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    Derivatives of 4-(2-aminoethyl)phenoxymethyl-phosphonic and -phosphinic acid and pharmaceutical and veterinary uses therefor
    1.
    发明授权
    Derivatives of 4-(2-aminoethyl)phenoxymethyl-phosphonic and -phosphinic acid and pharmaceutical and veterinary uses therefor 失效
    4-（2-氨基乙基）苯氧基甲基 - 膦酸和次膦酸的衍生物及其药用和兽用用途

    公开(公告)号：US5726165A

    公开(公告)日：1998-03-10

    申请号：US465486

    申请日：1995-06-05

    申请人： Lee James Beeley ,  Mervyn Thompson ,  David Kenneth Dean ,  Nikesh Rasiklal Kotecha ,  John Michael Berge ,  Robert William Ward

    发明人： Lee James Beeley ,  Mervyn Thompson ,  David Kenneth Dean ,  Nikesh Rasiklal Kotecha ,  John Michael Berge ,  Robert William Ward

    IPC分类号： C07C217/34 ,  C07D317/46 ,  C07F9/30 ,  C07F9/32 ,  C07F9/40 ,  A61K31/665 ,  A61K31/66 ,  C07F9/665

    CPC分类号： C07F9/3211 ,  C07C217/34 ,  C07D317/46 ,  C07F9/301 ,  C07F9/303 ,  C07F9/3223 ,  C07F9/4006 ,  C07C2101/14

    摘要： A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, or solvate thereof, wherein, R.sup.o represents an aryl group, optionally substituted; X represents O or S; R.sup.1 and R.sup.1a each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b): ##STR2## wherein R.sup.4 represent hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R.sup.5 represent hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy, cycloalkyloxy, hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R.sup.5 together with OR.sup.4 represents O(CH.sub.2).sub.n O wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.2 represents a moiety of formula (c): ##STR3## or an ester or amide thereof; a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.

    摘要翻译： 式（I）的化合物：其中，R 1表示任选被取代的芳基;（I）化合物或其药学上可接受的盐或其溶剂合物， X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺，或R 2表示式（b）的部分：其中R 4表示氢，烷基，羟烷基，芳烷基，芳烷氧基烷基或环烷基，R 5表示羟基，烷氧基，芳基烷氧基 ，羟烷基氧基，烷氧基烷氧基，芳基烷氧基烷氧基，环烷氧基，氢，烷基，取代烷基，环烷基，芳基，芳基烷基，芳基烷氧基烷基或R5与OR4一起表示O（CH2）nO，其中n为2,3或4; 并且R 3表示氢，卤素，烷基或烷氧基，或者R 3与R 2一起表示式（c）的部分：（c）或其酯或酰胺; 含有这种化合物的药物组合物，制备这种化合物的方法以及这种化合物在医药中的用途。

    1,6-naphthyridine anti-convulsants
    3.
    发明授权
    1,6-naphthyridine anti-convulsants 失效
    1,6-萘啶抗惊厥药

    公开(公告)号：US06245778B1

    公开(公告)日：2001-06-12

    申请号：US09424399

    申请日：1999-11-23

    申请人： Michael Stewart Hadley ,  John David Harling ,  Frank Peter Harrington ,  Mervyn Thompson ,  Robert William Ward

    发明人： Michael Stewart Hadley ,  John David Harling ,  Frank Peter Harrington ,  Mervyn Thompson ,  Robert William Ward

    IPC分类号： A61K314375

    CPC分类号： C07D471/04

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: where R1 is hydrogen, C1-6 alkyl optionally substituted by hydroxy or C1-4alkoxy, or C1-6 alkylphenyl; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, C1-6 alkylO-, C1-6 alkylS-, C1-6 alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3, CF3O, CF3CO—, C1-6alkylCO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, or —NR3R4 where R3 is hydrogen or C1-4 alkyl, and R4 is hydrogen, C1-4alkyl, —CHO, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups form a saturated carbocyclic ring optionally interrupted by oxygen; and X is selected from hydrogen, halogen, cyano, alkyl and alkoxy; are useful in the treatment and prophylaxis of inter alia epilepsy.

