| 摘要 |
Substituted piperazinone derivatives of formula (1) are tachykinin receptor antagonists and may be used in medicaments for the treatment of tachykinin-mediated diseases and other conditions such as asthma, cough and bronchitis. In formula (1); G1 is CH2 or C(O); Ar1 is a radical chosen from the group depicted in (2) and (3) above, wherein Z1 is 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF3, C1-C4 alkyl and C1-C4 alkoxy; R1 is hydrogen, a radical of the formula (4) depicted above, (CH2)qAr2 or CH2C(O)Ar2, wherein q is an integer from 1 to 4 and Ar2 is selected from the group depicted in (5) or (6) above, wherein Z2 is 1 to 3 substituents each independently chosen from the group consisting of hydrogen, halogen, benzyloxy, hydroxy, CF3, C1-C4 alkyl, and C1-C4 alkoxy R2 is hydrogen, C1-C4 alkyl, or CHO; and R3 is hydrogen or a radical chosen from same options as Ar1. An intermediate formed in the process of making compounds of formula (1) is depicted in formula (7). In formula (7); R2, R3 and Ar1 are as defined above, R5 is hydrogen, benzyl or C1-C4 alkyl; and R6 is hydrogen or C(O)OR7, wherein R7 is benzyl or C1-C4 alkyl.
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