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Compounds for the treatment of peripheral neuropathies
专利权人:
Novartis AG
发明人:
LEPPERT, David,WALLSTROEM, Erik,NUESSLEIN-HILDESHEIM, Barbara
申请号:
AU2013237657
公开号:
AU2013237657A1
申请日:
2013.10.02
申请国别(地区):
AU
年份:
2013
代理人:
摘要:
#$%^&*AU2013237657A120131024.pdf#####H:\fm\Interoven\NRPortbl\DCC\FMT\5580119_l.DOC-30/09/2013 ABSTRACT A compound of formula Al or A2 for use in the treatment of a demyelinating peripheral neuropathy: wherein A is COOR5 , OPO(OR5 )2, PO(OR5 )2, S0 20R 5 , POR5OR5 or 1 H-tetrazol-5-yl, R5 being H or an ester-forming group, optionally C1. 6alkyl W is a bond, C1-3alkylene or C2-3alkenylene Y is C6o1aryl or C2-gheteroaryl eg C3-gheteroaryl, optionally substituted by 1 to 3 radicals selected from halogen, OH, NO2, C1.6 alkyl, C1.6alkoxy halo-substituted C1.6 alkyl and halo-substituted C1.6alkoxy Z is chosen from Formula (I) : wherein the asterisks of Z indicate the point of attachment between -C(R 3)(R4)- and A of Formula (la) or (Ib), respectively R6 is chosen from hydrogen and C1.6 alkyl and J1 and J2 are independently methylene or a heteroatom chosen from S, 0 and NR5 wherein R5 is chosen from hydrogen and C1.6 alkyl and any alkylene of Z can be further substituted by one to three radicals chosen from halo, hydroxy, C1.6alkyl or R6 can be attached to a carbon atom of Y to form a 5-7 member ring R1 is C6o1aryl or C2-gheteroaryl eg C3-gheteroaryl, optionally substituted by C1. 6alkyl, C6-1oaryl, C61 oarylC1 .4alkyl, C3-gheteroaryl, C3-gheteroarylC1 .4alkyl, C3-8cycloalkyl, C3-8cycloalkylC1 .4alkyl, C38-heterocycloalkyl or C3.8heterocycloalkylC1. 4alkyl wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl of R1 may be substituted by 1 to 5 groups selected from halogen, C1.6 alkyl, C1.6alkoxy and halo substituted-C1 6 alkyl or -C1.6alkoxy R2 is H, C1.6 alkyl, halo substituted C1.6 alkyl, C2-6alkenyl or C2-6alkynyl and each of R3 and R4 , independently, is H, halogen, OH, C1.6 alkyl, C1.6 alkoxy or halo substituted C1.6 alkyl or C1.6 alkoxy and the N-oxide derivatives thereof or prodrugs thereof, or a pharmacologically acceptable salt, solvate or hydrate thereof.
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