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1. 发明授权

US08318772B2 Amine compounds and medical uses thereof 有权
标题翻译：胺化合物及其医疗用途
公开(公告)号：US08318772B2
公开(公告)日：2012-11-27
申请号：US13001379
申请日：2009-06-23
申请人： Bohua Zhong , Youzhi Zhang , Yanping Zhang , Rui Xue , Xinhua He , Yunfeng Li , Hongxia Chen , Nan Zhao , Meiying Li
发明人： Bohua Zhong , Youzhi Zhang , Yanping Zhang , Rui Xue , Xinhua He , Yunfeng Li , Hongxia Chen , Nan Zhao , Meiying Li
IPC分类号： A61K31/4535 , A61K31/4025 , A61K31/381 , A61K31/357 , A61K31/36 , C07D407/12 , C07D409/14 , C07D409/12
CPC分类号： C07D407/12 , C07D407/14 , C07D409/12 , C07D409/14
摘要： The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R1, R2 and n are given in the description, to a pharmaceutical composition containing the compound as active ingredient, and to use of the amine compound or its pharmaceutically acceptable salt for the manufacture of an anti-depressent drug.
摘要翻译：本发明涉及一种新的胺化合物或其药学上可接受的盐，其中X，R 1，R 2和n的定义在说明书中给出含有该化合物作为活性成分的药物组合物，以及使用该胺化合物或其药学上可接受的盐，用于制造抗抑郁药物。

2. 发明申请

US20110178127A1 AMINE COMPOUNDS AND MEDICAL USES THEREOF 有权
标题翻译：胺化合物及其医疗用途
公开(公告)号：US20110178127A1
公开(公告)日：2011-07-21
申请号：US13001379
申请日：2009-06-23
申请人： Bohua Zhong , Youzhi Zhang , Yangping Zhang , Rui Xue , Xinhua He , Yunfeng Li , Hongxia Chen , Nan Zhao , Melying Li
发明人： Bohua Zhong , Youzhi Zhang , Yangping Zhang , Rui Xue , Xinhua He , Yunfeng Li , Hongxia Chen , Nan Zhao , Melying Li
IPC分类号： A61K31/381 , C07D409/12 , C07D409/14 , C07D407/12 , A61K31/4025 , A61K31/4535 , A61K31/36 , A61K31/357 , A61P25/24
CPC分类号： C07D407/12 , C07D407/14 , C07D409/12 , C07D409/14
摘要： The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R1, R2 and n are given in the description, to a pharmaceutical composition containing the compound as active ingredient, and to use of the amine compound or its pharmaceutically acceptable salt for the manufacture of an anti-depressent drug.
摘要翻译：本发明涉及一种新的胺化合物或其药学上可接受的盐，其中X，R 1，R 2和n的定义在说明书中给出含有该化合物作为活性成分的药物组合物，以及使用该胺化合物或其药学上可接受的盐，用于制造抗抑郁药物。

3. 发明授权

US09187507B2 Acyclic nucleoside phosphonate derivatives and medical uses thereof 有权
标题翻译：非环型核苷膦酸衍生物及其医疗用途
公开(公告)号：US09187507B2
公开(公告)日：2015-11-17
申请号：US13514749
申请日：2010-06-21
申请人： Bohua Zhong , Xinhua He , Yongguang Wang , He Liu
发明人： Bohua Zhong , Xinhua He , Yongguang Wang , He Liu
IPC分类号： C07F9/6561 , A61K31/683
CPC分类号： C07F9/65616
摘要： The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein R1 is H or methyl; each R2 is independently —R3 or —OR3, each R3 is independently C1-C8 alkyl, C3-C8 cycloalkyl. The present invention further relates to a process for preparing the compounds of Formula I, a pharmaceutical composition comprising the compound, and the medical uses of the compound. The acyclic nucleoside phosphonate derivative of the present invention has activity against virus such as hepatitis B virus and good in vivo behavioral traits.
摘要翻译：本发明涉及无环核苷膦酸衍生物及其医疗用途。具体地说，本发明涉及对乙型肝炎病毒等病毒具有强效力和低细胞毒性的式I的无环核苷膦酸酯衍生物或其药学上可接受的盐，异构体，水合物或溶剂化物，其中R1是H或甲基 ; 每个R 2独立地是-R 3或-OR 3，每个R 3独立地是C 1 -C 8烷基，C 3 -C 8环烷基。本发明还涉及制备式I化合物的方法，包含该化合物的药物组合物和该化合物的医学用途。本发明的无环核苷膦酸酯衍生物具有抗乙型病毒等病毒的活性和体内行为特性良好的活性。

