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18 条记录 (耗时 0.017 秒)

    Tetrahydropyridine derivatives acting on muscarinic acetylcholine receptors
    2.
    发明授权
    Tetrahydropyridine derivatives acting on muscarinic acetylcholine receptors 失效
    作用于毒蕈碱乙酰胆碱受体的四氢吡啶衍生物

    公开(公告)号：US06716857B2

    公开(公告)日：2004-04-06

    申请号：US10273630

    申请日：2002-10-18

    申请人： Youseung Kim ,  Soon Bang Kang ,  Gyochang Keum ,  Min Seok Jang ,  Jae Yang Kong ,  Dae Young Jeong

    发明人： Youseung Kim ,  Soon Bang Kang ,  Gyochang Keum ,  Min Seok Jang ,  Jae Yang Kong ,  Dae Young Jeong

    IPC分类号： A61K3144

    CPC分类号： C07D401/06

    摘要： The present invention relates to novel tetrahydropyridine derivatives of formula 1 having an appropriately substituted pyrrolidinone and oxime, wherein m is 0 or 1, n is 1 or 2, R1 is hydrogen, C1-4alkyl, C2-4 alkynyl or aryl, R3 is C1-4 alkyl, which show high efficacy, low cholinergic adverse effects and high affinity for muscarinic acetylcholine receptor; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.

    摘要翻译： 本发明涉及具有适当取代的吡咯烷酮和肟的式1的新的四氢吡啶衍生物，其中m为0或1，n为1或2，R 1为氢，C 1-4烷基，C 2-4炔基或芳基， R 3是C 1-4烷基，其显示出高效力，低胆碱能不良反应和对毒蕈碱性乙酰胆碱受体的高亲和力; 及其药学上可接受的盐; 制备方法; 和包含这些化合物或盐的药物组合物。

    Method for the preparation of pyrido benzoxazine derivatives
    3.
    发明授权
    Method for the preparation of pyrido benzoxazine derivatives 失效
    吡啶并苯并恶嗪衍生物的制备方法

    公开(公告)号：US5952494A

    公开(公告)日：1999-09-14

    申请号：US443884

    申请日：1995-05-26

    申请人： Youseung Kim ,  Soon Bang Kang ,  Seonhee Park

    发明人： Youseung Kim ,  Soon Bang Kang ,  Seonhee Park

    IPC分类号： C07D498/06

    CPC分类号： C07D498/06

    摘要： There is disclosed a method for the preparation of pyrido benzoxazine derivative having the following formula I, that is improved in both production coat and yield.The method comprises reacting a compound of the following general formula II with tetraalkyl ammonium fluoride or with a mixture of tetraalkyl ammonium halide and metal fluoride in an organic solvent at a reaction temperature of about 30 to about 100.degree. C. for 1 to 3 hours under stirring; and reacting the resulting solution with a metal hydroxide or a metal carboxylate dissolved in water or in a mixture of water and alcohol, for 1 to 3 hours under heat. ##STR1## wherein X is a fluorine or chlorine atom and X.sub.1 and X.sub.2 each is a halogen atom or a nitro group, R is an alkyl group containing 1 to 4 carbon atoms and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each is an alkyd group or allyl group containing 1 to 8 carbon atoms.

    摘要翻译： 公开了制备具有下式I的吡啶并苯并恶嗪衍生物的方法，其在生产涂层和产率方面都得到改善。 该方法包括将下列通式II的化合物与四烷基氟化铵或四烷基卤化铵和金属氟化物的混合物在有机溶剂中在约30至约100℃的反应温度下反应1-3小时， 搅拌 并将所得溶液与溶于水中或在水和醇的混合物中的金属氢氧化物或金属羧酸酯反应1至3小时。 其中X为氟或氯原子，X 1和X 2各自为卤原子或硝基，R为含有1至4个碳原子的烷基，R 1，R 2，R 3和R 4各自为醇酸基或含烯丙基 1至8个碳原子。

    Method for the preparation of (-)piperazine benzoxazine derivatives
    7.
    发明授权
    Method for the preparation of (-)piperazine benzoxazine derivatives 失效
    （ - ）哌嗪苯并恶嗪衍生物的制备方法

    公开(公告)号：US5539110A

    公开(公告)日：1996-07-23

    申请号：US321360

    申请日：1994-10-11

    申请人： Youseung Kim ,  Soon Bang Kang ,  Seonhee Park

    发明人： Youseung Kim ,  Soon Bang Kang ,  Seonhee Park

    IPC分类号： C07D498/06

    CPC分类号： C07D498/06

    摘要： There is disclosed a method for the preparation of the antibacterial (-) piperazine benzoxazine derivative having formula I comprising the steps of reacting (+)2-aminomethylene-3-oxo-3-phenylpropionate derivative of formula II with a base in an organic polar solvent, to give a (-) benzoxazine derivative of formula III: and reacting the (-) benzoxazine derivative of formula III with a piperazine derivative of formula IV in an organic polar solvent. ##STR1##

