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    • 5. 发明授权
    • Therapeutic compounds for inhibiting interleukin-12 signals and method for using same
    • 用于抑制白细胞介素-12信号的治疗化合物及其使用方法
    • US06878715B1
    • 2005-04-12
    • US09544984
    • 2000-04-07
    • J. Peter KleinStephen J. KlausAnil M. KumarBaoqing Gong
    • J. Peter KleinStephen J. KlausAnil M. KumarBaoqing Gong
    • A61K31/00C07D239/54C07D473/04C07D473/06C07D473/10C07D487/04C07D495/04C07D513/04A61K31/522
    • C07D239/54A61K31/00C07D473/04C07D473/06C07D473/10C07D487/04C07D495/04C07D513/04
    • Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S. Each R1, R2 and R3 is substituted or unsubstituted and is independently selected from a member of the group consisting of hydrogen, halo, oxo, C(1-20)alkyl, C(1-20)hydroxyalkyl, C(1-20)thioalkyl, C(1-20)alkylamino, C(1-20)alkylaminoalkyl, C(1-20)aminoalkyl, C(1-20)aminoalkoxyalkenyl, C(1-20)aminoalkoxyalkynyl, C(1-20)diaminoalkyl, C(1-20)triaminoalkyl, C(1-20)tetraaminoalkyl, C(5-15)aminotrialkoxyamino, C(1-20)alkylamido, C(1-20)alkylamidoalkyl, C(1-20)amidoalkyl, C(1-20)acetamidoalkyl, C(1-20)alkenyl, C(1-20)alkynyl, C(3-8)alkoxyl, C(1-11)alkoxyalkyl, and C(1-20)dialkoxyalkyl.
    • 发现具有与五元环结构稠合的六元环结构的新型杂环化合物可用于治疗和预防与受白细胞介素-12(“IL-12”)影响的紊乱相关的症状或表现, ,例如,Th1细胞介导的疾病。 治疗化合物,药学上可接受的衍生物(例如分解的对映异构体,非对映异构体,互变异构体,其盐和溶剂合物)或其前药具有以下通式:每个X,Y和Z独立地选自C (R 3),N,N(R 3)和S.每个R 1,R 2和R 3是取代或未取代的,并且独立地选自氢,卤素,氧代,C(1-20)烷基,C (1-20)羟基烷基,C(1-20)硫代烷基,C(1-20)烷基氨基,C(1-20)烷基氨基烷基,C(1-20)氨基烷基,C(1-20)氨基烷氧羰基,C(1 (1-20)氨基烷基,C(1-20)四氨基烷基,C(5-15)氨基三烷氧基氨基,C(1-20)烷基酰氨基,C(1-20)烷基氨基烷基,C(1-20) )烷基酰氨基烷基,C(1-20)酰氨基烷基,C(1-20)乙酰氨基烷基,C(1-20)烯基,C(1-20)炔基,C(3-8)烷氧基,C(1-11)烷氧基烷基 ,和C(1-20)二烷氧基烷基。
    • 6. 发明授权
    • Therapeutic compounds for inhibiting interleukin-12 signaling and methods for using same
    • 用于抑制白细胞介素-12信号的治疗化合物及其使用方法
    • US06774130B2
    • 2004-08-10
    • US09288556
    • 1999-04-09
    • J. Peter KleinStephen J. KlausAnil M. KumarBaoqing Gong
    • J. Peter KleinStephen J. KlausAnil M. KumarBaoqing Gong
    • A61K31522
    • C07D473/04A61K31/00C07D473/06C07D487/04C07D495/04C07D513/04
    • Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S. Each R1, R2 and R3 is substituted or unsubstituted and is independently selected from a member of the group consisting of hydrogen, halo, oxo, C(1-20)alkyl, C(1-20)hydroxyalkyl, C(1-20)thioalkyl, C(1-20)alkylamino, C(1-20)alkylaminoalkyl, C(1-20)aminoalkyl, C(1-20)aminoalkoxyalkenyl, C(1-20)aminoalkoxyalkynyl, C(1-20)diaminoalkyl, C(1-20)triaminoalkyl, C(1-20)tetraaminoalkyl, C(5-15)aminotrialkoxyamino, C(1-20)alkylamido, C(1-20)alkylamidoalkyl, C(1-20)amidoalkyl, C(1-20)acetamidoalkyl, C(1-20)alkenyl, C(1-20)alkynyl, C(3-8)alkoxyl, C(1-11)alkoxyalkyl, and C(1-20)dialkoxyalkyl.
    • 发现具有与五元环结构稠合的六元环结构的新型杂环化合物可用于治疗和预防与受白细胞介素-12(“IL-12”)影响的紊乱相关的症状或表现, ,例如,Th1细胞介导的疾病。 治疗化合物,药学上可接受的衍生物(例如分解的对映异构体,非对映异构体,互变异构体,其盐和溶剂合物)或其前药具有以下通式:每个X,Y和Z独立地选自C (R 3),N,N(R 3)和S.每个R 1,R 2和R 3是取代或未取代的,并且独立地选自氢,卤素,氧代,C(1-20)烷基,C (1-20)羟基烷基,C(1-20)硫代烷基,C(1-20)烷基氨基,C(1-20)烷基氨基烷基,C(1-20)氨基烷基,C(1-20)氨基烷氧羰基,C(1 (1-20)氨基烷基,C(1-20)四氨基烷基,C(5-15)氨基三烷氧基氨基,C(1-20)烷基酰氨基,C(1-20)烷基氨基烷基,C(1-20) )烷基酰氨基烷基,C(1-20)酰氨基烷基,C(1-20)乙酰氨基烷基,C(1-20)烯基,C(1-20)炔基,C(3-8)烷氧基,C(1-11)烷氧基烷基 ,和C(1-20)二烷氧基烷基。