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Sulfoximin-substituted quinazolines and their use as inhibitors of MNK1 and / or MNK2 kinases
专利权人:
Evotec International GmbH
发明人:
BLUM, Andreas,GOTTSCHLING, Dirk,HECKEL, Armin,HEHN, Joerg,SCHMID, Bernhard,WIEDENMAYER, Dieter
申请号:
ES14732180
公开号:
ES2663788T3
申请日:
2014.06.23
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of formula ** (See formula) ** in which Ar is selected from a group consisting of: ** (See formula) ** in which X is CH or N; R3 is H, halogen, CN or -C (>; = O) -NH2; and R4 is selected from a group consisting of: ** (See formula) ** in which R7 is selected from a group consisting of H, CN, C1-6 alkyl, -O- (C1-3 alkyl), C2-4 alkynyl, C3-7 cycloalkyl, heterocyclyl, - (C1-3 alkyl) -heterocyclyl, - (C1-3 alkyl) -O-heterocyclyl, aryl, - (C1-3 alkyl) -aryl, 5- or heteroaryl 6 members, - (C1-3 alkyl) -heteroaryl, -COOH, - (C>; = O) -O- (C1-6 alkyl), - (C>; = O) - N>; = S (>; = O) (C1-3 alkyl) 2 and - (C>; = O) -NRN1RN2; wherein RN1 is H or C1-3 alkyl; and RN2 is selected from a group consisting of H, C1-6 alkyl, C2-5 alkynyl, C3-7 cycloalkyl, heterocyclyl, - (C1-3 alkyl) -heterocyclyl, - (C1-3 alkyl) -aryl and - SO2- (C1-3 alkyl); or RN1 and RN2 together with the N atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, 4-oxopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxo-thiomorpholinyl or a 1-ring - 1-imino-1,4-thiazinano oxide, which may be substituted with an OH, C1-3 alkyl or -O-C1-3 alkyl; and in which, in R4, each heterocyclyl is selected from a group consisting of saturated monocyclic ring systems of 4, 5 or 6 members containing 1, 2 or 3 heteroatoms independently selected from each other from the group consisting in O, S, N and NH, in which a group -CH2- can be replaced by a group -C (>; = O) - and in which each heterocyclyl group is optionally substituted with C1-3alkyl; wherein, in R4, each aryl is phenyl or naphthyl; wherein, in R4, each heteroaryl is selected from a group consisting of 5 or 6 membered monocyclic heteroaromatic ring systems containing 1, 2 or 3 heteroatoms independently selected from each other from the group consisting of O, S, N and NH, and is optionally substituted with C1-3 alkyl; wherein, in R4, each alkyl is optionally substituted with 1 or more F o
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