首页> 外国专利> Derivatives of the (3s, 4ar, 6s, 8ar) 6-phenylamino-1, 2, 3, 4, 4a, 5, 6, 7, 8, 8a-decahydro isoquinoline-3-carboxylic acid as excitatory amino acid receptor antagonists for the treatment of neurological disorders and neurodegenerative diseases

Derivatives of the (3s, 4ar, 6s, 8ar) 6-phenylamino-1, 2, 3, 4, 4a, 5, 6, 7, 8, 8a-decahydro isoquinoline-3-carboxylic acid as excitatory amino acid receptor antagonists for the treatment of neurological disorders and neurodegenerative diseases

机译:(3s,4ar,6s,8ar)6-苯基氨基-1、2、3、4、4a,5、6、7、8、8a-十氢异喹啉-3-羧酸的衍生物作为兴奋性氨基酸受体拮抗剂神经系统疾病和神经退行性疾病的治疗

摘要

The present invention provides novel compounds of Formula (I), or the pharmaceutically acceptable salts or prodrugs thereof, and methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine wherein R1 is H, CO2H, tetrazole, OH, or (C1-C4)alkyltetrazole; R2 is H, (C1-C6)alkyl, aryl, halo, CO2H, (C1-C6)alkyl-heterocycle, (C1-C6)alkyl-(substituted)heterocycle, (C1-C4)alkyl-N-SO2-aryl, NO2, NH2, CF3, or (C1-C6)alkoxy carbonyl, NSO2aryl; W, X, and Y each independently represent H, (C1,C6)alkyl, CO2H, halo, OH; heterocycle, substituted heterocycle, CF3, (CH2)nCO2H, (C1-C6)alkoxy, or (C1-C6)alkoxy carbonyl; or optionally, X and R2 together, along with the carbon atoms to which they are attached, form a fused-benzo group, or optionally, W and R1 together, along with the carbon atoms to which they are attached, form a fused-benzo group or a fused-triazole group; n is 0, 1, or 2, or a pharmaceutically acceptable salt or prodrug thereof.
机译:本发明提供了式(I)的新型化合物或其药学上可接受的盐或前药,以及用于治疗神经系统疾病和神经退行性疾病,特别是疼痛和偏头痛的方法,其中R 1为H,CO 2 H,四唑,OH或(C1- C4)烷基四唑; R 2是H,(C 1 -C 6)烷基,芳基,卤素,CO 2 H,(C 1 -C 6)烷基-杂环,(C 1 -C 6)烷基-(取代的)杂环,(C 1 -C 4)烷基-N-SO 2-芳基,NO 2,NH 2,CF 3或(C 1 -C 6)烷氧基羰基,NSO 2芳基; W,X和Y各自独立地代表H,(C 1,C 6)烷基,CO 2 H,卤素,OH;杂环,取代的杂环,CF 3,(CH 2)n CO 2 H,(C 1 -C 6)烷氧基或(C 1 -C 6)烷氧基羰基;或任选地,X和R 2连同它们所连接的碳原子一起形成稠合苯并基,或者任选地,W和R 1以及它们所连接的碳原子一起形成稠合苯并基。基团或稠合三唑基团; n为0、1或2,或其药学上可接受的盐或前药。

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