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N- (1- (substituted phenyl) ethyl) -9H-purine-6-amines as PI3K inhibitors
专利权人:
Incyte Holdings Corporation
发明人:
LI, Yun-Long,COMBS, Andrew P.,YUE, Eddy W.,MADUSKUIE JR., Thomas P.,SPARKS, Richard B.
申请号:
ES11811232
公开号:
ES2764848T3
申请日:
2011.12.19
申请国别(地区):
ES
年份:
2020
代理人:
摘要:
A compound of Formula I: ** (See formula) ** or a pharmaceutically acceptable salt thereof; wherein: Ar is ** (See formula) ** R1 is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; wherein said C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are each optionally substituted by 1, 2, 3, or 4 groups independently selected from halo, OH, CN, NR1aR2b, C1-6 alkoxy, and C1 -6 haloalkoxy; each R1a and R2b is independently selected from H and C1-6 alkyl; or any R1a and R2b together with the N atom to which they are attached form a 4-, 5-, 6- or 7-membered heterocycloalkyl group, which is optionally substituted with 1, 2, 3 or 4 substituents independently selected from C1-6 alkyl; R2 is selected from halo, CN, C1-6 alkyl, C1-6 haloalkyl, -L- (C1-6 alkyl), -L- (C1-6 haloalkyl), and -L- (C1-4 alkylene) n- Cy2 and - (C1-4 alkylene) n-Cy2; wherein said C1-6 alkyl in said C1-6 alkyl and -L- (C1-6 alkyl) is optionally substituted with 1, 2, 3 or 4 independently selected R2a groups; L is 0, NRB, S, S (O), S (O) 2, C (O), C (O) NRB, S (O) NRB, S (O) 2NRB, NRBC (O), NRBS (O ) and NRBS (O) 2; RA and RB are each independently selected from H and C1-6 alkyl; Cy2 is selected from C3-7 cycloalkyl, 4-7 membered heterocycloalkyl, phenyl and 5-6 membered heteroaryl; each of which is substituted with p independently selected R2a groups; where p is 0, 1, 2, 3, or 4; each R2a is independently selected from OH, NO2, CN, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, amino , C1-6 alkylamino, di (C1-6 alkyl) amino, thio, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, carbamyl, C1-6 alkylcarbamyl, di (C1-6 alkyl) carbamyl, carboxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonylamino, C1-6 alkylsulfonylamino, aminosulfonyl, C1-6 alkylaminosulfonyl, di (C1-6 alkyl) aminosulfonyl, aminosulfonylamino, C1-6 alkylaminosulfonylamino, di (C1-6 alkyl) aminosulfonylamino, aminocarbonylamino, C1-6 alkylamin
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