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1. 发明授权

US06417396B1 Quenching reagents for solution phase synthesis 失效
标题翻译：淬灭试剂进行溶液相合成
公开(公告)号：US06417396B1
公开(公告)日：2002-07-09
申请号：US09579075
申请日：2000-05-25
申请人： Sham Nikam
发明人： Sham Nikam
IPC分类号： C07C27302
CPC分类号： C07C303/38 , B01J2219/00599 , C07C231/02 , C07C231/24 , C07C273/1827 , C07C273/189 , C40B50/08 , C07C311/16 , C07C311/29
摘要： A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.
摘要翻译：一种提高所需化合物纯度的方法，包括：步骤（a）用至少一种能够选择性共价反应的双官能猝灭剂处理含有至少一种所需化合物的粗制反应产物，未反应的起始物和/或副产物与不需要的副产物或过量的试剂反应;步骤（b）使淬灭剂与未反应的起始原料和/或副产物共价反应，得到猝灭剂的衍生化合物：步骤（c）分离所需化合物以及新型猝灭剂及其在快速纯化合成中间体和产物合成，组合化学和自动化有机合成中的应用。

2. 发明授权

US5614508A Amino acid derivatives of substituted quinoxaline 2,3-dione derivatives as glutamate receptor antagonists 失效
标题翻译：取代喹喔啉2,3-二酮衍生物作为谷氨酸受体拮抗剂的氨基酸衍生物
公开(公告)号：US5614508A
公开(公告)日：1997-03-25
申请号：US474878
申请日：1995-06-07
申请人： Sham Nikam
发明人： Sham Nikam
IPC分类号： A61K31/495 , A61P3/08 , A61P9/00 , A61P9/06 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , C07C229/14 , C07C229/20 , C07D241/44 , C07F9/6509 , C07D241/52
CPC分类号： C07C229/14 , C07D241/44 , C07F9/650994
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。。

3. 发明授权

US5773444A Quinazolines as inhibitors of endothelin converting enzyme 失效
标题翻译：喹唑啉作为内皮素转化酶的抑制剂
公开(公告)号：US5773444A
公开(公告)日：1998-06-30
申请号：US837176
申请日：1997-04-14
申请人： Kyunghye Ahn , Xue-Min Cheng , Annette Marian Doherty , Edward Faith Elslager , Brian Kornberg , Chitase Lee , Daniele Leonard , Sham Nikam , Leslie Morton Werbel
发明人： Kyunghye Ahn , Xue-Min Cheng , Annette Marian Doherty , Edward Faith Elslager , Brian Kornberg , Chitase Lee , Daniele Leonard , Sham Nikam , Leslie Morton Werbel
IPC分类号： C07D239/74 , A61K31/505 , A61K31/517 , A61P43/00 , C07D239/90 , C07D239/91 , C07D239/94 , C07D401/12 , C07D403/12 , C07D453/02 , A61K31/495 , A61K31/535
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07D453/02
摘要： Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.
摘要翻译：描述了内皮素转化酶的新型喹唑啉抑制剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素和控制高血压，心肌梗死和缺血，代谢，内分泌和神经障碍，充血性心力衰竭，内毒素性和出血性休克，败血性休克，蛛网膜下腔出血，心律失常，哮喘，急性和慢性肾功能衰竭，环孢菌素A诱导的肾毒性，心绞痛，胃粘膜损伤，缺血性肠病，癌症，肺动脉高压，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，脑缺血和血管痉挛以及糖尿病。

4. 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。。

5. 发明申请

US20050282819A1 Heterocyclic substituted indane derivatives and related compounds for the treatment of schizophrenia 审中-公开
标题翻译：杂环取代的茚满衍生物和相关化合物用于治疗精神分裂症
公开(公告)号：US20050282819A1
公开(公告)日：2005-12-22
申请号：US11007486
申请日：2004-12-08
申请人： James Graham , Brian Kornberg , Sham Nikam , Dejian Xie
发明人： James Graham , Brian Kornberg , Sham Nikam , Dejian Xie
IPC分类号： A61K31/42 , A61K31/425 , A61K31/496 , A61K31/497 , C07D261/20 , C07D275/04 , C07D417/02 , C07D417/12
CPC分类号： C07D261/20 , C07D275/04 , C07D417/12
摘要： This invention relates to compounds of the formula 1 wherein J, M, G, m, X, R1, R2, R4, R5, R6, R7, R8, R9, Y, n, z, and R11 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.
摘要翻译：本发明涉及式1化合物，其中J，M，G，m，X，R 1，R 2，R 4， R 5，R 6，R 7，R 8，R 9， Y，n，z和R 11如说明书中所定义，含有它们的药物组合物及其在治疗中枢神经系统和其它疾病中的用途。

