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16 条记录 (耗时 0.032 秒)

    Glyoxalase inhibitors
    3.
    发明申请
    Glyoxalase inhibitors 审中-公开
    乙二醛酶抑制剂

    公开(公告)号：US20070015799A1

    公开(公告)日：2007-01-18

    申请号：US10556901

    申请日：2004-05-14

    申请人： Mark Ashton ,  Alan Davidson ,  Russell Thomas ,  Mark Whittaker

    发明人： Mark Ashton ,  Alan Davidson ,  Russell Thomas ,  Mark Whittaker

    IPC分类号： A61K31/4436 ,  A61K31/44 ,  A61K31/381

    CPC分类号： C07D405/04 ,  A61K31/10 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4436 ,  C07C323/62 ,  C07D213/85 ,  C07D217/26 ,  C07D409/04 ,  C07D409/14

    摘要： This invention relates to compounds of formula (I) which are glyoxalase I inhibitors, pharmaceutical salts or compositions comprising such compounds, and the use of such compositions and compounds to treat various conditions alleviated by the inhibition of glyoxalase 1. Wherein X is N or CH. R2 is H, CF3; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. R3 is H; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. Alternatively R2 and R3 together form an optionally substituted C3-4alkylene group wherein L3 and L4 are single bonds thus forming a C5-6 ring fused with the aromatic ring to which L3 and L4 are attached. L3 and L4 are independently selected from a single bond, optionally substituted C1-4 alkylene, -L9YN(OH)C(═O)L10- and -L9C(═O)N(OH)YL10-, wherein L9 and L10 are independently selected from optionally substituted C1-4 alkylene, C5-6 arylene, C1-4 alkylene-C5-6arylene and a single bond, wherein Y is NH or a single bond.

    摘要翻译： 本发明涉及作为乙二醛酶I抑制剂的式（I）化合物，包含这些化合物的药物盐或组合物，以及这些组合物和化合物用于治疗通过抑制乙二醛酶1减轻的各种病症的用途。其中X是N或CH 。 R 2是H，CF 3 N; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。 R 3是H; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。 或者R 2和R 3一起形成任选取代的C 3-4亚烷基，其中L 3和L 3 因此形成与L 3和L 4的芳环稠合的C 5〜6环， SUP>连接。 L 3和L 4独立地选自单键，任选取代的C 1-4亚烷基，-L 9， SUP-YN（OH）C（-O）L 10 - 和-L 9 C（ - ）N（OH）Y L 10 - ，其中L 9和L 10独立地选自任选取代的C 1-4 - 亚烷基，C 5-6 - 亚芳基，C 1-4亚烷基-C 5-6亚芳基和单键，其中Y是NH或单键。

    Benzoxazole acetonitriles
    4.
    发明申请
    Benzoxazole acetonitriles 审中-公开
    苯并恶唑乙腈

    公开(公告)号：US20070185104A1

    公开(公告)日：2007-08-09

    申请号：US10571323

    申请日：2004-09-10

    申请人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    发明人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    IPC分类号： A61K31/5377 ,  A61K31/506 ,  C07D413/14

    CPC分类号： C07D491/10 ,  C07D413/06 ,  C07D413/14

    摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylamino moiety. R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C1C6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano or hydroxy.

    摘要翻译： 本发明涉及苯并恶唑乙腈和含有该苯并恶唑乙腈的配方（I）的药物制剂。 所述苯并恶唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）。 本发明还涉及制备苯并恶唑乙腈（I）的方法。 A是嘧啶基，L是含有至少一个杂原子的仲或叔氨基或3-8元杂环烷基。 选自N，O，S或L是酰氨基部分。 R 1选自包含或由氢，磺酰基，氨基，C 1 -C 6 - 烷基，C 2 -C 6 - 亚烷基，C 2 -C 6 - 炔基或C 1 -C 烷氧基，芳基，卤素，羧基，氨基羰基，氰基或羟基。

    Triazoles as oxytocin antagonists
    6.
    发明申请
    Triazoles as oxytocin antagonists 失效
    三唑作为催产素拮抗剂

