Wyeth

Other

Ligand Pharmaceuticals, Inc.

Puwen Zhang

Jay Edward Wrobel

Andrew Fensome

James Patrick Edwards

Lin Zhi

Todd Kevin Jones

Christopher Michael Tegley

Eugene Anthony Terefenko

Gary Sondermann Grubb

Jeffrey Curtis Kern

John W Ullrich

Lori L Miller

Reinhold H W Bender

Eugene John Trybulski

Edward George Melenski

Horace Fletcher, Iii

Mark A Collins

Marci C Koko

Arthur Attilio Santilli

Casey Cameron McComas

An Thien Vu

Andrew Q Viet

Stephen Todd Cohn

Paige Erin Mahaney

Joseph Peter Sabatucci

Diane Deborah Harrison

Michael Anthony Marella

Richard Winneker

Joel Adam Goldberg

Reinhold R W Bender

Gavin David Heffernan

William Jay Moore

Fei Ye

Richard Dale Coghlan

Charles William Mann

Richard Page Woodworth, Jr

Callain Younghee Kim

David John O'Neill

Reinhold Hw Bender

Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R, R, R, R, R, and Qare defined herein.

Cyclothiocarbamate derivatives as progesterone receptor modulators

The present invention is directed to substituted benzothiadiazinedioxide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

Substituted benzothiadiazinedioxide derivatives and methods of their use

The present invention is directed to substituted propylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Substituted propylamine derivatives and methods of their use

The present invention is directed to arylamino-arylpropanolamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Arylamino-arylpropanolamine derivatives and methods of their use

This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein Rand Rmay be single substituents or fused to form spirocyclic rings.

Indoline derivatives

The present invention is directed to aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

Aryl sulfamide derivatives and methods of their use

The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Benzothiadiazolylphenylalkylamine derivatives and methods of their use

This invention provides progesterone receptor modulators having the structure: wherein Rto R, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.

7-aryl 1,5-dihydro-4,1-benzoxazepin-2(3H)-one derivatives and their use as progesterone receptor modulators

The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Phenylaminopropanol derivatives and methods of their use

This invention provides compounds of Formula (I): wherein Rand Rare independent substituents or are fused to form spirocyclic rings; R, R, and Rare as defined herein; and Ris a substituted benzene ring or a substituted five or six membered heterocyclic ring having in its backbone 1, 2, or 3 heteroatoms including O, S, SO, SOor NR; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.

Cyclocarbamate derivatives as progesterone receptor modulators

Compounds of formula I, wherein R-Rand n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided.  Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R-R, R, and Rare defined herein. 

5-aryl-indan-1-one oximes and analogs useful as progesterone receptor modulators

Compounds having the structure of formula I are provided. In formula I, Ris H, OH, substituted or unsubstituted Cto Calkyl, Cto Cperfluoroalkyl, or COR; Ris H, substituted or unsubstituted Cto Calkyl, aryl, substituted or unsubstituted Cto Calkoxy, substituted or unsubstituted Cto Caminoalkyl; Rand Rare H, substituted or unsubstituted Cto Calkyl, Cto Cperfluoroalkyl, substituted or unsubstituted Cto Calkenyl, substituted or unsubstituted Cto Calkynyl, substituted or unsubstituted Cto Ccycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or Rand Rare fused to form spirocyclic rings; Ris NHR, OR, NHSOR, or OSOR; Q is O, S, NR, or CRR; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions 

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Audubon, PA, United States of America

Puwen Zhang