发明名称 Compounds for the treatment of peripheral neuropathies
摘要 H:/fm/Interoven/NRPortbl/DCC/FMT/5580119_l.DOC-30/09/2013 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.
申请公布号 AU2013237657(A1) 申请公布日期 2013.10.24
申请号 AU20130237657 申请日期 2013.10.02
申请人 NOVARTIS AG 发明人 LEPPERT, DAVID;WALLSTROEM, ERIK;NUESSLEIN-HILDESHEIM, BARBARA
分类号 A61K31/397;A61K31/16;A61K31/195;A61K31/34;A61K31/401;A61K31/417;A61K31/42;A61K31/436;A61K31/452;A61K31/519;A61K31/52;A61K31/56;A61K31/675;A61K38/13;A61P25/00 主分类号 A61K31/397
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