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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 П. Джеффри (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),АЛЬКАСАР-ВАКА Мануэль Хесус
申请号:
RU2015101512
公开号:
RU2015101512A
申请日:
2013.06.19
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. The compound having the structure represented by the formula: or where R is 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 -C4 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 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, C1-C4 alkyl, C1-C4 monohaloalkyl, C1-C4 polyhaloalkyl, C1-C4 alkyloxy, hydroxy (C1 C4 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 R is selected from 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 Cy, if present, is selected from C3-C8 cycloalkyl, C2-C7 heterocycloalkyl, phenyl, monocyclic heteroaryl and bicyclic heteroaryl; and where Cy, if present, is substituted with 0,
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