Abstract: Novel thieno[3,2-c]pyridine derivatives of Formula I, ##STR1## in which Z is glutarimide, are useful antipsychotic agents with reduced side-effect liability.
Abstract: A series of psychotropic heterobicycloalkylpiperazine derivatives having the structure ##STR1## wherein V is a 3- or 4-membered unsaturated chain, containing all carbon atoms when 4-membered, or when a 3-membered chain, V contains an oxygen or sulfur atom as one of the members; R is H or C.sub.1-4 alkyl; W is CH, N, CH.sub.2, or a chemical bond; X is CH, N, SO.sub.2, or CO, with the proviso that both W and X cannot simultaneously be N; and Z is a heteroaromatic ring system. These compounds are useful antipsychotic and/or anxiolytic agents.
Abstract: Certain water-soluble polyanionic organic acid polymers in the weight range of from about 1,000 to 30,000 daltons may be use to inhibit aminoglycoside nephrotoxicity. These polyanionic polymers are homopolymers or copolymers comprised of monomers selected from acrylic, methacryclic, vinylsulfonic and maleic acids; and are in a pharmaceutically acceptable salt form.
Abstract: Certain 1-indolylalkyl-4-(alkoxypyrimidinyl)piperazines of Formula I are useful antidepressant agents. The ##STR1## substituents R.sup.1, R.sup.2 and R.sup.5 are hydrogen or lower alkyl; R.sup.3 and R.sup.4 are hydrogen, alkyl, alkoxy, alkythio, carboxamido, halo, or trifluoromethyl; R.sup.6 is alkoxy; and n is the integer 2 or 3.
Type:
Grant
Filed:
June 29, 1990
Date of Patent:
December 31, 1991
Assignee:
Bristol-Myers Squibb Co.
Inventors:
David W. Smith, Frank D. Yocca, Joseph P. Yevich, Ronald J. Mattson
Abstract: A process for protecting brain cells from ischemia and for treating ischemic and degenerative brain disorders. The process involves systemic administration of BMY 14802 or a pharmaceutically acceptable acid addition salt and/or hydrate.
Type:
Grant
Filed:
June 1, 1989
Date of Patent:
October 8, 1991
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Christopher G. Boissard, Duncan P. Taylor, Michael S. Eison
Abstract: "Buspirone hydrochloride can exist in two polymorphic forms and the newly discoverd lower melting form, which is thermodynamically favored at pharmaceutically relevant temperatures, offers advantage in manufacture of buspirone pharmaceutical compositions".
Abstract: Novel substituted benzamides of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined herein are useful in the treatment of emesis, and particularly chemotherapy-induced emesis in cancer patients. Some of the compounds are also useful in disorders relating to impaired gastric motility.
Abstract: A novel process utilizing adenosine deaminase to selectively produce .beta.-(D)-2',3'-dideoxyinosine in high yields from an .alpha.,.beta.-anomeric mixture. .beta.-(D)-2',3'-Dideoxyinosine so produced is useful as an antiviral and antibiotic agent.
Type:
Grant
Filed:
February 28, 1990
Date of Patent:
April 30, 1991
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Vittorio Farina, Daniel A. Benigni, Paul R. Brodfuehrer
Abstract: A series of psychotropic heterobicycloalkylpiperazine derivatives having the structure ##STR1## wherein V is a 3- or 4-membered unsaturated chain, containing all carbon atoms when 4-membered, or when a 3-membered chain, V contains an oxygen or sulfur atom as one of the members; R is H or C.sub.1-4 alkyl; W is CH, N, CH.sub.2, or a chemical bond; X is CH, N, SO.sub.2, or CO, with the proviso that both W and X cannot simultaneously be N; and Z is a heteroaromatic ring system. These compounds are useful antipsychotic and/or anxiolytic agents.
Abstract: A series of 5-halopyrimidin-2-ylpiperazinylalkyl derivatives having useful anti-ischemic properties for treatment and prevention of dirorders resulting from brain and/or spinal cord anoxia.
