Patent number: 6211234
Abstract:
Compounds of formula (I) are described wherein R1 is hydrogen, -(lower alkyl)q(CO2R6 or OH), —CN, —C(R7)═NOR8, NO2, —O(lower alkyl)R9, —C≡C—R10, —CR11═C(R12)(R13), —C(═O)CH2C(═O)CO2H, —CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4 and R5 are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.
Type:
Grant
Filed:
June 27, 1997
Date of Patent:
April 3, 2001
Assignee:
Rhone-Poulenc Rorer Limited
Inventors:
Peter Charles Astles, Mark Francis Harper, Neil Victor Harris, Iain McFarlane McLay, Roger John Aitchison Walsh, Richard Alan Lewis, Christopher Smith, Barry Porter, Clive McCarthy
Patent number: 6187812
Abstract: Phenylacetic acid derivatives of the formula I
where the substituents and the index have the following meanings:
X is oxygen or sulfur;
R is hydrogen or alkyl;
R1 is hydrogen or alkyl;
R2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;
m is 0, 1 or 2, it being possible for the R2 radicals to be different if m is 2;
R3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;
R4 is hydrogen, cyano, nitro, hydroxyl, amino, halogen,
unsubstituted or substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, alkenyl, alkenyloxy, alkenylthio, alkenylamino, N-alkenyl-N-alkylamino, alkynyl, alkynyloxy, alkynylthio, alkynylamino, N-alkynyl-N-alkylamino;
unsubstituted or substituted cycloalkyl, cycloalkoxy, cycloalkylthio, cycloalkylamino, N-cycloalkyl-N-alkylamino, cycloalkenyl, cycloalkenyloxy, cycloalkenylthio, cycloalkenylamino, N-cycloalkenyl-N-alkylamino, heterocyclyl, heterocyclyloxy, heterocycly
Type:
Grant
Filed:
February 3, 2000
Date of Patent:
February 13, 2001
Assignee:
BASF Aktiengesellschaft
Inventors:
Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz
Patent number: 6169103
Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
Type:
Grant
Filed:
February 24, 1999
Date of Patent:
January 2, 2001
Assignee:
Warner-Lambert
Inventors:
Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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