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    • 7. 发明申请
    • FUSED HETEROARYL PYRIDYL AND PHENYL BENZENESUFLONAMIDES AS CCR2 MODULATORS FOR THE TREAMENT OF INFLAMMATION
    • FUSED HETEROARYL PYRIDYL和PHENYL BENZENESUFLONAMIDES作为CCR2调节剂用于炎症反应
    • WO2009009740A1
    • 2009-01-15
    • PCT/US2008/069813
    • 2008-07-11
    • CHEMOCENTRYX, INC.KRASINSKI, AntoniPUNNA, SreenivasUNGASHE, SolomonWANG, QiangZENG, Yibin
    • KRASINSKI, AntoniPUNNA, SreenivasUNGASHE, SolomonWANG, QiangZENG, Yibin
    • A61K31/519C07D473/00C07D487/04A61P29/00
    • C07D487/04C07D213/79C07D213/81C07D213/84C07D471/04C07D471/12C07D473/00
    • Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2- mediated diseases and as controls in assays for the identification of CCR2 antagonists. A compound of the formula (I) or a salt thereof: where: R 1 and R 2 are each independently hydrogen, halogen, C 1-8 alkyl, -CN. or C 1-8 haloalkyl, provided that at least one of R1 1 or R 2 is other than hydrogen; each R 3 is independently hydrogen; R 4 is hydrogen; R 5 is halogen or C 1-8 alkyl; R 6 is hydrogen; X 1 is CR 7 , N or NO; X 2 and X 4 are N or NO; X 3 is CR 7 ; X 6 and X 7 are each independently selected from CR 7 , N, and NO; each R 7 is independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C 2-8 alkyl, substituted or unsubstituted C 2-8 alkeπyl, substituted or unsubstituted C 2-8 alkynyl, -CN. =O, -NO 2 , -OR 6 , -OC(O)R 8, -CO 2 R 8, -C(O)R 8 , -C(O)NR 0 R 8 , -OC(O)NR 9 R 8 , -NR 10 C(O)R 8 , -NR 10 C(O)NR 9 R 8 , -NR 9 R 8 , -NR 10 CO 2 R 8 , -SR 8 , -S(O)R 8 , -S(O) 2 R 8 , -S(O) 2 NR 9 R 8 , -NR 10 S(O) 2 R 8 , substituted or unsubstituted C 6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl and substituted or unsubstituted 3- to 10-membered heterocyclyl;
    • 提供了作为CCR2受体的有效拮抗剂的化合物。 化合物通常为芳基磺酰胺衍生物,并且可用于药物组合物,用于治疗CCR2-介导的疾病的方法和用于鉴定CCR2拮抗剂的测定中的对照。 式(I)的化合物或其盐:其中:R 1和R 2各自独立地为氢,卤素,C 1-8烷基,-CN。 或C 1-8卤代烷基,条件是R 11或R 2中的至少一个不是氢; 每个R 3独立地是氢; R4是氢; R5是卤素或C1-8烷基; R6是氢; X1为CR7,N或NO; X2和X4为N或NO; X3是CR7; X 6和X 7各自独立地选自CR 7,N和NO; 每个R 7独立地选自氢,卤素,取代或未取代的C 2-8烷基,取代或未取代的C 2-8烷基,取代或未取代的C 2-8炔基-CN。 = O,-NO 2,-OR 6,-OC(O)R 8,-CO 2 R 8,-C(O)R 8,-C(O)NR 0 R 8,-OC(O)NR 9 R 8,-NR 10 C(O) O)NR9R8,-NR9R8,-NR10CO2R8,-SR8,-S(O)R8,-S(O)2R8,-S(O)2NR9R8,-NR10S(O)2R8,取代或未取代的C6-10芳基, 或未取代的5-至10-元杂芳基和取代或未取代的3-至10-元杂环基;