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NMDA-RECEPTOR ANTAGONISTS WITH NEUROPROTECTIVE ACTION

机译:具有神经保护作用的NMDA受体拮抗剂

摘要

Compounds, pharmaceutical compositions and methods for treating or preventing disorders associated with NMDA receptor activity, including neuropathic pain, stroke, brain injury, epilepsy, and associated neurological conditions or neurodegeneration, are provided. Compounds having the general formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof, are each provided where (L) -Ar is substituted or unsubstituted, mono- or bicyclic aryl or heteroaryl; W is a bond, alkyl or alkenyl; X is a bond, NR or O, and each of R and R is independently H, alkyl, alkenyl or aralkyl, or R and R together form a 5-8 membered ring; R-R are selected from certain substituents or carbonyl; Y is a bond, O, S, SO, SO, CH, NH, N (alkyl) or NHC (= O); and Z is OH, NRR, NRSO (alkyl), NRC (O) NRR, NRC (O) O (alkyl), NR-dihydrothiazole or NR-dihydroimidazole, or where Z can merge with Ar to form selected heterocycles.
机译:提供了用于治疗或预防与NMDA受体活性有关的疾病的化合物,药物组合物和方法,包括神经性疼痛,中风,脑损伤,癫痫症以及相关的神经疾病或神经变性。提供具有通式I的化合物或其药学上可接受的盐,酯,前药或衍生物,其中(L)-Ar是取代或未取代的单环或双环芳基或杂芳基; W是键,烷基或烯基; X为键,NR或O,且R 1和R 2各自独立地为H,烷基,烯基或芳烷基,或R 1和R 2一起形成5-8元环; R-R选自某些取代基或羰基; Y为键,O,S,SO,SO,CH,NH,N(烷基)或NHC(= O); Z为OH,NRR,NRSO(烷基),NRC(O)NRR,NRC(O)O(烷基),NR-二氢噻唑或NR-二氢咪唑,或其中Z可与Ar合并形成选定的杂环。

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