发明名称 NOVEL IMIDAZOLE QUINOLINE-BASED IMMUNE SYSTEM MODULATORS
摘要 The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.;
申请公布号 US2014242121(A1) 申请公布日期 2014.08.28
申请号 US201214349254 申请日期 2012.10.03
申请人 JANUS BIOTHERAPEUTICS, INC. 发明人 Lipford Grayson B.;Zepp Charles M.
分类号 C07D471/04 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of Formula I or a pharmaceutically acceptable salt thereof,wherein X is absent or is an alkyl, cycloalkyl, aryl, aralkyl, or heterocycle; each occurrence of R1 is independently hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, heterocycle, or aryl; each occurrence of R2 and R3 is independently hydrogen, alkyl, cycloalkyl, OH, alkoxy, —(CH2)pNRaRb, or R2 and R3 together with the carbon atom to which they are bonded optionally form a (C3-C7)cycloalkyl; n is an integer of 2-4; each q is an integer of 1-2; Y is NR9 or O; R8 is hydrogen, alkyl, cycloalkyl, heterocycle, or aryl; R9 is H, Me, Et, n-Pr, i-Pr, n-Bu, i-Bu, t-Bu, CH2CMe3, Ph, CH2Ph, C(═O)R12, (CH2)pORa, and (CH2)pNRbRc, wherein R12 is alkyl, phenyl, or heterocycle; Ra, Rb and Rc are each independently hydrogen, or (C1-C4)alkyl, or Rb and Rc, together with the nitrogen atom to which they are attached, form a saturated or unsaturated heterocyclic ring containing from three to seven ring atoms, which ring may optionally contain another heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and may be optionally substituted by from one to four groups which may be the same or different selected from the group consisting of alkyl, phenyl and benzyl; and p is 2-4; or said R8 and R9 together with the nitrogen atom to which they are bonded optionally form a heterocycle comprising 1-4 heteroatoms, wherein the heterocycle is optionally substituted by (C1-C4)alkyl; or R1 and R8 optionally form a heterocycle comprising 2-4 heteroatoms, wherein the heterocycle is optionally substituted by (C1-C4)alkyl; R4 is hydrogen, halogen, cyano, nitro, CF3, OCF3, alkyl, cycloalkyl, alkenyl, aryl, heterocycle, ORa, —CH2ORa, SRa, S(═O)Ra, S(═O)2Ra, NRbRc, S(═O)2NRbRc, C(═O)ORa, C(═O)Ra, C(═O)NRbRc, OC(═O)Ra, OC(═O)NRbRc, NRbC(═O)ORa, NRbC(═O)Ra; R5 and R6 are each independently hydrogen, halogen, cyano, nitro, CF3, OCF3, alkyl, cycloalkyl, alkenyl, aryl, heterocycle, ORa, SRa, S(═O)Ra, S(═O)2Ra, NRbRc, S(═O)2NRbRc, C(═O)ORa, C(═O)Ra, C(═O)NRbRc, OC(═O)Ra, OC(═O)NRbRc, NRbC(═O)ORa, NRbC(═O)Ra, alkaryl, alkylheterocyclic, or NRb(CH2)pNRbRc; or said R5 and R6 together with the carbon atoms to which they are bonded optionally form a heterocycle comprising 1-4 heteroatoms, wherein the heterocycle is optionally substituted by (C1-C4)alkyl; L is absent or is alkyl or alkenyl containing from 2 to 10 carbon atoms; R7 is H, alkyl, heteroaryl or NR10R11, wherein the heteroaryl are optionally substituted by (C1-C4)alkyl; R10 and R11 are each independently hydrogen, alkyl, cycloalkyl, alkenyl, aryl or alkylaryl, or R10 and R11 together with the nitrogen atom to which they are bonded form a heterocycle; p is an integer of 0, 1, 2, 3, 4, 5, or 6; each occurrence of Ra is independently hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, heterocycle, or aryl; and each occurrence of Rb, and Rc is independently hydrogen, alkyl, cycloalkyl, heterocycle, aryl, or said Rb and Rc together with the nitrogen atom to which they are bonded optionally form a heterocycle comprising 1-4 heteroatoms, wherein the heterocycle is optionally substituted by (C1-C4)alkyl.
地址 Cambridge MA US