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СОЕДИНЕНИЯ БЕНЗОКСАЗОЛИНОНА С ИЗБИРАТЕЛЬНОЙ АКТИВНОСТЬЮ В ПОТЕНЦИАЛ-ЗАВИСИМЫХ НАТРИЕВЫХ КАНАЛАХ
专利权人:
МЕРК ШАРП И ДОУМ КОРП. (US)
发明人:
ПЕРО Джозеф Е. (US),ЛЕМАН Ханна Д. Дж. Ф. (US),КЕЛЛИ Майкл Дж. III (US),ЧЖАО Ляньинь (US),РОССИ Майкл А. (US),ЛИ Даньсу (US),ГИЛБЕРТ Кевин Ф. (US),УОЛКЕНБЕРГ Скотт (US),МАЛХИРН Джеймс (US),ЛЕЙТОН Марк
申请号:
RU2015119635
公开号:
RU2015119635A
申请日:
2013.10.23
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. A compound of formula or a pharmaceutically acceptable salt thereof with a selective activity as blockers of sodium ion channel Na1.7: Formula A, wherein: a) Ryavlyaetsya -H, Calkilom, alkoxy, -CN or halo b) "Het" is 6-membered heteroaryl moiety containing up to three heteroatoms selected from N, S and O, linked via any ring atom of the aryl moiety, available for binding, and optionally substituted with one or more "ring system substituents" which are alkyl, aryl, heteroaryl, , aralkyl, alkylaryl , Aralkenyl, heteroaralkyl, alkylheteroaryl, heteroaralkenyl, hydroxy, hydroxyalkyl, alkoxy, aryloxy, aralkoxy, acyl, aroyl, halo, nitro, cyano, carboxy, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, alkylsulfinyl, arylsulfinyl, geteroarilsulfinil, alkylthio , arylthio, heteroarylthio, aralkylthio, geteroaralkiltio, cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, RRN-, RRN-alkyl-, RRNC (O) - and RRNSO-, wherein each of R Ryavlyaetsya independently: hydrogen, alkyl, aryl and aralkyl and c) Rya S THE aryl radical with one or more ring system substituents which are independently for each occurrence: (i) heterocyclenyl (Ii) tseterotsiklil (Iii) or geteropirazinil (Iv) aminoalkil.2. A compound according to Claim. 1 or a salt thereof, wherein Ryavlyaetsya aryl residue with at least one "substituent koltsevoysistemy", which is a C-heterocycloalkyl residue, containing up to three geteroatomov.3. A compound of formula A with selective activity as blockers of sodium ion channel Na1.7: Formula A, wherein: a) Ryavlyaetsya -H, Calkilom, alkoxy, -CN or halo b) "Het" is a moiety of the formula: wherein one of
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