发明名称 ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASEINHIBITORS
摘要 The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer bei ng 1 or 2; R1 and R2each independently represents hydrogen C1-4alkyl, NR9R10, C 1- 4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae, wherein said C6- 12cycloalkyl or monovalent radical may optionally be substituted with one, o r where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl , C1-4alkyloxy, hydroxy, nitro, NR5R6, C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het2 and NR7R8, and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R 5 and R6 each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R1 and R8 each independently represent hydrogen or C1- 4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or Cl- 4alkyloxycarbonyl; L represents C1-4alkyl; Het1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar2 represents phenyl, naphtyl or indenyl.
申请公布号 CA2508621(A1) 申请公布日期 2004.07.08
申请号 CA20032508621 申请日期 2003.12.16
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR;VANHOOF, GRETA CONSTANTIA PETER;GILISSEN, RONALDUS ARNODUS HENDRIKA JOSEPH;VAN DER VEKEN, LOUIS JOZEF ELISABETH;JAROSKOVA, LIBUSE;LINDERS, JOANNES THEODORUS MARIA;WILLEMSENS, GUSTAAF HENRI MARIA
分类号 A61K31/165;A61K31/335;A61K31/40;A61K31/44;A61P3/04;A61P3/10;C07C233/11;C07C233/14;C07C233/22;C07C233/23;C07C233/32;C07C233/41;C07C233/58;C07C235/36;C07C235/40;C07C237/20;C07C237/22;C07C255/41;C07C255/57;C07C271/22;C07D207/12;C07D207/26;C07D207/27;C07D209/08;C07D209/18;C07D213/56;C07D215/08;C07D215/48;C07D217/06;C07D217/26;C07D243/08;C07D257/04;C07D277/40;C07D277/48;C07D295/088;C07D295/092;C07D295/155;C07D295/185;C07D309/12;C07D311/58;C07D311/64;C07D317/60;C07D317/72;C07D333/24;C07D333/68;C07D335/06;(IPC1-7):C07C233/11 主分类号 A61K31/165
代理机构 代理人
主权项
地址