Abstract: Compounds selected from the group consisting of a compound of the formula ##STR1## and compound of the formula ##STR2## wherein x is 1 or 2,Y is carbobenzoxy or benzoyl, andXR is ##STR3## have use as elastase enzyme inhibitors. Particularly potent are the L-proline diastereomers.Elastase Enzyme inhibitory compositions comprise a carrier and an elastase enzyme inhibiting amount of the compounds of the invention.A method of selectively inhibiting the enzyme elastase in an animal or a human in need of such treatment comprises administering to the animal or human an enzyme elastase inhibiting amount of one of the compounds of the invention or a composition thereof.
Type:
Grant
Filed:
October 27, 1988
Date of Patent:
April 16, 1991
Assignee:
University of Kentucky Research Foundation
Abstract: The present invention describes a dietary supplement for achieving a very high degree of chemotherapeutic activity through the synergistic combination of a low suboptimal dose of a D-glucarolactone-based dietary anticarcinogen (calcium glucarate) with a low suboptimal dose of retinoid-based anticarcinogen (4-hydroxyphenyl retinamide).
Type:
Grant
Filed:
November 13, 1989
Date of Patent:
April 16, 1991
Assignee:
Ohio State University Research Foundation
Inventors:
John P. Minton, Thomas E. Webb, Hussein M. Abou-Issa
Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents a C.sub.1-6 alkyl group;R.sub.2 represents a hydrogen atom or a C.sub.1-3 alkyl group;n represents zero or an integer from 1 to 3;and pharmaceutically acceptable salts thereof.The compounds are useful for the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.
Type:
Grant
Filed:
February 9, 1990
Date of Patent:
March 19, 1991
Assignee:
Glaxo Group Limited
Inventors:
Alexander W. Oxford, Peter C. North, Martin R. Johnson
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents a group ##STR2## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and A represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C.sub.1-4 alkyl group, and when (p,r,s) is (2,2,0) or (2,2,1) any A comprising 2 heteroatoms is optionally C-substituted by a methyl group, and when (p,r,s) is (2,1,0), (2,1,1) or (3,1,0) any A comprising 2 heteroatoms is optionally C-substituted by C.sub.1-2 alkyl and any A comprising one heteroatom is optionally C-substituted by a methyl group, and wherein compounds of formula (I) having two asymetric centers have the stereo-chemical configuration in which the group X and the (CH.sub.2).sub.
Type:
Grant
Filed:
March 7, 1989
Date of Patent:
November 6, 1990
Assignee:
Beecham Group P.L.C.
Inventors:
Barry S. Orlek, Michael S. Hadley, Howard E. Rosenberg, Harry J. Wadsworth