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    바닐로이드 수용체 길항물질로서의 신규 화합물, 이의이성체 또는 이의 약학적으로 허용가능한 염, 및 이를함유하는 약학 조성물
    2.
    发明公开
    바닐로이드 수용체 길항물질로서의 신규 화합물, 이의이성체 또는 이의 약학적으로 허용가능한 염, 및 이를함유하는 약학 조성물 有权
    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

    公开(公告)号：KR1020080007329A

    公开(公告)日：2008-01-18

    申请号：KR1020077024002

    申请日：2006-03-15

    Applicant: (주)아모레퍼시픽

    Inventor： 김희두 ,  서영거 ,  박형근 ,  오우택 ,  박설린 ,  김주현 ,  장미정 ,  박영호 ,  신송석 ,  김선영 ,  김진관 ,  정연수 ,  이기화 ,  최진규 ,  임경민 ,  고현주 ,  모주현 ,  김성일 ,  우병영

    IPC: C07C275/24 ,  C07C275/18 ,  A61K31/17

    CPC classification number: C07C275/24 ,  C07C311/08 ,  C07C311/11 ,  C07C323/62 ,  C07D211/46 ,  C07D295/088 ,  C07D295/155 ,  C07D309/12 ,  C07F7/0818

    Abstract: A compound as a vanilloid receptor antagonist is provided to obtain a pharmaceutical composition effective for preventing or treating pain, migraine, arthralgia, nerve injury, skin diseases, overactive bladder, irritable bowel syndrome, or the like. A compound as a vanilloid receptor antagonist, an isomer or a pharmaceutically acceptable salt thereof is represented by the following formula I. In formula I, X is NHCH2, CR11=CR12, NH, CHR11CHR12 or C=C, wherein each of R11 and R12 represents H, halogen, C1-C5 alkyl, C1-C5 alkoxy, halo(C1-C5)alkyl or phenyl; R1 is a C2-C5 alkenyl or C2-C5 alkynyl; R2 is H, halogen, nitro, cyano, C1-C5 alkyl, C1-C5 alkoxy, halo(C1-C5)alkyl, C2-C5 alkenyl, or C2-C5 alkynyl; R2 is H, halogen, nitro, cyano, C1-C5 alkyl, C1-C5 alkoxy, halo(C1-C5)alkyl, C2-C5 alkenyl, C2-C5 alkynyl, carboxyl, C1-C5 alkoxycarbonyl, C1-C5 alkylthio, phenyl or phenyl(C1-C3)alkyl, wherein is each phenyl group is non-substituted or substituted with at least one substituent; 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, hydroxy, C2-C5 alkenyloxy, C1-C5 alkoxy(C1-C5)alkoxy, C1-C5 alkoxy(C1-C5)alkoxy(C1-C5)alkyl, C1-C3 alkylpiperazinyl, piperazinyl(C1-C5)alkoxy, piperidinyl(C1-C5)alkoxy, C1-C5 alkoxy (C1-C5)alkylamino, C1-C7 alkylamino, morpholinyl, morpholinyl(C1-C5)alkyloxy, tetrahydropyranyloxy, phenyl or halogen, wherein each phenyl group is non-substituted or substituted with at least one substituent; each of R9 and R10 independently represents H, -SO2R13, -SOR13, C1-C5 alkyl, C1-C5 alkoxy, halo (C1-C5)alkyl, C2-C5 alkenyl, C1-C5 alkoxycarbonyl, C1-C5 alkylthio, phenyl or phenyl (C1-C3)alkyl, wherein each phenyl group is non-substituted or substituted with at least one substituent, and R13 is H, amino, C1-C5 alkyl, C2-C5 alkenyl, C1-C5 alkoxy, halo(C1-C5)alkyl, trifluoromethyl, phenyl or phenyl(C1-C3)alkyl.