4. 发明申请

US20120322764A1 Acyclic Nucleoside Phosphonate Derivatives and Medical Uses Thereof 有权
标题翻译：无环核苷磷酸衍生物及其用途
公开(公告)号：US20120322764A1
公开(公告)日：2012-12-20
申请号：US13514749
申请日：2010-06-21
申请人： Bohua Zhong , Xinhua He , Yongguang Wang , He Liu
发明人： Bohua Zhong , Xinhua He , Yongguang Wang , He Liu
IPC分类号： C07F9/6561 , A61P31/12 , A61P31/20 , A61K31/683
CPC分类号： C07F9/65616
摘要： The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein R1 is H or methyl; each R2 is independently —R3 or —OR3, each R3 is independently C1-C8 alkyl, C3-C8 cycloalkyl. The present invention further relates to a process for preparing the compounds of Formula I, a pharmaceutical composition comprising the compound, and the medical uses of the compound. The acyclic nucleoside phosphonate derivative of the present invention has activity against virus such as hepatitis B virus and good in vivo behavioral traits.
摘要翻译：本发明涉及无环核苷膦酸衍生物及其医疗用途。具体地说，本发明涉及对乙型肝炎病毒等病毒具有强效力和低细胞毒性的式I的无环核苷膦酸酯衍生物或其药学上可接受的盐，异构体，水合物或溶剂化物，其中R1是H或甲基 ; 每个R 2独立地是-R 3或-OR 3，每个R 3独立地是C 1 -C 8烷基，C 3 -C 8环烷基。本发明还涉及制备式I化合物的方法，包含该化合物的药物组合物和该化合物的医学用途。本发明的无环核苷膦酸酯衍生物具有抗乙型病毒等病毒的活性和体内行为特性良好的活性。

5. 发明申请

US20120041167A1 POLY(GLUTAMIC ACID)-DRUG CONJUGATE WITH AN AMINO ACID AS A LINKER 审中-公开
标题翻译：多糖（GLUTAMIC ACID）-DRUG与氨基酸连接的连接子
公开(公告)号：US20120041167A1
公开(公告)日：2012-02-16
申请号：US12521767
申请日：2007-11-07
申请人： Bohua Zhong , Jianxin Zhang , Lanfu Chen
发明人： Bohua Zhong , Jianxin Zhang , Lanfu Chen
IPC分类号： C08H1/00
CPC分类号： A61K31/706 , A61K31/337 , A61K31/365 , A61K47/645
摘要： A poly(glutamic acid)-drug conjugate with an amino acid as a linker, and nontoxic pharmaceutically acceptable salt thereof, are provided in the present invention. The drug is gemcitabine, paclitaxel or docetaxel. The α-carboxyl group in the amino acid is linked to 5′-hydroxy in gemcitabine molecule or linked to 2′-hydroxy in paclitaxel (docetaxel) molecule via an ester linkage. The α-amino group in the amino acid is linked to the carboxyl group in the poly-(L-glutamic acid) molecule via an amide linkage. The content of gemcitabine in the conjugate is 5-30% in weight, and the content of paclitaxel or docetaxel is 10-40% in weight.
摘要翻译：在本发明中提供了具有氨基酸作为连接体的聚（谷氨酸） - 药物偶联物及其无毒的药学上可接受的盐。该药物是吉西他滨，紫杉醇或多西紫杉醇。氨基酸中的α-羧基与吉西他滨分子中的5'-羟基连接，或通过酯键与紫杉醇（多西紫杉醇）分子中的2'-羟基连接。氨基酸中的α-氨基通过酰胺键与聚（L-谷氨酸）分子中的羧基连接。缀合物中吉西他滨的含量为5-30％，紫杉醇或多西紫杉醇的含量为10-40％。

