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92 条记录 (耗时 0.016 秒)

    COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
    23.
    发明公开
    COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
    和作业LINKS AT NK3受体及其应用在医学

    公开(公告)号：EP1812398A1

    公开(公告)日：2007-08-01

    申请号：EP05807869.2

    申请日：2005-11-10

    申请人： SmithKline Beecham Corporation

    发明人： SMITH, Paul William, GlaxoSmithKline ,  WYMAN, Paul Adrian, GlaxoSmithKline

    IPC分类号： C07D215/52 ,  A61K31/47 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24

    CPC分类号： C07D401/12 ,  C07D215/52 ,  C07D409/14

    摘要： The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl optionally substituted by 1, 2 or 3 halogen atoms which halogen atoms may be the same or different; R2 is C1-6alkyl, C3-6cycloalkyl or acetyl; X is oxygen or sulphur; a is 1, 2 or 3; b is 0 or 1; c is 0, 1 or 2; R3 is hydrogen or C1-6alkyl; R4 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxyC1-6alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-6alkyl; R5 is hydrogen; or R5 and R3, together with the nterconnecting atoms, form a 4, 5 or 6 membered ring; R6 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; and z is 0, 1 or 2; wherein when z is 1 or 2, Z is a halogen atom, and wherein when z is 2 the halogen atoms may be the same or different. Also disclosed are processes for their preparation, pharmaceutical compositions containing them and heir use as medicaments particularly in treating disorders of the Central Nervous System (CNS).

    COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
    24.
    发明公开
    COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
    在NK3受体上具有活性的化合物及其在医学上的用途

    公开(公告)号：EP1809606A1

    公开(公告)日：2007-07-25

    申请号：EP05802078.5

    申请日：2005-11-10

    申请人： SmithKline Beecham Corporation

    发明人： BRADLEY, Daniel Marcus, GlaxoSmithKline ,  PORTER, Roderick Alan, GlaxoSmithKline ,  SMITH, Paul William, GlaxoSmithKline ,  STEAD, Rachel Elizabeth Anne, GlaxoSmithKline ,  VONG, Antonio Kuok Keong, GlaxoSmithKline

    IPC分类号： C07D215/52 ,  A61K31/47 ,  A61P25/18 ,  A61P25/24

    CPC分类号： C07D409/04 ,  C07D215/52

    摘要： The invention also relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl or cyclohexyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; R2 is C1-6alkyl or C3-6cycloalkyl; n is 1 or 2; R3 is hydrogen, C1-6alkyl or C3-6cycloalkyl; X is -(C=O)- or -SO2-; R4 is C1-6alkyl, C1-6haloalkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6haloalkoxy, amino, monoC1-6alkylamino or diC1-6alkylamino, or R4 is heterocyclyl or carbocyclyl, either of which is optionally substituted independently by one or more halogen, C1-6alkyl, C1-6haloalkyl, C1-6alkoxy or C1-6haloalkoxy; R5 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms; and y is 0, 1 or 2; wherein when y is 1 or 2, Y is a halogen atom, and wherein when y is 2 the halogen atoms may be the same or different. Also disclosed are use of the compounds in treating diseases and conditions mediated by activation of the NK3 receptor, compositions containing the derivatives and processes for their preparation.

    摘要翻译： 本发明还涉及式（I）化合物，其药学上可接受的盐，溶剂合物或前药：其中R 1为苯基或环己基，其任一个任选被1,2或3个卤原子取代，所述卤原子可以相同 或不同; R2是C1-6烷基或C3-6环烷基; n是1或2; R3是氢，C1-6烷基或C3-6环烷基; X是 - （C = O） - 或-SO 2 - ; R 4是C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 1-6卤代烷氧基，氨基，单C 1-6烷基氨基或二C 1-6烷基氨基，或者R 4是杂环基或碳环基， 或更多卤素，C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基或C 1-6卤代烷氧基; R5为苯基或噻吩基，其任一个任选被1,2或3个卤素原子取代; y是0,1或2; 其中当y是1或2时，Y是卤素原子，并且其中当y是2时，卤素原子可以相同或不同。 还公开了所述化合物在治疗由NK3受体活化介导的疾病和病症中的用途，含有所述衍生物的组合物及其制备方法。

    QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 AND NK-2 RECEPTOR ANTAGONISTS
    27.
    发明公开
    QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 AND NK-2 RECEPTOR ANTAGONISTS 审中-公开
    喹啉-4-甲酰胺衍生物作为NK-3和NK-2受体拮抗剂

    公开(公告)号：EP1334088A1

    公开(公告)日：2003-08-13

    申请号：EP01983584.2

    申请日：2001-11-12

    申请人： GlaxoSmithKline S.p.A. ,  Laboratoire Glaxosmithkline S.A.S.

    发明人： FARINA, Carlo,Nikem Research S.r.l. ,  GIARDINA, Giuseppe,Nikem Research S.r.l. ,  GRUGNI, Mario,Nikem Research S.r.l. ,  NADLER, Guy Margue. Marie Gerard,Glaxosmithkline

    IPC分类号： C07D215/52 ,  A61K31/47 ,  A61K31/4709 ,  A61P11/06

    CPC分类号： C07D215/52

    摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: (I) wherein: R1 is H or C1-6 alkyl; R2 is aryl or C3-7 cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is R8R9; R8 is a single bond, C1-6 alkyl, or aryl; R9 is H, COO R10, or N R11R12; R10 is H or C1-6 alkyl; R11 and R12 are independently selected from H and C1-6 alkyl; R5 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R6 represents H or up to three substituents independently selected from the list consisting of: C¿1-6? alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- or di-C1-6 alkylamino; R7 is H or halo; a is 1-6; and any of R2, R5, R8, R10, R11 and R12 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy or oxo; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

    Novel cyclic anthranilic acid carboxylic acid derivatives
    30.
    发明公开
    Novel cyclic anthranilic acid carboxylic acid derivatives 失效
    新型环状邻氨基苯甲酸羧酸衍生物

    公开(公告)号：EP0403980A1

    公开(公告)日：1990-12-27

    申请号：EP90111353.0

    申请日：1990-06-15

    申请人： KYORIN PHARMACEUTICAL CO., LTD.

    发明人： Kohno, Yasushi ,  Kojima, Eisuke

    IPC分类号： C07D215/50 ,  C07D215/52 ,  A61K31/435

    CPC分类号： C07D471/06 ,  C07D215/50 ,  C07D215/52

    摘要： Cyclic anthranilic acid carboxylic acid derivatives of the following formula,
    wherein R¹ is hydrogen atom, carboxyl group, lower alkoxy carbonyl group having 1 to 3 carbon atoms, or phenyl group which may be substituted, R² and R⁴ are each independently a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group, R³ is a hydrogen atom, halogen atom, nitro group, amino group, cyano group, carbamoyl group, carboxyl group, lower alkanoylamino group having 1 to 4 carbon atoms, benzoylamino group, lower alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted by methyl group; the acid addition or alkali salts thereof, are useful as drugs treat autoimmune diseases, antirheumatic agents and thera­peutic or prophylactic agents to treat metabolic bone diseases.

    摘要翻译： 下式的环状邻氨基苯甲酸羧酸衍生物，其中R 1为氢原子，羧基，具有1-3个碳原子的低级烷氧基羰基或可被取代的苯基，R 2和R 4各自独立地为氢原子，低级 具有1-3个碳原子的烷基或苄基，R 3是氢原子，卤素原子，硝基，氨基，氰基，氨基甲酰基，羧基，具有1至4个碳原子的低级烷酰氨基，苯甲酰氨基， 具有1至3个碳原子的烷基磺酰基氨基或可以由甲基取代的苯基磺酰基氨基; 其酸加成盐或其碱盐可用作治疗自身免疫性疾病的药物，抗风湿剂和治疗或预防代谢性骨疾病的药物。