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1. 发明授权

US09018393B2 Method for preparing 2-(N-substituted)-amino-benzimidazole derivatives 有权
标题翻译： 2-（N-取代） - 氨基 - 苯并咪唑衍生物的制备方法
公开(公告)号：US09018393B2
公开(公告)日：2015-04-28
申请号：US13976865
申请日：2011-01-26
申请人： Yueheng Jiang , Tong Cai , Limin Que , Zhigang Lin
发明人： Yueheng Jiang , Tong Cai , Limin Que , Zhigang Lin
IPC分类号： C07D235/30 , C07C303/40 , C07D235/14
CPC分类号： C07D235/30 , C07C273/1836 , C07C303/40 , C07D235/14 , Y02P20/55 , C07C311/21 , C07C275/40
摘要： A method for preparing 2-(N-substituted)-amino-benzimidazole derivatives is provided, which comprises the following steps: (1) reacting a compound of 2-(N-protecting group)-O-aryl diamine with a compound of N-phenoxycarbonyl monosubstituted amine to obtain a compound of 2-(N-protecting group)-amino aryl urea; (2) in a suitable organic solvent, performing dehydrating cyclization reaction of the compound of 2-(N-protecting group)-amino aryl urea in the presence of an organic base and dichloro triphenylphosphine prepared by triphenylphosphine oxide with oxalyl chloride or diphosgene or triphosgene, or dibromo triphenylphosphine prepared by triphenylphosphine oxide with bromine, to produce a compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole; (3) deprotecting the resulting compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole to obtain the compound 2-(N-substituted)-amino-benzimidazole.
摘要翻译：提供了制备2-（N-取代的） - 氨基 - 苯并咪唑衍生物的方法，其包括以下步骤：（1）使2-（N-保护基）-O-芳基二胺的化合物与N - 苯氧基羰基单取代胺，得到2-（N-保护基） - 氨基芳基脲的化合物; （2）在合适的有机溶剂中，在有机碱和通过三苯基氧化膦与草酰氯或双光气或三光气制备的二氯三苯基膦存在下进行2-（N-保护基） - 氨基芳基脲的化合物的脱水环化反应或由三苯基膦氧化物与溴制备的二溴三苯基膦，得到1-保护基-2-（N-取代的） - 氨基 - 苯并咪唑的化合物; （3）将所得的1-保护基-2-（N-取代的） - 氨基 - 苯并咪唑化合物脱保护，得到化合物2-（N-取代的） - 氨基 - 苯并咪唑。

2. 发明授权

US07347988B2 Synthesis, uses and compositions of crystal hydrogels 失效
标题翻译：水凝胶的合成，用途和组成
公开(公告)号：US07347988B2
公开(公告)日：2008-03-25
申请号：US10295484
申请日：2002-11-15
申请人： Zhibing Hu , Xihua Lu , Jun Gao , Tong Cai , Gang Huang , Bo Zhou
发明人： Zhibing Hu , Xihua Lu , Jun Gao , Tong Cai , Gang Huang , Bo Zhou
IPC分类号： A61K7/021
CPC分类号： G02B1/04 , C08F220/56 , C08J3/075 , G01N2021/7723
摘要： A method is disclosed for creating hydrogels with ordered crystalline structures that exhibit a characteristic colored opalescence. In addition to the unique optical properties, these materials contain a large amount of water in their crosslinked networks. The manufacturing processes include synthesizing monodispersed hydrogel nanoparticles containing specific reactive functional groups, self-assembly of these particles to form a crystalline structure, and subsequent crosslinking neighboring spheres to stabilize the entire network. Polymerizing a hydrogel monomeric composition around the crystalline structure can enhance the mechanical strength. The resulting network is dimensionally and thermodynamically stabile under various pH and temperature conditions. The color and volume of these crystalline hydrogel networks can reversibly change in response to external stimuli such as temperature, pH and other environmental conditions. These new materials may lead to a variety of technological and artistic applications, ranging from sensors, displays, controlled drug delivery devices, jewelry and decorative consumer products.
摘要翻译：公开了一种用于产生具有有色晶体结构的水凝胶的方法，其具有特征性的着色乳光。除了独特的光学性能之外，这些材料在其交联网络中含有大量的水。制造方法包括合成包含特定反应性官能团的单分散水凝胶纳米颗粒，这些颗粒的自组装形成晶体结构，随后交联相邻球体以稳定整个网络。在晶体结构周围聚合水凝胶单体组合物可以增强机械强度。所得到的网络在各种pH和温度条件下在尺寸和热力学上是稳定的。这些结晶水凝胶网络的颜色和体积可以响应于诸如温度，pH和其他环境条件的外部刺激而可逆地改变。这些新材料可能导致各种技术和艺术应用，从传感器，显示器，受控药物输送装置，首饰和装饰消费品。

