Abstract:
본 발명은 바닐로이드 수용체(Vanilloid Receptor; VR)에 대한 조절제로서 신규한 티오우레아 유도체 및 이를 함유하는 약제학적 조성물에 관한 것이다. 바닐로이드 수용체의 활성과 연관된 질환에는 통증, 급성 통증, 만성 통증, 신경병적 통증, 수술후 통증, 편두통, 관절통, 신경병증, 신경손상, 당뇨병성 신경병, 신경변성 질환, 신경성 피부질환, 뇌졸중, 방광과민증, 과민성 장증후군, 천식과 만성폐색성 폐질환등 호흡기 이상, 피부, 눈, 점막의 자극, 발열, 위-십이지장궤양, 염증성 장 질환 및 염증성 질환 등이 포함될 수 있다. 본 발명은 이들 질환의 예방, 치료를 위한 약제학적 조성물을 제공한다. 바닐로이드 수용체, 티오우레아 유도체, 통증, 염증, 궤양
Abstract:
PURPOSE: A composition containing soybean extract isolated with low alcohol is provided to improve blood circulation and to treat obesity, diabetes, and hyperlipidemia. CONSTITUTION: A composition for improving blood circulation contains soybean extract isolating with 1-7% of C1-5 alcohol or fraction. The C1-5 alcohol is methanol, ethanol, isopropylalcohol, n-propylalcohol, n-butanol or isobutanol. The soybean extract or fraction contains adenosine. The fraction is an ethylacetate or butanol fraction. The composition suppresses thrombosis or cholesterol generation.
Abstract translation:目的:提供含有用低分子量分离的大豆提取物的组合物,以改善血液循环和治疗肥胖症,糖尿病和高脂血症。 构成:用于改善血液循环的组合物含有用1-7%的C1-5醇或级分分离的大豆提取物。 C 1-5醇是甲醇,乙醇,异丙醇,正丙醇,正丁醇或异丁醇。 大豆提取物或级分含有腺苷。 馏分是乙酸乙酯或丁醇馏分。 该组合物抑制血栓形成或胆固醇的产生。
Abstract:
PURPOSE: A compound as a vinilloid receptor antagonist, an isomer thereof, and a pharmaceutical composition containing thereof are provided to secure the remarkably improved balance of the vinilloid receptor 1 activity and the PK properties. CONSTITUTION: A compound, an isomer thereof, and pharmaceutically acceptable salt thereof has the structure marked with chemical formula 1. In the chemical formula 1, R1 is hydrogen, methyl, or ethyl. R2 and R3 are independently, the hydrogen, halogen, cyano, the methyl, the ethyl, methoxy, trifluoromethyl, vinyl, or acetylenyl. R4 is either the trifluoromethyl or fluoro.
Abstract:
PURPOSE: A novel compound which functions as a vanilloid receptor 1(VR1) antagonist is provided to prevent or treat disease related to hair growth, rhinitis, and pancreatitis. CONSTITUTION: A vanilloid receptor antagonist compound is denoted by chemical formula I. A pharmaceutical composition contains the compound, isomer, or pharmaceutically acceptable salt thereof. The composition is used for preventing or treating arthritis disease, neuropathy, HIV related neuropathy, nerve injury, neurodegeneration, cerebral apoplexy, urinary incontinence, cough, neuropathy/allergy/inflammation skin disease, atopic dermatitis, psoriasis, pruritus, the prurigo, acouesthesia, aliasing, bregma anaphylaxis, effluvium, or alopecia.
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.