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SUBSTITUTED Bicyclic Alcohol-Pyrazole Analogs as Allosteric Modulators of MGLUR5 Receptors
专利权人:
ВАНДЕРБИЛТ ЮНИВЕРСИТИ (US)
发明人:
КОНН Джеффри П. (US),ЛИНДСЛИ Крейг У. (US),СТОФФЕР Шон Р. (US),БАРТОЛОМЕ-НЕБРЕДА Хосе Мануэль (ES),МАКДОНАЛЬД Грегор Джеймс (BE),КОНДЕ-СЕЙДЕ Сусана (ES),ТУН Хань Минь (ES),ПЕНА-ПИНЬОН Мигель Анхель (E
申请号:
RU2015101532
公开号:
RU2015101532A
申请日:
2013.06.19
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. A compound having a structure represented by the formula: wherein R 1 represents aryl or heteroaryl and is substituted with 0, 1, 2 or 3 groups, each of which is independently selected from cyano, halogen, hydroxyl, C1-C4 alkyl, C1-C4 alkyloxy, C1-C4 monohaloalkyl and C1-C4 polyhaloalkyl; where each of R and R is independently selected from hydrogen and C1-C4 alkyl; where R is selected from hydrogen, halogen, cyano, C1-C4 alkyl, C1-C4 monohaloalkyl and C1-C4 polyhaloalkyl; where each of R and R is selected from hydrogen, halogen, -C4 alkyl, C1-C4 monohaloalkyl, C1-C4 polyhaloalkyl, C1-C4 alkyloxy, hydroxy (C1-C4a alkyl) and (C1-C4alkyloxy) - (C1-C4alkyl) -; or R and R are covalently bonded and, together with the intermediate carbon atom, form an optionally substituted 3-7 membered spirocycloalkyl; where each of R and R is selected from hydrogen, halogen, C1-C4 alkyl, C1-C4 monohaloalkyl, C1-C4 polyhaloalkyl, C1-C4 alkyloxy, hydroxy ( C1-C4alkyl) and (C1-C4alkyloxy) - (C1-C4alkyl) -; or R5a and R5b are covalently linked and, together with the intermediate carbon atom, form an optionally substituted 3-7 membered spirocycloalkyl; where R is selected from hydrogen, C1-C8 alkyl, C1-C8 monohaloalkyl, C1-C8 polyhaloalkyl, hydroxy (C1-C8 alkyl), (C1 -C6 alkyl) -O- (C1-C6 alkyl) -, (C1-C6 monohaloalkyl) -O- (C1-C6 alkyl) -, (C1-C6 polyhaloalkyl) -O- (C1-C6 alkyl) -, (C1-C6 alkyl) -NH - (C1-C6 alkyl) -, (C1-C6 alkyl) (C1-C6 alkyl) N- (C1-C6 alkyl) -, Cy, Cy- (C2-C6 alkyl) - and Cy-C (R) (R) - ; where Su, if present, is selected from C3-C8 cycloalkyl, C2-C7 heterocycloalkyl, phenyl, monocyclic heteroaryl and bicyclic heteroaryl; and where Su, if present, is substituted with 0, 1, 2 or 3 groups, each of which is independently selected from halogen, cyano, —NH, mono (C1-C6 alkyl) amino, di (C1-C6 alkyl) amino, C1-C4 alkyl , C1-C4alkyloxy, (C1-C4alkyloxy) - (C1-4alkyl) -, (C1-C4alkyloxy) - (C1-C4alkyloxy) -, C1-C4monohaloalkyl, C1-C4 polyhaloalkyl, (C1-C4 polyhaloalkyl) - (C1-
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