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1. 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。

2. 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。

3. 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。

4. 发明授权

US08940929B2 Preparation method of high-optical purity N2-[1 -(S)-ethoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine 有权
标题翻译：高光纯度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
公开(公告)号：US08940929B2
公开(公告)日：2015-01-27
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： C07C229/00 , C07C51/42 , C07C231/20
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。

5. 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。

6. 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。

7. 发明授权

US08143305B2 2,3-substituted indole derivatives for treating viral infections 失效
标题翻译：用于治疗病毒感染的2,3-取代的吲哚衍生物
公开(公告)号：US08143305B2
公开(公告)日：2012-03-27
申请号：US12675897
申请日：2008-08-27
申请人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih , Stephen J. Gavalas , Yueheng Jiang , Patrick A. Pinto , Haiyan Pu , Oleg B. Selyutin , Bancha Vibulbhan , Li Wang , Wanli Wu , Weiying Yang , Yuhua Huang , Hsueh-Cheng Huang , Robert Palermo , Boris Feld
发明人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih , Stephen J. Gavalas , Yueheng Jiang , Patrick A. Pinto , Haiyan Pu , Oleg B. Selyutin , Bancha Vibulbhan , Li Wang , Wanli Wu , Weiying Yang , Yuhua Huang , Hsueh-Cheng Huang , Robert Palermo , Boris Feld
IPC分类号： A01N43/38 , A61K31/40 , C07D209/04
CPC分类号： C07D417/14 , C07D209/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及2,3-取代的吲哚衍生物，包含至少一种2,3-取代的吲哚衍生物的组合物和使用2,3-取代的吲哚衍生物用于治疗或预防病毒感染或病毒相关的方法病人无序。

8. 发明申请

US20070054919A1 Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：吡嗪基取代的哌嗪 - 哌啶与CXCR3拮抗剂活性
公开(公告)号：US20070054919A1
公开(公告)日：2007-03-08
申请号：US11354138
申请日：2006-02-14
申请人： Stuart Rosenblum , Seong Kim , Qingbei Zeng , Michael Wong , Gopinadhan Anilkumar , Yueheng Jiang , Wensheng Yu , Joseph Kozlowski , Neng-Yang Shih , Bandarpalle Shankar , Brian McGuinness , Guizhen Dong , Lisa Zawacki , Douglas Hobbs , John Baldwin , Yuefei Shao
发明人： Stuart Rosenblum , Seong Kim , Qingbei Zeng , Michael Wong , Gopinadhan Anilkumar , Yueheng Jiang , Wensheng Yu , Joseph Kozlowski , Neng-Yang Shih , Bandarpalle Shankar , Brian McGuinness , Guizhen Dong , Lisa Zawacki , Douglas Hobbs , John Baldwin , Yuefei Shao
IPC分类号： A61K31/497 , C07D403/14
CPC分类号： C07D405/14 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：及其药学上可接受的盐，溶剂化物和酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

9. 发明授权

US08546420B2 4, 5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections 失效
标题翻译：用于治疗或预防HCV和相关病毒感染的5环环状吲哚衍生物
公开(公告)号：US08546420B2
公开(公告)日：2013-10-01
申请号：US12519728
申请日：2007-12-17
申请人： Gopinadhan N. Anilkumar , Yueheng Jiang , Stuart B. Rosenblum , Srikanth Venkatraman , Francisco Velazquez , Neng-Yang Shih , F. George Njoroge , Joseph A. Kozlowski
发明人： Gopinadhan N. Anilkumar , Yueheng Jiang , Stuart B. Rosenblum , Srikanth Venkatraman , Francisco Velazquez , Neng-Yang Shih , F. George Njoroge , Joseph A. Kozlowski
IPC分类号： A01N43/42 , A61K31/44 , C07D471/00 , C07D491/00
CPC分类号： C07D209/60 , C07D401/06 , C07D401/14 , C07D403/06 , C07D471/04 , C07D491/04
摘要： The present invention relates to 4,5-ring annulated indole derivatives of formula (I), compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient, wherein ring Z of formula (I), is cyclohexyl, cyclohexenyl, 6-membered heterocycloalkyl, 6-membered heterocycloalkenyl, 6-membered aryl or 6-membered heteroaryl, wherein R1, R2, R3, R6, R7 and R10 are as described herein.
摘要翻译：本发明涉及式（I）的4,5-环环状吲哚衍生物，包含至少一个4,5-环环状吲哚衍生物的组合物，以及使用4,5-环环状吲哚衍生物治疗或预防的方法病毒感染或病毒相关疾病，其中式（I）的环Z为环己基，环己烯基，6-元杂环烷基，6-元杂环烯基，6-元芳基或6-元杂芳基，其中R1， R2，R3，R6，R7和R10如本文所述。

10. 发明申请

US20110189127A1 TRICYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF 有权
标题翻译：三环吲哚衍生物及其使用方法
公开(公告)号：US20110189127A1
公开(公告)日：2011-08-04
申请号：US12997654
申请日：2009-06-10
申请人： Srikanth Venkatraman , Anilkumar Gopinadhan Nair , Kevin X. Chen , Francisco Valazquez , Qingbei Zeng , Duan Liu , Yueheng Jiang , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Stephen J. Gavalas , Patrick A. Pinto , Oleg B. Selyutin , Bancha Vibulbhan
发明人： Srikanth Venkatraman , Anilkumar Gopinadhan Nair , Kevin X. Chen , Francisco Valazquez , Qingbei Zeng , Duan Liu , Yueheng Jiang , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Stephen J. Gavalas , Patrick A. Pinto , Oleg B. Selyutin , Bancha Vibulbhan
IPC分类号： A61K31/4439 , C07D401/14 , C07D491/22 , A61K31/437 , A61K31/517 , A61K31/47 , A61K38/21 , A61K31/7052 , A61K39/00 , A61K39/395 , A61K31/7056 , A61P31/12
CPC分类号： C07D491/048 , C07D491/04 , C07D519/00
摘要： The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及三环吲哚衍生物，包含至少一种三环吲哚衍生物的组合物，以及使用三环吲哚衍生物治疗或预防患者病毒感染或病毒相关病症的方法。

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