    摘要翻译： 公开了制备具有式I的抗菌（ - ）哌嗪苯并恶嗪衍生物的方法，包括使式II的（+）2-氨基亚甲基-3-氧代-3-苯基丙酸酯衍生物与有机极性的碱反应的步骤 溶剂，得到式III的（ - ）苯并恶嗪衍生物，并使式III的（ - ）苯并恶嗪衍生物与式Ⅳ的哌嗪衍生物在有机极性溶剂中反应。 （一）图像（二）<图像>（三）

    (+) 2-benzoyl-3-(silyloxyprop-2(S)-yl)aminoacrylate derivatives and a method for preparing the same
    8.
    发明授权
    (+) 2-benzoyl-3-(silyloxyprop-2(S)-yl)aminoacrylate derivatives and a method for preparing the same 失效
    （+）2-苯甲酰基-3-（silyloxyprop-2（S） - 基）氨基丙烯酸酯衍生物及其制备方法

    公开(公告)号：US5516926A

    公开(公告)日：1996-05-14

    申请号：US452167

    申请日：1995-05-26

    申请人： Youseung Kim ,  Soon Bang Kang ,  Seonhee Park

    发明人： Youseung Kim ,  Soon Bang Kang ,  Seonhee Park

    IPC分类号： C07F7/10 ,  C07F7/18

    CPC分类号： C07F7/1852

    摘要： (+)2-benzoyl-3-(silyloxyprop-2(S)-yl)aminoacrylate derivative of following formula I which can be an useful starting material for producing a potent antibacterial compound and a method for the preparation of the same: ##STR1## wherein X is fluoro or chloro; X.sub.1 and X.sub.2 can be halogen or nitro; and R, R.sub.1, R.sub.2 and R.sub.3 each can be C.sub.1-8 alkyl group.

    摘要翻译： 可以作为制备有效抗菌化合物的有用原料的下式I的（+）2-苯甲酰基-3-（甲硅烷氧基-2（S） - 基）氨基丙烯酸酯衍生物及其制备方法（I）其中X是氟或氯; X1和X2可以是卤素或硝基; 并且R，R 1，R 2和R 3各自可以是C 1-8烷基。

    Process for preparation of (-)3(S)-methylbenzoxazine derivative
    10.
    发明授权
    Process for preparation of (-)3(S)-methylbenzoxazine derivative 失效
    （ - ）3（S） - 甲基苯并恶嗪衍生物的制备方法

    公开(公告)号：US5756731A

    公开(公告)日：1998-05-26

    申请号：US613299

    申请日：1996-03-11

    申请人： Youseung Kim ,  Soon Bang Kang ,  Eu Jin Ahn

    发明人： Youseung Kim ,  Soon Bang Kang ,  Eu Jin Ahn

    IPC分类号： B01J23/40 ,  B01J23/42 ,  B01J23/44 ,  C07B43/04 ,  C07B53/00 ,  C07B55/00 ,  C07B61/00 ,  C07D265/36

    CPC分类号： C07D265/36

    摘要： A process for preparing (-)3(S)-methylbenzoxazine derivative of formula (I) comprising the steps of reacting the compound of formula (II) with benzoic acid, triphenylphosphine and diethyl azodicarboxylate in an organic solvent to obtain the compound of formula (III); hydrogenating the compound of formula (III) in the presence of a metallic catalyst to provide the compound of formula (IV); hydrolyzing the compound of formula (IV) to give the compound of formula (V); and reacting the compound of formula (V) with diethyl azodicarboxylate, triphenylphosphine, and zinc chloride in an organic solvent. The obtained (-)3(S)-methylbenzoxazine derivative is a useful intermediate for preparing an antibacterial agent which has a potent bacteriocidal effect. ##STR1##

    摘要翻译： 制备式（I）的（ - ）3（S） - 甲基苯并恶嗪衍生物的方法，包括使式（II）化合物与苯甲酸，三苯基膦和偶氮二羧酸二乙酯在有机溶剂中反应，得到式 III）; 在金属催化剂存在下氢化式（III）化合物，得到式（Ⅳ）化合物; 水解式（Ⅳ）化合物，得到式（Ⅴ）化合物; 并在有机溶剂中使式（Ⅴ）化合物与偶氮二羧酸二乙酯，三苯基膦和氯化锌反应。 得到的（ - ）3（S） - 甲基苯并恶嗪衍生物是制备具有强效杀菌作用的抗菌剂的有用中间体。 （I）（II）（III）（IV）（V）\！