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1. 发明申请

US20130303753A1 PREPARATION METHOD OF ROCURONIUM 有权
标题翻译：罗非鱼的制备方法
公开(公告)号：US20130303753A1
公开(公告)日：2013-11-14
申请号：US13991316
申请日：2011-01-26
申请人： Zhiwen Zeng , Wenling Zhang , Peng Wang , Xini Zhang
发明人： Zhiwen Zeng , Wenling Zhang , Peng Wang , Xini Zhang
IPC分类号： C07J43/00
CPC分类号： C07J43/003
摘要： A method for preparing rocuronium is disclosed. 2β-(4-Morpholinyl)-16β-(1-pyrrolidinyl)-5α-androstan-3α-ol-17β-acetate is used as a starting material and is directly reacted with 3-bromopropene at ambient temperature to produce rocuronium.
摘要翻译：公开了一种制备罗库溴铵的方法。使用2beta-（4-吗啉基）-16β-（1-吡咯烷基）-5α-雄甾烷-3α-醇-17β-乙酸酯作为原料，并在环境温度下与3-溴丙烯直接反应产生罗库溴铵。

2. 发明授权

US09067965B2 Preparation method of rocuronium 有权
标题翻译：罗库溴铵的制备方法
公开(公告)号：US09067965B2
公开(公告)日：2015-06-30
申请号：US13991316
申请日：2011-01-26
申请人： Zhiwen Zeng , Wenling Zhang , Peng Wang , Xini Zhang
发明人： Zhiwen Zeng , Wenling Zhang , Peng Wang , Xini Zhang
IPC分类号： C07J43/00
CPC分类号： C07J43/003
摘要： A method for preparing rocuronium is disclosed. 2β-(4-Morpholinyl)-16β-(1-pyrrolidinyl)-5α-androstan-3α-ol-17β-acetate is used as a starting material and is directly reacted with 3-bromopropene at ambient temperature to produce rocuronium.
摘要翻译：公开了一种制备罗库溴铵的方法。 2＆bgr--（4-吗啉基）-16＆bgr-（1-吡咯烷基）-5α-雄甾烷-3α-醇-17β-乙酸乙酯作为起始原料，并与环境温度下的3-溴丙烯直接反应生成罗库溴铵。

3. 发明授权

US09024013B2 Method for purifying rocuronium bromide 有权
标题翻译：罗库溴铵净化方法
公开(公告)号：US09024013B2
公开(公告)日：2015-05-05
申请号：US14122679
申请日：2011-04-25
申请人： Zhiwen Zeng , Peng Wang , Wenling Zhang , Xini Zhang
发明人： Zhiwen Zeng , Peng Wang , Wenling Zhang , Xini Zhang
IPC分类号： C07J43/00
CPC分类号： C07J43/003 , C07J43/00
摘要： Provided is a method for purifying rocuronium bromide, which comprises: formulating crude rocuronium bromide to be purified into an aqueous solution, distilling off excess residue solvents at reduced pressure, absorbing by adding active carbon or silica gel, then filtrating, quick freezing the filtrate into ice, and then lyophilizing to obtain rocuronium bromide.
摘要翻译：本发明提供了罗苏溴铵的纯化方法，其特征在于，将粗制的罗库溴铵配制成水溶液，减压蒸馏除去过剩的残留溶剂，通过加入活性炭或硅胶吸收，然后过滤，将滤液快速冷冻冰，然后冻干得到罗库溴铵。

4. 发明授权

US5688653A 3-alkylamino-2-hydroxy-4-hydroxymethyl-2-cyclopenten-1-one advanced glycosylation endproducts and methods of use therefor 失效
标题翻译： 3-烷基氨基-2-羟基-4-羟甲基-2-环戊烯-1-酮先进的糖基化终产物及其使用方法
公开(公告)号：US5688653A
公开(公告)日：1997-11-18
申请号：US673217
申请日：1996-06-27
申请人： Peter C. Ulrich , Xini Zhang
发明人： Peter C. Ulrich , Xini Zhang
IPC分类号： C07C225/20 , G01N33/53 , G01N33/573 , G01N33/72 , C07C205/00 , C07K16/00
CPC分类号： C07C225/20 , G01N33/5308 , G01N33/573 , G01N33/723 , C07C2101/10
摘要： The present invention relates to advanced glycosylation endproducts (AGEs), and particularly to novel cyclopentenone aminoreductones, 3-alkylamino-2-hydroxy-4-hydroxymethyl-2-cyclopenten-1-ones. Such AGEs can be used in various diagnostic and therapeutic methods.
摘要翻译：本发明涉及高级糖基化终产物（AGE），特别涉及新的环戊烯酮氨基转移酶，3-烷基氨基-2-羟基-4-羟甲基-2-环戊烯-1-酮。这样的AGE可以用于各种诊断和治疗方法。

