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作為11-β羥基類固醇去氫酶抑制劑之金鋼烷基吡咯啶-2-酮衍生物
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
JAROSKOVA, LIBUSE,贾诺可,賈諾可,LINDERS, JOANNES THEODORUS MARIA,林德斯,BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR,布克,VAN DER VEKEN, LOUIS JOZEF ELISABETH,樊德肯
申请号:
TW094114610
公开号:
TWI357896B
申请日:
2005.05.06
申请国别(地区):
TW
年份:
2012
代理人:
摘要:
the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl-, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl-; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy-optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, hydroxy, cyano or C1-4alkyloxy-optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, C1-4alkyl or Ar2—C1-4alkyl-; R6 represents hydrogen, hydroxy, halo, C1-4alkyl or C1-4alkyoxy-; R7 represents hydrogen or R7 and R5 taken together with the carbon atom to which they are attached from a —C2-alkyl-linker; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl.其N-氧化物形式、醫藥可接受之加成鹽類及立體化學異構形式,其中n是1或2;M代表一個直接鍵結或C1-3烷基聯結,視情況以一或兩個選自C1-4烷基、C1-3烷基氧基-C1-4烷基-、羥基-C1-4烷基-、羥基、C1-3烷基氧基-或苯基-C1-4烷基的取代基取代;R1及R2各獨立代表氫、鹵基、氰基、羥基、視情況鹵基取代之C1-4烷基、C1-4烷基氧基-,視情況以一個或可能處兩或三個選自羥基、Ar1及鹵基的取代基取代;R3代表氫、鹵基、C1-4烷基、C1-4烷基氧基-、氰基或羥基;R4代表氫、鹵基、C1-4烷基、羥基、氰基或C1-4烷基氧基-,視情況以一個或可能處兩或三個選自羥基及鹵基的取代基取代;R5代表氫、C1-4烷基或Ar2-C1-4烷基-;R6代表氫、羥基、鹵基、C1-4烷基或C1-4烷基氧基-;R7代表氫、或R7及R5與附於其上之碳原子一起形成一個-C2-烷基聯結;Ar1及Ar2各獨立代表苯基或萘基,其中該苯基及萘基視情況以C1-4烷基、C1-4烷基氧基-或苯基C1-4烷基取代。
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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