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1. 发明申请

US20140011856A1 SALT FORM OF TYROSINE KINASE INHIBITOR 有权
标题翻译：酪氨酸激酶抑制剂的盐形式
公开(公告)号：US20140011856A1
公开(公告)日：2014-01-09
申请号：US14023486
申请日：2013-09-11
申请人： JIANGSU SIMCERE PHARMACEUTICAL R&D Co., Ltd
发明人： Feng TANG , Qiu JIN , Wei LI , Tian ZHU , Yang HU , Feng SHAO
IPC分类号： A61K31/4045
CPC分类号： A61K31/4045 , C07D209/42
摘要： Provided are acid addition salts of (Z)—N-[2-(diethylamino)ethyl]-2-methyl-7-(1,2-dihydro-5-fluoro-2-oxo-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indol-3-carboxamide, wherein the salt comprising at least one of a number of salts including L-malate, hydrochloride, phosphate, L-tartrate, benzenesulfonate, sulfate, methanesulfonate, succinate, citrate, fumarate, p-toluenesulfonate, hydrobromate, L-mandelate, lactate, acetate or maleate salt. Also provided is a pharmaceutical composition comprising the salt compounds, and a method of treatment by administering a therapeutically effective amount of the salt compounds as preparation of medicaments.
摘要翻译：提供（Z）-N- [2-（二乙基氨基）乙基] -2-甲基-7-（1,2-二氢-5-氟-2-氧代-3H-吲哚-3-亚基） -4,5,6,7-四氢-1H-吲哚-3-甲酰胺，其中所述盐包含多种盐，包括L-苹果酸盐，盐酸盐，磷酸盐，L-酒石酸盐，苯磺酸盐，硫酸盐，甲磺酸盐，琥珀酸盐，柠檬酸盐，富马酸盐，对甲苯磺酸盐，氢溴酸盐，L-扁桃酸盐，乳酸盐，乙酸盐或马来酸盐。还提供了包含盐化合物的药物组合物，以及通过施用治疗有效量的盐化合物作为药物制剂的治疗方法。

2. 发明授权

US08084621B2 3-Pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives and uses thereof 有权
标题翻译： 3-吡咯并[b]环己基-2-二氢吲哚啉酮衍生物及其用途
公开(公告)号：US08084621B2
公开(公告)日：2011-12-27
申请号：US12517351
申请日：2007-12-03
申请人： Feng Tang , Han Shen , Qiu Jin , Lei Ding , Jie Yang , Xiaojin Yin , Shiyue Lu
发明人： Feng Tang , Han Shen , Qiu Jin , Lei Ding , Jie Yang , Xiaojin Yin , Shiyue Lu
IPC分类号： C07D209/02 , A61K31/40
CPC分类号： C07D209/42 , C07D401/14 , C07D403/14
摘要： 3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.
摘要翻译：式（I）的3-吡咯并[b]亚环己基-2-二氢 - 二氢吲哚酮衍生物或其药学上可接受的盐和用途。用于制备上述化合物的式（II）的中间体。生物测定显示，上述化合物及其药学上可接受的盐可调节蛋白激酶（PK）的活性，抑制酪氨酸激酶（PTK）的活性并抑制多种肿瘤细胞。

3. 发明申请

US20120231011A1 ANTI-VEGF MONOCLONAL ANTIBODY AND PHARMACEUTICAL COMPOSITION COMPRISING SAID ANTIBODY 有权
标题翻译：抗VEGF单克隆抗体和包含抗体的药物组合物
公开(公告)号：US20120231011A1
公开(公告)日：2012-09-13
申请号：US13393185
申请日：2010-08-27
申请人： Pierre Li , Yaohuang ke , Yongke Zhang , Weimin Zhu , Guoliang Yu , Fanxin Ma , Xin Fan
发明人： Pierre Li , Yaohuang ke , Yongke Zhang , Weimin Zhu , Guoliang Yu , Fanxin Ma , Xin Fan
IPC分类号： C07K16/22 , A61K39/395 , A61P3/10 , A61P25/28 , A61P3/04 , C12N5/07 , A61P25/00
CPC分类号： C07K16/22 , A61K2039/505 , C07K2317/24 , C07K2317/565 , C07K2317/76 , C07K2317/92
摘要： The present invention provides an anti-VEGF monoclonal antibody, which has the variable region of heavy chain comprising the amino acid sequences of SEQ ID NO. 1, SEQ ID NO. 2 and SEQ ID NO. 3, and/or the variable region of light chain comprising the amino acid sequences of SEQ ID NO. 4, SEQ ID NO. 5 and SEQ ID NO. 6. The antibody can be produced by the cell line with the preservation number of CGMCC NO. 3233. The invention also provides the use of said antibody for the manufacture of medicaments for the treatment of a disease that is relevant to VEGF, wherein further provided are pharmaceutical composition, agents, kits and chips comprising said antibody, as well as the cell line with the preservation number of CGMCC NO. 3233.
摘要翻译：本发明提供了一种抗VEGF单克隆抗体，其具有包含SEQ ID NO：1的氨基酸序列的重链可变区。 1，SEQ ID NO： 2和SEQ ID NO。 3，和/或包含SEQ ID NO：1的氨基酸序列的轻链的可变区。 4，SEQ ID NO： 5和SEQ ID NO：抗体可以通过具有CGMCC NO保存数的细胞系产生。本发明还提供了所述抗体用于制备用于治疗与VEGF相关的疾病的药物的用途，其中还提供了包含所述抗体的药物组合物，试剂，试剂盒和切片以及细胞系保存号码为CGMCC NO。 3233。