    Abstract translation: 提供作为香草素受体拮抗剂的化合物以获得有效预防或治疗疼痛，偏头痛，关节痛，神经损伤，皮肤疾病，膀胱过度活动症，肠易激综合征等的药物组合物。 作为香草酸受体拮抗剂的化合物，其异构体或其药学上可接受的盐由下式I表示。在式I中，X为NHCH 2，CR 11 = CR 12，NH，CHR 11 CHR 12或C = C，其中R 11和R 12 表示H，卤素，C 1 -C 5烷基，C 1 -C 5烷氧基，卤代（C 1 -C 5）烷基或苯基; R1是C2-C5烯基或C2-C5炔基; R2是H，卤素，硝基，氰基，C1-C5烷基，C1-C5烷氧基，卤代（C1-C5）烷基，C2-C5烯基或C2-C5炔基; R2是H，卤素，硝基，氰基，C1-C5烷基，C1-C5烷氧基，卤代（C1-C5）烷基，C2-C5烯基，C2-C5炔基，羧基，C1-C5烷氧羰基，C1-C5烷硫基， 苯基或苯基（C1-C3）烷基，其中每个苯基是未取代的或被至少一个取代基取代; R3是H，C1-C5烷基，C1-C5烷氧基或卤代（C1-C5）烷基; R 4，R 5，R 6，R 7和R 8各自独立地表示H，羧基，C 1 -C 5烷基，硝基，C 2 -C 5烯基，C 1 -C 5烷氧基，C 2 -C 5炔基，卤代（C 1 -C 5）烷基，C 1 -C 5烷硫基 ，C1-C5烷基磺酰基，C1-C5烷基羰基，C1-C5烷氧基羰基，羟基，C2-C5链烯氧基，C1-C5烷氧基（C1-C5）烷氧基，C1-C5烷氧基（C1-C5）烷氧基（C1-C5）烷基 （C1-C5）烷氧基，C1-C5烷氧基（C1-C5）烷基氨基，C1-C7烷基氨基，吗啉基，吗啉基（C1-C5）烷氧基，四氢吡喃基氧基， 苯基或卤素，其中每个苯基未被取代或被至少一个取代基取代; R 9和R 10各自独立地表示H，-SO 2 R 13，-SOR 13，C 1 -C 5烷基，C 1 -C 5烷氧基，卤代（C 1 -C 5）烷基，C 2 -C 5烯基，C 1 -C 5烷氧基羰基，C 1 -C 5烷硫基，苯基或 苯基（C1-C3）烷基，其中每个苯基未被取代或被至少一个取代基取代，R 13是H，氨基，C 1 -C 5烷基，C 2 -C 5烯基，C 1 -C 5烷氧基，卤代（C1- C5）烷基，三氟甲基，苯基或苯基（C1-C3）烷基。

    바닐로이드 수용체 길항물질로서의 신규 화합물, 이의이성체 또는 이의 약학적으로 허용가능한 염, 및 이를함유하는 약학 조성물
    3.
    发明公开
    바닐로이드 수용체 길항물질로서의 신규 화합물, 이의이성체 또는 이의 약학적으로 허용가능한 염, 및 이를함유하는 약학 조성물 有权
    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

    公开(公告)号：KR1020070114821A

    公开(公告)日：2007-12-04

    申请号：KR1020077024004

    申请日：2006-03-17

    Applicant: (주)아모레퍼시픽

    Inventor： 서영거 ,  김희두 ,  박형근 ,  오우택 ,  이용실 ,  박설린 ,  유정현 ,  박영호 ,  신송석 ,  김선영 ,  김진관 ,  정연수 ,  이기화 ,  최진규 ,  임경민 ,  고현주 ,  모주현 ,  김성일 ,  배준호

    IPC: C07C275/24 ,  C07C275/18 ,  A61K31/17

    CPC classification number: C07C275/24 ,  C07C311/08 ,  C07C311/11 ,  C07C323/62 ,  C07D211/46 ,  C07D295/088 ,  C07D295/155 ,  C07D309/12 ,  C07F7/0818

    Abstract: 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.

    Abstract translation: 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。

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