    摘要翻译： 式（I）化合物及其药学上可接受的盐：其中R 1是氢，任选被羟基或C 1-4烷氧基取代的C 1-6烷基或C 1-6烷基苯基; R 2是氢或至多三个选自卤素，NO 2，CN的取代基 ，N 3，C 1-6烷基，C 1-6烷基，C 1-6烷基，C 3-6环烷基，C 3-6环烷基-C 1-4烷基 - ，C 1-6烯基，C 1-6炔基，CF 3，CF 3 O，CF 3 CO-， C 3-6烷基CO-，C 3-6环烷基CO-，C 3-6环烷基-C 1-4烷基CO-，苯基，苯氧基，苄氧基，苯甲酰基，苯基-C 1-4烷基 - 或-NR 3 R 4，其中R 3是氢或C 1-4烷基，R 4是氢， 4个烷基，-CHO，-CO 2 C 1-4烷基或-COC 1-4烷基;或两个R 2基团形成任选被氧中断的饱和碳环; X选自氢，卤素，氰基，烷基和烷氧基;可用于处理和 特别是癫痫预防。

    Substituted benzamide derivatives and pharmaceutical compositions containing them
    4.
    发明授权
    Substituted benzamide derivatives and pharmaceutical compositions containing them 失效
    取代的苯甲酰胺衍生物和含有它们的药物组合物

    公开(公告)号：US06395759B1

    公开(公告)日：2002-05-28

    申请号：US09319124

    申请日：1999-06-01

    申请人： Mervyn Thompson ,  Antonio Kuok Keong Vong ,  Robert William Ward

    发明人： Mervyn Thompson ,  Antonio Kuok Keong Vong ,  Robert William Ward

    IPC分类号： A61K31445

    CPC分类号： C07D211/26 ,  C07D207/09

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, where G is a methylene or ethylene linkage; R1 is hydrogen, C1-6alkylO—; R2 is hydrogen, halogen, CN, N3, trifluoromethyldiazirinyl, CF3, CF3O—, CF3S—, CF3CO—, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO—, C1-6alkylCO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4-alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl and substituted benzoyl, phenyl-C1-4alkyl-, C1-6alkylSO2—, (C1-4alkyl)2NSO2— or (C1-4alkyl)NHSO2—; R3 is hydrogen, halogen, CN, N3, trifluoromethyldiazirinyl, C1-6alkylO—, C1-6alkylS—, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3CO—, C1-6alkylCO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, or —NR5R6 where R5 is hydrogen or C1-4alkyl; and R6 is hydrogen, C1-4alkyl, —CHO, —CO2C1-4alkyl or —COC1-4alkyl; R4 is hydrogen, C1-6alkyl, C1-6alkenyl, or C1-6alkynyl, are useful in the prevention and treatment of anxiety, mania, depression disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse such as cocaine, nicotine, alcohol and benzodiazepines, disorders treatable and/or preventable with anti-convulsive agents, such as epilepsy including post-traumatic epilepsy, Parkinson's disease, psychosis, migraine, etc.

    摘要翻译： 式（I）化合物及其药学上可接受的盐，其中G是亚甲基或亚乙烯键; R1是氢，C1-6烷基， R2是氢，卤素，CN，N3，三氟甲基二氮丙烯基，CF3，CF3O-，CF3S-，CF3CO-，C1-6烷基，C3-6环烷基，C3-6环烷基C1-4烷基 - ，C1-6烷基， - C1-6烷基， 苯基，苯甲酰基，苯基-C 1-4烷基，C 1-6烷基SO 2 - ，（C 1-4烷基）2 NSO 2 - 或（C 1 -C 4烷基） 4烷基）NHSO 2 - ; R 3是氢，卤素，CN，N 3，三氟甲基二氮嗪基，C 1-6烷基O - ，C 1-6烷基-S-，C 1-6烷基，C 3-6环烷基，C 3-6环烷基-C 1-4烷基 - ，C 1-6烯基，C 1-6炔基，CF 3 CO-， 苯基，苯氧基，苄氧基，苯甲酰基，苯基-C 1-4烷基 - 或-NR 5 R 6，其中R 5是氢或C 1-4烷基; R 3是C 1-4烷基， 并且R 6是氢，C 1-4烷基，-CHO，-CO 2 C 1-4烷基或-COC 1-4烷基; R4是氢，C1-6烷基，C1-6链烯基或C1-6炔基，可用于预防和治疗与蛛网膜下腔出血或神经性休克相关的焦虑，躁狂症，抑郁症，与滥用物质相关的作用 可卡因，尼古丁，酒精和苯并二氮杂，可用抗惊厥药治疗和/或预防的疾病，如癫痫，包括创伤后癫痫，帕金森病，精神病，偏头痛等。

