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New derivatives of N- (4- (azetidine-1-carbonyl) phenyl) - (hetero-) arylsulfonamide as modulators of pyruvate kinase M2 (PKM2)
专利权人:
Agios Pharmaceuticals; Inc.
发明人:
SALITURO, Francesco G.,SAUNDERS, Jeffrey O.,YAN, Shunqi
申请号:
ES11808773
公开号:
ES2564952T3
申请日:
2011.12.16
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of formula (I): ** Formula ** or a pharmaceutically acceptable salt thereof, where: A is aryl or heteroaryl, where aryl or heteroaryl is optionally substituted and aryl or heteroaryl is optionally fused to an optionally substituted carbocyclyl or an optionally substituted heterocyclyl; X is selected from -NH-S (O) 2-, -N (alkyl) -S (O) 2-, -S (O) 2-N (H) - and -S (O) 2-N (alkyl ) -; R1a is selected from hydrogen, alkyl and arylalkyl; and R1b is selected from OR3, N (alkyl) R3 and NHR3; or R1a is alken-1-yl and R1b is absent; each R2 is independently selected from halo, haloalkyl, alkyl, alkoxy and hydroxyl; R3 is selected from hydrogen, alkyl, optionally substituted aryl, optionally substituted heteroaryl, arylalkyl, C (O) Ra and C (O) N (H) Ra, where Ra is selected from alkyl, alkenyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl ; and where any portion of aryl or heteroaryl of Ra is optionally substituted; each R4 is independently selected from haloalkyl, alkyl, alkoxy and hydroxyl; n is 0, 1, or 2; m is 0, 1, or 2; where: "alkyl" refers to a C1-C12 monovalent hydrocarbon chain which may be a straight chain or a branched chain, containing the indicated number of carbon atoms; "haloalkyl" refers to an alkyl in which one or more hydrogen atoms are replaced by halo; "alkenyl" refers to a straight or branched C2-C12 monovalenate hydrocarbon chain containing 2-12 carbon atoms and having one or more double bonds; "alkoxy" refers to a radical -O-alkyl; "aryl" refers to a system of aromatic, monocyclic, bicyclic, tricyclic hydrocarbon rings; "arylalkyl" refers to an alkyl portion in which an alkyl hydrogen atom is replaced by an aryl group; "carbocyclyl" refers to a non-aromatic, monocyclic, bicyclic or tricyclic hydrocarbon ring system. "heteroaryl" refers to a system of completely aromatic monocyclic rings of 5 to 8 members, bicyclic of 8 to 12 members or tricyclic of 11 to 14 members that has 1 to 3 heteroatoms if they are monocyclic, 1 to 6 heteroatoms i
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