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82 条记录 (耗时 0.05 秒)

    Indole derivatives and their use
    71.
    发明授权
    Indole derivatives and their use 失效
    吲哚衍生物及其用途

    公开(公告)号：US5250538A

    公开(公告)日：1993-10-05

    申请号：US864734

    申请日：1992-04-07

    申请人： Lone Jeppesen ,  Peter H. Andersen ,  Louis B. Hansen ,  Peter Farrup ,  John B. Hansen

    发明人： Lone Jeppesen ,  Peter H. Andersen ,  Louis B. Hansen ,  Peter Farrup ,  John B. Hansen

    IPC分类号： C07D401/12 ,  C07D403/12 ,  A61K31/445

    CPC分类号： C07D401/12 ,  C07D403/12

    摘要： Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.

    摘要翻译： 式（I）的吲哚衍生物其中R 1，R 2，R 3和R 4可以是氢或任选被卤素取代的低级烷基; A1表示含有2至4个碳原子的直链或支链亚烷基链; R5是氢或直链或支链烷基; A2是含有2至6个碳原子的直链或支链，饱和或不饱和烃链; 并且R6被选自由各种结构组成的组，已被发现显示出中枢神经系统活性。

    HETEROAROMATIC GLUCOKINASE ACTIVATORS
    73.
    发明申请
    HETEROAROMATIC GLUCOKINASE ACTIVATORS 审中-公开
    异氟烷激酶

    公开(公告)号：US20110130402A1

    公开(公告)日：2011-06-02

    申请号：US13022937

    申请日：2011-02-08

    申请人： Lone Jeppesen ,  Marit Kristiansen

    发明人： Lone Jeppesen ,  Marit Kristiansen

    IPC分类号： A61K31/426 ,  C07D277/46 ,  C07D417/12 ,  C07D417/04 ,  C07D277/54 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/454 ,  A61P3/10

    CPC分类号： C07D277/46 ,  C07D277/54

    摘要： The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators which increase insulin secretion for the treatment of type II diabetes.

    摘要翻译： 本发明描述了2,3-二取代的N-杂芳族丙酰胺，其中3-位上的取代是任选取代的苯环，2-位上的取代是烷基或环烷基; 包含它们的药物组合物; 及其使用方法。 丙酰胺是增加胰岛素分泌以治疗II型糖尿病的葡糖激酶激活剂。

    Urea Glucokinase Activators
    74.
    发明申请
    Urea Glucokinase Activators 失效
    尿素葡萄糖激酶活化剂

    公开(公告)号：US20090105482A1

    公开(公告)日：2009-04-23

    申请号：US11994862

    申请日：2006-07-14

    申请人： Jesper Lau ,  Anthony Murray ,  Per Vedso ,  Marit Kristiansen ,  Lone Jeppesen

    发明人： Jesper Lau ,  Anthony Murray ,  Per Vedso ,  Marit Kristiansen ,  Lone Jeppesen

    IPC分类号： C07D277/54 ,  C07D285/135

    CPC分类号： C07D277/48

    摘要： The invention provides a compound of general formula (I) wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments.The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.

    摘要翻译： 本发明提供了通式（I）的化合物，其中取代基在本申请中进一步定义，以及在所附实施方案中描述的其它实施方案。 本发明还提供本发明化合物用于制备用于治疗各种疾病的药物的用途，例如， 用于治疗2型糖尿病。

    Heterocyclic compounds, their preparation and use
    78.
    发明授权
    Heterocyclic compounds, their preparation and use 失效
    杂环化合物，其制备和用途

    公开(公告)号：US5741785A

    公开(公告)日：1998-04-21

    申请号：US385250

    申请日：1995-02-08

    申请人： Lone Jeppesen

    发明人： Lone Jeppesen

    IPC分类号： A61K31/495 ,  A61P1/08 ,  A61P3/08 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  C07D487/04 ,  A61K31/675 ,  C07F9/576

    CPC分类号： C07D487/04

    摘要： Imidazo�1,2-a!quinoxalinone derivatives of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are the same or independently are H, alkyl, alkoxy, halogen, NO.sub.2, NH.sub.2, CF.sub.3, CN, SO.sub.2 CH.sub.3, SO.sub.2 CF.sub.3, SO.sub.2 NR'R" or a 5- or 6-membered N-containing heterocyclic ring, optionally substituted, and R', R" are independently H or alkyl; and R.sup.4 is H or CH.sub.2 -R.sup.6 ; and R.sup.6 is H, halogen, POR'"R"", NR.sup.7 R.sup.8 or a 5- or 6-membered N-containing heterocyclic ring optionally substituted, and R'", R"" are independently hydroxy or alkoxy; and ##STR2## R.sup.7, R.sup.8 are the same or independently are H, or alkyl optionally substituted; and n is 1, 2 or 3; R.sup.5 is ##STR3## and R.sup.9 is OH, alkoxy, H or NR.sup.10 R.sup.11 ; and R.sup.10, R.sup.11 are the same or independently are H, NH.sub.2 or OH; and X is O or S; and Y is O, S or NH.sub.2, and pharmaceutically acceptable salts thereof, have affinity for the AMPA receptors and are antagonists in connection with this type of receptor which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.

    摘要翻译： 其中R1，R2，R3相同或独立地为H，烷基，烷氧基，卤素，NO2，NH2，CF3，CN，SO2CH3，SO2CF3，SO2NR的通式为“IMAGE”的咪唑并[1,2-a]喹喔啉酮衍生物 “R”或5或6元含氮杂环，任选取代，R'，R“独立地为H或烷基; R4为H或CH2-R6; 并且R 6是H，卤素，POR“R”“，NR 7 R 8或任选被取代的5或6元含氮杂环，R”'，R“'独立地是羟基或烷氧基 ; 和R 7，R 8相同或独立地为H或任选取代的烷基; n为1,2或3; R 5是OH，烷氧基，H或NR 10 R 11; R 10，R 11相同或独立地为H，NH 2或OH; X为O或S; 并且Y是O，S或NH 2及其药学上可接受的盐对AMPA受体具有亲和力，并且是与这种受体有关的拮抗剂，这使得它们可用于治疗CNS疾病，特别是在治疗CN 许多由兴奋性氨基酸的多动症引起的适应症。

    Heterocyclic compounds, their use and preparation
    79.
    发明授权
    Heterocyclic compounds, their use and preparation 失效
    杂环化合物，其使用和制备

    公开(公告)号：US5559106A

    公开(公告)日：1996-09-24

    申请号：US350744

    申请日：1994-12-07

    申请人： Poul Jacobsen ,  Flemming E. Nielsen ,  Lone Jeppesen

    发明人： Poul Jacobsen ,  Flemming E. Nielsen ,  Lone Jeppesen

    IPC分类号： A61K31/495 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  C07D487/04 ,  C07F9/6561 ,  A61K31/675 ,  C07F9/6524

    CPC分类号： C07D487/04 ,  C07F9/6561

    摘要： Quinoxaline compounds of the general formula ##STR1## wherein R.sup.1 is COX', POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are hydroxy or alkoxy, and R.sup.6, R.sup.7, R.sup.8 and R.sup.9 independently are hydrogen, alkyl, halogen, NH.sub.2, NO.sub.2, CN, CF.sub.3, SO.sub.2 NY'Y" or COZ' wherein Z' is NY'Y" or alkyl and Y' and Y" independently are hydrogen or alkyl, triazolyl, imidazolyl, imidazolyl substituted with phenyl or alkyl, or R.sup.6 and R.sup.7, or R.sup.8 and R.sup.9, together form a further fused ring, are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

    摘要翻译： 其中R1是COX'，POX'X“或被COX'或POX'X”取代的烷基的喹喔啉化合物，X'和X“独立地是羟基或烷氧基，R6，R7 ，R8和R9独立地是氢，烷基，卤素，NH2，NO2，CN，CF3，SO2NY'Y“或COZ”，其中Z'是NY'Y“或烷基，Y'和Y'独立地是氢或 烷基，三唑基，咪唑基，被苯基或烷基取代的咪唑基，或R6和R7或R8和R9一起形成另外的稠环，可用于治疗由兴奋性神经递质的多动症引起的适应症。