Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
Type:
Grant
Filed:
September 26, 2002
Date of Patent:
March 1, 2005
Assignee:
G. D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
August 12, 2003
Date of Patent:
March 1, 2005
Assignee:
G. D. Searle & Co.
Inventors:
Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
Abstract: A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein each of R1, R2 and R3 is independently selected from hydrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R1, R2 and R3 must be a substituent other than hydrido, and with the further proviso that when each of R1 and R3 is hydrido, then R2 cannot be chloro; wherein R4 is hydrido; wherein R5 is alkyl; and wherein R6 is tetrazolyl; or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
Abstract: A method of using an MMP inhibitor and optionally radiation therapy, and one or more antineoplastic agents of the topoisomerase class selected from the group consisting of irinotecan and topotecan, as a combination therapy for the treatment of neoplasia is disclosed.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
February 22, 2005
Assignee:
G. D. Searle & Co.
Inventors:
John P. McKearn, Gary Gordon, James J. Cunningham, Stephen T. Gately, Alane T. Koki, Jaime L. Masferrer
Abstract: 2-Amino-benzoxazinones are identified for use in the treatment of Herpes Simplex Virus. A subject is treated for Herpes Simplex Virus by treating with an effective amount of 2-amino-benzoxazinones.
Type:
Application
Filed:
September 13, 2004
Publication date:
February 10, 2005
Applicants:
G.D. Searle & Co., Asahi Chemical Industry Co., Ltd.
Abstract: A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by Formula I wherein R-R4 are as defined herein, or a pharmaceutically-acceptable salt thereof.
Type:
Application
Filed:
December 8, 2003
Publication date:
February 10, 2005
Applicant:
G.D. Searle & Co.
Inventors:
Norman Abood, Daniel Flynn, Daniel Becker, Brian Bax, Hui Li, Roger Nosal, Lori Schretzman, Clara Villamil
Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein Q, R1, R2, R3 and R4 are as described in the specification.
Abstract: Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.
Type:
Grant
Filed:
December 23, 2002
Date of Patent:
February 1, 2005
Assignee:
G. D. Searle & Co.
Inventors:
John S Ng, Claire S Przybyla, Shu-Hong Zhang
Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
July 22, 2002
Date of Patent:
January 25, 2005
Assignee:
G. D. Searle & Co.
Inventors:
Michael L Vazquez, Richard A. Mueller, John J. Talley, Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: A class of dihydrobenzopyrans, dihydrobenzothiopyrans, tetrahydroquinolines, tetrahydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula (I) wherein X, A1, A2, A3, A4, R, R?, R1 and R2 are as described in the specification.
Type:
Application
Filed:
August 2, 2004
Publication date:
January 13, 2005
Applicant:
G.D. Searle & Co.
Inventors:
Donald Rogier, Jeffery Carter, John Talley
Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
February 24, 2004
Publication date:
January 6, 2005
Applicant:
G.D. Searle & Co.
Inventors:
Michael Vazquez, Richard Mueller, John Talley, Daniel Getman, Gary DeCrescenzo, John Freskos
Abstract: A cDNA clone having a base sequence for human tissue factor inhibitor (TFI) has been developed and characterized and the amino acid sequence of the TFI has been determined.
Type:
Application
Filed:
July 9, 2004
Publication date:
December 30, 2004
Applicant:
G. D. SEARLE & CO.
Inventors:
Tze Chein Wun, Kuniko K. Kretzmer, George J. Broze
Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
January 2, 2004
Publication date:
December 30, 2004
Applicant:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Application
Filed:
January 20, 2004
Publication date:
December 23, 2004
Applicant:
G. D. Searle & Co.
Inventors:
Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
Abstract: The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of an integrin antagonist and an antineoplastic agent.
Type:
Grant
Filed:
October 5, 2001
Date of Patent:
December 21, 2004
Assignee:
G.D. Searle & Co.
Inventors:
John P. McKearn, Gary Gordon, James J. Cunningham, Stephen T. Gately, Alane T. Koki, Jaime L. Masferrer
Abstract: The present invention relates to a class of compounds represented by the Formula I
or a pharmaceutically acceptable salt thereof, wherein
A is
pharmaceutical compositions thereof and methods of using such compounds and compositions as &agr;v&bgr;3 antagonists.
Type:
Grant
Filed:
December 18, 1998
Date of Patent:
December 14, 2004
Assignee:
G. D. Searle & Co.
Inventors:
Peter Gerrard Ruminski, Michael Clare, Paul Waddell Collins, Bipinchandra Nanubhai Desai, Richard John Lindmark, Joseph Gerace Rico, Thomas Edward Rogers, Mark Andrew Russell
Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
March 30, 2004
Publication date:
November 18, 2004
Applicant:
G.D. Searle & Co.
Inventors:
Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.
Abstract: Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney.