发明名称 Kinase inhibitors
摘要 The present invention relates to novel compounds of formula (I); that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases.
申请公布号 US9499535(B2) 申请公布日期 2016.11.22
申请号 US201213506509 申请日期 2012.04.23
申请人 ORIGENIS GMBH 发明人 Thormann Michael;Treml Andreas;Almstetter Michael;Koestler Roland;Yehia Nasser
分类号 A61K31/55;A61K31/54;A61K31/535;C07D471/04 主分类号 A61K31/55
代理机构 Licata & Tyrrell P.C. 代理人 Licata & Tyrrell P.C.
主权项 1. A compound of formula (I) wherein A is NH, O, S, C═O, NR3 or CR4R5;Cy is an optionally substituted phenylene group or an optionally substituted heteroarylene group having 6 ring atoms and 1, 2 or 3 heteroatoms selected from O, S and N, orCy is an optionally substituted oxazole, thiazole, isoxazole, 1,2,5-thiadiazole, furan, thiophene, 1,2,3-thiadiazole, 1,2,5-oxadiazole, 1,2,3-oxadiazole, 1H-imidazole, 1H-1,2,4-triazole, 1H-1,2,3-triazole, 1H-tetrazole, 4H-1,2,4-triazole, 1H-pyrazole, 1,2,5-selenadiazole, 1,3-selenazole, selenophene, 2H-1,2,3-triazole, 1,3-dithiol-1-ium, 1,4-dithiine or a regioisomer thereof;R1 is an optionally substituted alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group;R2 is a hydrogen atom or methyl group;R3 is an alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group;R4 is a hydrogen atom, NO2, N3, OH, SH, NH2 or an alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group; andR5 is a hydrogen atom, NO2, N3, OH, SH, NH2 or an alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group;or a pharmaceutically acceptable salt, ester, solvate or hydrate or a pharmaceutically acceptable formulation thereof.
地址 Martinsried DE
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