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Bicyclic derivatives useful as DPP-1 inhibitors
专利权人:
Janssen Pharmaceutica; N.V.
发明人:
LAWSON, Edward C.,GHOSH, Shyamali,DESJARLAIS, Renee L.,HLASTA, Dennis J.,SCHUBERT, Carsten
申请号:
ES10798434
公开号:
ES2573698T3
申请日:
2010.12.17
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of formula (1 L) ** Formula ** wherein R 1 is selected from the group consisting of C 1-4 alkyl, -C (O) -NH 2, C 3-6 cycloalkyl, phenyl and 5- to 6-membered heteroaryl; wherein the heteroaryl is optionally substituted with one or more substituents independently selected from halogen and C1-4alkyl; n is an integer from 0 to 1; L is selected from the group consisting of ** Formula ** -CH2CH2-N- (CH3), -CH2CH2-N- (CH2CH3) and -CH2CH2CH2-NRA-; wherein RA is selected from the group consisting of hydrogen, methyl and ethyl; Y is selected from the group consisting of N and CH; X is selected from the group consisting of N (RB), O and S; wherein RB is selected from the group consisting of hydrogen and C1-4alkyl; R2 is selected from the group consisting of hydrogen, halogen, nitro, -CO2H, -C (O) -NRCRD, -Q, -O-Q and - C (O) -NH-Q; wherein RC and RD are each selected independently from the group consisting of hydrogen and C1-4alkyl; alternatively, RC and RD are taken together with the nitrogen atom to which they are attached to form a ring structure selected from the group consisting of piperidine-1-yl, piperazine-1-yl, pyrolidine-1--yl, morpholine- 4-yl, 1,2,3,4-tetrahydroquinoline-1-yl and 1,2,3,4 tetrahydro-isoquinoline-2-yl; wherein Q is selected from the group consisting of aryl, aralkyl, heterocyclyl, benzo [d] [1,3] dioxolyl and 2,3-dihydro-benzo [b] [1,4] dioxinyl; wherein the aryl or heterocyclyl, either alone or as part of a substituent group, is optionally substituted with one or more substituents independently selected from the group consisting of halogen, cyano, C1-4alkyl, halogenated C1-4alkyl, C1-4alkoxy , halogenated C1-4alkoxy, -CO2H, -C (O) -NRERF, -SO2-NRERF and phenyl; wherein RE and RF are each independently selected from the group consisting of hydrogen and C1-4alkyl; and wherein the heterocyclyl contains one or more heteroatoms S, said heterocyclyl may also be optionally substituted in said one or more heteroatoms S with one to two oxo groups;
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