Wyeth

Other

Ligand Pharmaceuticals, Inc.

Mark A Collins

James Patrick Edwards

Lin Zhi

Todd Kevin Jones

Jay Edward Wrobel

Christopher Michael Tegley

Valerie A Mackner

Andrew Fensome

Puwen Zhang

Eugene Anthony Terefenko

Syed Muzafar Shah

Panolil C Raveendranath

Gary Sondermann Grubb

Michael Z Kagan

Leonard Alexander McDonald

Fangming Kong

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

This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein, T is O, S, or absent; R, and Rare each, independently, hydrogen, alkyl, substituted alkyl; or Rand Rare taken together form a ring and together contain &#x2014;CH(CH)CH&#x2014;, &#x2014;CHCHCMeCHCH&#x2014;, &#x2014;O(CH)CH&#x2014;, &#x2014;O(CH)O&#x2014;, &#x2014;CHCHOCHCH&#x2014;, or &#x2014;CHCHNRCHCH&#x2014;; n=1-5; p=1-4; q=1-4; Ris hydrogen, OH, NH, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or COR; Ris hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; Ris hydrogen, halogen, CN, NH, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; Ris hydrogen, alkyl, or substituted alkyl; Ris hydrogen, alkyl, substituted alkyl, or COR; Ris hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; Ris hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.

Cyanopyrroles

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 Rand Rare selected from the group of H, optionally substituted Cto Calkyl, alkenyl, alkynyl, or alkynyl groups Cto Ccycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORor NRCOR; or Rand Rare fused to form an optionally substituted ring structure as defined herein; Rand Rare as defined herein; Ris H, OH, NH, COR, or optionally substituted Cto Calkyl, Cto Calkenyl, or alkynyl groups; Ris as defined herein; Qis S, NR, or CRR; Ris an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring.

This invention provides a progesterone receptor antagonist of formula 1 having the structurewherein T is O, S, or absent; R, and Rare each, independently, hydrogen, alkyl, substituted alkyl; or Rand Rare taken together form a ring and together contain &#x2014;CH(CH)CH&#x2014;, &#x2014;CHCHCMeCHCH&#x2014;, &#x2014;O(CH)CH&#x2014;, &#x2014;O(CH)O&#x2014;, &#x2014;CHCHOCHCH&#x2014;, or &#x2014;CHCHNRCHCH&#x2014;;

This invention provides estra-5(10),7-dien-3&bgr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&agr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&bgr;-ol-17-one 3-alkali metal salt, and estra-5(10),7-dien-3&agr;-ol-17-one 3-alkali metal salt which are useful as estrogenic agents.

Estradienes

2,1-benzisothiazoline 2,2-dioxides

This invention relates to cyclic combination therapies utilizing, in combination with a progestin, an estrogen, or both, progesterone receptor antagonists of the general structure:

Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides

Growing community of inventors

Norristown, PA, United States of America

Mark A Collins