    公开(公告)号：US20050187275A1

    公开(公告)日：2005-08-25

    申请号：US10498356

    申请日：2002-12-19

    申请人： Anna Quattropani ,  Matthias Schwarz ,  Russell Thomas ,  Thomas Coulter

    发明人： Anna Quattropani ,  Matthias Schwarz ,  Russell Thomas ,  Thomas Coulter

    IPC分类号： A61K31/4196 ,  A61P1/16 ,  A61P9/04 ,  A61P9/12 ,  A61P13/12 ,  A61P15/06 ,  A61P15/12 ,  A61P15/14 ,  A61P27/02 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D407/12

    CPC分类号： C07D403/12 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D405/06 ,  C07D405/12

    摘要： The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.

    摘要翻译： 本发明涉及特别用作药物活性化合物的式（I）的三唑衍生物以及含有这种三唑衍生物的药物制剂。 所述三唑可用于治疗和/或预防早产，早产，痛经，不适当的血管加压素分泌，充血性心力衰竭，动脉高血压，肝硬化，肾病综合征和高眼压症。 特别地，本发明涉及显示催产素和/或加压素受体的显着调节，特别是拮抗活性的三唑衍生物。 更优选地，所述化合物可用于治疗和/或预防由催产素和/或加压素介导的疾病状态。 本发明还涉及新的三唑衍生物及其制备方法。

    Benzimidazole Acetonitriles
    7.
    发明申请
    Benzimidazole Acetonitriles 审中-公开
    苯并咪唑乙腈

    公开(公告)号：US20070203134A1

    公开(公告)日：2007-08-30

    申请号：US10571470

    申请日：2004-09-10

    申请人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    发明人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    IPC分类号： A61K31/5377 ,  A61K31/506 ,  C07D413/14 ,  C07D403/02

    CPC分类号： C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) (I). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S or L is an acylamino moiety; R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, cyano or hydroxy; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C2-C6alkenyl, C2-C6-alkynyl, or C1-C6-alkoxy.

    摘要翻译： 本发明涉及苯并咪唑乙腈和含有式（I）的苯并咪唑乙腈的药物制剂。 所述苯并咪唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）（I））。 本发明还涉及制备苯并恶唑乙腈的方法。 G是嘧啶基; L是含有至少一个选自N，O，S或L的杂原子的氨基或3-8元杂环烷基是酰氨基部分; R 1选自氢，磺酰基，氨基，羧基，氨基羰基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷基， C 2 -C 6 - 烯基，C 2 -C 6 - 炔基或C 1 -C 6 - C 1 -C 6 - 烷氧基，芳基，卤素，氰基或羟基; R 2选自包含或由氢，C 1 -C 6 - 烷基，C 2 H 2基团组成的组 C 1 -C 6亚烷基，C 2 -C 6亚炔基或C 1 -C 6亚烷基， 6 - 烷氧基。

    Pyrrolidine oxadiazole-and thiadiazole oxime derivatives being oxytocin receptor antagonists
    9.
    发明申请
    Pyrrolidine oxadiazole-and thiadiazole oxime derivatives being oxytocin receptor antagonists 审中-公开
    吡咯烷恶二唑和噻二唑肟衍生物是催产素受体拮抗剂

    公开(公告)号：US20060229343A1

    公开(公告)日：2006-10-12

    申请号：US11449802

    申请日：2006-06-09

    申请人： Matthias Schwarz ,  Anna Quattropani ,  Patrick Page ,  Russell Thomas ,  Vincent Pomel

    发明人： Matthias Schwarz ,  Anna Quattropani ,  Patrick Page ,  Russell Thomas ,  Vincent Pomel

    IPC分类号： A61K31/433 ,  A61K31/4245 ,  C07D413/14 ,  C07D417/14

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. B is a oxadiazole or thiadiazole group.

    摘要翻译： 本发明涉及用作药物活性化合物的吡咯烷恶二唑和噻二唑衍生物，以及含有这种吡咯烷恶二唑衍生物的药物制剂。 所述吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。 特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。 更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。 本发明还涉及新型吡咯烷衍生物及其制备方法。 B是恶二唑或噻二唑基。