3. 发明申请

US20080044472A1 Photoresponsive Hydrogels 审中-公开
标题翻译：光反应性水凝胶
公开(公告)号：US20080044472A1
公开(公告)日：2008-02-21
申请号：US10587229
申请日：2005-01-24
申请人： Antonio Garcia , Rohit Rosario , John Gust , Mark Hayes , Manuel Marquez , Zhibing Hu , Tong Cai
发明人： Antonio Garcia , Rohit Rosario , John Gust , Mark Hayes , Manuel Marquez , Zhibing Hu , Tong Cai
IPC分类号： A61K31/407 , A61K31/711 , A61K45/00 , A61K9/14 , A61P29/00
CPC分类号： C08F2/50 , A61K47/34
摘要： Disclosed are photoresponsive hydrogels. The compositions disclosed herein can be prepared by polymerizing a hydrogel precursor and a spiropyran. The properties of the disclosed compositions can be changed by exposure to light, pH, and temperature. Methods of using the disclosed compositions to deliver pharmaceutical actives are also disclosed.
摘要翻译：公开了光响应水凝胶。本文公开的组合物可以通过聚合水凝胶前体和螺吡喃来制备。所公开的组合物的性质可以通过暴露于光，pH和温度而改变。还公开了使用所公开的组合物递送药物活性物质的方法。

4. 发明申请

US20130345436A1 method for preparing 2-(N-substituted)-amino-benzimidazole derivatives 有权
标题翻译：制备2-（N-取代） - 氨基 - 苯并咪唑衍生物的方法
公开(公告)号：US20130345436A1
公开(公告)日：2013-12-26
申请号：US13976865
申请日：2011-01-26
申请人： Yueheng Jiang , Tong Cai , Limin Que , Zhigang Lin
发明人： Yueheng Jiang , Tong Cai , Limin Que , Zhigang Lin
IPC分类号： C07D235/30
CPC分类号： C07D235/30 , C07C273/1836 , C07C303/40 , C07D235/14 , Y02P20/55 , C07C311/21 , C07C275/40
摘要： A method for preparing 2-(N-substituted)-amino-benzimidazole derivatives is provided, which comprises the following steps: (1) reacting a compound of 2-(N-protecting group)-O-aryl diamine with a compound of N-phenoxycarbonyl monosubstituted amine to obtain a compound of 2-(N-protecting group)-amino aryl urea; (2) in a suitable organic solvent, performing dehydrating cyclization reaction of the compound of 2-(N-protecting group)-amino aryl urea in the presence of an organic base and dichloro triphenylphosphine prepared by triphenylphosphine oxide with oxalyl chloride or diphosgene or triphosgene, or dibromo triphenylphosphine prepared by triphenylphosphine oxide with bromine, to produce a compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole; (3) deprotecting the resulting compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole to obtain the compound 2-(N-substituted)-amino-benzimidazole.
摘要翻译：提供了制备2-（N-取代的） - 氨基 - 苯并咪唑衍生物的方法，其包括以下步骤：（1）使2-（N-保护基）-O-芳基二胺的化合物与N - 苯氧基羰基单取代胺，得到2-（N-保护基） - 氨基芳基脲的化合物; （2）在合适的有机溶剂中，在有机碱和通过三苯基氧化膦与草酰氯或双光气或三光气制备的二氯三苯基膦存在下进行2-（N-保护基） - 氨基芳基脲的化合物的脱水环化反应或由三苯基膦氧化物与溴制备的二溴三苯基膦，得到1-保护基-2-（N-取代的） - 氨基 - 苯并咪唑的化合物; （3）将所得的1-保护基-2-（N-取代的） - 氨基 - 苯并咪唑化合物脱保护，得到化合物2-（N-取代的） - 氨基 - 苯并咪唑。

