380201-68-3Relevant articles and documents
Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
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, (2008/06/13)
The invention relates to compounds of the formula wherein R1 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, halogen, 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)mCH(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; R2 is hydrogen, lower alkyl, halogen or lower alkoxy; R3 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—; X1/X2 are independently from each other hydrogen, hydroxy or lower alkoxy or may be together an oxo group; Y1/Y2 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.
