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New heteroarylamide derivatives that have antiandrogenic properties
专利权人:
Aranda Pharma Ltd
发明人:
RATILAINEN, Jari,KOISTINAHO, Milla,MUONA, Anu
申请号:
ES13703633
公开号:
ES2640119T3
申请日:
2013.01.11
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A heteroarylamide derivative having the formula (I) ** (See formula) ** and pharmaceutically acceptable N-oxides, stereoisomers and salts thereof; wherein R 'and R "are each independently selected from the group consisting of H and alkyl; z is an integer from 0 to 3; X is selected from the group consisting of O, S, S (O) , SO2, NR12, in which R12 is selected from the group consisting of H, alkyl, and COR, in which R is hydrogen or alkyl; CH2 and CO; or when z is 0, then X can be N and forms together with R11 a heterocyclic ring selected from the group consisting of morpholine, 1,2,4-triazole, imidazole and N-substituted imidazole; and R11, when it does not form a ring with X, as defined, is selected from the group that consists of alkyl, alkenyl, (per) haloalkyl, haloalkenyl, CN-alkyl and an aryl, heteroaryl, an aliphatic or heteroaliphatic ring, of 3-7-members optionally substituted with 1-5 substituents selected from the group consisting of alkyl, alkoxy , hydroxy, halogen, (per) haloalkyl, CN, NO2, COR, COOR, CONHR, NR2, NHCOCF3, NHCOR, NHCONHR, NHCOOR, OCONHR, NHSO2R, NHCSCH3, SR, SOR and SO2R, in which R is as defined above; RB is a heteroaromatic ring having 6 ring members and optionally substituted in one or more of the carbon atoms, in which 1 or 2 ring members are N atoms and the other ring members are carbon atoms, or RB is an optionally substituted phenyl group, the substituent (s) in RB being selected from the group consisting of alkyl, alkoxy, hydroxy, halogen, (per) haloalkyl, CN, NO2, COR, COOR, CONHR, NR2, NHCOCF3 , NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, in which R is as defined above; NHCSCH3, SR, SOR and SO2R, in which R is as defined; or, when RB is an optionally substituted phenyl group, then two adjacent substituents can also form with the carbon atoms to which a substituted or unsubstituted aliphatic, heteroaliphatic or heteroaromatic ring is attached; and RA is a heteroaromatic mono- or bicyclic ring system that has 6 to 10 ring members and is
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