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COMPOUNDS FOR THE TREATMENT OF PERIPHERAL NEUROPATHIES
专利权人:
노파르티스 아게
发明人:
레퍼트, 다비드,발스트롬, 에릭,뉘슬레인-힐데스하임, 바바라
申请号:
KR1020117006165
公开号:
KR1016189060000B1
申请日:
2009.08.17
申请国别(地区):
KR
年份:
2016
代理人:
摘要:
The present invention relates to compounds of formula (A1) or (A2) for use in the treatment of dehydrative peripheral neuropathy, and N-oxide derivatives or prodrugs thereof, or a pharmacologically acceptable salt, solvate or hydrate thereof . <; Formula (A1) >; [In the above formula, A is COOR 5 , OPO (OR 5 ) 2 , PO (OR 5 ) 2, SO 2 OR 5 , POR 5 OR 5 or 1H-tetrazol-5-yl wherein R 5 is H or an ester- 1-6 alkyl), and; W is a bond, C 1-3 alkylene or C 2-3 alkenylene; Y is a C 6-10 aryl or C 2-9 heteroaryl group (e.g., C 3-9 heteroaryl), and halogen, OH, NO 2, C 1-6 alkyl, C 1-6 alkoxy; Halo-substituted C 1-6 alkyl and halo-optionally substituted with 1 to 3 radicals selected from 6alkoxy-substituted C 1; Z is selected from the following formula (I); (I) (Wherein the asterisk of Z has the formula Ia or formula Ib, each -C (R 3) (R 4 ) - , and represents the point of attachment between the A; R 6 is hydrogen and C 1- is selected from 6-alkyl; J 1 and J 2 are independently methylene, or S, O and NR 5 heteroatoms selected from and; wherein R 5 is hydrogen and C 1- is selected from 6 alkyl, any alkylene of Z are halo, hydroxy, C 1-6 may be further substituted by one to three radicals selected from alkyl or; or R 6 is attached to the carbon atom of Y may form a 5-to 7-membered ring); R 1 is C 6-10 aryl or C 2-9 heteroaryl group (e.g., C 3-9 heteroaryl) and, C 1-6 alkyl, C 6-10 aryl, C 6-10 aryl C 1-4 alkyl, C 3-9 heteroaryl, C 3-9 heteroaryl, C 1-4 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl, C 1-4 alkyl, C 3-8 heterocycloalkyl or C 3- it is optionally substituted with alkyl 4-8 heterocycloalkyl C 1; Wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl of R 1 is halogen, C 1-6 alkyl, C 1-6 alkoxy and halo-substituted -C 1-6 alkyl, -C 1-6 alkoxy group selected from <; / RTI >; R 2 is H, C 1-6 alkyl, halo-substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; R 3 and R 4 are each independently H, halogen, OH, C 1-6 alkyl, C 1-6 alkoxy or halo-substituted C 1-6
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