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תולדות תיאזול ואזול, תכשירים רוקחיים המכילים אותן ושימושן בהכנת תרופות
专利权人:
PULMAGEN THERAPEUTICS (SYNERGY) LIMITED
发明人:
申请号:
IL18926708
公开号:
IL189267A
申请日:
2008.02.04
申请国别(地区):
IL
年份:
2013
代理人:
摘要:
Pharmaceutical compositions for inhalation comprising compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiritory tract diseases: wherein (i) R 1 is C 1 -C 6 -alkyl or hydrogen; and R 2 is hydrogen or a group -R 7 , -Z-Y-R 7 , -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 , -Z-NR 9 -C(O)O-R 7 , or -Z-C(O)-R 7 ; and R 3 is a lone pair, or C 1 -C 6 -alkyl; or (ii) R 1 and R 3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R 2 is a lone pair or a group -R 7 , -Z-Y-R 7 , -Z-NR 9 R 10 , -Z-CO-NR 9 R 10 , -Z-NR 9 -C(O)O-R 7 ; or; -Z-C(O)-R 7 ; or (iii) R 1 and R 2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group -Y-R 7 , -Z-Y-R 7 , -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 ; -Z-NR 9 -C(O)OR 7 ; or; -Z-C(O)-R 7 ; and R 3 is a lone pair, or C 1 -C 6 -alkyl; R 4 and R 5 are independently selected from the group consisting of aryl, aryl-fused-heterocycloalkyl, heteroaryl, C 1 -C 6 -alkyl, cycloalkyl; R 6 is -OH, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, hydroxy-C 1 -C 6 -alkyl, nitrile, a group CONR 8 2 or a hydrogen atom; A is an oxygen or a sulfur atom; X is an alkylene, alkenylene or alkynylene group; R 7 is an C 1 -C 6 -alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C 1 -C 8 -alkyl)-, heteroaryl(C 1 -C 8 -alkyl)-, cycloalkyl or heterocycloalkyl group; R 8 is C 1 -C 6 -alkyl or a hydrogen atom; Z is a C 1 -C 16 -alkylene, C 2 -C 16 -alkenylene or C 2 -C 16 -alkynylene group; Y is a bond or oxygen atom; R 9 and R 10 are independently a hydrogen atom, C 1 -C 6 -alkyl, aryl, aryl-fused-heterocycloalkyl, aryl-fused-cycloalkyl, heteroaryl, aryl(C 1 -C 6 -alkyl)-, or heteroaryl(C 1 -C 6 -alkyl)- group; or R 9 and R 10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 4-8 atoms, opti
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