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9 条记录 (耗时 0.044 秒)

    Quinoxalinediones
    6.
    发明授权
    Quinoxalinediones 失效
    喹喔啉

    公开(公告)号：US06333326B1

    公开(公告)日：2001-12-25

    申请号：US09367303

    申请日：1999-08-02

    申请人： Alan Stobie ,  Elisabeth Colette Louise Gautier ,  David Charles Waite ,  Robert James Crook

    发明人： Alan Stobie ,  Elisabeth Colette Louise Gautier ,  David Charles Waite ,  Robert James Crook

    IPC分类号： C07D40114

    CPC分类号： C07D401/14

    摘要： This invention relates to 2,3(1H,4H)-quinoxalinedione derivatives which are selective antagonists of N-methyl-D-aspartate receptors. More particularly, this invention relates to 5-triazolyl-2,3(1H,4H)-quinoxalinedione derivatives and to the preparation of, compositions containing, and the uses of, such derivatives. It also relates to a method for treating acute neurodegeneration disorders and chronic neurological disorders.

    摘要翻译： 本发明涉及作为N-甲基-D-天冬氨酸受体的选择性拮抗剂的2,3（1H，4H） - 喹喔啉二酮衍生物。 更具体地说，本发明涉及5-三唑基-2,3（1H，4H） - 喹喔啉二酮衍生物及其制备方法，含有这些衍生物的用途和用途。 它还涉及治疗急性神经变性疾病和慢性神经障碍的方法。

    Quinoxalinediones
    7.
    发明授权
    Quinoxalinediones 失效
    喹喔啉

    公开(公告)号：US06376490B1

    公开(公告)日：2002-04-23

    申请号：US09157806

    申请日：1998-09-04

    申请人： David John Bull ,  Christopher Lee Carr ,  Michael Jonathan Fray ,  Elisabeth Colette Louise Gautier ,  Charles Eric Mowbray ,  Alan Stobie

    发明人： David John Bull ,  Christopher Lee Carr ,  Michael Jonathan Fray ,  Elisabeth Colette Louise Gautier ,  Charles Eric Mowbray ,  Alan Stobie

    IPC分类号： A61K315377

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： The invention provides compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 5-membered ring heteroaryl group containing 3 or 4 nitrogen heteroatoms which is linked to the quinoxalinedione ring by a ring carbon or nitrogen atom said group being optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by 1 or 2 substituents each independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, C3-C7 cycloalkyloxy, —COOH, C1-C4 alkoxycarbonyl, —CONR3R4, —NR3R4, —S(O)p(C1-C4 alkyl), —SO2NR3R4, aryl, aryloxy, aryl(C1-C4)alkoxy, and het, said C1-C4alkyl being optionally substituted by C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, halo(C1C4)alkoxy, C3-C7 cycloalkyloxy, C3-C7 cycloalkyl (C1-C4) alkoxy, —COOH, C1-C4 alkoxycarbonyl, —CONR3R4, —NR3R4,—S(O)p(C1-C4 alkyl), —SO2(aryl), —SO2NR3R4 morpholino, aryl, aryloxy, aryl(C1-C4)alkoxy or het, and said C2-C4 alkenyl being optionally substituted by aryl; and R1 and R2 are each independently selected from H, fluoro, chloro, bromo, C1-C4 alkyl and halo(C1-C4)alkyl. The compounds are useful as NDMA receptor antagonists for treating acute neurodegenerative and chronic neurological disorders.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中R是含有3或4个氮杂原子的5元环杂芳基，其通过环碳或氮原子与喹喔啉二酮环连接，所述基团为 任选地苯并稠合并任选被取代的，包括在苯并稠合部分中的1或2个独立地选自C 1 -C 4烷基，C 2 -C 4烯基，C 3 -C 7环烷基，卤素，羟基，C 1 -C 4烷氧基，C 3 -C（C 1 -C 4）烷氧基，-COOH，C 1 -C 4烷氧基羰基，-CONR 3 R 4，-NR 3 R 4，-S（O）p（C 1 -C 4烷基），-SO 2 NR 3 R 4，芳基，芳氧基，芳基（C 1 -C 4）烷氧基， 任选被C 3 -C 7环烷基，卤素，羟基，C 1 -C 4烷氧基，卤代（C 1 -C 4）烷氧基，C 3 -C 7环烷基氧基，C 3 -C 7环烷基（C 1 -C 4）烷氧基，-COOH，C 1 -C 4烷氧基羰基 ，-CONR 3 R 4，-NR 3 R 4，-S（O）p（C 1 -C 4烷基），-SO 2（芳基），-SO 2 NR 3 R 4吗啉代，芳基，芳氧基，芳基（C 1 -C 4）烷氧基或杂原子， 任选地被取代 由芳基 并且R 1和R 2各自独立地选自H，氟，氯，溴，C 1 -C 4烷基和卤代（C 1 -C 4）烷基。 该化合物可用作治疗急性神经变性和慢性神经障碍的NDMA受体拮抗剂。