5. 发明授权

US07989505B2 Synthesis of columnar hydrogel colloidal crystals in water-organic solvent mixture 失效
标题翻译：在水 - 有机溶剂混合物中合成柱状水凝胶胶体晶体
公开(公告)号：US07989505B2
公开(公告)日：2011-08-02
申请号：US11524703
申请日：2006-09-21
申请人： Zhibing Hu , Jun Zhou , Tong Cai , Shijun Tang , Manuel Marquez
发明人： Zhibing Hu , Jun Zhou , Tong Cai , Shijun Tang , Manuel Marquez
IPC分类号： C08J3/05 , C08J3/075 , B01F3/12
CPC分类号： C30B5/00 , C30B29/58
摘要： The compositions of hydrogel colloidal crystals are made from mixing an aqueous suspension of poly-N-isopropylacrylamide (“PNIPAM”)-co-allylamine microgels with dichloromethane, forming a PNIPAM-co-allylamine/dichloromethane mixture. The PNIPAM-co-allylamine/dichloromethane mixture is incubated for a period of time at a given temperature, forming the colloidal crystal material. The colloidal crystals can be stabilized by diffusing a glutaric dialdehyde solution into the colloidal crystal material. The concentration of polymer matrix microgels can determine the orientation of random or columnar crystals.
摘要翻译：水凝胶胶体晶体的组成通过将聚-N-异丙基丙烯酰胺（“PNIPAM”） - 共 - 烯丙基胺微凝胶的水悬浮液与二氯甲烷混合，形成PNIPAM-共 - 烯丙基胺/二氯甲烷混合物来制备。将PNIPAM-共 - 烯丙基胺/二氯甲烷混合物在给定温度下温育一段时间，形成胶体晶体材料。可以通过将戊二醛溶液扩散到胶体晶体材料中来稳定胶体晶体。聚合物基质微凝胶的浓度可以确定随机或柱状晶体的取向。

6. 发明申请

US20100261814A1 Synthesis of columnar hydrogel colloidal crystals in water-organic solvent mixture 失效
标题翻译：在水 - 有机溶剂混合物中合成柱状水凝胶胶体晶体
公开(公告)号：US20100261814A1
公开(公告)日：2010-10-14
申请号：US11524703
申请日：2006-09-21
申请人： Zhibing Hu , Jun Zhou , Tong Cai , Shijun Tang , Manuel Marquez
发明人： Zhibing Hu , Jun Zhou , Tong Cai , Shijun Tang , Manuel Marquez
IPC分类号： C08K5/02 , C08L33/24
CPC分类号： C30B5/00 , C30B29/58
摘要： The compositions of hydrogel colloidal crystals are made from mixing an aqueous suspension of poly-N-isopropylacrylamide (“PNIPAM”)-co-allylamine microgels with dichloromethane, forming a PNIPAM-co-allylamine/dichloromethane mixture. The PNIPAM-co-allylamine/dichloromethane mixture is incubated for a period of time at a given temperature, forming the colloidal crystal material. The colloidal crystals can be stabilized by diffusing a glutaric dialdehyde solution into the colloidal crystal material. The concentration of polymer matrix microgels can determine the orientation of random or columnar crystals.
摘要翻译：水凝胶胶体晶体的组成通过将聚-N-异丙基丙烯酰胺（“PNIPAM”） - 共 - 烯丙基胺微凝胶的水悬浮液与二氯甲烷混合，形成PNIPAM-共 - 烯丙基胺/二氯甲烷混合物来制备。将PNIPAM-共 - 烯丙基胺/二氯甲烷混合物在给定温度下温育一段时间，形成胶体晶体材料。可以通过将戊二醛溶液扩散到胶体晶体材料中来稳定胶体晶体。聚合物基质微凝胶的浓度可以确定随机或柱状晶体的取向。

