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2. 发明申请

US20100113540A1 Azole and Thiazole Derivatives and Their Use 审中-公开
公开(公告)号：US20100113540A1
公开(公告)日：2010-05-06
申请号：US12063216
申请日：2006-08-08
申请人： Nicholas Charles Ray , Richard James Bull , Harry Finch , Marco van den Heuvel , Jose Antonio Bravo
发明人： Nicholas Charles Ray , Richard James Bull , Harry Finch , Marco van den Heuvel , Jose Antonio Bravo
IPC分类号： A61K31/421 , C07D263/32 , A61P9/00 , A61P11/06 , A61P13/00
CPC分类号： C07D263/32 , C07D277/28 , C07D413/06 , C07D413/12
摘要： Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiratory tract diseases: wherein (i) R1 is C1-C6-alkyl or hydrogen; and R2 is hydrogen or a group —R7, —Z—Y—R7, —Z—NR9R10; —Z—CO—NR9R10, —Z—NR9—[AE11]C(O)O—R7, or —Z—C(O)—R7; and R3 is a lone pair, or C1C6-alkyl; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring and R2 is a lone pair or a group —R7, —Z—Y—R7, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—[AE12]C(O)O—R7; or; —Z—C(O)—R7; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R7, —Z—Y—R7, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—[AE13]C(O)O—R7; or; —Z—C(O)—R7; and R3 is a lone pair, or C1-C6-alkyl; R4 and R5 are independently selected from the group consisting of aryl, ary-tfused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl; R6 is —OH, C1-C6-alkyl, C1-C6-alkoxy, hydroxy-C1-C6-alkyl, nitrile, a group CONR82 or a hydrogen atom; A is an oxygen or a sulfur atom; X is an alkylene, alkenylene or alkynylene group; R7 is an C1-C6-alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group; R8 is C1-C6-alkyl or a hydrogen atom; Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R9 and R10 are independently a hydrogen atom, C1-C6-alkyl, aryl, aryl-fused-heterocycloalkyl, aryl-fused-cycloalkyl, heteroaryl, aryl(C1-C6-alkyl)-, or heteroaryl(C1-C6-alkyl)- group; or R9 and R10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 48 atoms, optionally containing a further nitrogen or oxygen atom.

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