 0 or 1 and y is 0 or 1 (provided that
x=1 when y=0 and x=0 when y=1);
n is 0 or 1; X is H or CN;
and wherein R1, R2, R3 and R4 are as described herein.
A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
Type:
Grant
Filed:
February 16, 2001
Date of Patent:
May 28, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jeffrey A. Robl, Richard B. Sulsky, David J. Augeri, David R. Magnin, Lawrence G. Hamann, David A. Betebenner
Abstract: Benzoazepines of the following formula
wherein R1, R1a, R2, R9k, L, Q, X, Y and Z are as described herein, and analogs thereof are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
Abstract: A method is provided for preventing or reducing the risk of onset of a cardiovascular event by administering an HMG CoA reductase inhibitor such as pravastatin, to a patient which has one or more risk factors for a coronary and/or cerebrovascular event such as hypercholesterolemia.
Type:
Grant
Filed:
January 18, 1994
Date of Patent:
April 9, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Bruce D. Behounek, Mark E. McGovern, Adeoye Y. Olukotun
Abstract: Lactam inhibitors are provided which have the structure
X is
wherein
Y is O or S and R4 is
R7O— or R8
and R1, R2, R3, R5, R6, R7, and R8, are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants, and are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating cardiovascular diseases associated with thromboses and for treating asthma and related diseases are also provided.
Type:
Grant
Filed:
August 7, 2000
Date of Patent:
February 5, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Gregory S. Bisacchi, Steven M. Seiler, R. Michael Lawrence, James C. Sutton, Jr., William A. Slusarchyk, Guohua Zhao
Abstract: Caprolactam inhibitors are provided which have the structure
including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrugs thereof, wherein n is 1 to 5; and
and Y R1, R2, R3, R5, R5a, R6, R7, R8, R9 and R10 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.
Type:
Grant
Filed:
February 2, 2000
Date of Patent:
October 2, 2001
Assignee:
Bristol-Myers Squibb Company
Inventors:
Philip D. Stein, Gregory S. Bisacchi, Yan Shi, Stephen P. O'Connor, Chi Li
Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure
including pharmaceutically acceptable salts thereof, or prodrug esters thereof,
A is
where Z is N or CH, or where Z is
or CH2 when is a single bond;
and wherein L1, R, R1, R3, R3′, R3a, R3b, R4, R4′, R5, R5a, X,
are as defined herein.
Abstract: The (R)-enantiomer of 4-[[(cyanoimino)-[(1,2,2-trimethylpropyl)amino]methyl]amino]-benzonitrile as well as the corresponding (S)-enantiomer are useful for promoting hair growth such as in male pattern baldness.
Type:
Grant
Filed:
July 12, 2000
Date of Patent:
July 17, 2001
Assignee:
Bristol-Myers Squibb Company
Inventors:
Karnail S. Atwal, Joyce Chou, Seshadri Neervannan
Abstract: A method is provided for preventing a cerebral infarction by administering to a patient a combination of an ADP-receptor blocking antiplatelet drug, such as clopidogrel, in combination with an antihypertensive agent such as an angiotensin AII antagonist (for example, irbesartan), an ACE inhibitor (for example, fosinopril) or a NEP/ACE inhibitor such as omapatrilat.
Abstract: A method is provided for treating schizophrenia in a mammalian species by administering an ACE inhibitor, such as captopril, alone or with a neuroleptic such as cholecystokinin, fluphenazine or haloperidol.
Type:
Grant
Filed:
September 12, 1991
Date of Patent:
February 13, 2001
Assignee:
E.R. Squibb & Sons, Inc.
Inventors:
Abraham Sudilovsky, Joram Feldon, Ina Weiner, A. David Smith, John N. P. Rawlins
Abstract: A process is provided for preparing chiral cyclopropane carboxylic acids, preferably of the structure ##STR1## which are intermediates used in preparing acyl guanidine sodium/proton exchange (NHE) inhibitors.
Type:
Grant
Filed:
June 10, 1999
Date of Patent:
December 12, 2000
Assignee:
Bristol-Myers Squibb co.
Inventors:
Bang-Chi Chen, Joseph E. Sundeen, Jeffrey T. North, Annie J. Pullockaran, Saleem Ahmad, Shung C. Wu, Karnail S. Atwal, Sundeep Dugar
Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure ##STR1## where A, B, D, Q, X.sup.1, R, R.sup.1, X.sup.2 and R.sup.2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.
Type:
Grant
Filed:
August 17, 1999
Date of Patent:
November 21, 2000
Assignee:
Bristol-Myers Squibb Company
Inventors:
John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear