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8 条记录 (耗时 0.023 秒)

    Cyclic amine derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists
    1.
    发明授权
    Cyclic amine derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists 失效
    取代喹喔啉2,3-二酮的环胺衍生物作为谷氨酸受体拮抗剂

    公开(公告)号：US6110911A

    公开(公告)日：2000-08-29

    申请号：US272482

    申请日：1999-03-19

    申请人： Brian Edward Kornberg ,  Sham Shridhar Nikam ,  Michael Francis Rafferty ,  Po-Wai Yuen

    发明人： Brian Edward Kornberg ,  Sham Shridhar Nikam ,  Michael Francis Rafferty ,  Po-Wai Yuen

    IPC分类号： C07D241/44 ,  A61K31/4985 ,  A61K31/55

    CPC分类号： C07D241/44

    摘要： A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.

    摘要翻译： 教导了一系列用作神经保护剂的取代喹喔啉2,3-二酮。 还教导了新的中间体，制备方法和含有这些化合物的药物组合物。 这些化合物是谷氨酸拮抗剂，可用于治疗由血栓栓塞或出血性脑卒中，脑血管痉挛，低血糖症，心脏骤停，癫痫持续状态，围产期窒息，缺氧，癫痫发作，疼痛，阿尔茨海默病， 帕金森病和亨廷顿疾病。

    Piperidine derivatives as subtype selective N-Methyl-D-Aspartate antagonists
    5.
    发明授权
    Piperidine derivatives as subtype selective N-Methyl-D-Aspartate antagonists 失效
    哌啶衍生物作为亚型选择性N-甲基-D-天冬氨酸拮抗剂

    公开(公告)号：US06642256B2

    公开(公告)日：2003-11-04

    申请号：US09998479

    申请日：2001-11-30

    申请人： Brian Edward Kornberg ,  Russell Andrew Lewthwaite ,  David Manning ,  Sham Shridhar Nikam ,  Ian Leslie Scott

    发明人： Brian Edward Kornberg ,  Russell Andrew Lewthwaite ,  David Manning ,  Sham Shridhar Nikam ,  Ian Leslie Scott

    IPC分类号： A01N4340

    CPC分类号： C07D413/14 ,  C07D417/14

    摘要： Described are piperidines of Formula I and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, central nervous system disorders, depression, trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, pain, especially chronic pain, neuropathic pain, or surgical pain, or urinary incontinence.

    摘要翻译： 描述了式I的哌啶及其药学上可接受的盐。 式I的化合物是可用于治疗脑血管病症的NMDA受体通道复合物的拮抗剂，例如中风，脑缺血，中枢神经系统疾病，抑郁症，创伤，低血糖症，神经变性疾病，焦虑，偏头痛，抽搐， 帕金森病，氨基糖苷类抗生素诱导的听力损失，精神病，青光眼，CMV视网膜炎，阿片类药物耐受或戒断，疼痛，特别是慢性疼痛，神经性疼痛或手术疼痛或尿失禁。

    Sulfonamide derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists
    6.
    发明授权
    Sulfonamide derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists 失效
    取代喹喔啉2,3-二酮的磺酰胺衍生物作为谷氨酸受体拮抗剂

    公开(公告)号：US6096744A

    公开(公告)日：2000-08-01

    申请号：US72117

    申请日：1998-05-04

    申请人： Brian Edward Kornberg ,  Sham Shridhar Nikam

    发明人： Brian Edward Kornberg ,  Sham Shridhar Nikam

    IPC分类号： C07D241/44 ,  A61K31/498

    CPC分类号： C07D241/44

    摘要： A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.

    摘要翻译： 教导了一系列用作神经保护剂的取代喹喔啉2,3-二酮。 还教导了新的中间体，制备方法和含有这些化合物的药物组合物。 这些化合物是谷氨酸拮抗剂，可用于治疗由血栓栓塞或出血性脑卒中，脑血管痉挛，低血糖症，心脏骤停，癫痫持续状态，围产期窒息，缺氧，癫痫发作，疼痛，阿尔茨海默病， 帕金森病和亨廷顿疾病。

    Hydroxamate inhibitors of endothelin converting enzyme
    8.
    发明授权
    Hydroxamate inhibitors of endothelin converting enzyme 失效
    内皮素转化酶的羟肟酸盐抑制剂

    公开(公告)号：US5663296A

    公开(公告)日：1997-09-02

    申请号：US373911

    申请日：1995-01-17

    申请人： Annette Marian Doherty ,  Brian Edward Kornberg ,  Sham Nikam

    发明人： Annette Marian Doherty ,  Brian Edward Kornberg ,  Sham Nikam

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/083 ,  C07K5/113 ,  C07K14/575 ,  A61K38/06

    CPC分类号： C07K5/06034 ,  C07K14/57536 ,  C07K5/06156 ,  C07K5/0808 ,  C07K5/1021 ,  A61K38/00

    摘要： Hydroxamate compounds of the following formula are disclosed:R--AA.sup.3 --AA.sup.4 --AA.sup.5 --AA.sup.6 --NH--OR.sup.2wherein AA.sup.3 --AA.sup.6 represent amino acid residues. The disclosed compounds are inhibitors of endothelin converting enzyme, and as such are useful for the treatment of disorders resulting from overproduction of endothelin, i.e., acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, hypertension, myocardial infarction, metabolic, endocrinological, neurological disorders, congestire heart failure, endotoxic shock and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease, cerebral vasospasm, restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, ischemic bowel disease, and diabetes.

    摘要翻译： 公开了下式的羟基甲酸酯化合物：R-AA3-AA4-AA5-AA6-NH-OR2，其中AA3-AA6代表氨基酸残基。 所公开的化合物是内皮素转化酶的抑制剂，因此可用于治疗由过量产生的内皮素引起的疾病，即急性和慢性肾功能衰竭，环孢菌素A诱导的肾毒性，高血压，心肌梗塞，代谢，内分泌，神经系统 疾病，充血性心力衰竭，内毒素性休克和出血性休克，败血性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病，脑血管痉挛，再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病，胃粘膜损伤，缺血 肠病和糖尿病。