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1. 发明授权

US6110911A Cyclic amine derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists 失效
标题翻译：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。

2. 发明授权

US06455698B1 Conformationally semi-constrained quinoxaline 2,3-diones as neuroprotective agents 失效
标题翻译：构象半限制喹喔啉2,3-二酮作为神经保护剂
公开(公告)号：US06455698B1
公开(公告)日：2002-09-24
申请号：US09971237
申请日：2001-10-04
申请人： Brian Edward Kornberg , Sham Shridhar Nikam , Michael Francis Rafferty
发明人： Brian Edward Kornberg , Sham Shridhar Nikam , Michael Francis Rafferty
IPC分类号： C07D24128
CPC分类号： C07D401/04 , C07D241/44 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D413/04 , C07D413/06 , C07D417/04
摘要： A process is disclosed for the preparation of a compound of formula A process is also disclosed for preparing a compound of formula
摘要翻译：公开的制备式A化合物的方法也用于制备式的化合物

3. 发明授权

US06340758B1 Conformationally semi-constrained quinoxaline 2,3-diones as neuroprotective agents 失效
标题翻译：构象半限制喹喔啉2,3-二酮作为神经保护剂
公开(公告)号：US06340758B1
公开(公告)日：2002-01-22
申请号：US09199627
申请日：1998-11-25
申请人： Brian Edward Kornberg , Sham Shridhar Nikam , Michael Francis Rafferty
发明人： Brian Edward Kornberg , Sham Shridhar Nikam , Michael Francis Rafferty
IPC分类号： C07D24138
CPC分类号： C07D401/04 , C07D241/44 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D413/04 , C07D413/06 , C07D417/04
摘要： Described are neuroprotective agents of Formula I wherein R is an amino acid or nitrogen heterocyclic ring which is saturated or unsaturated of from 5 to 8 members which may have additional oxygen or sulfur atoms therein. The other provisions or substituents are described in the specification.
摘要翻译：描述了式I的神经保护剂，其中R是饱和或不饱和的5至8个成员的氨基酸或氮杂环，其可以在其中具有额外的氧或硫原子。其他规定或取代基在说明书中描述。

4. 发明授权

US5874426A Cyclic amine derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists 失效
标题翻译：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：US5874426A
公开(公告)日：1999-02-23
申请号：US474877
申请日：1995-06-07
申请人： Brian Edward Kornberg , Sham Nikam , Michael Francis Rafferty , Po-Wai Yuen
发明人： Brian Edward Kornberg , Sham Nikam , Michael Francis Rafferty , Po-Wai Yuen
IPC分类号： A61K31/495 , A61K31/535 , A61K31/55 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07D241/44 , C07D401/06 , C07D403/06 , C07D491/113
CPC分类号： C07D241/44
摘要： A novel series of substituted quinoxaline 2,3-diones of Formula I ##STR1## 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：教导了一种用作神经保护剂的式I的一系列取代的喹喔啉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。

5. 发明授权

US5654303A Alkyl amine derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists 失效
标题翻译：取代的喹喔啉2,3-二酮的烷基胺衍生物作为谷氨酸受体拮抗剂
公开(公告)号：US5654303A
公开(公告)日：1997-08-05
申请号：US474876
申请日：1995-06-07
申请人： Brian Edward Kornberg , Sham Nikam , Michael Francis Rafferty
发明人： Brian Edward Kornberg , Sham Nikam , Michael Francis Rafferty
IPC分类号： A61K31/495 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07D241/44 , C07D405/12 , C07D241/52 , C07D241/54
CPC分类号： C07D405/12 , 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, 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，阿尔茨海默病，帕金森病和亨廷顿病引起的脑卒中，脑缺血或脑梗塞。。