5. 发明申请

US20080021044A1 N-[2-[[(DIAMINOMETHYLENE)AMINO]OXY]ETHYL]-3-[(2,2-DIFLUORO-2-PHENYLETHYL)AMINO]-6-METHYL-2-OXO-1(2H)-PYRAZINEACETAMIDE 审中-公开
标题翻译： N- [2 - [[（二氨基乙烯基）氨基]氧基]乙基] -3 - [（2,2-二氟-2-苯基）氨基] -6-甲基-2-氧代-1（2H） - 吡嗪胺
公开(公告)号：US20080021044A1
公开(公告)日：2008-01-24
申请号：US11751155
申请日：2007-05-21
申请人： Mitul Patel , Christopher Nilsen , Mayra Reyes , Michael Humora , Yun Qian , Fuqiang Liu , Xini Zhang , Kirk Sorgi
发明人： Mitul Patel , Christopher Nilsen , Mayra Reyes , Michael Humora , Yun Qian , Fuqiang Liu , Xini Zhang , Kirk Sorgi
IPC分类号： A61K31/4965 , A61P7/02 , C07D241/08
CPC分类号： C07D241/20
摘要： The present invention is directed to N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-s-oxo-1(2H)-pyrazineacetamide, pharmaceutical compositions containing said compound and methods of treatment comprising inhibiting a serine protease using said compound. The present invention is further directed to a process for the preparation of the N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2H)-pyrazineacetamide as a free base. The present invention is further directed to a process for the preparation of pharmaceutically acceptable salts of N-[2-[[(aminoiminomethyl)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2H)-pyrazineacetamide.
摘要翻译：本发明涉及N- [2 - [[（二氨基亚甲基）氨基]氧基]乙基] -3 - [（2,2-二氟-2-苯基乙基）氨基] -6-甲基-3-氧代-1（ 2H） - 吡嗪乙酰胺，含有所述化合物的药物组合物和治疗方法，包括使用所述化合物抑制丝氨酸蛋白酶。本发明进一步涉及制备N- [2 - [[（二氨基亚甲基）氨基]氧基]乙基] -3 - [（2,2-二氟-2-苯乙基）氨基] -6- 甲基-2-氧代-1（2H） - 吡嗪乙酰胺，为游离碱。本发明进一步涉及制备N- [2 - [[（氨基亚氨基甲基）氨基]氧基]乙基] -3 - [（2,2-二氟-2-苯基乙基）氨基] -6-甲基-2-氧代-1（2H） - 吡嗪乙酰胺。

6. 发明授权

US5948896A Processes for preparing 13-deoxy anthracycline derivatives 失效
标题翻译：制备13-脱氧蒽环类衍生物的方法
公开(公告)号：US5948896A
公开(公告)日：1999-09-07
申请号：US910218
申请日：1997-08-13
申请人： Xini Zhang
发明人： Xini Zhang
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H17/08 , C07H15/24
CPC分类号： A61K31/704 , C07H15/252
摘要： A process for the preparation of 13-deoxy deoxyanthracycline derivatives.
摘要翻译：一种制备13-脱氧脱氧尿素环衍生物的方法。