Abstract: Various metabolites and prodrug formulations of 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]deca ne-7,9-dione which are particularly useful in the treatment of psychotic disorders, especially derivatives thereof which have been oxygenated at specified sites about the original structure, rearranged compounds, and prodrug formulations of these species. One particularly desired group of compounds have the general Formula I where ##STR1## R.sup.1 is hydrogen, hydroxyl, alkoxy, acyloxy and oxo; R.sup.2 is hydrogen, methyl, hydroxyl, alkoxy, and acyloxy;R.sup.3 is hydrogen, hydroxyl, and methoxy:R.sup.4 is hydrogen, methyl and oxo; andX is S, SO, and SO.sub.2.
Type:
Grant
Filed:
July 24, 1989
Date of Patent:
September 11, 1990
Assignee:
Bristol-Myers Company
Inventors:
Joseph A. Cipollina, Edward H. Ruediger
Abstract: A series of 1,4-disubstituted piperazine derivatives comprised of indol-3-ylalkyl and substituted pyridin-2-yl substituent groups. These compounds are useful as antidepressant agents.
Type:
Grant
Filed:
April 14, 1989
Date of Patent:
September 4, 1990
Assignee:
Bristol-Myers Squibb Company
Inventors:
David W. Smith, Frank D. Yocca, Joseph P. Yevich, Ronald J. Mattson
Abstract: A series of 1,4-dihydropyridin-3,5-yl dicarboxylic acid amides and esters incorporating an arylpiperazinylalkyl moiety have been prepared possessing the general formula ##STR1## wherein R.sup.4 is cycloalkyl, aryl or hetaryl, generally with electron-withdrawing substituents; R.sup.2 and R.sup.6 are lower alkyl, alkanol, alkoxyalkyl, or alkylaminoalkyl; R.sup.5 is R.sup.2 or arylpiperazinylalkyl; X is O or NH; Y is lower alkylene, alkoxyalkylene, alkylaminoalkylene; and Z is phenyl, substituted pheny, pyridinyl, substituted pyridinyl, or pyrimidinyl. Compounds of this series demonstrate activity as calcium and alpha-adrenergic blockers in in vitro testing and antihypertensive, anti-ischemic, and platelet function inhibiting actions in in vivo screens.
Type:
Grant
Filed:
December 18, 1987
Date of Patent:
January 23, 1990
Assignee:
Bristol-Myers Company
Inventors:
Graham S. Poindexter, Davis L. Temple, Jr.
Abstract: A series of psychotropic acyclic amide derivatives having the structure ##STR1## wherein R is alkyl, alkenyl, cycloalkyl- and bicycloalkyl-methyl; and Z is a heterocyclic group comprised of pyrimidine, benzisothiazole, thienopyridine, and furopyridine. These compounds are useful antipsychotic and/or anxiolytic agents.
Abstract: A process for resolving a racemic modification of .beta.-adrenergic aryl- or hetaryl-oxypropanolamines such as (.+-.)-2-[2-hydroxy-3-[[2-(1H-indol-3-yl)-)-1,1-dimethylethyl]amino]propox y]benzonitrile into its individual enantiomers is described. The process comprises converting the racemic modification into a pair of diastereomeric urea derivativesby reaction with a chiral aralkylisocyanate; separation into the individual diastereomers; and facile regeneration of the starting amine by cleavage of the intermediate urea compound using hydrazine. This final step is improved by the addition of an .alpha.-keto carboxylic acid, such as pyruvic acid, which functions as a scavenger of nucleophilic by-products.
Type:
Grant
Filed:
March 30, 1988
Date of Patent:
July 18, 1989
Assignee:
Bristol-Myers Company
Inventors:
Ronald D. Dennis, Terence M. Dolak, William E. Kreighbaum
Abstract: Tiospirone and its pharmaceutically acceptable salts are useful in alleviation of vascular or vascular-related headaches such as migraine, cluster, muscle-contraction, and combined headaches.
Type:
Grant
Filed:
October 25, 1988
Date of Patent:
July 11, 1989
Assignee:
Bristol-Myers Company
Inventors:
Davis L. Temple, Michael F. Rafferty, Michael S. Eison, Stacy N. Suberg