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    • 11. 发明公开
    • 바닐로이드 수용체 길항물질로서의 신규 화합물, 이의이성체 또는 이의 약학적으로 허용가능한 염, 및 이를함유하는 약학 조성물
    • 新化合物,其异构体,或其药学上可接受的盐作为VANILLOID受体拮抗剂; 和含有它们的药物组合物
    • KR1020070114821A
    • 2007-12-04
    • KR1020077024004
    • 2006-03-17
    • (주)아모레퍼시픽
    • 서영거김희두박형근오우택이용실박설린유정현박영호신송석김선영김진관정연수이기화최진규임경민고현주모주현김성일배준호
    • C07C275/24C07C275/18A61K31/17
    • C07C275/24C07C311/08C07C311/11C07C323/62C07D211/46C07D295/088C07D295/155C07D309/12C07F7/0818
    • A compound as a vanilloid receptor antagonist is provided to obtain a high activity in preventing or treating pain, migraine, arthralgia, neuralgia, neural diseases, neural injury, skin diseases, irritable bowel syndrome, inflammatory diseases, cardiac diseases, etc. A compound as a vanilloid receptor antagonist is a compound represented by the following formula Ia or an isomer and/or pharmaceutically acceptable salt thereof. In formula Ia, X is CR11=CR12 or C=C, wherein each of R11 and R12 independently represents H, a halogen atom, C1-C5 alkyl or phenyl; each of R1 and R2 independently represents H, carboxyl, C1-C5 alkyl, halogen, nitro, C1-C5 alkoxy, halo(C1-C5)alkyl, C1-C5 alkylcarbonyl, C1-C5 alkylcarbonylamino, C1-C5 alkylsulfonylamino, phenylsulfonylamino, C1-C5 alkylthio, C1-C5 alkylsulfonyl or C1-C5 alkoxycarbonyl; R3 is H, C1-C5 alkyl, C1-C5 alkoxy or halo(C1-C5)alkyl; each of R4, R5, R6, R7 and R8 independently represents H, carboxyl, C1-C5 alkyl, nitro, C2-C5 alkenyl, C1-C5 alkoxy, C2-C5 alkynyl, halo(C1-C5)alkyl, C1-C5 alkylthio, C1-C5 alkylsulfonyl, C1-C5 alkylcarbonyl, C1-C5 alkoxycarbonyl, phenyl or halogen, wherein the phenyl is non-substituted or substituted with at least one substituent selected from carboxyl, C1-C5 alkyl, halogen, nitro, C2-C5 alkenyl, C1-C5 alkoxy, halo(C1-C5)alkyl, C1-C5 alkylcarbonyl, C1-C5 alkylthio, C1-C5 alkylsulfonyl and C1-C5 alkoxycarbonyl; R9 is C1-C5 alkylsulfonyl or C2-C5 alkenylsulfonyl; and R10 is H, with the proviso that when R3 is not H, R11 and R13 cannot represent H at the same time.
    • 提供了一种作为香草素受体拮抗剂的化合物,用于预防或治疗疼痛,偏头痛,关节痛,神经痛,神经疾病,神经损伤,皮肤病,肠易激综合征,炎性疾病,心脏病等中的高活性。 香草酸受体拮抗剂是由下式Ia表示的化合物或其异构体和/或其药学上可接受的盐。 在式Ia中,X是CR 11 = CR 12或C = C,其中R 11和R 12各自独立地表示H,卤素原子,C 1 -C 5烷基或苯基; R1和R2各自独立地表示H,羧基,C1-C5烷基,卤素,硝基,C1-C5烷氧基,卤代(C1-C5)烷基,C1-C5烷基羰基,C1-C5烷基羰基氨基,C1-C5烷基磺酰基氨基,苯基磺酰基氨基, C1-C5烷硫基,C1-C5烷基磺酰基或C1-C5烷氧基羰基; R3是H,C1-C5烷基,C1-C5烷氧基或卤代(C1-C5)烷基; R4,R5,R6,R7和R8各自独立地表示H,羧基,C1-C5烷基,硝基,C2-C5烯基,C1-C5烷氧基,C2-C5炔基,卤代(C1-C5)烷基,C1-C5 烷基硫代,C 1 -C 5烷基磺酰基,C 1 -C 5烷基羰基,C 1 -C 5烷氧基羰基,苯基或卤素,其中苯基是未取代的或被至少一个选自羧基,C 1 -C 5烷基,卤素,硝基, C5链烯基,C1-C5烷氧基,卤代(C1-C5)烷基,C1-C5烷基羰基,C1-C5烷硫基,C1-C5烷基磺酰基和C1-C5烷氧基羰基; R9为C1-C5烷基磺酰基或C2-C5链烯基磺酰基; R 10为H,条件是当R3不为H时,R11和R13不能同时表示H。