发明名称 |
PYRROLIDINYL DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS |
摘要 |
The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein
n is 1 or 2;L represents 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;M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy;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;or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo;R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy;R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy;R5 represents hydrogen, C1-4alkyl or Ar2—C1-4alky-;R6 represents hydrogen, halo, C1-4alkyl or C1-4alkyoxy-;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;
for use as a medicine.
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申请公布号 |
US2015183735(A1) |
申请公布日期 |
2015.07.02 |
申请号 |
US201514656752 |
申请日期 |
2015.03.13 |
申请人 |
Janssen Pharmaceutica N.V. |
发明人 |
Jaroskova Libuse;Linders Joannes Theodorus Maria;Buyck Christophe Francis Robert Nestor;Van Der Veken Louis Jozef Elisabeth;Dimitrov Vladimir Dimtchev;Nikiforov Theo Teofanov |
分类号 |
C07D207/267;C07D405/06;C07D211/76;C07D207/26 |
主分类号 |
C07D207/267 |
代理机构 |
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代理人 |
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主权项 |
1. A compound having the formulaan N-oxide forms, a pharmaceutically acceptable addition salts or a stereochemically isomeric forms thereof, wherein
n is 1; L represents a C1-linker optionally substituted with one or two C1-4alkyl substituents M represents a C1-3alkanediyl linker R1 and R2 are taken together with the phenyl ring to which they are attached to form naphthyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2—C1-4alkyl-; R6 represents hydrogen, halo, C1-4alkyl or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphthyl wherein said phenyl and naphthyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl. |
地址 |
Beerse BE |