PYRAZOLE DERIVATIVES AS PROGESTERONE RECEPTOR ANTAGONISTS

2006
OA: closed

Abstract

Compounds of formula (I), or pharmaceutically acceptable derivatives thereof , wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het R3 represents OH, CN, Het, -R4- C1-6alkyl, or CONR5R6 R4 represents ~CO2-, or ~O- R5 and R6 independently represent H, C 1- 6alkyl (optionally substituted by OR7) or C3-8cycloalkyl R7 represents H or C1-6alkyl Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom (s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelv ic pain syndrome.

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europepmc
last seen: 2026-07-08T06:14:57.058073+00:00