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:
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:
본 발명은 후보 물질을 처리한 피부 각질 세포에서 연장 효소(elongase)의 발현 정도를 확인하는 단계를 포함하는 아토피 피부염 개선용 물질 스크리닝 방법을 개시한다. 또한 본 발명은 피부의 연장 효소 발현 정도 분석부를 포함하는 아토피 피부염 진단 키트를 개시한다.
Abstract:
PURPOSE: A novel compound is provided to prevent or treat diseases mediated by a cannabinoid 1 receptor. CONSTITUTION: A compound of chemical formula 1 or a prodrug, an isomer, a pharmaceutically acceptable salt, a hydrate, or a solvate thereof is provided. A pharmaceutical composition contains the compound of chemical formula 1, the prodrug, the isomer, the pharmaceutically acceptable salt, the hydrate, or the solvate thereof. The pharmaceutical composition is used for preventing or treating diseases mediated by cannabinoid 1 receptor. The diseases medicated by cannabinoid 1 receptor are obesity.
Abstract:
본 발명은 바닐로이드 수용체(바닐로이드 수용체 1; VR1; TRPV1) 길항물질로서의 신규 화합물, 이의 이성체 또는 이의 약학적으로 허용가능한 염, 및 이를 함유하는 약학 조성물에 관한 것이다. 본 발명은 통증, 편두통, 관절통, 신경통, 신경병, 신경 손상, 피부 질환, 방광 과민증, 과민성 장 증후군, 긴급 배변, 호흡기 장애, 피부, 눈 또는 점막의 자극, 위-십이지장 궤양, 염증성 질환, 귀 질환, 또는 심장 질환과 같은 질환을 예방하거나 치료하기 위한 약학 조성물을 제공한다.
Abstract:
본 발명은 바닐로이드 수용체(바닐로이드 수용체 1; VR1; TRPV1) 길항물질로서의 신규 화합물, 이의 이성체 또는 이의 약학적으로 허용가능한 염, 및 이를 함유하는 약학 조성물에 관한 것이다. 본 발명은 통증, 편두통, 관절통, 신경통, 신경병, 신경 손상, 피부 질환, 방광 과민증, 과민성 장 증후군, 긴급 배변, 호흡기 장애, 피부, 눈 또는 점막의 자극, 위-십이지장 궤양, 염증성 질환, 귀 질환, 또는 심장 질환과 같은 질환을 예방하거나 치료를 위한 약학 조성물을 제공한다.
Abstract:
본 발명은 하기 화학식 1의 화합물, 그것의 이성질체 또는 약제학적으로 허용 가능한 염을 유효 성분으로 포함하는 피부 노화 방지용 조성물에 관한 것이다. (화학식 1)
본 발명에 따른 조성물에 포함되는 화학식 1의 화합물, 그것의 이성질체 또는 약제학적으로 허용 가능한 염은 피부 자극을 유발하지 않으면서, 신경 통증감각 수용체(TRPV1: Transient Receptor Potential family V 1) 길항제로 작용하여, 매트릭스 메탈로프로티아제(matrix metalloprotease) 활성 억제 효과를 발휘하는 바, 피부 노화 방지용 조성물의 유효 성분으로 적합하게 사용될 수 있다. 피부 노화 방지