7. 发明授权

US09586912B2 2-substituted-2H-1, 2, 3-triazole derivative and its preparation method 有权
标题翻译： 2-取代-2H-1,2,3-三唑衍生物及其制备方法
公开(公告)号：US09586912B2
公开(公告)日：2017-03-07
申请号：US14422646
申请日：2012-08-24
申请人： Yueheng Jiang , Limin Que , Tong Cai , Dongguang Qin
发明人： Yueheng Jiang , Limin Que , Tong Cai , Dongguang Qin
IPC分类号： C07D249/04 , C07D405/04 , C07D405/06
CPC分类号： C07D249/04 , C07D405/04 , C07D405/06
摘要： Disclosed is a 2-substituted-2H-1,2,3-triazole derivative, a compound as represented by formula I or II. Also disclosed is a preparation method of the compound as represented by formula I or II, in particular to a preparation method of 2-substituted-4-bromo-5-chloro-1H-1,2,3-triazole, 2-substituted-4-bromo-5-iodo-1H-1,2,3-triazole, and 2-substituted-5-chloro-1H-1,2,3-triazole-4-carboxylic acid. The preparation methods of the present invention are simple and feasible, and has high yield of the obtained compounds.
摘要翻译：公开了2-取代-2H-1,2,3-三唑衍生物，由式I或II表示的化合物。还公开了式I或II表示的化合物的制备方法，特别是2-取代-4-溴-5-氯-1H-1,2,3-三唑的制备方法，2-取代的 4-溴-5-碘-1H-1,2,3-三唑和2-取代-5-氯-1H-1,2,3-三唑-4-羧酸。本发明的制备方法简单可行，得到的化合物的收率高。

8. 发明申请

US20130178651A1 PREPARATION METHOD OF HIGH-OPTICAL PURITY N2-[1-(S)-ETHOXYCARBONYL-3-PHENYLPROPYL]-N6-TRIFLUOROACETYL-L-LYSINE 有权
标题翻译：高光固化N2- [1-（S） - 乙氧羰基-3-苯基丙基] -N6-三氟乙酰基-L-赖氨酸的制备方法
公开(公告)号：US20130178651A1
公开(公告)日：2013-07-11
申请号：US13822690
申请日：2010-09-29
申请人： Limin Que , Yueheng Jiang , Zhigang Lin , Tong Cai
发明人： Limin Que , Yueheng Jiang , Zhigang Lin , Tong Cai
IPC分类号： C07C51/42
CPC分类号： C07C51/42 , C07B2200/07 , C07C231/20 , C07C233/47
摘要： Disclosed is a preparation method of high-optical purity N2-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine. The method includes: adding crude N2-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine to one or more organic solvents, and then reacting with an organic acid to form a salt, which is precipitated, thereby achieving the purpose of separation and purification; next, adding the obtained solid or mother concentrate into deionized water, and then adding an inorganic base or an organic base for basification, so as to adjust the pH value, removing the organic acid, filtering, washing and drying, to obtain the high-optical purity N2-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine, where the molar ratio of 1S-isomer to 1R-isomer is equal to or greater than 99:1.
摘要翻译：公开了高光学纯度N2- [1-（S） - 乙氧基羰基-3-苯基丙基] -N6-三氟乙酰基-L-赖氨酸的制备方法。该方法包括：向一种或多种有机溶剂中加入粗N2- [1-（S） - 乙氧基羰基-3-苯基丙基] -N6-三氟乙酰基-L-赖氨酸，然后与有机酸反应形成盐，沉淀，从而达到分离纯化的目的; 然后，将得到的固体或母体浓缩物加入去离子水中，然后加入无机碱或有机碱进行碱化，调节pH值，除去有机酸，过滤，洗涤和干燥，光学纯度N2- [1-（S） - 乙氧基羰基-3-苯基丙基] -N6-三氟乙酰基-L-赖氨酸，其中1S-异构体与1R-异构体的摩尔比等于或大于99:1。

