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1. 发明授权

US08722698B2 Berbamine derivatives 有权
标题翻译：伯胺衍生物
公开(公告)号：US08722698B2
公开(公告)日：2014-05-13
申请号：US12783535
申请日：2010-05-19
申请人： David Horne , Jun Xie , Angela L. Perkins Harki , Richard Jove , Sangkil Nam , Wendong Huang , Rongzhen Xu
发明人： David Horne , Jun Xie , Angela L. Perkins Harki , Richard Jove , Sangkil Nam , Wendong Huang , Rongzhen Xu
IPC分类号： C07D491/18 , A61K31/4745
CPC分类号： C07D491/147 , A61K31/4745
摘要： The invention provides novel berbamine derivatives, and compositions or pharmaceutical compositions thereof. These berbamine derivatives have shown higher potency in killing cancer/tumor cells comparing to berbamine, and can be used in cancer/tumor treatments.
摘要翻译：本发明提供新颖的柏柏胺衍生物及其组合物或药物组合物。与berbamine相比，这些berbamine衍生物在杀死癌症/肿瘤细胞方面表现出较高的效力，可用于癌症/肿瘤治疗。

2. 发明授权

US09428519B2 Acylated derivative of homoharringtonine, preparation method therefor, and application thereof 有权
标题翻译：高粱醇酮的酰化衍生物及其制备方法及其应用
公开(公告)号：US09428519B2
公开(公告)日：2016-08-30
申请号：US14239372
申请日：2012-08-20
申请人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
发明人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
IPC分类号： A61K31/55 , C07D491/147 , C07D491/20
CPC分类号： C07D491/147 , C07D491/20
摘要： The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and relates to novel homoharringtonine acylated derivatives of formula (I) and formula (II) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
摘要翻译：本发明属于天然药物和药物化学领域，涉及式（I）和式（II）的新型高粱醇丁酰化衍生物及其药学上可接受的盐，涉及制备这些化合物的方法，含有这些化合物及其在制备抗肿瘤药物中的应用。

3. 发明申请

US20140206669A1 AMINATED DERIVATIVE OF HOMOHARRINGTONINE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF 有权
标题翻译：海马林的胺化衍生物，其制备方法及其应用
公开(公告)号：US20140206669A1
公开(公告)日：2014-07-24
申请号：US14239464
申请日：2012-08-20
申请人： Frank Rong , Rongzhen Xu , Fuwen Xie , Hongxi Lai
发明人： Frank Rong , Rongzhen Xu , Fuwen Xie , Hongxi Lai
IPC分类号： C07D493/16
CPC分类号： C07D493/16 , C07D491/20
摘要： The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel aminated homoharringtonine derivatives of formula (I) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
摘要翻译：本发明属于天然药物和药物化学领域，具体涉及式（I）的新型胺化的同型异亮氨酸衍生物及其药学上可接受的盐，用于制备这些化合物的方法，含有这些化合物的组合物及其用途在制备抗肿瘤药物。

4. 发明申请

US20130131153A1 CULLIN 5 AS A REGULATOR OF HSP90 CLIENTS: A NEW TARGET FOR DRUG DEVELOPMENT 审中-公开
标题翻译： CULLIN 5作为HSP90客户的监管者：药物开发的新目标
公开(公告)号：US20130131153A1
公开(公告)日：2013-05-23
申请号：US13510093
申请日：2010-11-16
申请人： Xiao-Fang Yu , Elana S. Ehrlich , Rongzhen Xu
发明人： Xiao-Fang Yu , Elana S. Ehrlich , Rongzhen Xu
IPC分类号： G01N33/573 , C12Q1/68
CPC分类号： G01N33/573 , C12Q1/68 , G01N33/5011 , G01N2333/9015
摘要： Cullin5 (Cul5) E3 ubiquitin ligase is shown to be linked with the heat shock protein 90 (Hsp90) chaperone complex. Hsp90 participates in the folding of its client proteins into their functional conformation. Many Hsp90 clients have been reported to be aberrantly expressed in a number of cancers. Cul5 is shown to interact with members of the Hsp90 chaperone complex as well as the Hsp90 client, ErbB2, Cul5 is recruited to the site of ErbB2 at the plasma membrane and subsequent induction of polyubiquitination and proteasomal degradation. Cul5 is also involved in the regulation of another Hsp90 client, Hif-1α Cul5 degradation of ErbB2 occurs independently of ElonginB-ElonginC function. The involvement of Cul5 in Hsp90 client regulation has implications in the effectiveness of Hsp90 targeted chemotherapy, which is currently undergoing clinical trials. The link between Cul5 and Hsp90 client regulation may represent an avenue for cancer drug development.
摘要翻译： Cullin5（Cul5）E3泛素连接酶显示与热休克蛋白90（Hsp90）伴侣复合物连接。 Hsp90参与将其客户蛋白质折叠成其功能构象。据报道，许多Hsp90客户在许多癌症中异常表达。 Cul5显示与Hsp90伴侣复合物以及Hsp90客户端的成员相互作用，ErbB2，Cul5被引入到质膜上的ErbB2位点，随后诱导多泛素化和蛋白酶体降解。 Cul5也参与另一个Hsp90客户端的调控，Hif-1al Cul5 ErbB2的降解独立于ElonginB-ElonginC功能发生。 Cul5参与Hsp90客户监管对Hsp90靶向化疗的有效性有影响，目前正在进行临床试验。 Cul5和Hsp90客户监管之间的联系可能代表了癌症药物开发的途径。

5. 发明申请

US20140343047A1 TETRANDRINE DERIVATIVES WITH SUBSTITUTED 5-CARBON, PREPARATION METHOD AND USE THEREOF 有权
标题翻译：具有取代的5碳的四氢呋喃衍生物，其制备方法和用途
公开(公告)号：US20140343047A1
公开(公告)日：2014-11-20
申请号：US14239759
申请日：2012-08-20
申请人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
发明人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
IPC分类号： C07D491/22
CPC分类号： C07D491/22 , C07D491/147 , C07D491/18
摘要： The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 5-substituted tetrandrine derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.
摘要翻译：本发明属于天然药物和药物化学领域，具体涉及式（I）的新型5-取代四甲基环戊二烯衍生物及其药学上可接受的加合物，其络合物和盐，用于制备这些化合物，药物含有这些化合物的组合物及其在制备抗肿瘤药物中的用途。

6. 发明授权

US09676789B2 Aminated derivative of homoharringtonine, preparation method therefor, and application thereof 有权
公开(公告)号：US09676789B2
公开(公告)日：2017-06-13
申请号：US14239464
申请日：2012-08-20
申请人： Frank Rong , Rongzhen Xu , Fuwen Xie , Hongxi Lai
发明人： Frank Rong , Rongzhen Xu , Fuwen Xie , Hongxi Lai
IPC分类号： C07D493/16 , C07D491/20
CPC分类号： C07D493/16 , C07D491/20
摘要： The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel aminated homoharringtonine derivatives of formula (I) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.

7. 发明授权

US09133207B2 Tetrandrine derivatives with substituted 5-carbon, preparation method and use thereof 有权
标题翻译：具有取代的5碳的替康德林衍生物，其制备方法和用途
公开(公告)号：US09133207B2
公开(公告)日：2015-09-15
申请号：US14239759
申请日：2012-08-20
申请人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
发明人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
IPC分类号： C07D491/18 , C07D491/22 , C07D491/147
CPC分类号： C07D491/22 , C07D491/147 , C07D491/18
摘要： The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 5-substituted tetrandrine derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.
摘要翻译：本发明属于天然药物和药物化学领域，具体涉及式（I）的新型5-取代四甲基环戊二烯衍生物及其药学上可接受的加合物，其络合物和盐，用于制备这些化合物，药物含有这些化合物的组合物及其在制备抗肿瘤药物中的用途。

8. 发明申请

US20140303147A1 ACYLATED DERIVATIVE OF HOMOHARRINGTONINE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF 有权
标题翻译： HOMOHARRINGTONINE的衍生物衍生物及其制备方法及其应用
公开(公告)号：US20140303147A1
公开(公告)日：2014-10-09
申请号：US14239372
申请日：2012-08-20
申请人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
发明人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
IPC分类号： C07D491/147
CPC分类号： C07D491/147 , C07D491/20
摘要： The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and relates to novel homoharringtonine acylated derivatives of formula (I) and formula (II) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
摘要翻译：本发明属于天然药物和药物化学领域，涉及式（I）和式（II）的新型高粱醇丁酰化衍生物及其药学上可接受的盐，涉及制备这些化合物的方法，含有这些化合物及其在制备抗肿瘤药物中的应用。

9. 发明申请

US20130178470A1 HETEROCYCLIC AMINOBERBAMINE DERIVATIVES, THE PREPARATION PROCESS AND USE THEREOF 有权
标题翻译：杂环氨基胺衍生物，制备方法及其用途
公开(公告)号：US20130178470A1
公开(公告)日：2013-07-11
申请号：US13821667
申请日：2011-09-09
申请人： Rongzhen Xu , Fuwen Xie , Hongxi Lai , Frank Rong
发明人： Rongzhen Xu , Fuwen Xie , Hongxi Lai , Frank Rong
IPC分类号： C07D491/056
CPC分类号： C07D491/056 , A61K31/4738 , C07D491/18
摘要： The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.
摘要翻译：本发明涉及式I的新颖的伯巴胺衍生物或其药学上可接受的盐，其制备方法，包含所述化合物的药物组合物及其在制备抗肿瘤药物中的用途。

10. 发明申请

US20130158068A1 DICARBOXIMIDE DERIVATIVES OF BERBAMINE, THE PREPARATION AND USE THEREOF 有权
标题翻译：伯胺的二恶唑衍生物，其制备和用途
公开(公告)号：US20130158068A1
公开(公告)日：2013-06-20
申请号：US13819111
申请日：2011-08-25
申请人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
发明人： Rongzhen Xu , Frank Rong , Fuwen Xie , Hongxi Lai
IPC分类号： C07D471/04 , C07D401/14
CPC分类号： C07D471/04 , C07D401/14 , C07D491/16
摘要： The present invention relates to a novel dicarboximide derivative of berbamine represented by formula I, including, but not limited to, a phthalimide derivative of berbamine and an aromatic heterocyclic dicarboximide derivative of berbamine, or a pharmaceutically acceptable salt thereof, to a process for preparation of the same, to a pharmaceutical composition comprising said compound and to use thereof in manufacture of an antitumor medicament.
摘要翻译：本发明涉及由式I表示的伯巴胺的新型二羧酰亚胺衍生物，其包括但不限于柏柏胺的邻苯二甲酰亚胺衍生物和伯巴胺的芳族杂环二甲酰亚胺衍生物或其药学上可接受的盐，用于制备相同，涉及包含所述化合物的药物组合物及其在制造抗肿瘤药物中的用途。

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