发明名称 2,4-Pyrimidinediamine compounds and their uses
摘要 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.
申请公布号 US9162989(B2) 申请公布日期 2015.10.20
申请号 US201514626471 申请日期 2015.02.19
申请人 Rigel Pharmaceuticals, Inc. 发明人 Singh Rajinder;Argade Ankush;Payan Donald G.;Molineaux Susan;Holland Sacha J.;Clough Jeffrey;Keim Holger;Bhamidipati Somasekhar;Sylvain Catherine;Li Hui;Rossi Alexander B.
分类号 C07D239/48;A61K31/506;A61K31/519;C07D401/12;C07D401/14;C07D403/12;C07D403/14;C07D405/12;C07D405/14;C07D409/12;C07D409/14;C07D413/10;C07D413/12;C07D413/14;C07D417/12;C07D417/14;A61K31/505;A61K31/5377;A61K31/538;A61K31/5383;A61K31/551;A61K45/06;C07D498/04;C07D265/36;A61K31/5395;C07D495/04;C07F5/02;C07D498/14 主分类号 C07D239/48
代理机构 Klarquist Sparkman, LLP 代理人 Young Travis;Klarquist Sparkman, LLP
主权项 1. A compound according to Formula (I):or a salt thereof, wherein: R2 and R4 are different and independently are each phenyl substituted with one or more of the same or different R8 groups; R5 is fluoro; R8 is selected from Ra, Rb, Ra substituted with one or more of the same or different Ra or Rb, ORa substituted with one or more of the same or different Ra, —(CH2)m—Rb, —(CHRa)m—Rb, —O—(CH2)m—Rb, —O—(CHRa)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 or —NH—(CHRa)m—Rb; each Ra is independently selected from hydrogen, (C1-C6)alkyl, (C3-C8)cycloalkyl, cyclohexyl, (C4-C11)cycloalkylalkyl, (C5-C10)aryl, phenyl, (C6-C16) arylalkyl, benzyl, 3-8 membered cycloheteroalkyl, morpholinyl, piperazinyl, homopiperazinyl, piperidinyl, 4-11 membered cycloheteroalkylalkyl, 5-10 membered heteroaryl, or 6-16 membered heteroarylalkyl; each Rb is independently selected from ═O, ORa, (C1-C3) haloalkyloxy, ═S, ═SRa, ═NRa, ═NONRa, —NRcRc, halogen, —CF3, —CN, —OCN, —SCN, —NO, NO2, ═N2, —N3, —S(O)Ra, —S(O)2Ra, —S(O)2ORa, —S(O)2NRcRc, —OS(O)Ra, —OS(O)2Ra, —OS(O)2ORa, —OS(O)2NRcRc, —C(O)Ra, —C(O)ORa, —C(O)NRcRc, —C(NH)NRcRc, OC(O)Ra, —OC(O)ORa, —OC(O)NRcRc, —OC(NH)NRcRc, [NHC(O)]Ra, —[NHC(O)]ORa, [NHC(O)]NRcRc or —[NHC(NH)]NRcRc; each Rc is independently Ra, or, alternatively, each Rc is taken together with the nitrogen atom to which it is bonded to form a 5 to 8-membered cycloheteroalkyl or heteroaryl which may optionally include one or more of the same or different additional heteroatoms and which is optionally substituted with one or more of the same or different Ra or suitable Rb groups; at least one R8 is Rb; and each m is independently an integer from 1 to 3.
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