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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。
    • 9. 发明公开
    • 신규 티오카르밤산 유도체 및 이를 함유하는 약제학적조성물
    • 作为VANILLOID受体(VR)的拮抗剂和含有该化合物的药物组合物的甲硫氨酸衍生物
    • KR1020020030010A
    • 2002-04-22
    • KR1020010050094
    • 2001-08-20
    • 주식회사 아모레퍼시픽그룹
    • 서영거오우택김희두이지우박형근박영호이정범
    • C07C333/02
    • C07D333/20A61K31/165A61K31/17A61K31/175C07C271/12C07C311/08C07C327/44C07C333/04C07C333/08C07C335/12C07D209/08C07D213/40C07D213/73C07D213/75C07D213/79
    • PURPOSE: A thiocarbamate derivative as an antagonist for vanilloid receptor(VR) and a pharmaceutical composition containing the same compound are provided, thereby effectively inhibiting the diseases associated with the activation of vanilloid receptor(VR). CONSTITUTION: The thiocarbamate derivative as an antagonist for vanilloid receptor(VR) is represented by formula(I), in which R1 is Ar'-(CH3)m- wherein Ar' is phenyl substituted or unsubstituted with halogen or C1 to C5 lower alkyl, pyridinyl, thiophenyl, naphthalenyl or trifluoromethylphenyl and m is 1, 2, 3 or 4, or -(CH2)n-CHPh2, -CH2CH2CH(Ph)CH2Ph wherein n is 1 or 2; Y is S or O; Z is O, -CH2, NR3, CHR3 wherein R3 is hydrogen, C1 to C5 lower alkyl, benzyl or penethyl; R2 is hydrogen, C1 to C6 lower alkyl or cycloalkyl, dimethyl or Ar"-(CH2)p wherein Ar" is phenyl substituted or unsubstituted with halogen or trifluoromethyl, or pyridinyl substituted or unsubstituted with carboxyl, amino, methansulfonylamino or t-butoxycarbonyl, imidazol or indolyl wherein p is 0, 1, 2, 3 or 4; A is O or -CH2; and Ar is a compound wherein R4 and R5 is the same or different, and hydrogen, hydroxy, methoxy, nitro, cyano, benzyloxy, amino, methansulfonylamino, halogen, C1 to C5 lower alkyl, -NHCO2CH3, -NHC(=O)CH3, trifluoromethyl, sulfamoyl, carboxyl, -OCH2OCH3 or methoxycarbonyl, pyridine substituted or unsubstituted with carboxyl, amino, methansulfonylamino, penethylaminocarbonyl or t-butoxycarbonyl, indolyl or imidazolyl.
    • 目的:提供作为香草素受体(VR)拮抗剂的硫代氨基甲酸酯衍生物和含有相同化合物的药物组合物,从而有效抑制与香草素受体(VR)的活化相关的疾病。 构成:作为香草素受体(VR)的拮抗剂的硫代氨基甲酸酯衍生物由式(I)表示,其中R 1是Ar' - (CH 3)m - ,其中Ar'是被卤素取代或未取代的苯基或C 1至C 5的低级烷基 ,吡啶基,噻吩基,萘基或三氟甲基苯基,m为1,2,3或4,或 - (CH 2)n -CHCH 2,-CH 2 CH 2 CH(Ph)CH 2 Ph,其中n为1或2; Y为S或O; Z为O,-CH2,NR3,CHR3,其中R3为氢,C1至C5低级烷基,苄基或penethyl; R 2是氢,C 1至C 6低级烷基或环烷基,二甲基或Ar“ - (CH 2)p,其中Ar”是被卤素或三氟甲基取代或未取代的苯基,或被羧基,氨基,甲磺酰氨基或叔丁氧基羰基取代或未取代的吡啶基, 咪唑或吲哚基,其中p为0,1,2,3或4; A为O或-CH 2; 并且Ar是其中R 4和R 5相同或不同的化合物,氢,羟基,甲氧基,硝基,氰基,苄氧基,氨基,甲磺酰氨基,卤素,C1至C5低级烷基,-NHCO2CH3,-NHC(= O)CH3 三氟甲基,氨磺酰基,羧基,-OCH 2 OCH 3或甲氧基羰基,用羧基取代或未取代的吡啶,氨基,甲磺酰氨基,苯乙基氨基羰基或叔丁氧基羰基,吲哚基或咪唑基。