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    • 2. 发明公开
    • 레시니페라톡신 약리기를 함유하여 강력한 바닐로이드수용체의 효현제 및 진통제로서 사용하는 바닐로이드동족체 및 이를 함유하는 약학적 조성물
    • 含有葡萄糖苷酸药物的VANILLOID类似物作为血清VANILLOID受体激动剂及其组合物及其用途
    • KR1020010014495A
    • 2001-02-26
    • KR1020000008164
    • 2000-02-21
    • 이지우주식회사 아모레퍼시픽그룹
    • 이지우오우택박영호서영거박형근김희두
    • C07C217/00
    • PURPOSE: Provided is a vanilloid analogue which contains resiniferatoxin pharmacophores so as to be useful as a potent vanilloid receptor agonists and analgesics. Also, a pharmaceutical composition is provided which contains an effective amount of the same, as an active ingredient and a pharmaceutically acceptable carrier, and which is used for treating bladder hypersensitivity. CONSTITUTION: A vanilloid analogue is represented by the formula (1) wherein, X is an oxygen atom or a sulfur atom; A is -NHCH2- or -CH2; R1 is a substituted or unsubstituted alkylaryl group having 1-4 carbons, or R4CO-(in which, R4 is an alkyl group having 1-18 carbons, an alkenyl group having 2-18 carbons, or a substituted or unsubstituted aryl group having 6-10 carbons); R2 is a hydrogen atom, an alkyl group having 1-6 carbons, an alkoxy group having 1-6 carbons, a haloalkyl group having 1-6 carbons or a halogen atom; R3 is a hydrogen atom, an alkyl group having 1-4 carbons, an amino alkyl group, a diacid monoester group, or an alpha-alkylacid group; and * represents a chiral carbon atom.
    • 目的:提供含有树脂毒素药效学的香草素类似物,以便用作有效的香草素受体激动剂和镇痛药。 此外,提供含有有效量的作为活性成分和药学上可接受的载体的药物组合物,其用于治疗膀胱过敏。 构成:香草素类似物由式(1)表示,其中X是氧原子或硫原子; A是-NHCH 2 - 或-CH 2; R1是取代或未取代的具有1-4个碳原子的烷基芳基或R4CO-(其中R4是具有1-18个碳原子的烷基,具有2-18个碳原子的链烯基或具有6个碳原子的取代或未取代的芳基 -10碳); R2是氢原子,具有1-6个碳的烷基,具有1-6个碳原子的烷氧基,具有1-6个碳原子的卤代烷基或卤素原子; R3是氢原子,具有1-4个碳原子的烷基,氨基烷基,二酸单酯基或α-烷基酸基; 和*表示手性碳原子。