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1. 发明授权

US08685997B2 Camptothecin derivatives and their use 有权
标题翻译：喜树碱衍生物及其用途
公开(公告)号：US08685997B2
公开(公告)日：2014-04-01
申请号：US12282397
申请日：2007-01-17
申请人： Wei Lu , Jian Ding , Heyong Gao , Liping Lin , Yi Chen
发明人： Wei Lu , Jian Ding , Heyong Gao , Liping Lin , Yi Chen
IPC分类号： A61K31/44 , C07D471/00
CPC分类号： C07D491/22
摘要： New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
摘要翻译：具有以下结构式（I）的新的喜树碱衍生物，它们的用途和含有它们的药物组合物。本发明化合物具有良好的抗肿瘤活性和在水中的良好溶解性，可用于药物的开发。

2. 发明申请

US20090325996A1 CAMPTOTHECIN DERIVATIVES AND THEIR USE 有权
标题翻译： CAMPTOTHECIN衍生物及其用途
公开(公告)号：US20090325996A1
公开(公告)日：2009-12-31
申请号：US12282397
申请日：2007-01-17
申请人： Wei Lu , Jian Ding , Heyong Gao , Liping Lin , Yi Chen
发明人： Wei Lu , Jian Ding , Heyong Gao , Liping Lin , Yi Chen
IPC分类号： A61K31/4375 , C07D491/22 , A61P35/00
CPC分类号： C07D491/22
摘要： New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
摘要翻译：具有以下结构式（I）的新的喜树碱衍生物，它们的用途和含有它们的药物组合物。本发明化合物具有良好的抗肿瘤活性和在水中的良好溶解性，可用于药物的开发。

3. 发明申请

US20080234287A1 SULFUR-CONTAINING NAPHTHALIMIDE DERIVATIVES 审中-公开
标题翻译：含硫磺酰胺衍生物
公开(公告)号：US20080234287A1
公开(公告)日：2008-09-25
申请号：US12116452
申请日：2008-05-07
申请人： Xuhong Qian , Yonggang Li , Yufang Xu , Jian Ding , Liping Lin , Zehong Miao , Hong Zhu , Baoyuan Qu
发明人： Xuhong Qian , Yonggang Li , Yufang Xu , Jian Ding , Liping Lin , Zehong Miao , Hong Zhu , Baoyuan Qu
IPC分类号： A61K31/497 , C07D221/18 , A61K31/4365 , C07D401/14 , A61P35/00
CPC分类号： C07D495/06 , C07D221/14 , C07D405/12 , C07D513/06 , C09B57/08 , C09B69/102 , C09B69/109
摘要： The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5- or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.
摘要翻译：本发明公开了新型含硫萘二甲酰亚胺衍生物及其制备及应用。本发明的萘二甲酰亚胺衍生物的共轭平面通过引入5或6元杂芳环和/或引入S杂原子而增大，从而增加了萘二甲酰亚胺的抗肿瘤活性。本发明化合物对人肺癌，胃癌，肝癌，白细胞增多症等各种肿瘤细胞的增殖具有显着的抑制活性。细胞增殖的抑制是剂量依赖性的。

4. 发明授权

US07541463B2 Sulfur-containing naphthalimide derivatives 失效
标题翻译：含硫萘酰亚胺衍生物
公开(公告)号：US07541463B2
公开(公告)日：2009-06-02
申请号：US11263591
申请日：2005-10-31
申请人： Xuhong Qian , Yonggang Li , Yufang Xu , Jian Ding , Liping Lin , Zehong Miao , Hong Zhu , Baoyuan Qu
发明人： Xuhong Qian , Yonggang Li , Yufang Xu , Jian Ding , Liping Lin , Zehong Miao , Hong Zhu , Baoyuan Qu
IPC分类号： A61K31/4365 , C07D221/18 , C07D471/06
CPC分类号： C07D495/06 , C07D221/14 , C07D405/12 , C07D513/06 , C09B57/08 , C09B69/102 , C09B69/109
摘要： The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5-or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.
摘要翻译：本发明公开了新型含硫萘二甲酰亚胺衍生物及其制备及应用。本发明的萘二甲酰亚胺衍生物的共轭平面通过掺入5-或6-元杂芳环和/或引入S杂原子而增大，从而增加了萘二甲酰亚胺的抗肿瘤活性。本发明化合物对人肺癌，胃癌，肝癌，白细胞增多症等各种肿瘤细胞的增殖具有显着的抑制活性。细胞增殖的抑制是剂量依赖性的。

5. 发明申请

US20060111367A1 Sulfur-containing naphthalimide derivatives 失效
公开(公告)号：US20060111367A1
公开(公告)日：2006-05-25
申请号：US11263591
申请日：2005-10-31
申请人： Xuhong Qian , Yonggang Li , Yufang Xu , Jian Ding , Liping Lin , Zehong Miao , Hong Zhu , Baoyuan Qu
发明人： Xuhong Qian , Yonggang Li , Yufang Xu , Jian Ding , Liping Lin , Zehong Miao , Hong Zhu , Baoyuan Qu
IPC分类号： A61K31/496 , A61K31/4743 , A61K31/473 , C07D498/02 , C07D403/02
CPC分类号： C07D495/06 , C07D221/14 , C07D405/12 , C07D513/06 , C09B57/08 , C09B69/102 , C09B69/109
摘要： The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5-or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.

