Claims for Patent: 9,416,112

Summary for Patent: 9,416,112

Title:	2,4-pyrimidinediamine compounds and their uses
Abstract:	The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
Inventor(s):	Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
Assignee:	Rigel Pharmaceuticals Inc
Application Number:	US14/485,045
Patent Claims:	1. A compound according to the formula: or a salt thereof, wherein: R2 is selected from phenyl mono-substituted at the 3- or 5-position with an R8 group and phenyl di- or tri-substituted with the same or different R8 groups, provided R2 is not 3,4,5-trimethoxyphenyl; R4 is phenyl substituted with one or more of the same or different R8 groups; R2 and R4 are different; R5 is halogen; R6 is hydrogen; each R8 is selected from the group consisting of Ra, Rb, —O—(CH2)m—Rb C(O)NH—(CH2)m—Rb, —C(O)NH—(CHRa)m—Rb, —O—(CH2)m—C(O)NH—(CH2)m—Rb, —O—(CHRa)m—C(O)NH—(CHRa)m—Rb, —NH—(CH2)m—Rb, —NH—(CHRa)m—Rb, -; each Ra is independently selected from the group consisting of (C1-C6) alkyl, (C3-C8) cycloalkyl, cyclohexyl, phenyl, (C6-C16) arylalkyl, benzyl, 3-8 membered cycloheteroalkyl, morpholinyl, 4-11 membered cycloheteroalkylalkyl and 5-10 membered heteroaryl; each Rb is independently selected from the group consisting of —ORd, (C1-C3) haloalkyloxy, halogen, —CF3, —S(O)Rd, —S(O)2Rd, —S(O)2ORd, —S(O)2NRcRc, —OS(O)Rd, —OS(O)2Rd, —OS(O)2ORd, —OS(O)2NRcRc, —C(O)Rd, —C(O)ORd, —C(O)NRcRc, —OC(O)Rd, —OC(O)ORd, —OC(O)NRcRc, —OC(NH)NRcRc; each Rc is independently hydrogen or Ra; each Rd is independently hydrogen or Ra; and each m is independently an integer from 1 to 3. 2. The compound of claim 1, wherein R2 is phenyl di-substituted with the same or different R8 groups. 3. The compound of claim 1, wherein R2 is 3,4-disubstituted. 4. The compound of claim 1, wherein R4 is mono-substituted with an R8 group. 5. The compound of claim 4, wherein R4 is ortho-substituted with the R8 group. 6. The compound of claim 4, wherein R4 is meta-substituted with the R8 group. 7. The compound of claim 4, wherein R4 is para-substituted with the R8 group. 8. The compound of claim 1, wherein R5 is fluoro. 9. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier, diluent or excipient. 10. The composition of claim 9, wherein the compound is in the form of a pharmaceutically acceptable salt. 11. The compound of claim 5, wherein R5 is fluoro. 12. The compound of claim 5, wherein R5 is chloro. 13. The compound of claim 1, wherein R2 is phenyl tri-substituted with the same or different R8 groups. 14. The compound of claim 13, wherein R4 is mono-substituted with an R8 group. 15. The compound of claim 14, wherein R4 is mono-substituted with an R8 group. 16. The compound of claim 14, wherein R4 is ortho-substituted with the R8 group. 17. The compound of claim 14, wherein R4 is meta-substituted with the R8 group. 18. The compound of claim 14, wherein R4 is para-substituted with the R8 group. 19. The compound of claim 15, wherein R5 is fluoro. 20. The compound of claim 15, wherein R5 is chloro.