6. 发明授权

US07119100B2 Oripavine derivatives and their uses as pharmaceuticals 有权
标题翻译：奥哌拉滨衍生物及其作为药物的用途
公开(公告)号：US07119100B2
公开(公告)日：2006-10-10
申请号：US10489656
申请日：2002-09-13
申请人： Bohua Zhong , Zehui Gong , Yaping Wang , Yongshao Liu
发明人： Bohua Zhong , Zehui Gong , Yaping Wang , Yongshao Liu
IPC分类号： A61K31/44
CPC分类号： C07D489/12
摘要： The present invention relates to oripavine derivatives of formula (I), wherein R1 is hydrogen or methyl, R2 is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R3 is thiophenyl ethyl or cycloalkyl methyl where the cycloalkyl has 3 to 6 carbon atoms, or non-toxic pharmaceutically acceptable salts thereof. These compounds can be used for the preparation of analgesics or abstinence agents of opium habit-forming drugs.
摘要翻译：本发明涉及式（I）的oripavine衍生物，其中R 1是氢或甲基，R 2是甲基，环丙基甲基，环丁基甲基或烯丙基，其中环烷基具有3至6个碳原子的噻吩基乙基或环烷基甲基，或其无毒的药学上可接受的盐。这些化合物可用于制备鸦片习性形成药物的止痛剂或禁欲剂。

7. 发明申请

US20110306633A1 SELECTIVE M4 RECEPTOR ANTAGONIST AND ITS MEDICAL USE 审中-公开
标题翻译：选择性M4受体拮抗剂及其医疗用途
公开(公告)号：US20110306633A1
公开(公告)日：2011-12-15
申请号：US12521859
申请日：2007-11-07
申请人： Bohua Zhong , Jianquan Zheng , Liyun Wang , He Liu , Lanfu Chen , Keliang Liu
发明人： Bohua Zhong , Jianquan Zheng , Liyun Wang , He Liu , Lanfu Chen , Keliang Liu
IPC分类号： A61K31/439 , A61P25/16 , C07D221/22
CPC分类号： C07D221/22
摘要： The present invention provides a selective M4 receptor antagonist, levorotatory demethylated phencynonate or its nontoxic pharmaceutically acceptable salt, a pharmaceutical composition comprising this compound, and a use thereof in the manufacture of a medicament for the treatment of motion dysfunction, such as, tremor, rigor and the like caused by Parkinson's disease (PD). The structure, of the compound is shown in Formula IIa:
摘要翻译：本发明提供选择性M4受体拮抗剂，左旋去甲基化的苯甲酸盐或其无毒的药学上可接受的盐，包含该化合物的药物组合物及其在制备用于治疗运动功能障碍的药物中的用途，例如颤抖，严重性和类似因素引起的帕金森病（PD）。该化合物的结构如式IIa所示：

8. 发明申请

US20050070564A1 Oripavine derivatives and their uses as medicines 有权
标题翻译：奥曲连衍生物及其作为药物的用途
公开(公告)号：US20050070564A1
公开(公告)日：2005-03-31
申请号：US10489656
申请日：2002-09-13
申请人： Bohua Zhong , Zehui Gong , Yaping Wang , Yongshao Liu
发明人： Bohua Zhong , Zehui Gong , Yaping Wang , Yongshao Liu
IPC分类号： B42F1/00 , C07D489/12 , A61K31/485
CPC分类号： C07D489/12
摘要： The present invention relates to oripavine derivatives of formula (I), wherein R1 is hydrogen or methyl, R2 is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R3 is thiophenyl ethyl or cycloalkyl methyl where the cycloalkyl has 3 to 6 carbon atoms, or nontoxic pharmaceutically acceptable salts thereof. These compounds can be used for the preparation of analgesics or abstinence agents of opium habit-forming drugs.
摘要翻译：本发明涉及式（I）的oripavine衍生物，其中R 1是氢或甲基，R 2是甲基，环丙基甲基，环丁基甲基或烯丙基，R 3是噻吩基乙基或环烷基甲基，其中环烷基具有3至6个碳原子，或其无毒的药学上可接受的盐。这些化合物可用于制备鸦片习性形成药物的止痛剂或禁欲剂。

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