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Activadores de PKM2 bicíclicos
专利权人:
Agios Pharmaceuticals; Inc.
发明人:
SALITURO, Francesco,SAUNDERS, Jeffrey
申请号:
ES11811257
公开号:
ES2569712T3
申请日:
2011.12.21
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Acceptable compound of formula (Ia) or pharmaceutically acceptable salt thereof, wherein: X and Y are each independently selected from O and N (-L-R1) each L is independently selected from a bond, -C (O) -, - (CRaRb) m-, -C (5 O) N (Rc) - or -C (O) O- A is aryl or heteroaryl each of which is substituted with 0-3 occurrences of Rd each R1 is independently selected from hydrogen, C1-4 alkyl, C1-4 haloalkyl, alkyl-O-alkylene, C3-10 cycloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl wherein each alkylene-O-alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl and heterocyclylalkyl is substituted with 0-3 occurrences of Rf and each alkyl and haloalkyl is substituted with 0-3 occurrences of Rg each Ra and Rb each independently selected from hydrogen, C1-4 alkyl, or Ra and Rb attached to the same carbon atom are taken together with the carbon atom to form a cycloalkyl each Rc is independently selected from hydrogen and C1-4alkyl each Rd is independently selected from halo, C1-4 haloalkyl, C1-4, nitro, cyano, -OH, and -O (C1-4 alkyl), or two Rd alkyl attached thereto carbon atoms or adjacent carbon atoms taken together with the / atom (s) to which they are attached form an optionally substituted heterocyclyl each Rf is independently selected from halo, C1-4 haloalkyl, C1-4, nitro, cyano, -OH, and -O (C1-4 alkyl), or two Rf alkyl attached thereto carbon atoms or adjacent carbon atoms taken together with the atoms to which they are attached form an optionally substituted heterocyclyl each Rg is independently selected from nitro, cyano, -OH, and -O (C1-4 alkyl) or two Rg, attached thereto carbon atoms or adjacent carbon atoms, taken together with the atoms to which they are attached form a optionally substituted heterocyclyl each R2 is independently selected from halo, C1-4 haloalkyl, C1-4 alkyl, C1-4 alkoxy and hydroxy h is 1, 2 or 3 each m is independently 1, 2 or 3 and each n is independently 0, 1, 2 or 3 provided th
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