Trisubstituted thiophenes as progesterone receptor modulators

Details Trisubstituted thiophenes as progesterone receptor modulators Trisubstituted thiophenes as progesterone receptor modulators

2005-10-21

2009-12-29

Chang, Celia (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S326000, C546S171000, C546S193000, C546S212000

Reexamination Certificate

active

07638525

ABSTRACT:
The present invention is directed to novel trisubstituted thiophene derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical usage of these compounds are related to hormonal contraception, the treatment and/or prevention of secondary dysmenorrhea, amenorrhea, dysfunctional uterine bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon or prostate. Additional uses of the invention include stimulation of food intake.

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Noack, A. et al.: “Synthesis and characterisation ofN,N-disubstituted 2-amino-5-acylthiophenes and 2-amino-5-acylthiazoles”; Tetrahedron 58 (2002) pp. 2137-2146.
Liebscher, Jurgen: “Reactions of 3-Amino and 3-Hydroxythioacrylamides with Alkylating Reagents-Synthesis of N,N-Disubstituted 2-Aminothiophenes”, Journal f. prakt. Chemie. Band 325, Heft 1, 1983, S. 168-172.
PCT International Search Report for Int'l Appln. No. PCT/US2005/037827 dated Mar. 8, 2006.

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