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New Pyrazolopyrimidine derivative and its purposes as MALT1 inhibitor
专利权人:
Novartis AG;诺华股份有限公司;諾華股份有限公司
发明人:
C.皮索特索德曼,J.奎安卡德,A.施拉普巴赫,O.西米克,M.廷特尔诺特布洛莱伊,M.廷特爾諾特布洛萊伊,T.佐勒
申请号:
MOJ003711
公开号:
MOJ003711B
申请日:
2019.06.10
申请国别(地区):
MO
年份:
2019
代理人:
摘要:
The invention discloses the pyrazolo-pyrimidine derivatives of new formula (I) or its pharmaceutically acceptable salt,In formula (I),R1 be halogen,Cyano or the C1-C3 alkyl being optionally optionally substituted by halogen; R2 be optionally by C1-C6 alkyl,C2-C6 alkenyl,Hydroxyl,Bis--C1-C6 alkyl amino of N, N-,The mono- C1-C6 alkyl amino of N-,O-Rg,Rg,Phenyl or C1-C6 alkoxy replace C1-C6 alkyl one or more times,Wherein the alkoxy can optionally by C1-C6 alkoxy,Bis--C1-C6 alkyl amino of N, N-,Rg or phenyl replace; Optionally by C1-C6 alkyl,Bis--C1-C6 alkyl amino of N, N- or the alkyl-substituted C3-C6 naphthenic base of C1-C6 alkoxy -C 1-C6,And/or atom of two optional substituent groups in conjunction with them is formed together the heterocycle of the ring-type containing 1-2 O atom or loop coil 4-6 member saturation; The phenyl optionally replaced by C1-C6 alkoxy; The heteroatomic 5-6 unit's heteroaryl ring of N and O is selected from 1-3,The ring is optionally optionally replaced by the C1-C6 alkyl that amino or hydroxyl replace; Rg; Or bis--C1-C6 alkyl amino-carbonyl of N, N-; And R be it is independent by Ra replace secondary or multiple phenyl,It is independent by Rb replace 2- pyridyl group one or more times,It is independent to replace 3- pyridyl group one or more times or independence to be replaced by Rd 4- pyridyl group one or more times by Rc; It can usually interact with MALT1 proteolysis and/or automatic protein hydrolysing activity,Especially it can inhibit the activity. The invention also discloses the synthesis of the new pyrazolo-pyrimidine derivatives, its purposes as drug, especially by the interaction with MALT1 proteolysis and/or automatic protein hydrolysing activity.本發明公開了新的式(I)的吡唑并‑嘧啶衍生物或其藥學上可接受的鹽,在式(I)中,R1爲鹵素、氰基或任選被鹵素取代的C1‑C3烷基;R2爲任選被C1‑C6烷基、C2‑C6鏈烯基、羥基、N,N‑二‑C1‑C6烷基氨基、N‑單‑C1‑C6烷基氨基、O‑Rg、Rg、苯基或C1‑C6烷氧基取代一或多次的C1‑C6烷基,其中所述烷氧基可以任選被C1‑C6烷氧基、N,N‑二‑C1‑C6烷基氨基、Rg或苯基取代;任選被C1‑C6烷基、N,N‑二‑C1‑C6烷基氨基或C1‑C6烷氧基‑C1‑C6烷基取代的C3‑C6環烷基,和/或兩個所述任選的取代基與它們所結合的原子一起形成含
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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