American Cyanamid Company

Wyeth

John P Dusza

Jay Donald Albright

Andrew S Tomcufcik

Joseph P Joseph

Seymour Bernstein

Amedeo A Failli

Thomas Joseph Caggiano

Kevin Anthony Memoli

Jay Scott Shumsky

Eugene John Trybulski

Shin S Tseng

Aranapakam Mudumbai Venkatesan

Fuk-Wah Sum

Dennis W Powell

Walter E Meyer

Goro Asato

Joseph William Epstein

Lawrence W Torley

Pamela K Baker

Bernard D Johnson

Robert F Church

Mark Anthony Ashwell

Jehan F Bagli

Daniel B Moran

Robert A Hardy, Jr

Albert John Molinari

Bernard Beer

Seymour Berstein

Peter S Chan

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

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

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:

Tricyclic vasopressin agonists

N-methyl-N-(3-&lcub;3-&lsqb;2-thienylcarbonyl&rsqb;-pyrazol-&lsqb;1,5-&agr;&rsqb;-pyrimidin-7-yl&rcub;phenyl)acetamide, and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Compositions containing N-methyl-N-(3-&lcub;3-&lsqb;2-thienylcarbonyl&rsqb;-pyrazol-&lsqb;1,5-&agr;&rsqb;-pyrimidin-7-yl&rcub;phenyl)acetamide, as well as pharmaceutically acceptable salts thereof, are also disclosed.

N-methyl-N-(3-&lcub;3-&lsqb;2-thienylcarbonyl&rsqb;-pyrazol-&lsqb;1, 5-&agr;&rsqb;-pyrimidin-7-yl&rcub;phenyl)acetamide and compositions and methods related thereto

Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Tricyclic benzazepine vasopressin antagonists

Disclosed are 3-substituted-7-[3-(imidazol-1-yl)phenyl]-pyrazolo[1,5-a]pyrimidines of the formula: ##STR1## wherein R.sup.1, R.sup.3 and R.sup.4 are defined in the specification which compounds have anxiolytic, anti-convulsant, sedative-hypnotic and skeletal muscle relaxant activity.

3-Substituted-7-[3-(imidazol-1-yl)phenyl]-pyrazolo[1,5-a]pyrimidines

Novel N-((dialkylamino)methylene)-substituted-pyrazolo(1,5-a)pyrimidine-3-carbox amide and N-((dialkylamino)methylene)-substituted-4,5-dihydropyrazolo-(1,5-a)-pyrimi dine-3-carboxamide compounds are disclosed which are useful as neurotropic and/or anxiolytic and/or anti-hypertensive agents in mammals.

N-(dialkylamino)methylene)-substituted

A novel process for producing .alpha.-[(dialkylamino)substituted-methylene].beta.-oxo-(substituted) propanenitriles of the formula: ##STR1## where R, R.sub.1 and R.sub.2 are defined in the specification by reacting a substituted isoxazole with a diaklyamide dimethylacetal is provided.

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Nanuet, NY, United States of America

John P Dusza