1,3,8-TRIAZA-SPIRO'4,5!DECAN-4-ONE DERIVATIVES AS NEUROKININ RECEPTOR ANTAGONISTS

摘要

The invention relates to compounds of the formula (I) wherein R<1> is hydrogen, lower alkyl, lower alkenyl, phenyl or the following groups -(CH2)m-non aromatic heterocyclyl, which is optionally substituted by lower alkyl, or is -(CH2)m-heteroaryl, which is optionally substituted by one or two substituents selected from the group consisting of lower alkyl, lower alkoxy, holgen, CF3, benzyl or cyano, or is -(CH2)m-C(O)-NRR', -(CH2)m-C(O)-lower alkyl, -(CH2)m-C(O)-O-lower alkyl, -(CH2)m-O-lower alkyl, -(CH2)m-CH[C(O)-O-lower alkyl]2, -(CH2)m-CH(OH)-CH2-O-phenyl, -(CH2)m-CH(CF3)OH, -(CH2)m-OH, -(CH2)m-CN, -(CH2)m-NRR', -(CH2)m-cycloalkyl or -(CH2)m-CHF2; R<2> is hydrogen, lower alkyl, halogen or lower alkoxy; R<3> is lower alkyl, lower alkoxy, halogen or CF3; R,R' are the same or different and are hydrogen or lower alkyl; X is > N-, > C = or > CH-; X<1>/X<2> are independently from each other hydrogen, hydroxy or lower alkoxy or may be together an oxo group; Y<1>/Y<2> are independently from each other hydrogen, lower alkyl, -(CH2)m-phenyl or may be together an oxo group; Z is a bond, -CH2- or -C(O)-; m is 0, 1, 2, 3 or 4; n is 2 or 3; n' 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.