PL377501A1

Adamantyl acetamides as 11-beta hydroxysteroid dehydrogenase inhibitors

Abstract

N-oxide forms, pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is an integer of 1 or 2; R1 and R2 are each independently hydrogen, C1-4alkyl, NR9R10, C3-6alkyloxy; or R1 and R2 together with the carbon atom to which they are attached form C3-6cycloalkyl; and wherein n is 2, or R1 or R2 may be absent to give an unsaturation; R3 is C6-12cycloalkyl, preferably selected from cylooctanyl and cyclohexyl, or R3 is a monovalent radical having one of the following formulas, said C6-12cycloalkyl or monovalent radical being optionally substituted by one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halogen or hydroxyl; Q is Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halogen, 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 halogen atoms, preferably trifluoromethyl; R5 and R6 are each independently hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R1 and R8 are each independently hydrogen or C1-4alkyl; R9 and R10 are each independently hydrogen, C1-4alkyl or C1-4alkyloxycarbonyl; L is C1-4alkyl; Het1 is a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het2 is piperidinyl, pyrrolidinyl or morpholinyl; Ar2 is phenyl, naphthyl or indenyl.

Term

Term ended

Projected expiry passed 16 December 2023, 2.8 years ago.

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0214832European Patent Office (EPO)W
0214832European Patent Office (EPO)W
PCTEP0214832
WO2002EP14832

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