6. 发明授权

US06395930B1 Quenching reagents for solution phase synthesis 失效
公开(公告)号：US06395930B1
公开(公告)日：2002-05-28
申请号：US09577393
申请日：2000-05-25
申请人： Sham Nikam
发明人： Sham Nikam
IPC分类号： C07C32102
CPC分类号： C07C303/38 , B01J2219/00599 , C07C231/02 , C07C231/24 , C07C273/1827 , C07C273/189 , C40B50/08 , C07C311/29 , C07C311/16
摘要： A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.

7. 发明授权

US6121488A Quenching reagents for solution phase synthesis 失效
标题翻译：淬灭试剂进行溶液相合成
公开(公告)号：US6121488A
公开(公告)日：2000-09-19
申请号：US157869
申请日：1998-09-21
申请人： Sham Nikam
发明人： Sham Nikam
IPC分类号： C07B61/00 , C07C231/02 , C07C231/24 , C07C273/18 , C07C303/38 , C07C311/16 , C07C311/29 , C40B50/08 , C07C273/02
CPC分类号： C07C303/38 , C07C231/02 , C07C231/24 , C07C273/1827 , C07C273/189 , B01J2219/00599 , C40B50/08
摘要： A method for enhancing the purity of a desired compound comprising:Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents;Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: andStep (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.
摘要翻译：一种提高所需化合物纯度的方法，包括：步骤（a）用至少一种能够选择性共价反应的双官能猝灭剂处理含有至少一种所需化合物的粗制反应产物，未反应的起始物和/或副产物不需要的副产物或多余试剂; 步骤（b）使淬灭剂与未反应的起始原料和/或副产物共价反应，得到猝灭剂的衍生化合物：和步骤（c）分离所需化合物以及新的淬灭剂及其制备方法用于快速纯化合成中间体和产品的合成，组合化学和自动化的有机合成。

8. 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。

9. 发明授权

US5658902A Quinazolines as inhibitors of endothelin converting enzyme 失效
标题翻译：喹唑啉作为内皮素转化酶的抑制剂
公开(公告)号：US5658902A
公开(公告)日：1997-08-19
申请号：US363104
申请日：1994-12-22
申请人： Kyunghye Ahn , Xue-Min Cheng , Annette Marian Doherty , Edward Faith Elslager , Brian Kornberg , Chitase Lee , Daniele Leonard , Sham Nikam , Leslie Morton Werbel
发明人： Kyunghye Ahn , Xue-Min Cheng , Annette Marian Doherty , Edward Faith Elslager , Brian Kornberg , Chitase Lee , Daniele Leonard , Sham Nikam , Leslie Morton Werbel
IPC分类号： C07D239/74 , A61K31/505 , A61K31/517 , A61P43/00 , C07D239/90 , C07D239/91 , C07D239/94 , C07D401/12 , C07D403/12 , C07D453/02 , C07D405/12
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07D453/02
摘要： Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.
摘要翻译：描述了内皮素转化酶的新型喹唑啉抑制剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素和控制高血压，心肌梗死和缺血，代谢，内分泌和神经障碍，充血性心力衰竭，内毒素性和出血性休克，败血性休克，蛛网膜下腔出血，心律失常，哮喘，急性和慢性肾功能衰竭，环孢菌素A诱导的肾毒性，心绞痛，胃粘膜损伤，缺血性肠病，癌症，肺动脉高压，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，脑缺血和血管痉挛以及糖尿病。

10. 发明授权

US06172065B2 Urea and thiourea derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists 失效
标题翻译：取代喹喔啉2,3-二酮的尿素和硫脲衍生物作为谷氨酸受体拮抗剂
公开(公告)号：US06172065B2
公开(公告)日：2001-01-09
申请号：US09066442
申请日：1998-04-29
申请人： Sham Nikam
发明人： Sham Nikam
IPC分类号： A61K31498
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。

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