7. 发明授权

US5935927A Compositions and methods for stimulating amyloid removal in amyloidogenic diseases using advanced glycosylation endproducts 失效
标题翻译：使用高级糖基化终产物刺激淀粉样变性疾病中淀粉样蛋白去除的组合物和方法
公开(公告)号：US5935927A
公开(公告)日：1999-08-10
申请号：US501127
申请日：1996-08-10
申请人： Michael P. Vitek , Anthony Cerami , Richard J. Bucala , Peter C. Ulrich , Helen Vlassara , Xini Zhang
发明人： Michael P. Vitek , Anthony Cerami , Richard J. Bucala , Peter C. Ulrich , Helen Vlassara , Xini Zhang
IPC分类号： G01N33/68 , A61K31/047 , A61K31/15 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/425 , A61K31/428 , A61K31/655 , A61K31/7028 , A61K31/715 , A61K38/00 , A61K38/16 , A61K39/395 , A61K45/00 , A61P3/08 , A61P3/10 , A61P9/00 , A61P25/00 , A61P25/28 , A61P43/00 , C07D277/82 , C07D417/12 , C07H15/26 , C07K14/47 , C07K14/575 , A61K31/135 , A61K31/70
CPC分类号： A61K31/425 , A61K31/15 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/655 , C07K14/4711 , C07K14/575 , A61K38/00
摘要： The present invention relates generally to methods and compositions for treating amyloidogenic diseases such as Alzheimer's disease and the development of type II diabetes, in which deposition of amyloid in organs such as the brain and pancreas interfere with neurological function and insulin release, respectively. The methods and compositions are directed toward increasing the activity of scavenger cells within the body at recognizing and removing amyloid deposits from affected tissues and organs. Scavenger cells may be targeted to amyloid deposits by means of spontaneously-occurring chemical modifications called advanced glycosylation endproducts (AGEs). Compositions are described which increase scavenger cell activity towards AGE-modified amyloid. Amyloid removal may also be enhanced by increasing AGE levels in amyloid deposits within the body by administering AGE-modified amyloid targeting agents, which after becoming situated at sites containing amyloid, subsequently attract scavenger cells to degrade attendant amyloid. These methods and associated compositions result in a decrease in the extent of amyloid deposits in tissues, reducing the attendant pathology.
摘要翻译： PCT No.PCT / US95 / 01380 Sec。 371日期：1996年8月10日 102（e）日期1996年8月10日PCT提交1995年2月2日PCT公布。第WO95 / 20979号公报日期：1995年8月10日本发明一般涉及用于治疗淀粉样变性疾病如阿尔茨海默氏病和II型糖尿病发展的方法和组合物，其中淀粉样蛋白沉积在诸如脑和胰腺的器官中干扰神经功能和胰岛素释放，分别。所述方法和组合物旨在增加识别和去除受影响组织和器官中的淀粉样蛋白沉积物中体内清除细胞的活性。清除细胞可以通过称为晚期糖基化终产物（AGE）的自发发生的化学修饰来靶向淀粉样蛋白沉积物。描述了增加AGE修饰的淀粉样蛋白的清除细胞活性的组合物。通过施用AGE修饰的淀粉样蛋白靶向剂，其在位于含有淀粉样蛋白的位点后，随后吸引清道细胞降解伴随的淀粉样蛋白，也可以通过增加体内淀粉样蛋白沉积物中的AGE水平来增强淀粉样蛋白的去除。这些方法和相关组合物导致组织中淀粉样蛋白沉积的程度降低，减少伴随的病理。

8. 发明授权

US5814664A 3-alkylamino-2-hydroxy-4-hydroxymethyl-2-cyclopenten-1-one advanced glycosylation endproducts and methods of use therefor 失效
标题翻译： 3-烷基氨基-2-羟基-4-羟甲基-2-环戊烯-1-酮先进的糖基化终产物及其使用方法
公开(公告)号：US5814664A
公开(公告)日：1998-09-29
申请号：US880565
申请日：1997-06-23
申请人： Peter C. Ulrich , Xini Zhang
发明人： Peter C. Ulrich , Xini Zhang
IPC分类号： G01N33/53 , G01N33/573
CPC分类号： G01N33/573 , G01N33/5308 , Y10S436/815 , Y10T436/104998 , Y10T436/105831 , Y10T436/173845 , Y10T436/200833
摘要： The present invention relates to advanced glycosylation endproducts, and particularly to the use of novel cyclopentenone aminoreductones, 3-alkylamino-2 -hydroxy-4-hydroxymethyl-2-cyclopenten-1-ones. Such AGEs can be used in various diagnostic and therapeutic methods.
摘要翻译：本发明涉及高级糖基化终产物，特别涉及新的环戊烯酮氨基还原酮，3-烷基氨基-2-羟基-4-羟甲基-2-环戊烯-1-酮的用途。这样的AGE可以用于各种诊断和治疗方法。

