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ACETAMIDES D'ADAMANTYLE UTILES COMME INHIBITEURS DE LA DESHYDROGENASE 11-BETA HYDROXYSTEROIDE
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
LINDERS, JOANNES THEODORUS MARIA,WILLEMSENS, GUSTAAF HENRI MARIA,GILISSEN, RONALDUS ARNODUS HENDRIKA JOSEPH,BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR,VANHOOF, GRETA CONSTANTIA PETER,VAN DER VEKEN, LOUIS
申请号:
CA2508621
公开号:
CA2508621C
申请日:
2003.12.16
申请国别(地区):
CA
年份:
2013
代理人:
摘要:
The N-oxide forms, the pharmaceutically acceptable addition salts and thestereochemically isomeric forms thereof, wherein n represents an integer being1 or 2; R1 and R2each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which theyare attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may beabsent to form an unsaturated bond; R3 represents a C6-12cycloalkyl,preferably selected from cylo-octanyl and cyclohexyl or R3 represents amonovalent radical having one of the following formulae, wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, orwhere possible two, three or more substituents selected from the groupconsisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 orAr2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted withone or where possible two or more substituents selected from halo, C1-4alkyl,C1-4alkyloxy, hydroxy, nitro, NR5R6, C1-4alkyloxy substituted with one orwhere possible two, three or more substituents each independently selectedfrom hydroxycarbonyl, Het2 and NR7R8, and C1-4alkyl substituted with one orwhere possible two or three halo substituents, preferably trifluoromethyl; R5and R6 each independently represent hydrogen, C1-4alkyl, or C1-4alkylsubstituted 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 heterocycleselected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het2 representspiperidinyl, pyrrolidinyl or morpholinyl; Ar2 represents phenyl, naphtyl orindenyl.
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