Invention Grant
- Patent Title: 2,4-diamino-pyrimidine compounds and method for making and using the compounds
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Application No.: US16893981Application Date: 2020-06-05
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Publication No.: US11524955B2Publication Date: 2022-12-13
- Inventor: Yan Chen , Rose Yen , Jiaxin Yu , Vanessa Taylor , Rajinder Singh
- Applicant: Rigel Pharmaceuticals, Inc.
- Applicant Address: US CA South San Francisco
- Assignee: Rigel Pharmaceuticals, Inc.
- Current Assignee: Rigel Pharmaceuticals, Inc.
- Current Assignee Address: US CA South San Francisco
- Agency: Klarquist Sparkman, LLP
- Main IPC: C07D239/48
- IPC: C07D239/48 ; C07D403/12 ; C07D401/14 ; C07D405/14

Abstract:
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.
Public/Granted literature
- US20200299276A1 2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS Public/Granted day:2020-09-24
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