American Home Products Corporation

Wyeth

Kevin Anthony Memoli

Amedeo A Failli

Jay Scott Shumsky

Ivo L Jirkovsky

Steven W Felman

Thomas Joseph Caggiano

Eugene John Trybulski

John P Dusza

Donald P Strike

Joseph Peter Sabatucci

Robert J Steffan

William Sanders

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

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.

Tricyclic hydroxy carboxamides and derivatives thereof tocolytic oxytocin receptor antagonists

Substituted tetrahydro-pyrimidine-2(1H)-thione HDL-C elevators useful as antiatherosclerotic agents

This invention provides compounds of formula 1 having the structure

Substitued tetrahydro-1,3,5-triazin-2&lsqb;1H&rsqb;-thiones as anti-atherosclerotic agents

This invention provides compounds of formula 1 having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are each independently, hydrogen, halogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkyl, alkoxy, aryloxy, fluoroalkoxy, trifluoromethyl, alkylthio, alkylsulfony, --SCF.sub.3, nitro, alkylamino, or dialkylamino;

Substituted tetrahydro-1,3,5-triazin-2[1H]-thiones as

The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.8 is alkyl containing 1 to 3 carbon atoms which possess blood-glucose lowering activity, to processes for preparation thereof, pharmaceutical compositions comprising the same, and to the method of using the same in the reduction of excess cholesterol in human beings and animals.

Heterocyclic oxime carbamates

The present invention relates to novel 4- or 5-(substituted sulfonyl) methyl-3(2H)-furanones having the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, or halogen substituted phenyl; or R.sup.1 and R.sup.2 are joined by 5 to 7 carbon atoms;

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Cranbury, NJ, United States of America

Kevin Anthony Memoli