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NOVEL PYRAZOLO PYRIMIDINE DERIVATIVES AND THEIR USE AS MALT1 INHIBITORS
专利权人:
发明人:
申请号:
HK17103468.8
公开号:
HK1229801A
申请日:
2017.04.06
申请国别(地区):
HK
年份:
2017
代理人:
摘要:
The present invention describes new pyrazolo-pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof (I) wherein, R1 is halogen, cyano, or C1-C3alkyl optionally substituted by halogen R2 is C1-C6alkyl optionally substituted one or more times by C1-C6alkyl, C2-C6alkenyl, hydroxyl, N,N-di-C1-C6alkyl amino, N-mono-C1-C6alkyl amino, O-Rg, Rg, phenyl, or by C1-C6alkoxy wherein said alkoxy again may optionally be substituted by C1-C6alkoxy, N,N-di-C1-C6alkyl amino, Rg or phenyl C3-C6cycloalkyl optionally substituted by C1-C6alkyl, N,N-di-C1-C6alkyl amino or C1-C6alkoxy-C1-C6alkyl, and/or two of said optional substituents together with the atoms to which they are bound may form an annulated or spirocyclic 4 - 6 membered saturated heterocyclic ring comprising 1 - 2 O atoms phenyl optionally substituted by C1-C6alkoxy a 5 - 6 membered heteroaryl ring having 1 to 3 heteroatoms selected from N and O said ring being optionally substituted by C1-C6alkyl which may be optionally substituted by amino or hydroxy Rg or N,N-di-C1-C6alkyl amino carbonyl and R is phenyl independently substituted two or more times by Ra, 2-pyridyl independently substituted one or more times by Rb, 3-pyridyl independently substituted one or more times by Rc, or 4-pyridyl independently substituted one or more times by Rd which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.La présente invention concerne de nouveaux dérivés pyrazolo-pyrimidine de formule (I) ou un sel pharmaceutiquement acceptable desdits dérivés. Dans la formule (I), R1 représente halogène, cyano ou C1-C3alkyle éventuellement substitué par halogène R2 représente C1-C6 alkyle éventuellement substitué une ou plusieurs fois par
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