    Pyrazolopyridines and pyrazolopyridazines as antidiabetics
    5.
    发明授权
    Pyrazolopyridines and pyrazolopyridazines as antidiabetics 失效
    吡唑并吡啶类和吡唑并吡啶类作为抗糖尿病药

    公开(公告)号：US07109199B2

    公开(公告)日：2006-09-19

    申请号：US10381292

    申请日：2001-09-19

    申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

    发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

    IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/4162 ,  A61P3/10

    CPC分类号： C07D471/04 ,  C07D213/85 ,  C07D487/04

    摘要： The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclyl and the alkyl moieties may each independently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention includes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

    摘要翻译： 本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可各自独立地为未取代或取代的未取代或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自独立地为未取代或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明包括制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

    Pyrazolopyridines and pyrazolopyridazines as antidiabetics
    8.
    发明授权
    Pyrazolopyridines and pyrazolopyridazines as antidiabetics 失效
    吡唑并吡啶类和吡唑并吡啶类作为抗糖尿病药

    公开(公告)号：US07297792B2

    公开(公告)日：2007-11-20

    申请号：US11422338

    申请日：2006-06-06

    申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

    发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

    IPC分类号： C07D413/00

    CPC分类号： C07D471/04 ,  C07D213/85 ,  C07D487/04

    摘要： The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclcyl and the alkyl moieties may each inedepently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention inlcudes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

    摘要翻译： 本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可以各自独立地是未取代的或取代的，未取代的或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自是未取代的或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明涉及制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

    Method and compounds
    9.
    发明授权
    Method and compounds 失效
    方法和化合物

    公开(公告)号：US06719520B2

    公开(公告)日：2004-04-13

    申请号：US10446553

    申请日：2003-05-28

    申请人： Matthew Paul Coghlan ,  Ashley Edward Fenwick ,  David Haigh ,  Julie Caroline Holder ,  Robert John Ife ,  Alastair David Reith ,  David Glynn Smith ,  Robert William Ward

    发明人： Matthew Paul Coghlan ,  Ashley Edward Fenwick ,  David Haigh ,  Julie Caroline Holder ,  Robert John Ife ,  Alastair David Reith ,  David Glynn Smith ,  Robert William Ward

    IPC分类号： A61K3140

    CPC分类号： C07D207/456 ,  C07D401/04 ,  C07D403/04

    摘要： A method for the treatment of conditions associated with a need for inhibition of GSK-3, such as diabetes, dementias such as Alzheimer's disease and manic depression which method comprises the administration of a pharmaceutically effective, non-toxic amount of a compound of formula (I): or a pharmaceutically acceptable derivative thereof, wherein: R is hydrogen, alkyl, aryl, or aralkyl; R1 is hydrogen, alkyl, aralkyl, hydroxyalkyl or alkoxyalkyl; R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; R3 is hydrogen, substituted or unsubstituted alkyl, cycloalkyl, alkoxyalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl or aralkyl wherein the aryl moiety is substituted or unsubstituted; or, R1 and R3 together with the nitrogen to which they are attached form a single or fused, optionally substituted, saturated or unsaturated heterocylic ring; to a human or non-human mammal in need thereof, and compounds of formula I.

    摘要翻译： 用于治疗与需要抑制GSK-3（例如糖尿病，痴呆症如阿尔茨海默病和躁狂抑郁症）有关的病症的方法包括施用药学上有效的无毒量的式（I）化合物 I）：或其药学上可接受的衍生物，其中：R是氢，烷基，芳基或芳烷基; R 1是氢，烷基，芳烷基，羟基烷基或烷氧基烷基; R 2是取代或未取代的芳基或取代或 未取代的杂环基; R 3是氢，取代或未取代的烷基，环烷基，烷氧基烷基，取代或未取代的芳基，取代或未取代的杂环基或芳烷基，其中芳基部分是取代或未取代的; 或R 1和R 3与它们所连接的氮一起形成单个或稠合的，任选取代的饱和或不饱和杂环;给需要的人或非人哺乳动物，以及 公式一