9. 发明授权

US06410598B1 Compositions and methods for advanced glycosylation endproduct-mediated modulation of amyloidosis 失效
标题翻译：用于高级糖基化终末产物介导的淀粉样变性调节的组合物和方法
公开(公告)号：US06410598B1
公开(公告)日：2002-06-25
申请号：US08477364
申请日：1995-06-07
申请人： Michael P. Vitek , Anthony Cerami , Richard J. Bucala , Peter C. Ulrich , Helen Vlassara , Xini Zhang
发明人： Michael P. Vitek , Anthony Cerami , Richard J. Bucala , Peter C. Ulrich , Helen Vlassara , Xini Zhang
IPC分类号： A01N3752
CPC分类号： A61K31/15 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/425 , A61K31/655 , A61K38/00 , C07K14/4711 , C07K14/575
摘要： The present invention relates generally to the non-enzymatic glycosylation of amyloidogenic proteins and the consequent formation of advanced glycosylation endproducts (AGEs). It has been found that formation of AGE-amyloidogenic proteins can enhance amyloidosis. The invention further relates to compositions and methods for the prevention and treatment of amyloidosis associated with amyloid diseases, particularly neurodegenerative disease and Type II diabetes, and more particularly Alzheimer's disease. In a specific example, aggregation of an amyloidogenic peptide, &bgr;AP, is enhanced by the glycosylation reaction of &bgr;AP to form AGE-&bgr;AP as defined herein. Accordingly, the invention extends to a method for modulating the in vivo aggregation of amyloid polypeptides and associated amyloidosis by controlling the formation and presence of AGE-amyloid polypeptide. A corresponding diagnostic utility comprises the measurement of the course and extent of amyloidosis by a measurement of the presence and amount of AGEs and particularly, AGE-amyloid. An assay is included that may use the AGE-amyloid polypeptide of the present invention to identify disease states characterized by the presence of AGE-amyloid. Additionally, such an assay can be utilized to monitor therapy and thus adjust a dosage regimen for a given disease state characterized by the presence of AGE-amyloid.
摘要翻译：本发明一般涉及淀粉样蛋白形成蛋白的非酶糖基化，从而形成晚期糖基化终产物（AGEs）。已经发现AGE-淀粉样蛋白生成蛋白的形成可以增强淀粉样变性。本发明进一步涉及用于预防和治疗与淀粉样蛋白病，特别是神经变性疾病和II型糖尿病，更特别是阿尔茨海默病有关的淀粉样变性的组合物和方法。在具体实例中，通过βAP的糖基化反应来增强淀粉样蛋白原肽βAP的聚集，从而形成如本文所定义的AGE-βAP。因此，本发明延伸到通过控制AGE-淀粉样蛋白多肽的形成和存在来调节淀粉样蛋白多肽的体内聚集和相关淀粉样变性的方法。相应的诊断实用程序包括测量AGEs，特别是AGE-淀粉样蛋白的存在和量的淀粉样变性的过程和程度。包括可以使用本发明的AGE-淀粉样蛋白多肽来鉴定以AGE-淀粉样蛋白的存在为特征的疾病状态的测定。另外，这种测定可用于监测治疗，并因此调整特征在于AGE-淀粉样蛋白存在的给定疾病状态的剂量方案。

10. 发明授权

US5942605A 5-imino-13-deoxy anthracycline derivatives, their uses, and processes for preparing them 失效
标题翻译： 5-亚氨基-13-脱氧蒽环类衍生物，其用途及其制备方法
公开(公告)号：US5942605A
公开(公告)日：1999-08-24
申请号：US33659
申请日：1998-03-03
申请人： Xini Zhang , Richard D. Olson
发明人： Xini Zhang , Richard D. Olson
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/04 , A61P37/06 , C07H15/252 , C07H15/24
CPC分类号： A61K31/704 , C07H15/252
摘要： 5-imino-13-deoxy anthracycline derivatives, medical uses of 5-imino-13-deoxy anthracycline derivatives and methods for preparing 5-imino-13-deoxy anthracycline derivatives.
摘要翻译： 5-亚氨基-13-脱氧蒽环类衍生物，5-亚氨基-13-脱氧蒽环类衍生物的医药用途及5-亚氨基-13-脱氧蒽环类衍生物的制备方法。

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