发明申请
- 专利标题: 2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS
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申请号: US17988062申请日: 2022-11-16
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公开(公告)号: US20230095835A1公开(公告)日: 2023-03-30
- 发明人: Yan Chen , Rose Yen , Jiaxin Yu , Vanessa Taylor , Rajinder Singh
- 申请人: Rigel Pharmaceuticals, Inc.
- 申请人地址: US CA South San Francisco
- 专利权人: Rigel Pharmaceuticals, Inc.
- 当前专利权人: Rigel Pharmaceuticals, Inc.
- 当前专利权人地址: US CA South San Francisco
- 主分类号: C07D403/12
- IPC分类号: C07D403/12 ; C07D239/48 ; C07D401/14 ; C07D405/14
摘要:
Compounds within the scope of the present invention have a Formula 1 or a salt or produg thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
公开/授权文献
- US3236157A Fluid motors 公开/授权日:1966-02-22
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