6. 发明授权

US6127418A GABA analogs to prevent and treat gastrointestinal damage 有权
标题翻译： GABA类似物可预防和治疗胃肠损伤
公开(公告)号：US6127418A
公开(公告)日：2000-10-03
申请号：US284710
申请日：1999-04-19
申请人： Lionel Bueno , Maria Chovet , Laurent Diop , Antonio Guglietta , Hilary J. Little , Michael Francis Rafferty , Jiayuan Ren , Charles Price Taylor, Jr. , William P. Watson
发明人： Lionel Bueno , Maria Chovet , Laurent Diop , Antonio Guglietta , Hilary J. Little , Michael Francis Rafferty , Jiayuan Ren , Charles Price Taylor, Jr. , William P. Watson
IPC分类号： A61K31/195 , A61K31/197 , A61K31/40 , A61K31/405 , A61K31/42 , A61K31/54 , A61K31/60
CPC分类号： A61K31/42 , A61K31/195 , A61K31/197 , A61K31/40 , A61K31/405 , A61K31/54 , A61K31/60
摘要： The present invention is directed to a method for preventing visceral and gastrointestinal damage such as gastric ulcers by administering a gamma-aminobutyric acid (GABA) analog and for treating gastrointestinal diseases such as inflammatory bowel disorders (IBD), functional bowel disorders (FBD) including dyspepsia and other visceral pain.
摘要翻译： PCT No.PCT / US98 / 17082 Sec。 371 1999年4月19日第 102（e）1999年4月19日PCT PCT 1998年8月18日PCT公布。 WO99 / 08671 PCT出版物日期1999年2月25日本发明涉及一种通过施用γ-氨基丁酸（GABA）类似物和用于治疗诸如炎性肠病（IBD），功能性肠胃肠疾病的胃内溃疡等内脏和胃肠道损伤的方法疾病（FBD）包括消化不良和其他内脏痛。

7. 发明授权

US06495715B2 Calcium channel blockers 失效
标题翻译：钙通道阻滞剂
公开(公告)号：US06495715B2
公开(公告)日：2002-12-17
申请号：US09769798
申请日：2001-01-25
申请人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder
发明人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder
IPC分类号： C07C5703
CPC分类号： C07D295/215 , C07B2200/07 , C07C237/10 , C07C2601/16 , C07D211/58
摘要： The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
摘要翻译：本发明提供了阻断下文所示的式I的钙通道的化合物。本发明还提供了使用式I化合物治疗中风，脑缺血，头部创伤或癫痫的方法以及含有下列化合物的药物组合物：一级方程式

8. 发明授权

US06469038B1 Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers 失效
标题翻译：杂芳基烷基α取代肽基胺钙通道阻断剂
公开(公告)号：US06469038B1
公开(公告)日：2002-10-22
申请号：US09663603
申请日：2000-09-18
申请人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
发明人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
IPC分类号： A61K31425
CPC分类号： C07D213/56 , C07D277/30
摘要： The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
摘要翻译：本发明提供了阻断下文所示的式I的钙通道的化合物。本发明还提供了使用式I化合物治疗中风，脑缺血，头部外伤，哮喘，肌萎缩性侧索硬化或癫痫的药物的方法以及药物含有式I化合物的组合物。

9. 发明授权

US06180677B2 Tyrosine-derived compounds as calcium channel antagonists 失效
标题翻译：酪氨酸衍生化合物作为钙通道拮抗剂
公开(公告)号：US06180677B2
公开(公告)日：2001-01-30
申请号：US09381938
申请日：1999-09-27
申请人： Michael Francis Rafferty , Yuntao Song
发明人： Michael Francis Rafferty , Yuntao Song
IPC分类号： A61K3803
CPC分类号： A61K31/4453 , A61K31/137 , A61K31/165 , A61K31/195
摘要： The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.
摘要翻译：本发明提供了阻断钙通道并具有式I的化合物及其药学上可接受的盐，酯和前药，其中R 1和R 2独立地为H，苯基环戊基羰基，C 1 -C 7烷基，环己基甲基，苄基，C 1 -C 5烷基苄基或C 1 -C 5烷氧基苄基，A是-C（O） - 或-CH 2 - ; R 3是H或-CH 3; R 4是C 1 -C 4烷基或哌啶-1-基乙基; R 5是苯基 - （CH 2） C 1 -C 4烷基苯基 - （CH 2）n - 或卤代苯基 - （CH 2）n - 并且n为1或2.本发明还提供了含有式I化合物的药物组合物及其用于治疗中风，脑缺血，头部创伤和癫痫的方法。

10. 发明授权

US06989448B2 Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers 失效
公开(公告)号：US06989448B2
公开(公告)日：2006-01-24
申请号：US10254416
申请日：2002-09-25
申请人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
发明人： Lain-Yen Hu , Michael Francis Rafferty , Todd Robert Ryder , Anthony Denver Sercel , Yuntao Song
IPC分类号： C07D401/00 , C07D211/08 , A61K31/445 , A61K31/47
CPC分类号： C07D213/56 , C07D277/30
摘要： The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.

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