Abstract: The invention relates to substituted polycyclic aryl and heteroaryl 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. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
July 1, 2003
Assignee:
Pharmacia Corporation
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: Amino pyrazole derivatives of the formula:
which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active ingredient are described. The amino pyrazole derivatives are useful in the treatment of disorders and diseases associated with the NPY receptor subtype Y5.
Type:
Grant
Filed:
February 22, 2001
Date of Patent:
March 11, 2003
Inventors:
Cheryl P. Kordik, Scott L. Dax, Chi Luo, Allen B. Reitz, James J. McNally, Timothy W. Lovenberg
Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula
wherein:
R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl;
R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2;
n is 0 or 1;
R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons;
and all crystalline forms and the pharmaceutically acceptable salts thereof.
Abstract: A method of controlling a plant disease caused by a fungus comprising applying a 5-amino-pyrazole of the formula
wherein,
R1, R2, R3, R4, R5 and Y are as defined in the specification.
Type:
Grant
Filed:
February 20, 2001
Date of Patent:
September 3, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Markus Heil, Thomas Bretschneider, Hans-Christian Militzer, Astrid Mauler-Machnik, Klaus Stenzel
Abstract: The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and antiatherosclerotic activity. The present invention moreover relates to the preparation of these compounds and their use for the production of medicaments, and also medicaments comprising them.
Abstract: Disclosed is a process of making substituted pyrazoles from substituted benzophenone hydrazones with a variety of 1,3-bifunctional substrates under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds.
Type:
Grant
Filed:
October 27, 2000
Date of Patent:
June 18, 2002
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
James A. Baron, Vittorio Farina, Nizar Haddad
Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
Type:
Application
Filed:
November 29, 2001
Publication date:
May 16, 2002
Applicant:
Pharmacia Corporation
Inventors:
John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Balekudru Devadas
Abstract: 3-ureido-pyrazole derivatives represented by formula (I):
where R, R1 and R2 are as described herein, or pharmnaceutically acceptable salts thereof; are useful, for example, for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
Abstract: N-Phenylpyrazole derivatives of the formula:
wherein
R1 represents optionally halogenated alkyl;
R2 represents halogen, cyano, nitro, cycloalkyl, alkenyl, thiocyanato, optionally alkyl substituted sulphamoyl, optionally alkyl substituted carbamoyl, alkoxycarbonyl, alkanoyl or optionally halogenated alkyl; and R3 represents a hydrogen atom or a group N″R′″ or a variety of other groupings. These compounds possess arthropodicidal, plant nematocidal, anthelmintic and anti-protozoal properties; their preparation, compositions containing them and their use are described.
Type:
Grant
Filed:
July 16, 1999
Date of Patent:
April 16, 2002
Assignee:
Rhone-Poulenc Agriculture Ltd.
Inventors:
Leslie Roy Hatton, Ian George Buntain, David William Hawkins, Edgar William Parnell, Christopher John Pearson, David Alan Roberts
Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula
wherein:
R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl;
R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2;
n is 0 or 1;
R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons;
and all crystalline forms and the pharmaceutically acceptable salts thereof.
Abstract: A process is provided for the preparation of a compound of formulae (IA) (sidenafil) and (IB)
comprising reacting a compound of formula (IIA) and (IIB) respectively in the presence of —OR, wherein R in the case of formation of compound (IA) is CH2CH3 and R in the case of formation of compound (IB) is CH2CH2CH3, where X is a leaving group:
Type:
Grant
Filed:
October 8, 1999
Date of Patent:
March 27, 2001
Assignee:
Pfizer Inc.
Inventors:
Peter James Dunn, Philip Charles Levett
Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula
wherein:
R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl;
R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2;
n is 0 or 1;
R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons;
and all crystalline forms and the pharmaceutically acceptable salts thereof.