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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。
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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。
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公开(公告)号:US20080161353A1
公开(公告)日:2008-07-03
申请号:US11901941
申请日:2007-09-19
IPC分类号: A61K31/4725 , A61P25/00 , A61K31/47
CPC分类号: C07D215/48 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/00 , C07D215/24 , C07D215/26 , C07D215/28 , C07D215/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14 , Y02A50/411 , A61K2300/00
摘要: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
摘要翻译: 本发明描述了治疗受试者神经学病症的方法,其包括向有需要的受试者施用治疗有效量的下式化合物或其药学上可接受的盐,水合物或溶剂化物。
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公开(公告)号:US06333326B1
公开(公告)日:2001-12-25
申请号:US09367303
申请日:1999-08-02
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。
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公开(公告)号:US07692011B2
公开(公告)日:2010-04-06
申请号:US10530137
申请日:2003-10-03
申请人: Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Brenda Kwan Yi Leung
发明人: Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Brenda Kwan Yi Leung
IPC分类号: C07D239/70
CPC分类号: A61K31/4375 , A61K31/435 , A61K31/436 , A61K31/47 , A61K31/473 , A61K31/4745 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/5025 , A61K31/517 , A61K31/519 , C07C233/54 , C07D239/88 , C07D241/42 , C07D471/04
摘要: The present invention relates to neurologically active 8-hydroxy- or 8-mercapto-quinazolinones. Also disclosed are processes for the preparation of these compounds and their use as pharmaceutical or veterinary agents, in particular for the treatment of neurological conditions, more specifically neurodegenerative conditions, such as Alzheimer's disease.
摘要翻译: 本发明涉及神经活性8-羟基或8-巯基喹唑啉酮。 还公开了用于制备这些化合物的方法及其作为药物或兽药的用途,特别是用于治疗神经病症,更具体地说是神经变性病症如阿尔茨海默氏病。
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公开(公告)号:US07619091B2
公开(公告)日:2009-11-17
申请号:US10521902
申请日:2003-07-16
IPC分类号: C07D215/38
CPC分类号: C07D215/48 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/00 , C07D215/24 , C07D215/26 , C07D215/28 , C07D215/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14 , Y02A50/411 , A61K2300/00
摘要: The present invention relates to a method for the treatment, amelioration and/or prophylaxis of a neurological condition, in particular neurodegenerative disorders which comprises the administration of an effective amount of a compound of formula (I): to a subject in need thereof. The present invention also relates to a compound of formula (II) and processes for its preparation.
摘要翻译: 本发明涉及一种治疗,改善和/或预防神经系统疾病,特别是神经变性疾病的方法,其包括向有需要的受试者施用有效量的式(I)化合物。 本发明还涉及式(II)的化合物及其制备方法。
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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。
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公开(公告)号:US08975278B2
公开(公告)日:2015-03-10
申请号:US11901941
申请日:2007-09-19
IPC分类号: A01N43/42 , A61K31/47 , C07D215/00 , C07D215/38 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/26 , C07D215/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14
CPC分类号: C07D215/48 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D215/00 , C07D215/24 , C07D215/26 , C07D215/28 , C07D215/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D417/12 , C07D417/14 , Y02A50/411 , A61K2300/00
摘要: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
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公开(公告)号:US20100160346A1
公开(公告)日:2010-06-24
申请号:US12717631
申请日:2010-03-04
申请人: Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Brenda Kwan Yi Leung
发明人: Kevin Jeffrey Barnham , Elisabeth Colette Louise Gautier , Gaik Beng Kok , Brenda Kwan Yi Leung
IPC分类号: A61K31/519 , C07D487/04
CPC分类号: A61K31/4375 , A61K31/435 , A61K31/436 , A61K31/47 , A61K31/473 , A61K31/4745 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/5025 , A61K31/517 , A61K31/519 , C07C233/54 , C07D239/88 , C07D241/42 , C07D471/04
摘要: The present invention relates to neurologically-active compounds, processes for their preparation and their use as pharmaceutical or veterinary agents, in particular for the treatment of neurological conditions, more specifically neurodegenerative conditions such as Alzheimer's disease.
摘要翻译: 本发明涉及神经活性化合物,其制备方法及其作为药物或兽药的用途,特别是用于治疗神经病症,更具体地说是神经变性疾病如阿尔茨海默病。
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