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US 12,577,248 B2Granted
Substituted [1,2,4]triazolo[1,5-a]pyrazines as spleen tyrosine kinase inhibitors
AssigneeNanjing Ruijie Pharma Co., Ltd.
InventorsJunbo Zhang, Shuhao Zhu, Xiaoxin Qi
Life of this patent
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Abstract
The present invention provides compounds of Formula (I) which can be used as Syk inhibitors and potently as therapeutic agents against diseases mediated by Syk.
Claims21
A compound of Formula (I):
- or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
- wherein:
- R3 is benzodioxolyl, 2H-1,4-benzoxazin-3(4H)-onyl, 2H-pyrido[3,2-b][1,4]oxazin-3(4H)-onyl, pyrazolyl, thiazolyl, pyridinyl, pyrazinyl, indolyl, isoindolyl, indazolyl, or benzothiazolyl, wherein the benzodioxolyl, 2H-1,4-benzoxazin-3(4H)-onyl, 2H-pyrido[3,2-b][1,4]oxazin-3(4H)-onyl, pyrazolyl, thiazolyl, pyridinyl, pyrazinyl, indolyl, isoindolyl, indazolyl, or benzothiazolyl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C(O)NHR5, C(O)OH, NH2, OC1-6 alkyl, and C3-8 cycloalkyl;
- R4 is benzodioxolyl, phenyl, or pyridinyl;
- wherein the benzodioxolyl, phenyl, or pyridinyl is optionally substituted with one, two, or three substituents independently selected from the group consisting of halo, C1-6 alkyl, OC1-6 alkyl, piperazinyl, 4-hydroxy-4-methylpiperazin-1-yl, C3-8 cycloalkoxy, morpholin-4-yl, 1,1-dioxothiomorpholin-4-yl, 2,5-diazabicyclo[2.2.1]heptan-2-yl, 2-oxa-6-azaspiro[3.3]heptan-6-yl, and 2-oxa-6-azaspiro[3.4]octan-6-yl;
- wherein each C1-6 alkyl and OC1-6 alkyl substituent is optionally and independently substituted with one, two, or three independently selected halo substituents;
- wherein each piperazinyl substituent is optionally and independently substituted with one or two substituents independently selected from the group consisting of C1-6 alkyl, CF3, CH2CF3, CH(OH)CH3, CH2CH2OH, CH(OCH3)CH3, CH2CH2OCH3, S(O)2CH3, S(O)2CH2CH3, C3-8 cycloalkyl, and C2-6 cycloalkoxy;
- and
- wherein each 2,5-diazabicyclo[2.2.1]heptan-2-yl substituent is optionally and independently substituted with one or two substituents independently selected from the group consisting of C1-6 alkyl and C2-6 cycloalkoxy;
- and
- each R5 is independently H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or OC(O)phenyl.
8 more elements
Dependencies are inferred from the claim text.