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11 条记录 (耗时 0.031 秒)

    Substituted quinazolines and analogs and use thereof
    1.
    发明授权
    Substituted quinazolines and analogs and use thereof 有权
    取代的喹唑啉和类似物及其用途

    公开(公告)号：US06465472B1

    公开(公告)日：2002-10-15

    申请号：US09654839

    申请日：2000-09-01

    申请人： Ravi Upasani ,  Sui X. Cai ,  Nancy C. Lan ,  Yan Wang ,  George Field ,  David B. Fick

    发明人： Ravi Upasani ,  Sui X. Cai ,  Nancy C. Lan ,  Yan Wang ,  George Field ,  David B. Fick

    IPC分类号： C07D23726

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D239/82 ,  C07D249/08 ,  C07D491/04

    摘要： The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus. Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.

    摘要翻译： 本发明涉及作为AMPA受体的拮抗剂或阳性调节剂的新型喹唑啉和杂环，以及其用于治疗，预防或改善与中风，全身和局灶性缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗 或改善神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病，帕金森病和唐氏综合征，治疗，预防或改善兴奋性氨基酸过度刺激的不良后果，治疗，预防或改善焦虑，精神病，惊厥，慢性 疼痛，青光眼，视网膜炎，尿失禁，肌肉痉挛和诱导麻醉，以及治疗或改善兴奋性氨基酸缺乏症如精神分裂症，肌阵挛的不良后果。 阿尔茨海默病和营养不良和神经发育不良，以及认知和学习增强剂。

    Substituted quinazolines and analogs and the use thereof
    2.
    发明授权
    Substituted quinazolines and analogs and the use thereof 失效
    取代的喹唑啉和类似物及其用途

    公开(公告)号：US06765006B2

    公开(公告)日：2004-07-20

    申请号：US10219755

    申请日：2002-08-16

    申请人： Ravi Upasani ,  Sui X. Cai

    发明人： Ravi Upasani ,  Sui X. Cai

    IPC分类号： C07D23726

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D239/82 ,  C07D249/08 ,  C07D491/04

    摘要： The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.

    摘要翻译： 本发明涉及作为AMPA受体的拮抗剂或阳性调节剂的新型喹唑啉和杂环，以及其用于治疗，预防或改善与中风，全身和局灶性缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗 或改善神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病，帕金森病和唐氏综合征，治疗，预防或改善兴奋性氨基酸过度刺激的不良后果，治疗，预防或改善焦虑，精神病，惊厥，慢性 疼痛，青光眼，视网膜炎，尿失禁，肌肉痉挛和诱导麻醉，以及治疗或改善兴奋性氨基酸缺乏症如精神分裂症，肌阵挛，阿尔茨海默病和营养不良及神经发育不良后果，以及认知和学习增强剂 。

    Alkyl, azido, alkoxy, and fluoro-substituted and fused quinoxalinediones
    4.
    发明授权
    Alkyl, azido, alkoxy, and fluoro-substituted and fused quinoxalinediones 失效
    烷基，叠氮基，烷氧基和氟取代和稠合的喹喔啉

    公开(公告)号：US5631373A

    公开(公告)日：1997-05-20

    申请号：US289603

    申请日：1994-08-11

    申请人： Sui X. Cai ,  Eckard Weber ,  John F.W. Keana ,  Sunil Kher

    发明人： Sui X. Cai ,  Eckard Weber ,  John F.W. Keana ,  Sunil Kher

    IPC分类号： A61K31/495 ,  A61K51/04 ,  A61P3/08 ,  A61P9/10 ,  A61P25/00 ,  A61P43/00 ,  C07D241/38 ,  C07D241/44 ,  C07D487/04 ,  C07D491/04 ,  C07C241/36

    CPC分类号： C07D491/04 ,  A61K51/0459 ,  C07D241/38 ,  C07D241/44 ,  C07D487/04

    摘要： Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, and inducing anesthesia are disclosed by administering to an animal in need of such treatment an alkyl or azido-substituted 1,4-dihydroquinoxaline-2,3-dione or pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.

    摘要翻译： 治疗或预防与中风，局部缺血，CNS创伤，低血糖症和手术相关的神经元损失的方法，以及治疗神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征，治疗或预防不良后果 通过向需要这种治疗的动物施用烷基或叠氮基取代的1,4-二氢喹喔啉-2,3-二酮来公开兴奋性氨基酸的多动症以及治疗焦虑症，慢性疼痛，抽搐和诱导麻醉 或其药学上可接受的盐，其与甘氨酸受体具有高结合性。

    4-hydroxy-3-nitro-1,2-dihydroquinolin-2-ones and the use thereof as excitatory amino acid and glycine receptor antagonists
    5.
    发明授权
    4-hydroxy-3-nitro-1,2-dihydroquinolin-2-ones and the use thereof as excitatory amino acid and glycine receptor antagonists 失效
    4-羟基-3-硝基-1,2-二氢喹啉-2-酮及其作为兴奋性氨基酸和甘氨酸受体拮抗剂的用途

    公开(公告)号：US5622965A

    公开(公告)日：1997-04-22

    申请号：US101244

    申请日：1993-08-02

    申请人： Sui X. Cai ,  Eckard Weber ,  John F. W. Keana

    发明人： Sui X. Cai ,  Eckard Weber ,  John F. W. Keana

    IPC分类号： A61K31/47 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  C07D215/22 ,  C07D215/38

    CPC分类号： C07D215/22 ,  A61K31/47

    摘要： Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a substituted or unsubstituted 4-hydroxy-3-nitro-1,2-dihydroquinolin-2-one or pharmaceutically acceptable salts thereof which have high binding to the glycine receptor.