6. 发明申请

US20140128421A1 CAMPTOTHECIN COMPOUND CONTAINING STABLE 7-MEMBERED LACTONE RING, PREPARATION METHOD AND USE 有权
标题翻译：包含稳定的7会员手环的化合物，制备方法和用途
公开(公告)号：US20140128421A1
公开(公告)日：2014-05-08
申请号：US14112583
申请日：2012-04-13
申请人： Wei Lv , Shanbao Yu , Yu Luo , Yi Chen , Jian Ding
发明人： Wei Lv , Shanbao Yu , Yu Luo , Yi Chen , Jian Ding
IPC分类号： C07D491/22
CPC分类号： C07D491/22
摘要： Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.
摘要翻译：提供了如通式I所示的含有7-元内酯环的喜树碱化合物及其药学上可接受的盐以及其制备方法和用途。在通式Ⅰ中，R 1是H，C 1 -C 3烷基，乙酰基或丙酰基; R2是H，C1〜C6烷基，C3〜C6环烷基，哌啶基; 或被氨基取代的C 1-6烷基; R3是H，C1〜C3烷基或被氨基取代的C1〜C6烷基; R4是H，羟基或C1〜C6烷氧基; R5是H或C1〜C6烷氧基; 或R 4和R 5彼此连接形成-OCH 2 O-或-OCH 2 CH 2 O-。该化合物具有良好的抗肿瘤活性，可以通过口服给药，静脉内注射和肌内注射等临床使用。

7. 发明授权

US09115150B2 Camptothecin compound containing stable 7-membered lactone ring, preparation method and use 有权
标题翻译：喜树碱化合物含有稳定的7元内酯环，制备方法和用途
公开(公告)号：US09115150B2
公开(公告)日：2015-08-25
申请号：US14112583
申请日：2012-04-13
申请人： Wei Lv , Shanbao Yu , Yu Luo , Yi Chen , Jian Ding
发明人： Wei Lv , Shanbao Yu , Yu Luo , Yi Chen , Jian Ding
IPC分类号： C07D491/22
CPC分类号： C07D491/22
摘要： Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.
摘要翻译：提供了如通式I所示的含有7-元内酯环的喜树碱化合物及其药学上可接受的盐以及其制备方法和用途。在通式I中，R 1是H，C 1 -C 3烷基，乙酰基或丙酰基; R2是H，C1〜C6烷基，C3〜C6环烷基，哌啶基; 或被氨基取代的C 1-6烷基; R3是H，C1〜C3烷基或被氨基取代的C1〜C6烷基; R4是H，羟基或C1〜C6烷氧基; R5是H或C1〜C6烷氧基; 或R 4和R 5彼此连接形成-OCH 2 O-或-OCH 2 CH 2 O-。该化合物具有良好的抗肿瘤活性，可以通过口服给药，静脉内注射和肌内注射等临床使用。

8. 发明申请

US20130324542A1 [1,2,4]TRIAZOLO[4,3-B][1,2,4]TRIAZINE COMPOUNDS, PREPARATION METHOD AND USE THEREOF 审中-公开
标题翻译： [1,2,4]三唑[4,3-B] [1,2,4]三嗪化合物，其制备方法及其用途
公开(公告)号：US20130324542A1
公开(公告)日：2013-12-05
申请号：US13992048
申请日：2011-12-08
申请人： Wenhu Duan , Meiyu Geng , Fang Chen , Jing Ai , Yi Chen , Zhengsheng Zhan , Yongcong Lv , Ying Wang , Jian Ding
发明人： Wenhu Duan , Meiyu Geng , Fang Chen , Jing Ai , Yi Chen , Zhengsheng Zhan , Yongcong Lv , Ying Wang , Jian Ding
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to a structurally novel [1,2,4]triazolo[4,3-b][1,2,4]triazine compounds represented by formula (I) or formula (II), pharmaceutically acceptable salts thereof, prodrugs thereof, hydrates or solvates thereof, and also relates to a preparation method of the compounds, a pharmaceutical composition including a therapeutically effective amount of the compounds, as well as the use thereof as protein tyrosine kinase inhibitors, particularly as c-Met inhibitors, in the preparation of medicaments for the prevention and/or treatment of diseases associated with c-Met abnormality.
摘要翻译：本发明涉及由式（I）或式（II）表示的结构上新的[1,2,4]三唑并[4,3-b] [1,2,4]三嗪化合物，其药学上可接受的盐，前体药物其还涉及本发明化合物的制备方法，包含治疗有效量的化合物的药物组合物，以及其作为蛋白酪氨酸激酶抑制剂，特别是作为c-Met抑制剂的用途，制备用于预防和/或治疗与c-Met异常有关的疾病的药物。

9. 发明申请

US20140296216A1 PYRIMIDO[4,5-D]PYRIMIDINYL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：吡咯二酮[4,5-D]吡啶化合物，药物组合物及其用途
公开(公告)号：US20140296216A1
公开(公告)日：2014-10-02
申请号：US14125304
申请日：2011-12-21
申请人： Ke Ding , Shaohua Chang , Shilin Xu , Lianwen Zhang , Zhengchao Tu , Jian Ding , Meiyu Geng , Yi Chen
发明人： Ke Ding , Shaohua Chang , Shilin Xu , Lianwen Zhang , Zhengchao Tu , Jian Ding , Meiyu Geng , Yi Chen
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/551
摘要： A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.
摘要翻译：公开了式（I）或（II）的化合物和该化合物在制备用于治疗癌症的药物中的用途。该研究表明，该化合物可抑制多种肿瘤细胞的生长，可用于靶向表皮生长因子受体（EGFR），特别是可以单独或多次EGFR（T790M）突变抑制肿瘤细胞。因此，该化合物可用作EGFR抑制剂治疗癌症，具有较大的应用价值。

10. 外观设计

USD740433S1 Hand-held massaging device 有权
标题翻译：手持按摩器
公开(公告)号：USD740433S1
公开(公告)日：2015-10-06
申请号：US29461275
申请日：2013-07-20
申请人： Megan Zhu , Jian Ding
设计人： Megan Zhu , Jian Ding
CPC分类号： A61H15/0085

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