Derivatives of 1,3,5 estra - (10), tetraeno 16 - 3 - substituted, procedures for their preparation, Pharmaceutical Preparations Containing them, and their use for preparing medicaments
ULRICH DR. BOTHE,MATTHIAS DR. BUSEMANN,OLIVER MARTIN DR. FISCHER,NAOMI DRA. BARAK,ANDREA DRA. ROGERI,TOBIAS DR. MARQUARDT,CHRISTIAN DR. STEGMANN
申请号：
ARP130102438
公开号：
AR092025A1
申请日:
2013.07.10
申请国别(地区):
AR
年份:
2015
代理人:
摘要：
They are inhibitors of AKR1C3 which is a multifunctional enzyme, especially useful in bleeding disorders and endometriosis. Claim 1: Compounds of the formula (1) wherein A is pyridin-3-yl, pyrimidin-5-yl, pyrimidin-4-yl, pyrazin-2-yl, pyridazin-4-yl, pyridazin-3-yl, optionally mono- or disubstituted with fluorine, chlorine, nitrile, hydroxyl, carboxyl, trifluoromethyl, pentafluoroethyl, methoxy, ethoxy, trifluoromethoxy, -OCH₂CF₃,-SO₂CH₃,-SO CH CH- (C 3DO) CH1. Lease of c83218331 and 83242431；-CH OH -C (CH) OH -CONH- (C 3DO) NHCH- (C 3DO) NHCH CH- (C 3DO) N (CH)-SO₂NH₂,-SO₂NHCH₃,-SO N (CH)R1 es-o-cr74919； r7495y-y, r74919 and r7495son, independent of each other,a. Hydrogen, methyl, ethyl, propyl, isopropyl, phenyl, 4-fluorophenil, 3-fluorophenil, 2-fluorophenil, ch83323-o-ch-83222 -；-Ch8322； - cf8323o r74919 and r7495n together - (ch832225) - 8345； - n = 2, 3, 4 or 5, or r7491 and r7495n together - Ch 832222222 -；-CH₂-NH-CH₂-,-CH -N (CH) -CH --CH CH -O-CH CH --CH CH -NH-CH CH --CH CH -N (CH) -CH CH --O-CR R -CR R -Y RR74966,R74977,R758484 is hydrogen or r74977；R758484 is hydrogen and r758080；R7496son, independent of each other,methyl, ethyl or together are - (CH₂) ₙ- with n = 2, 3, 4, 5 or are together -CH₂-O-CH₂- or -CH₂CH₂-O-CH₂CH₂-,O R758080,R74969 is hydrogen and r74977；R7584son, independent of each other,Methyl, ethyl, cf83238ch8322, or together - (ch8322) - 8345； - con n = 2, 3, 4, 5, ch8322； - o-ch8322； - ch8322 -；-CH CH -NH-CH CH --CH CH -N (CH) -CH CH --0-0-0-0-CH₂-NH-CH₂-,-CH -N (CH) -CH -O R74966,R74977,R758484 is hydrogen, r758080 is methyl, ethyl, trifluoromethyl or r758080；R74966,R758484 is hydrogen, r74977 is methyl, ethyl, trifluoromethyl, hydroxy, thyroid, trifluoromethyl, or r74966；R758484 is hydrogen and r758080；R7497son, independent of each other,-- y, c8322-y, cr7501； - cr688r8305； - r690-y, r7501；R688a,R83055,R690 is hydrogen, or r7501；R688a,R83055 is hydrogen, r690 is methyl, ethyl, trifluoroethane, or r83055；R690 is hydrogen and r75011,R688s
