发明名称 Modulators of sphingosine phosphate receptors
摘要 Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.
申请公布号 US9382217(B2) 申请公布日期 2016.07.05
申请号 US201414311825 申请日期 2014.06.23
申请人 The Scripps Research Institute 发明人 Roberts Edward;Rosen Hugh;Brown Steven;Guerrero Miguel A.;Peng Xuemei;Poddutoori Ramulu
分类号 C07D271/06;A61K31/4245;C07D401/04;C07D413/04;C07D413/14;C07D471/04;C07D263/32 主分类号 C07D271/06
代理机构 Schwegman Lundberg & Woessner, P.A. 代理人 Schwegman Lundberg & Woessner, P.A.
主权项 1. A method of treatment of a malcondition in a patient having such malcondition, wherein the malcondition is multiple sclerosis, transplant rejection or adult respiratory distress syndrome, comprising administering to the patient an effective dose of a compound of formula (I), or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof:wherein a dashed line signifies that a single bond or a double bond can be present, provided that there are two double bonds and three single bonds in the ring comprising A1, A2, and A3; A1 and A3 are N and A2 is O; L1 and L2 are each independently a bond; J independently at each occurrence is F, Cl, Br, I, OR′, OC(O)N(R′)2, CN, CF3, OCF3, R′, methylenedioxy, ethylenedioxy, N(R′)2, SR′, SOR′, SO2R′, SO2N(R′)2, SO3R′, C(O)R′, C(O)C(O)R′, C(O)CH2C(O)R′, C(S)R′, C(O)OR′, OC(O)R′, OC(O)OR′, C(O)N(R′)2, OC(O)N(R′)2, C(S)N(R′)2, (CH2)0-2NHC(O)R′, N(R′)N(R′)C(O)R′, N(R′)N(R′)C(O)OR′, N(R′)N(R′)CON(R′)2, N(R′)SO2R′, N(R′)SO2N(R′)2, N(R′)C(O)OR′, N(R′)C(O)R′, N(R′)C(S)R′, N(R′)C(O)N(R′)2, N(R′)C(S)N(R′)2, N(COR′)COR′, N(OR′)R′, C(═NH)N(R′)2, C(O)N(OR′)R′, or C(═NOR′)R′, wherein R′ is independently at each occurrence hydrogen or an alkyl, cycloalkyl, aryl, heterocyclyl, or heteroaryl wherein any alkyl, cycloalkyl, aryl, heterocyclyl or heteroaryl is substituted with 0-3 J; R5 a group of formula a-i mono- or pluri-substituted with J, wherein a wavy line indicates a point of attachment; R6 is phenyl mono- or pluri-substituted with J.
地址 La Jolla CA US