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 US2015005297(A1) 申请公布日期 2015.01.01
申请号 US201414485045 申请日期 2014.09.12
申请人 Singh Rajinder;Argade Ankush;Payan Donald;Molineaux Susan;Holland Sacha;Clough Jeffrey;Keim Holger;Bhamidipati Somasekhar;Sylvain Catherine;Li Hui;Rossi Alexander 发明人 Singh Rajinder;Argade Ankush;Payan Donald;Molineaux Susan;Holland Sacha;Clough Jeffrey;Keim Holger;Bhamidipati Somasekhar;Sylvain Catherine;Li Hui;Rossi Alexander
分类号 C07D239/48;C07D409/12;C07D413/12;C07D403/12;C07D401/12;C07D405/12 主分类号 C07D239/48
代理机构 代理人
主权项 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; 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, —S—(CH2)m—Rb, —O—CHRaRb, —O—CRa(Rb)2, —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, —S—(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, —NH[(CH2)mRb], —N[(CH2)mRb]2, —NH—C(O)—NH—(CH2)m—Rb, —NH—C(O)—(CH2)m—CHRbRb and —NH—(CH2)m—C(O)—NH—(CH2)m—Rb; each Ra is independently selected from the group consisting of (C1-C6) alkyl, (C3-C8) cycloalkyl, cyclohexyl, (C4-C11) cycloalkylalkyl, (C5-C10) aryl, phenyl, (C6-C16) arylalkyl, benzyl, 2-6 membered heteroalkyl, 3-8 membered cycloheteroalkyl, morpholinyl, piperazinyl, homopiperazinyl, piperidinyl, 4-11 membered cycloheteroalkylalkyl, 5-10 membered heteroaryl and 6-16 membered heteroarylalkyl; each Rb is a suitable group independently selected from the group consisting of ═O, —ORd, —OH, (C1-C3) haloalkyloxy, halogen, —CF3, —NC, —OCN, —SCN, —NO, —NO2, ═N2, —N3, —S(O)Rd, —S(O)2Rd, —S(O)2ORd, —S(O)NRcRc, —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, —OC(NRa)NRcRc, —[NHC(O)]nRd, —[NRaC(O)]nRd, —[NHC(O)]nORd, —[NRaC(O)]nORd, —[NHC(O)]nNRcRc, —[NRaC(O)]nNRcRc, —[NHC(NH)]nNRcRc and —[NRaC(NRa)]nNRcRc; each Rc is independently hydrogen or 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 may optionally be substituted with one or more of the same or different Ra or suitable Rb groups; each Rd is independently hydrogen or Ra; each m is independently an integer from 1 to 3; and each n is independently an integer from 0 to 3, with the provisos that the compound is not N2,N4-bis(3-methylphenyl)-5-fluoro-2,4-pyrimidinediamine;N2,N4-bis(3-chlorophenyl)-5-fluoro-2,4-pyrimidinediamine;N2,N4-bis(2,5-dimethylphenyl)-5-fluoro-2,4-pyrimidinediamine;N2,N4-bis(3,4-dimethylphenyl)-5-fluoro-2,4-pyrimidinediamine;N2,N4-bis(2,4-dimethylphenyl)-5-fluoro-2,4-pyrimidinediamine;N2,N4-bis(3-bromophenyl)-5-fluoro-2,4-pyrimidinediamine;N2,N4-bis[(3-chloro-4-methoxyphenyl)]-5-fluoro-2,4-pyrimidinediamine;orN2,N4-Bis(3-chloro-4-methoxy)-5-fluoro-2,4-pyrimidinediamine.
地址 Belmont CA US