Wyeth

American Home Products Corporation

Jay Scott Shumsky

Amedeo A Failli

Thomas Joseph Caggiano

Kevin Anthony Memoli

Eugene John Trybulski

John P Dusza

Joseph Peter Sabatucci

Robert J Steffan

William Sanders

Mark A Ashwell

David K Williams

Donald P Strike

Eugene J Trybulski

A compound of the formulae (I) or (II): wherein:Y is a moiety selected from NR or &#x2014;(CH);wherein R is hydrogen or (C-C) lower alkyl,and n is 1;  (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C-C) lower alkyl, halogen, cyano, CF, hydroxy, (C-C) lower alkoxy, (C-C) lower alkoxy carbonyl, carboxy, &#x2014;CONH, &#x2014;CONH[(C-C) lower alkyl], &#x2014;CON[(C-C) lower alkyl]; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C-C) lower alkyl, halogen or (C-C) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C-C) lower alkyl, halogen, cyano, CF, hydroxy, (C-C) lower alkoxy, or (C-C) lower alkoxy carbonyl, carboxy, &#x2014;CONH, &#x2014;CONH[(C-C) lower alkyl], &#x2014;CON[(C-C) lower alkyl]; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C-C) lower alkyl, (C-C) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C-C) lower alkyl, halogen, or (C-C) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C-C) lower alkyl, halogen, or (C-C) lower alkoxy; Ris a moiety of the formula and R, R, R, Rand Rare, independently, selected from a group consisting of hydrogen, (C-C) lower alkyl, OCH, halogen, CF, &#x2014;SCH, OCF, SCF, or CN;or a pharmaceutically acceptable salt, or pro-drug form thereof.

Biphenyl vasopressin agonists

The present invention provides compounds of the general formulas: wherein Y is NR or &#x2014;(CH); R is H or alkyl; 'Z' represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; 'W' represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; &#x201c;X&#x201d; represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

Cyclohexylphenyl vasopressin agonists

The present invention provides tricyclic carboxamide compounds and methods and pharmaceutical compositions for their use in treatment, prevention, or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and/or suppression of preterm labor, suppression of labor at term prior to caesarean deliver, and for the treatment of dysmenorrhea. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Cyclohexenyl phenyl carboxamides tocolytic oxytocin receptor antagonists

A compound of the formulae (I) or (II): wherein: represents: represents: represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C&#x2013;C) lower alkyl, halogen, or (C&#x2013;C) lower alkoxy; and R, R, R, Rand Rare, independently, selected from a group consisting of hydrogen, (C&#x2013;C) lower alkyl, OCH, halogen, CF, &#x2014;SCH, OCF, SCF, or CN;or a pharmaceutically acceptable salt, or pro-drug form thereof.

The present invention provides novel tricyclic benzodiazepine carboxamides compounds and methods and pharmaceutical compositions utilizing them for the treatment and/or prevention and/or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and/or suppression suppression of preterm labor, suppression of labor at term prior to caesarean delivery, and for the treatment of dysmenorrhea. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Cyclohexylphenyl carboxamides tocolytic oxytocin receptor antagonists

This invention provides novel tricyclic diazepine compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and/or prevention and/or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including treatment of preterm labor, dysmenorrhea, endometritis, and for suppressing labor prior to caesarean delivery. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Tricyclic diazepines tocolytic oxytocin receptor antagonists

This invention provides novel substituted tricyclic pyridyl carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Tricyclic pyridyl carboxamides and derivatives thereof tocolytic oxytocin receptor antagonists

The present invention provides compounds of the general formulas: wherein Y is NR or &#x2014;(CH); R is H or alkyl 'Z' represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; 'W' represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; &#x201c;X&#x201d; represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

A compound of the formulae (I) or (II):wherein:

This invention provides novel substituted tricyclic carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea and endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Growing community of inventors

Hightstown, NJ, United States of America

Jay Scott Shumsky