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Aminoalkyl-quinazolones substituted with pyrimidine as phosphatidylinositol 3-kinase inhibitors
专利权人:
Gilead Calistoga LLC
发明人:
EVARTS, Jerry,PATEL, Leena,TREIBERG, Jennifer,PERREAULT, Stephane,YEUNG, Arthur,PURVIS, Lafe,KIM, Musong
申请号:
ES13821357
公开号:
ES2677919T3
申请日:
2013.12.20
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound having the structure of Formula (II): ** Formula ** or a pharmaceutically acceptable salt or solvate thereof, wherein: R1 is: unsubstituted aryl; unsubstituted heteroaryl; unsubstituted cycloalkyl; unsubstituted alkyl; aryl, heteroaryl, or cycloalkyl substituted with 1 or 2 substituents independently selected from the group consisting of halo, -OR1a, -C (O) OR1a, -C (O) R1a, NH2, alkyl, haloalkyl, and C1-6 substituted alkyl with OH or NH2, where R1a is H, alkyl, haloalkyl, NH2, or -O (C1-6 alkyl); or alkyl substituted with OH; n is 0, 1, 2 or 3; each R2 is independently halo, OH, CN, haloalkyl, unsubstituted alkyl, alkyl substituted with 1 to 5 substituents selected from hydroxyl, haloalkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, amino, cyano, halo, and carboxyl, or R2 it is SO2R2a, where R2a is alkyl; R3 is: unsubstituted aryl or aryl substituted with 1 to 5 substituents selected from halo, OR, -C (O) NR2, -SO2NR2, alkyl, haloalkyl, heterocycloalkyl, heteroaryl, alkoxy, amino, cyano, and carboxyl, where each R it is independently selected from hydrogen, alkyl, and haloalkyl; unsubstituted heteroaryl or heteroaryl substituted with 1 to 5 substituents selected from alkyl, haloalkyl, halo, NH2, OR, -C (O) OR, heterocycloalkyl, aryl, and cyano, where each R is independently selected from hydrogen, alkyl, and haloalkyl ; unsubstituted heterocycloalkyl or heterocycloalkyl substituted with 1 to 5 substituents selected from alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, alkoxy, amino, cyano, halo, carboxyl, and hydroxyl; or R3 is: C6-12 unsubstituted aryl; C6-12 aryl substituted with 1 or 2 substituents independently selected from the group consisting of halo, alkyl, haloalkyl, aryl, cyano, -OR3a, -C (O) NR3aR3b, -SO2R3a, -SO2NR3aR3b, and alkyl substituted with NR3aR3b, in where R3a and R3b are independently hydrogen, C1-6 alkyl, or -SO2R3c, wherein R3c is alkyl; C3-12 heteroaryl not substituted with 1 or 2 heteroatoms independently selected fr
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