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434 条记录 (耗时 0.016 秒)

    Cinnoline-3-carboxylic acid derivatives as 5-HT3 antagonists
    71.
    发明公开
    Cinnoline-3-carboxylic acid derivatives as 5-HT3 antagonists 失效
    噌啉-3-碳酸酯5-HT3拮抗剂。

    公开(公告)号：EP0560604A1

    公开(公告)日：1993-09-15

    申请号：EP93301843.4

    申请日：1993-03-11

    申请人： Mitsubishi Chemical Corporation

    发明人： Maruyama, Akira ,  Ogawa, Shigeru ,  Yamazaki, Satoshi ,  Tobe, Akihiro

    IPC分类号： C07D451/04 ,  A61K31/435 ,  C07D451/06 ,  C07D453/02

    CPC分类号： C07D451/04 ,  C07D451/06 ,  C07D453/02

    摘要： A novel cinnoline derivative having an antagonistic activity against serotonin 5-HT 3 receptor, its pharmaceutically acceptable salts, its N-oxide derivatives or solvates thereof, and pharmaceutical formulations containing the same for the prevention and/or treatment of various disorders such as nausea and/or emesis caused by anticancer drugs or the X-ray treatment, central nervous disorders such as anxiety and/or neuropathy, gastroenteric diseases such as indigestion, chronic gastritis, digestive ulcer and irritable bowel syndromes, hemicrania cluster headache, trigeminal neuralgia or arrhythmia has the following formula :

    摘要翻译： 对5-羟色胺5-HT 3受体具有拮抗活性的新颖的噌啉衍生物，其药学上可接受的盐，其N-氧化物衍生物或溶剂化物，以及含有其的预防和/或治疗各种疾病如恶心和/ 或由抗癌药物或X线治疗引起的呕吐，焦虑和/或神经病变等中枢神经障碍，消化不良，慢性胃炎，消化性溃疡和肠易激综合征等胃肠疾病，脑血管性头痛，三叉神经痛或心律不齐等， 以下公式： g

    2-piperidino-1-alkanol derivatives as antiischemic agents
    76.
    发明公开
    2-piperidino-1-alkanol derivatives as antiischemic agents 失效
    2-哌啶子基-1-链烷醇 - 衍生物抗血清Wirkstoffe。

    公开(公告)号：EP0398578A2

    公开(公告)日：1990-11-22

    申请号：EP90304975.7

    申请日：1990-05-09

    申请人： PFIZER INC.

    发明人： Chenard, Bertrand Leo

    IPC分类号： C07D451/02 ,  A61K31/33 ,  A61K31/695 ,  C07D211/54 ,  C07D211/48 ,  C07D491/10 ,  C07D451/06 ,  C07D207/12 ,  C07F7/18

    CPC分类号： C07D451/02 ,  C07D211/48 ,  C07D211/52 ,  C07D211/54 ,  C07D211/70 ,  C07D451/04 ,  C07D451/06

    摘要： 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula
    wherein Q is S or CH=CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y 1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y 1 are taken separately and Y is hydrogen or OH, and Y 1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

    摘要翻译： 其中Q是S或CH = CH的式（CHEM）的2-（8-氮杂双环[3.2.1]辛-8-基） X为H，OH或其它芳香取代基; R是氢，烷基，烯基或炔基; Y和Y 1相同，分别为芳基亚甲基或芳烷基亚甲基（或相应的环氧衍生物）或Y和Y 1，Y为氢或OH，Y 1为芳基，芳烷基，芳硫基， 或芳氧基; 和结构相关的2-（哌啶子基）链烷醇; 药物组合物; 治疗CNS疾病的方法; 和可用于制备所述化合物的中间体。

    Novel compounds
    78.
    发明公开
    Novel compounds 失效
    新的连接。

    公开(公告)号：EP0235878A2

    公开(公告)日：1987-09-09

    申请号：EP87300192.9

    申请日：1987-01-09

    申请人： BEECHAM GROUP PLC

    发明人： King, Francis David Beecham Pharmaceuticals

    IPC分类号： C07D451/04 ,  C07D451/06 ,  C07D451/14 ,  C07D453/02 ,  A61K31/435 ,  A61K31/46

    CPC分类号： C07D451/04 ,  C07D451/06 ,  C07D451/14 ,  C07D453/02

    摘要： Compounds of formula (I), and pharmaceutically acceptable salts thereof:
    wherein

    L is NH or O;

    X is a moiety capable of hydrogen bonding to the NH group depicted in formula (I);

    R₁ and R₂ are independently selected from hydrogen, halogen, CF₃, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, C 1-7 acyl, C 1-7 acylamino, C 1-6 alkylsulphonylamino, N-(C 1-6 alkylsulphonyl)-N-C 1-4 alkylamino, C 1-6 alkylsulphinyl, carboxy, C 1-6 alkoxycarbonyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C 1-4 alkylamino optionally N-substituted by one or two groups selected from C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl groups or optionally N-disubstituted oy C 4-5 polymethylene; and
    Z is a group of formula (a), (b) or (c)
    wherein n is 2 or 3; p is l or 2; q is l to 3; r is l to 3: and
    R₃ or R₄ is C 1-7 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-2 alkyl or C 2-7 alkenyl-C 1-4 alkyl; having 5-HT M-receptor antagonist activity, a process for their preparation and their use as pharmaceuticals.

    Neues Nortropinderivat, Verfahren zu seiner Herstellung und seine Verwendung
    80.
    发明公开
    Neues Nortropinderivat, Verfahren zu seiner Herstellung und seine Verwendung 失效
    新Nortropinderivat，其制备方法及其使用的过程。

    公开(公告)号：EP0128437A2

    公开(公告)日：1984-12-19

    申请号：EP84106030.4

    申请日：1984-05-26

    申请人： BOEHRINGER INGELHEIM KG ,  BOEHRINGER INGELHEIM INTERNATIONAL GmbH

    发明人： Banholzer, Rolf, Dr.

    IPC分类号： C07D451/06 ,  C07D451/10

    CPC分类号： C07D451/06 ,  C07D451/10

    摘要： Die Erfindung betrifft die als Zwischenprodukt zur Herstellung wertvoller Pharmazeutika (z.B. spasmolytisch und bronchospasmolytisch wirksamer quartärer Benzilsäure-N-ß-fluorethylnortropinester) oder auch als pharmazeutischer Wirkstoff geeignete Verbindung N-ß-Fluorethylnortropin.
    Diese Verbindung kann beispielsweise durch N-Alkylierung von Nortropin mit 2-Bromfluorethan hergestellt werden.
    Ihre Acylierung mit Benzilsäureimidazolid führt zum Benzilsäure-N-β-fluorethylnortropinester, der seinerseits mit Quaternierungsmitteln zu den pharmakologisch interessanten quartären Benzilsäure-N-ß-fluorethylnortropinestern umgesetzt werden kann.

    摘要翻译： 本发明涉及一种中间有价值药物（例如，解痉和bronchospasmolytisch有效季苄酸-N-β-fluorethylnortropinester）的制备或作为药物合适的化合物是N-β-Fluorethylnortropin。 该化合物例如可以通过降托品的N-烷基化用2- Bromfluorethan来制备。 您与Benzilsäureimidazolid导致苄酸-N-β-fluorethylnortropinester，这反过来又可以与季铵化剂的药理上有用的季苄酸-N-β-fluorethylnortropinestern反应酰化。