American Home Products Corporation

Wyeth

Other

American Home Products Company

Amedeo A Failli

Robert J Steffan

Thomas Joseph Caggiano

Jay Scott Shumsky

Wenling Kao

Eugene John Trybulski

Oleg I Bleyman

Kevin Anthony Memoli

Magid A Abou-Gharbia

Anthony F Kreft, Iii

John H Musser

John P Dusza

Craig E Caufield

James Albert Nelson

Uresh Shantilal Shah

William Sanders

Dennis Michael Kubrak

Donald P Strike

Dominick Anthony Quagliato

Gavin David Heffernan

Robert L Vogel

Joseph Peter Sabatucci

Richard Dale Coghlan

Annette L Banker

Emily S Shen

Gary Paul Stack

Christopher A Demerson

Mark Anthony Ashwell

Guy A Schiehser

Koji Nakanishi

William Jay Moore

Deborah Ann Evrard

Brian Hugh Ridgway

Patrick Michael Andrae

Katherine L Molnar-Kimber

Albert John Molinari

Susan Christman Croce

Alexander A Grinfeld

Alexander A Greenfield

Mark A Ashwell

David C Hu

Yanqiu Chen

David K Williams

Jay Donald Albright

Arthur Attilio Santilli

Jerauld S Skotnicki

Annmarie Louise Sabb

Reinhardt Bernhard Baudy

Jehan F Bagli

Dahui Zhou

Eugene J Trybulski

Madelene M Antane

William Ronald Solvibile

Anita Wai-Yin Chan

Jianxin Ren

Lalitha Krishnan

Robert Lewis Vogel

Yanfang Li

Molly Hoke

Charles Guinosso

Antonia Nikitenko

Robert M Kearney

Jean Yi-ching Sze

Charles John Stanton, Iii

Magid A Abou-Charbia

Oleg J Bleyman

Peter S Chan

Mark Antony Ashwell

Aranapakam Madumbai Venkatesan

Amy Tsai-Ting Lee

This invention provides pyrrolobenzodiazepine arylcarboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists, as well as pharmaceutical compositions and methods of treatment utilizing these compounds. 

Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists

The invention provides compounds of formula or a pharmaceutically acceptable salt thereof, wherein R, R, R, R, and B are as defined in the accompanying specification. Methods of making such compounds are also provided.

Pyrrolobenzodiazepines and heterocyclic carboxamide derivatives as follicle stimulating hormone receptor (FSH-R) antagonists

This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2). 

Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists

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

Synthetic methods are provided for production of compounds of the formula: where R, R, R, R, R, R, R, R, R, R, R, R, Rand Rare as defined in the specification.

Processes for preparing 6-alkyl-5-arylsulfonyl-dihydrophenanthridines

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

The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HTreceptors and modulating serotonin levels.

Cycloalkyfused indole, benzothiophene, benzofuran and idene derivatives

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

Compounds of the formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Antidepressant arylpiperazine derivatives of hetrocycle-fused benzodioxans

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.

The present invention provides novel tricyclic diazepine compounds and methods and pharmaceutical compositions utilizing them for the treating or preventing disorders including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, congestive heart failure or for inducing temporary delay of urination, and in conditions with increased vascular resistance and coronary vasoconstriction; and for the treating or preventing disorders remedied or alleviated by oxytocin antagonist activity, including suppression of preterm labor, dysmenorrhea, endometritis, and for suppressing labor at term prior to caesarean delivery. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Cyclohexenyl phenyl diazepines vasopressin and oxytocin receptor modulators

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Princeton Junction, NJ, United States of America

Amedeo A Failli