    摘要翻译： 治疗或预防与中风，局部缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的治疗或预防方法，治疗或预防多动症的不良后果 通过向需要这种治疗的动物施用取代或未取代的4-羟基-3-硝基-1,2-二氢喹啉-2-酮，通过给予兴奋性氨基酸以及治疗焦虑症，慢性疼痛，抽搐和诱导麻醉， 其与甘氨酸受体具有高结合性的一种或其药学上可接受的盐。

    1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes and the use thereof
    6.
    发明授权
    1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes and the use thereof 失效
    1,2,3,4-四氢喹啉-2,3,4-三酮-3或4-肟及其用途

    公开(公告)号：US5475007A

    公开(公告)日：1995-12-12

    申请号：US69005

    申请日：1993-05-28

    申请人： Sui X. Cai ,  John F. W. Keana ,  Eckard Weber

    发明人： Sui X. Cai ,  John F. W. Keana ,  Eckard Weber

    IPC分类号： A61K31/47 ,  A61K51/04 ,  A61P9/10 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  C07D215/38 ,  C07D215/42

    CPC分类号： C07D215/42 ,  A61K31/47 ,  A61K51/0455 ,  C07D215/38 ,  A61K2121/00

    摘要： Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oxime or pharmaceutically acceptable salts thereof which have high binding to the glycine receptor.

    摘要翻译： 治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的治疗或预防方法，治疗或预防多动症的不良后果 通过向需要这种治疗的动物施用取代或未取代的1,2,3,4-四氢喹啉-2,3,4-四氢喹啉， 与甘氨酸受体具有高结合性的三酮-3或4-肟或其药学上可接受的盐。

    Chemical functionalization of surfaces
    8.
    发明授权
    Chemical functionalization of surfaces 失效

    公开(公告)号：US5582955A

    公开(公告)日：1996-12-10

    申请号：US495005

    申请日：1995-06-26

    申请人： John F. W. Keana ,  Martin N. Wybourne ,  Sui X. Cai ,  Mingdi Yan

    发明人： John F. W. Keana ,  Martin N. Wybourne ,  Sui X. Cai ,  Mingdi Yan

    IPC分类号： C08F8/30 ,  C08F8/34 ,  G03C5/00

    CPC分类号： C08F8/30 ,  C08F8/34 ,  Y10S430/143

    摘要： Methods for covalently modifying surfaces of various substrates are disclosed, along with various substrates having surfaces modified by such methods. Candidate surfaces include various polymeric, siliceous, metallic, allotrophic forms of carbon, and semiconductor surfaces. The surfaces are exposed to a reagent, having molecules each comprising a nitrenogenic group and a functionalizing group, in the presence of energized charged particles such as electrons and ions, photons, or heat, which transform the nitrenogenic reagent to a nitrene intermediate. The nitrene covalently reacts with any of various chemical groups present on the substrate surface, thereby effecting nitrene addition of the functionalizing groups to the substrate surface. The functionalizing groups can then participate in downstream chemistry whereby any of a large variety of functional groups, including biological molecules, can be covalently bonded to the surface, thereby dramatically altering the chemical behavior of the surface. Such functionalizations of the surface can be done in a single reactive step or in multiple reactive steps.

    Azepine synthesis via a diels-alder reaction
    10.
    发明授权
    Azepine synthesis via a diels-alder reaction 失效
    通过diels-alder反应进行Azepine合成

    公开(公告)号：US5476933A

    公开(公告)日：1995-12-19

    申请号：US341154

    申请日：1994-11-16

    申请人： John F. W. Keana ,  Anthony P. Guzikowski ,  Daniel F. Nogales ,  Sui X. Cai

    发明人： John F. W. Keana ,  Anthony P. Guzikowski ,  Daniel F. Nogales ,  Sui X. Cai

    IPC分类号： C07D223/16 ,  C07D223/32 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D15/04 ,  A61K31/55

    CPC分类号： C07D223/16 ,  C07D223/32 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.

    摘要翻译： 公开了通过包括Diels-Alder反应的多步合成来制备氮杂的方法。 还公开了治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的治疗或预防方法，治疗或预防不良后果 兴奋性氨基酸的多动症以及治疗焦虑症，慢性疼痛，抽搐，诱导麻醉和治疗或预防阿片剂耐受性的公开通过向需要这种治疗的动物施用与NMDA甘氨酸位点具有高结合性的吖庚因 。