| 摘要 |
A compound of formula (I) is described wherein L is CH or N; M is CH or N; provided that L and M are not both CH; R1 is hydrogen, C1-6 alkyl (optionally substituted) and when M is CH R1 can also be NHS(O)2R6, NHS(O)2NHR7, NHC(O)R7 or NHC(O)NHR7; R2 is phenyl or heteroaryl, either of which is optionally substituted; R3 is hydrogen or C1-4 alkyl; R4 is hydrogen, methyl, ethyl, allyl or cyclopropyl; R5 is phenyl, heteroaryl, phenylNH, heteroarylNH, phenyl(C1-2)alkyl, heteroaryl(C1-2)alkyl, phenyl(C1-2 alkyl)NH or heteroaryl(C1-2 alkyl)NH; wherein the phenyl and heteroaryl rings of R5 are optionally substituted; R6 is C1-6 alkyl (optionally substituted); R7 is hydrogen, C1-6 alkyl (optionally substituted); R8 and R9 are, independently, hydrogen or C1-4 alkyl, or together with a nitrogen or oxygen atom, may join to form a 5- or 6-membered ring which is optionally substituted with C1-4 alkyl; C(O)H or C(O)(C1-4 alkyl); R10 and R11 are, independently, hydrogen or C1-4 alkyl, or may join to form a 5- or 6- membered ring which is optionally substituted; or a pharmaceutically acceptable salt thereof or a solvate thereof. A proviso explains that when R1 is hydrogen or unsubstituted alkyl, R4 is hydrogen, methyl or ethyl, L is CH and M is N, then the phenyl or heteroaryl part of R5 is substituted by one of: S(O)kC1-4 alkyl, NHC(O)NH2, C(O)(C1-4 alkyl), CHF2, CH2F, CH2CF3 or OCF3, and optionally further substituted. Processes for preparing the compound of formula (I) are also described. One process is described to involve coupling an intermediate of formula (V), which is also claimed, with an acid. The compound is described to be used in the manufacture of a composition for treating a CCR5 mediated disease state.
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