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Quinazolines substituted with sulfoximine for pharmaceutical compositions
专利权人:
Evotec International GmbH
发明人:
KLEY, Joerg,BLUM, Andreas,GOTTSCHLING, Dirk,HEHN, Joerg P.,WIEDENMAYER, Dieter,KLEY JOERG,BLUM ANDREAS,GOTTSCHLING DIRK,HEHN JOERG P,WIEDENMAYER DIETER
申请号:
ES14808895
公开号:
ES2693520T3
申请日:
2014.11.28
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of Formula ** Formula ** wherein Ar is ** Formula ** wherein X is CH or N; R3 is H, halogen, CN or -C (>; = O) -NH2; and R4 is ** Formula ** wherein ---- is a single or double bond; n is 0 or 1; And it is O or NRN1; RN1 is selected from the group consisting of H, C1-3 alkyl, -C (O) -C1-3 alkyl, -C (O) -O- (CH2) 1-3-phenyl, and -SO2-C1- alkyl 3; R7 is selected from the group consisting of F, CN, OH, -O- (C1-3 alkyl), -O- (CH2) 1-3- (C3-7 cycloalkyl), -O- (CH2) 1- 3-phenyl, -O-oxetanyl and -OC (O) -C 1-4 alkyl; and R9 is H or R9 together with R7 form -CH2- or - (CH2) 2-; wherein each alkyl group mentioned in the definition of RN1 and R7 is optionally substituted with one or more of F u-O- (C1-3 alkyl); R1 is ** Formula ** wherein R5 is selected from a group consisting of C1-5 alkyl, C2-3 alkenyl, C2-3 alkynyl, C3-7 cycloalkyl, heterocyclyl, heteroaryl and aryl, wherein each group R 5 alkyl is optionally substituted with one or more of F or with an -O- (C 1-3 alkyl), -O-C 3-7 cycloalkyl, -O-heterocyclyl, C 3-7 cycloalkyl, heterocyclyl or phenyl; and R6 is C1-3 alkyl which is optionally substituted with one or more of F, or wherein R5 and R6, together with the sulfur atom to which they are attached, form a saturated or partially unsaturated heterocycle of 3 to 7 elements which , in addition to the sulfur atom, may contain an additional heteroatom selected from the group consisting of O, S and NRN2, wherein RN2 is H, C1-3 alkyl, -C (>; = O) - (C1-3 alkyl) ), -C (>; = O) -O- (C 1-4 alkyl), -C (>; = O) - (C 1-3 alkyl) -O- (C 1-4 alkyl), -C (>; = O) -NH2, -C (>; = O) -NH (C1-3 alkyl), -C (>; = O) -N (C1-3 alkyl) 2 or -SO2 (C1-4 alkyl); and wherein R5, R6 and the heterocycles formed by R5 and R6, together with the sulfur atom to which they are attached, can each be independently substituted with halogen, CN, OH, C1-3 alkyl or -O- (alkyl C1-3); and R2 is selected from a group consisting of halogen, CN, OH, C1-3 alkyl, C3-5 cycloalkyl and -O- (C1-3 alk
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