The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 13, 2022

Filed:

Jun. 05, 2020
Applicant:

Rigel Pharmaceuticals, Inc., South San Francisco, CA (US);

Inventors:

Yan Chen, Foster City, CA (US);

Rose Yen, San Francisco, CA (US);

Jiaxin Yu, Foster City, CA (US);

Vanessa Taylor, San Francisco, CA (US);

Rajinder Singh, Belmont, CA (US);

Assignee:

Rigel Pharmaceuticals, Inc., South San Francisco, CA (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 239/48 (2006.01); C07D 403/12 (2006.01); C07D 401/14 (2006.01); C07D 405/14 (2006.01);
U.S. Cl.
CPC ...
C07D 403/12 (2013.01); C07D 239/48 (2013.01); C07D 401/14 (2013.01); C07D 405/14 (2013.01);
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; Ris selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and Rand Rare independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 ICof from 0.003 μM to 3.7 μM; a TAK1 ICof 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.


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