发明名称 Pyrazolopyrimidine derivatives
摘要 Compounds of the formula (I), in which X, R1 and R2 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.
申请公布号 US8741896(B2) 申请公布日期 2014.06.03
申请号 US201013502554 申请日期 2010.09.24
申请人 Merck Patent GmbH 发明人 Buchstaller Hans Peter;Emde Ulrich;Klein Markus;Esdar Christina;Bomke Joerg
分类号 A61K31/5377;C07D413/14;A61K31/4985;C07D487/02 主分类号 A61K31/5377
代理机构 代理人
主权项 1. A compound selected from the following compounds:Compound No.Name and/or structure“A65” 4-(1H-Indol-6-yl)-1-methyl-6-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidine“A97” 4-(1H-Indol-4-yl)-1-methyl-6-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidine“A129”4-(1H-Benzimidazol-5-yl)-1-methyl-6-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidine“A161”4-(1H-Indazol-4-yl)-1-methyl-6-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidine“A193”5-(1-Methyl-6-morpholin-4-yl-1H-pyrazolo[3,4-d]-pyrimidin-4-yl)pyridin-2-ylamine“A196”“A228”“A229”“A257”Ethyl [4-(6-aminopyridin-3-yl)-6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidin-1-yl]acetate“A258”2-[4-(6-Aminopyridin-3-yl)-6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidin-1-yl-ethanone“A259”Ethyl [4-(2-aminopyrimidin-5-yl)-6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidin-1-yl]acetate“A260”2-[4-(2-Aminopyrimidin-5-yl)-6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidin-1-yl-ethanone“A261”2-[4-(2-Aminopyrimidin-5-yl)-6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidin-1-yl]-1-morpholin-4-yl-ethanone“A262”2-[4-(2-Aminopyrimidin-5-yl)-6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidin-1-yl]-1-(4-methyl-piperazin-1-yl)ethanoneor a pharmaceutically usable salt, tautomer or stereoisomer thereof, including mixtures thereof in all ratios.
地址 Darmstadt DE