| abstract |
The present invention relates to novel 1-heteroarylpyrrolidine, piperidine and monopiperidine derivatives, their preparation, intermediates used in their preparation, pharmaceutical compositions containing them, and their use in the preparation of pharmaceutical compositions. In the compounds of formula (I), X is an oxygen or sulfur atom or an amino group or an alkyl substituted imino group; R1, R2, R3 and R4 are each independently hydrogen, halogen, hydroxy or optionally substituted alkyl or alkoxy; A is optionally substituted alkylene; D is oxygen or sulfur; E is oxygen, sulfur or imino, N-alkyl or CR11R12; G is alkyl or alkenyl and in each case may be substituted; R 5 and R 6 each independently represent a hydrogen atom or an alkyl group or form a heterocyclic ring; R7 is hydrogen or alkyl, alkenyl, COR8, SO2R8, CONR9R10, CO2R8 or SO2NR9R10; R8 is cycloalkyl, alkenyl, aryl1 or optionally substituted alkyl; R 9 and R 10 independently of one another are hydrogen, alkenyl, cycloalkyl or optionally substituted alkyl; R11 and R12 are each independently hydrogen, aryl, alkenyl or alkyl; p is 0, 1 or 2; "aryl" means phenyl or naphthyl, each of which may be optionally substituted; "aryl" is phenyl, naphthyl or benzyl, each of which may be optionally substituted; "cycloalkyl" means a cycloalkyl group which may be optionally substituted; and het is a monocyclic or bicyclic heterocyclic group; provided that the compound is methyl-1- (5-chloro-2-benzoxazolyl) proline different. SHE |