Abstract: The present invention provides novel prodrug derivatives of fluorooxindoles having the general Formula I wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer, and R1, R2, R3, R4 and X are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.
Abstract: The S-stereoisomer of 6-hydroxy-buspirone is an effective treatment for anxiety, depression, and other psychogenic disorders. The S-isomer may provide reduced potential for adverse effects and a longer duration of action compared to the racemic mixture and with buspirone.
Type:
Grant
Filed:
July 22, 2002
Date of Patent:
November 23, 2004
Assignee:
Bristol-Myers Squibb Company
Inventors:
Joseph P. Yevich, Robert F. Mayol, Jianqing Li, Frank Yocca
Abstract: The R-stereoisomer of 6-hydroxy-buspirone is an effective treatment for anxiety, depression, and other psychogenic disorders. The R-isomer exhibits greater receptor specificity than the S-isomer and should have reduced potential for the adverse effects associated with the racemic mixture and with buspirone.
Type:
Grant
Filed:
July 22, 2002
Date of Patent:
February 3, 2004
Assignee:
Bristol-Myers Squibb Company
Inventors:
Joseph P. Yevich, Robert F. Mayol, Jianqing Li, Frank Yocca
Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of oxadiazole, thiadiazole and thiadiazole oxide derivatives of dihydropyridines of Formula I.
wherein B is
with X being O, S or
and X1 is O or S. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
Type:
Grant
Filed:
July 2, 2001
Date of Patent:
July 22, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Graham S. Poindexter, Mendi Higgins, James Guy Breitenbucher
Abstract: A method of treating pain with acetaminophen comprises the concurrent administration of a hydroxyazapirone selected from 6-hydroxybuspirone or 3-hydroxygepirone. This combination of agents results in a more morphine-like analgesic response characterized by rapid onset and greater pain relief.
Type:
Grant
Filed:
April 4, 2002
Date of Patent:
July 15, 2003
Assignees:
Laboratories UPSA, Bristol-Myers Squibb Company
Inventors:
Francoise Camborde, Alix Cloarec, Charles Conway
Abstract: A method of treating pain with acetaminophen comprises the concurrent administration of an azapirone such as buspirone. This combination of agents surprisingly results in a strengthened analgesic response characterized by rapid onset, greater pain relief, and a longer duration of action.
Type:
Grant
Filed:
May 17, 2001
Date of Patent:
May 20, 2003
Assignees:
Laboratories, UPSA, Bristol-Myers Squibb Company
Inventors:
Francoise Camborde, Alix Cloarec, Charles Conway
Abstract: A method of treating pain with acetaminophen comprises the concurrent administration of buspirone. This combination of agents surprisingly results in a morphine-like analgesic response characterized by rapid onset, greater pain relief, and a longer duration of action.
Type:
Grant
Filed:
January 4, 2001
Date of Patent:
January 28, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Francoise Camborde, Alix Cloarec, Charles Conway
Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprises of amino and piperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1.
where X is CH or N
As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
Type:
Grant
Filed:
May 10, 2001
Date of Patent:
November 12, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Graham S. Poindexter, Marc Bruce, Sing-Yuen Sit, Scott W. Martin
Abstract: Compounds of Formula I:
wherein Ar, Y, m, and Z are as defined in the specification, are useful antipsychotic and antidepressant agents demonstrating potent inhibition of 5-HT reuptake and dopamine D2 receptor antagonism.
Type:
Grant
Filed:
December 12, 2000
Date of Patent:
November 5, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Ronald J. Mattson, Joseph P. Yevich, Jun Yuan, Arlene S. Eison, Derek Denhart
Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of 4-alkyl and cycloalkyl derivatives of dihydropyridines of Formula I.
As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
Abstract: A series of antagonists of NPY have been synthesized and are comprised of squarate derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I).
As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
Abstract: There is provided a series of arylacetamidoalanyl derivatives of benzodiazepinones of Formula I
wherein R1 through R7 and n are defined herein, which are inhibitors of &bgr;-amyloid peptide (&bgr;-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extract cellular deposition of amyloid.
Type:
Grant
Filed:
July 2, 2001
Date of Patent:
August 13, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Prasad V. Chaturvedula, Suresh Yeola, Shikha Vig
Abstract: A series of antagonists of NPY have been synthesized and are comprised of thiourea linked piperazine and piperidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1.
where Z is NR7R8 or
and X is CH or N.
As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
Abstract: An improved method of treatment for anxiety and/or depression provides a quicker and more robust anxiolytic/antidepressant activity to a patient suffering from depression. The method comprises the concurrent administration of effective doses of certain azapirones, such as buspirone, given in a manner that suppresses formation of the 1-(2-pyrimidinyl)piperazine metabolite; and a 5-HT1A autosomal receptor antagonist, such as pindolol.
Abstract: Compounds of formula I are useful antidepressant agents
demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or indolyl.
Type:
Grant
Filed:
December 21, 1999
Date of Patent:
May 1, 2001
Assignee:
Bristol-Myers Squibb Company
Inventors:
Michael A. Poss, David R. Tortolani, Ronald J. Mattson, Joseph P. Yevich
Abstract: 6-Hydroxy-8-[4-[4-(2-pyrimidinyl)-piperazinyl]-butyl]-8-azaspiro[4.5]-7,9-d ione and its pharmaceutically acceptable salts and hydrates are useful in the alleviation of anxiety.
Abstract: Extended-release nefazodone compositions containing nefazodone hydrochloride, ionic and non-ionic gelling polymers, an insoluble hydrophilic agent, and optional pharmaceutically acceptable excipients demonstrate pH-modulated release of nefazodone. These compositions are formulated into unit dosage forms for improved oral administration. The improvements comprise an extended drug release profile providing comparative levels of nefazodone with respect to immediate release dosage forms and, additionally, demonstrating the lack of a food effect.
Type:
Grant
Filed:
April 26, 1999
Date of Patent:
November 7, 2000
Assignee:
Bristol-Myers Squibb Company
Inventors:
Andrew B. Dennis, Peter Timmins, Alison C. Hodsdon
Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of heteroaryl derivatives of imidazolone compounds of Formula 1. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
Abstract: There is provided novel aryloxyanilides and related compounds of the formula ##STR1## wherein R.sup.1 is --OR, --CO.sub.2 R, or halogen with R being C.sub.1-4 alkyl;R.sup.2 is R, cyclopropyl, C.sub.2-4 alkenyl or --CH.sub.2 OR; andX is O, S, CH.sub.2, NR, SO, SO.sub.2 or COwhich are melatonergic agents and are useful in the treatment of circadian rhythm-related disorders and other conditions affected by melatonin activity.