9. 发明申请

US20100076105A1 MONODISPERSE THERMO-RESPONSIVE MICROGELS OF POLY(ETHYLENE GLYCOL) ANALOGUE-BASED BIOPOLYMERS, THEIR MANUFACTURE, AND THEIR APPLICATIONS 审中-公开
标题翻译：聚乙二醇（乙烯甘油）基于模拟物的生物聚合物的单体热响应微胶囊，其制备及其应用
公开(公告)号：US20100076105A1
公开(公告)日：2010-03-25
申请号：US12502842
申请日：2009-07-14
申请人： Zhibing Hu , Tong Cai , Chenglin Chi , Manuel Marquez
发明人： Zhibing Hu , Tong Cai , Chenglin Chi , Manuel Marquez
IPC分类号： C08L33/10 , C08F2/48
CPC分类号： C08F2/48 , C08L33/02 , C08L33/26 , C08L2666/04
摘要： Composition, processes, techniques, and apparatus for synthesizing monodisperse microgels based on poly(ethylene glycol) (PEG) derivative polymers by using precipitation polymerization. These microgels are hydrophilic and have the adjustable volume phase transition temperature in aqueous environment. Microgels can be added with various functional groups. These microgels in water can self-assemble into various phases, including a crystalline phase. Hydrogel films with iridescent colors were formed using these microgels as crosslinkers to connect poly(ethylene glycol) chains. The colors of these hydrogel films change with changes of environment such temperature, pH, salt concentration, etc.
摘要翻译：通过使用沉淀聚合法合成基于聚（乙二醇）（PEG）衍生物聚合物的单分散微凝胶的组合物，方法，技术和装置。这些微凝胶是亲水性的，并且在水性环境中具有可调节的体积相转变温度。微凝胶可以加入各种官能团。水中的这些微凝胶可以自组装成各种相，包括结晶相。使用这些微凝胶作为交联剂形成具有彩虹色的水凝胶膜以连接聚（乙二醇）链。这些水凝胶膜的颜色随温度，pH，盐浓度等环境变化而变化。

10. 发明申请

US20150232431A1 2-SUBSTITUTED-2H-1, 2, 3-TRIAZOLE DERIVATIVE AND ITS PREPARATION METHOD 审中-公开
标题翻译： 2-取代的2H-1,2,3-三唑衍生物及其制备方法
公开(公告)号：US20150232431A1
公开(公告)日：2015-08-20
申请号：US14422646
申请日：2012-08-24
申请人： Yueheng Jiang , Limin Que , Tong Cai , Dongguang Qin
发明人： Yueheng Jiang , Limin Que , Tong Cai , Dongguang Qin
IPC分类号： C07D249/04 , C07D405/04 , C07D405/06
CPC分类号： C07D249/04 , C07D405/04 , C07D405/06
摘要： Disclosed is a 2-substituted-2H-1,2,3-triazole derivative, a compound as represented by formula I or II. Also disclosed is a preparation method of the compound as represented by formula I or II, in particular to a preparation method of 2-substituted-4-bromo-5-chloro-1H-1,2,3-triazole, 2-substituted-4-bromo-5-iodo-1H-1,2,3-triazole, and 2-substituted-5-chloro-1H-1,2,3-triazole-4-carboxylic acid. The preparation methods of the present invention are simple and feasible, and has high yield of the obtained compounds.
摘要翻译：公开了2-取代-2H-1,2,3-三唑衍生物，由式I或II表示的化合物。还公开了式I或II表示的化合物的制备方法，特别是2-取代-4-溴-5-氯-1H-1,2,3-三唑的制备方法，2-取代的 4-溴-5-碘-1H-1,2,3-三唑和2-取代-5-氯-1H-1,2,3-三唑-4-羧酸。本发明的制备方法简单可行，得到的化合物的收率高。

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