    Antithrombotic agents
    8.
    发明授权
    Antithrombotic agents 失效
    抗血栓药

    公开(公告)号：US06180627B2

    公开(公告)日：2001-01-30

    申请号：US09372200

    申请日：1999-08-11

    申请人： Julian Blagg ,  Alan Daniel Brown ,  Elisabeth Colette Louise Gautier ,  Julian Duncan Smith ,  Andrew Brian McElroy

    发明人： Julian Blagg ,  Alan Daniel Brown ,  Elisabeth Colette Louise Gautier ,  Julian Duncan Smith ,  Andrew Brian McElroy

    IPC分类号： A61K315355

    CPC分类号： C07D401/14 ,  A61K38/00 ,  C07D403/14 ,  C07K5/06139 ,  C07K5/06191

    摘要： Compounds of formula (I): Are antithrombotic agents, having utility in a variety of therapeutic areas including the prevention and/or treatment of deep vein thrombosis (DVT) after surgery, major medical illness, paralysis, malignancy, prolonged immobilisation trauma, application of lower limb plaster casts, or fractures of the lower limbs or pelvis; recurrent DVT; DVT during pregnancy when there is a previous history thereof; reocclusion following thrombolytic therapy; chronic arterial obstruction; peripheral vascular disease; acute myocardial infarction; unstable angina; atrial fibrillation; thrombotic stroke; transient ischaemic attacks; disseminated intravascular coagulation; coagulation in extra-corporeal circuits; occlusion of aterio-venous shunts and blood vessel grafts (including coronary artery by-pass grafts); and restenosis and occlusion following angioplasty.

    摘要翻译： 式（I）化合物：抗血栓形成剂，可用于各种治疗领域，包括手术后预防和/或治疗深静脉血栓形成（DVT），主要医学疾病，麻痹，恶性肿瘤，长期固定创伤，应用 下肢石膏或下肢或骨盆骨折; 复发DVT; 怀孕期间DVT有先前的病史; 溶栓治疗后再闭塞; 慢性动脉阻塞; 周边血管疾病; 急性心肌梗塞; 不稳定型心绞痛; 房颤; 血栓性脑卒中 短暂性脑缺血发作; 弥散性血管内凝血; 额外体内循环中的凝血; 静脉分流术和血管移植物（包括冠状动脉旁路移植物）的闭塞; 以及血管成形术后的再狭窄和闭塞。

    Antithrombotic agents
    9.
    发明授权
    Antithrombotic agents 失效
    抗血栓药

    公开(公告)号：US06417203B1

    公开(公告)日：2002-07-09

    申请号：US09662241

    申请日：2000-09-14

    申请人： Julian Blagg ,  Alan Daniel Brown ,  Elisabeth Colette Louise Gautier ,  Julian Duncan Smith ,  Andrew Brian McElroy

    发明人： Julian Blagg ,  Alan Daniel Brown ,  Elisabeth Colette Louise Gautier ,  Julian Duncan Smith ,  Andrew Brian McElroy

    IPC分类号： A61K314439

    CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14

    摘要： Compounds of formula (I): are antithrombotic agents, having utility in a variety of therapeutic areas including the prevention and/or treatment of deep vein thrombosis (DVT) after surgery, major medical illness, paralysis, malignancy, prolonged immobilisation trauma, application of lower limb plaster casts, or fractures of the lower limbs or pelvis; recurrent DVT; DVT during pregnancy when there is a previous history thereof; reocclusion following thrombolytic therapy; chronic arterial obstruction; peripheral vascular disease; acute myocardial infarction; unstable angina; atrial fibrillation; thrombotic stroke; transient ischaemic attacks; disseminated intravascular coagulation; coagulation in extra-corporeal circuits; occlusion of arterio-venous shunts and blood vessel grafts (including coronary artery by-pass grafts); and restenosis and occlusion following angioplasty.

    摘要翻译： 式（I）化合物是抗血栓形成剂，可用于各种治疗领域，包括手术后预防和/或治疗深静脉血栓形成（DVT），主要医学疾病，麻痹，恶性肿瘤，长期固定创伤，应用 下肢石膏或下肢或骨盆骨折; 复发DVT; 怀孕期间DVT有先前的病史; 溶栓治疗后再闭塞; 慢性动脉阻塞; 周边血管疾病; 急性心肌梗塞; 不稳定型心绞痛; 房颤; 血栓性脑卒中 短暂性脑缺血发作; 弥散性血管内凝血; 额外体内循环中的凝血; 静脉分流和血管移植物（包括冠状动脉旁路移植物）的闭塞; 以及血管成形术后的再狭窄和闭塞。