Abstract: This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain.
Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.
Type:
Grant
Filed:
March 18, 1993
Date of Patent:
April 5, 1994
Assignee:
Eli Lilly and Company
Inventors:
Raymond F. Brown, J. Jeffry Howbert, Karen L. Lobb, David A. Neel, Jon K. Reel, Beverley Greenwood
Abstract: The invention relates to a compound of formula (I) ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halo, hydroxy, nitro, C.sub.1-4 alkylcarbonyl, hydroxy-C.sub.1-4 alkyl, R.sup.3 is hydrogen or optionally substituted phenylsulphonyl, R.sup.4 is optionally substituted phenyl, benzofuranyl or dihydrobenzofuranyl, and R.sup.5 is hydrogen or C.sub.1-4 alkyl; and salts thereof. These compounds are useful dopaminergic agents.
Type:
Grant
Filed:
November 19, 1991
Date of Patent:
November 2, 1993
Assignee:
Lilly Industries Limited
Inventors:
Barry P. Clark, Graham H. Timms, David E. Tupper
Abstract: 3,4,4-trisubstitutedpiperidinyl-N-alkylcarboxylates and intermediates for their preparation are provided. These piperidine-N-alkylcarboxylates are useful as peripheral opioid antagonists.
Abstract: 2-Methyl-10-(4-methyl-1-piperazinyl)-4H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.
Type:
Grant
Filed:
May 22, 1992
Date of Patent:
July 20, 1993
Assignee:
Lilly Industries Limited
Inventors:
Jiban K. Chakrabarti, Terrence M. Hotten, David E. Tupper