17-HYDROXY-17-PENTAFLUOROETHYL-ESTRA-4,9(10)-DIEN-11-ARYL DERIVATIVES, METHOD OF PRODUCTION THEREOF AND USE THEREOF FOR TREATMENT OF DISEASES

• Main Authors: WOLFGANG SCHWEDE, ANDREA ROTGERI, CARSTEN MOLLER, ULRICH KLAR, WILHELM BONE
• Format: Patent
• Language: English; Japanese
• Published: 08.10.2015
• Subjects: CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY; STEROIDS

PROBLEM TO BE SOLVED: To provide production of very potent competitive progesterone receptor antagonists available.SOLUTION: Compounds of Formula (I): wherein Ris a residue Y or a phenyl ring once or twice substituted with the residue Y; Y is selected from SRetc.; Ris H, C-C-alkyl, C-C-aralkyl or aryl; Ris C-C-alkyl or aryl; Ris S(O)R; Ris phenyl or 4-methylphenyl; X is O, NOR, NNHSOR; Ris H, C-C-alkyl or aryl; Rand Rare independently H, C-C-alkyl, aryl or 3- to 8-membered saturated/unsaturated heterocyclic ring. 【課題】利用可能な非常に強力な競合的プロゲステロン受容体拮抗薬の製造。【解決手段】一般式（I）の化合物：（R1は残基Yか、残基Yで12置換されたフェニル環；YはSR2等から選択され；R2はＨ、C1〜C6-アルキル、C7〜C10-アラルキル又はアリール；R3は、C1〜C6-アルキル又はアリール；R4はS(O)2R6基；R6はフェニル又は4-メチルフェニル；XはＯ、NOR7、NNHSO2R7；R7はＨ、C1〜C10-アルキル又はアリール；R9及びR10は各々独立に、Ｈ、C1〜C10-アルキル、アリール又は3〜8員の飽和／不飽和の複素環）。【選択図】なし