Abstract: A series of diazinylpiperidine compounds of Formula I ##STR1## wherein X is an ethylene chain or a 1,2-benzo ring; Y is carbonyl or methylene; R.sup.1 is hydrogen or lower alkyl; and Z is an R.sup.2, R.sup.3 -disubstituted diazinyl ring selected from pyridazine, pyrimidine, and pyrazine ring systems. Pharmacologic and neuroanatomical testing demonstrates that compounds of the series act to enhance cerebral function in mammals, particularly when there is a deficit in normal cerebral functioning. Specific pharmacologic test results indicate that compounds of Formula I possess cognition and memory enhancing activity.
Type:
Grant
Filed:
August 28, 1987
Date of Patent:
May 2, 1989
Assignee:
Bristol-Myers
Inventors:
Ronald J. Mattson, Joseph P. Yevich, Michael S. Eison
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: 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: Gepirone and its pharmaceutically acceptable salts are useful in alleviation of panic disorders which can take the form of clinical syndromes comprising, for example, panic attacks, agoraphobia and phobic anxiety.
Type:
Grant
Filed:
July 29, 1987
Date of Patent:
November 1, 1988
Assignee:
Bristol-Myers Company
Inventors:
Neil Kurtz, Roger E. Newton, Davis L. Temple, Jr.
Abstract: Gepirone and its pharmaceutically acceptable salts are useful in alleviation of certain primary depressive disorders, such as major depression with melancholia and atypical depression.
Type:
Grant
Filed:
March 2, 1987
Date of Patent:
September 13, 1988
Assignee:
Bristol-Myers Company
Inventors:
Jerry M. Cott, Neil Kurtz, Donald S. Robinson
Abstract: Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is a substituted pyridin-2-yl ring and the second substituent is a butylene chain attached to cyclic imide heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione, spirocyclopentylthiazolidinedione, or morpholine-2,6-dione. The compounds have psychotropic properties and 2-[4-[4-(2,4-dioxo-1-thia-3-azaspiro[4.5]nonane-3-yl)butyl]-1-piperazinyl] -pyridine-3-carboxaldehyde is a typical embodiment having selective antipsychotic activity.
Type:
Grant
Filed:
September 30, 1986
Date of Patent:
July 12, 1988
Assignee:
Bristol-Myers Company
Inventors:
James S. New, Walter G. Lobeck, Jr., Joseph P. Yevich
Abstract: Disubstituted 1,4-piperazinyl derivatives are disclosed wherein one substituent is a bicyclic fused-ring furo-, pyrrolo-, cyclopentadieno-, or thieno-pyridine heterocyclic system and the second substituent is an alkylene chain attached to cyclic imide heterocycles, such as azaspiro[4.5]decanediones, dialkylglutarimides, thiazolidinediones, succinimides, and morpholine-2,6-diones; or a benzylic carbinol moiety. These compounds have potent antipsychotic and serotonin antagonist activities. 4-[4-[4-(4-Furo[3,2-c]pyridinyl)-1-piperazinyl]butyl]-3,5-morpholinedione is an example of a typical embodiment having selective antipsychotic activity.
Abstract: A new and novel process for the preparation of encainide (4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]-benzanilide) has been developed. The process utilizes .alpha.-picoline, O-nitrobenzaldehyde, and anisoyl chloride as starting materials.
Abstract: A series of nootropic compounds of the following formula: ##STR1## and its pharmaceutically acceptable acid addition salts, wherein: R.sup.2 is hydrogen, lower alkyl, aryl which is optimally substituted, or hetaryl;R.sup.7 is hydrogen or is combined with R.sup.9 as a fused benzo-ring;R.sup.8 is hydrogen or lower alkyl; andR.sup.9 is lower alkyl, or R.sup.9 can be combined with R.sup.8 to give a 2-pyrrolidinone, a phthalimide, or isoindolone ring system.Pharmacological testing demonstrates that the series possesses cognition and memory enhancing actions and/or mild CNS simulation.
Abstract: 8-[4-[4-(1-Oxo-1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5 ]decane-7,9-dione is an antipsychotic agent having reduced side effect liability.
Type:
Grant
Filed:
April 24, 1985
Date of Patent:
April 7, 1987
Assignee:
Bristol-Myers Company
Inventors:
Joseph P. Yevich, Walter G. Lobeck, Jr.
Abstract: Buspirone and its pharmaceutically acceptable salts are useful in alleviation of panic disorders which can take the form of clinical syndromes comprising, for example, panic attacks, agoraphobia and phobic anxiety.
Type:
Grant
Filed:
October 25, 1985
Date of Patent:
January 6, 1987
Assignee:
Bristol-Myers Company
Inventors:
Neil M. Kurtz, Roger E. Newton, Davis L. Temple, Jr.
Abstract: Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is a substituted pyridin-2-yl ring and the second substituent is a butylene chain attached to cyclic imide heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione, spirocyclopentylthiazolidinedione, or morpholine-2,6-dione. The compounds have psychotropic properties and 2-[4-[4-(2,4-dioxo-1-thia-3-azaspiro[4.5]nonane-3-yl)butyl]-1-piperazinyl] pyridine-3-carboxaldehyde is a typical embodiment having selective antipsychotic activity.
Type:
Grant
Filed:
January 16, 1985
Date of Patent:
October 28, 1986
Assignee:
Bristol-Myers Company
Inventors:
James S. New, Walter G. Lobeck, Jr., Joseph P. Yevich
Abstract: Dipeptides having the formula ##STR1## wherein A is halogen, hydrogen, lower alkyl, or lower alkoxy; B is hydrogen or lower alkyl, or A and B are taken together to form an ortho-methylene or ethylene bridge; R is hydrogen, lower alkyl, or phenylalkyl; and X.sup.1 and X.sup.2 are independently chosen from hydroxy or lower alkoxy; are inhibitors of angiotensin-converting enzyme and can be used for the treatment of hypertension in mammals.