4. 发明申请

US20100210822A1 MODIFIED RECOMBINANT HUMAN ENDOSTATIN AND USES THEREOF 有权
标题翻译：改性重组人内皮素及其用途
公开(公告)号：US20100210822A1
公开(公告)日：2010-08-19
申请号：US12676766
申请日：2008-09-04
申请人： Wenbing Yao , Hong Tian , Xiangyang Xu , Hairui Li , Yue Dong , Xiangdong Gao
发明人： Wenbing Yao , Hong Tian , Xiangyang Xu , Hairui Li , Yue Dong , Xiangdong Gao
IPC分类号： C07K14/78
CPC分类号： C07K14/78 , A61K38/00 , A61K47/48215 , A61K47/60
摘要： Provided is a kind of modified recombinant human endostatin that has the structure of CH3O—(CH2CH2O)m—CH2CH2CH2—NαH-Endostar, wherein the average molecular weight of CH3O—(CH2CH2O)m—CH2CH2CH2— is 20-40 kD. The modified recombinant human endostatin enhances the stability in vivo, improves blood drug concentration, prolongs half-life, markedly increases the activity of inhibiting the endothelial cells proliferation, thus reduces drug dosage and decreases administration frequency. Its application for preparing anti-tumor pharmaceutical compositions is also provided.
摘要翻译：提供了一种具有CH3O-（CH2CH2O）m-CH2CH2CH2-NαH-Endostar结构的一种修饰的重组人内皮抑素，其中CH 3 O-（CH 2 CH 2 O）m -CH 2 CH 2 CH 2的平均分子量为20-40kD。修饰的重组人内皮抑素增强体内的稳定性，改善血药浓度，延长半衰期，显着增加抑制内皮细胞增殖的活性，从而降低药物用量，降低给药频率。还提供其制备抗肿瘤药物组合物的应用。

5. 发明授权

US08658684B2 Pharmaceutical composition and its use in the preparation of a medicament for the treatment of cerebrovascular diseases 有权
标题翻译：药物组合物及其在制备用于治疗脑血管疾病的药物中的用途
公开(公告)号：US08658684B2
公开(公告)日：2014-02-25
申请号：US12920579
申请日：2009-03-03
申请人： Xiaojin Yin , Shibao Yang , Xiaoqiang Li , Zheng Jiang , Jian He , Anyuan Zhang , Xin Huang
发明人： Xiaojin Yin , Shibao Yang , Xiaoqiang Li , Zheng Jiang , Jian He , Anyuan Zhang , Xin Huang
IPC分类号： A61K31/415
CPC分类号： A61K31/045 , A61K31/4152 , C07D231/22
摘要： A pharmaceutical composition comprises 3-methyl-1-phenyl-2-pyrazolin-5-one and borneol, and can be used to prepare the medicine for treating cerebrovascular diseases.
摘要翻译：药物组合物包含3-甲基-1-苯基-2-吡唑啉-5-酮和冰片，可用于制备治疗脑血管疾病的药物。

6. 发明申请

US20110003873A1 PHARMACEUTICAL COMPOSITION AND ITS USE IN THE PREPARATION OF A MEDICAMENT FOR THE TREATMENT OF CEREBROVASCULAR DISEASES 有权
标题翻译：药物组合物及其在制备用于治疗脑血管病的药物中的应用
公开(公告)号：US20110003873A1
公开(公告)日：2011-01-06
申请号：US12920579
申请日：2009-03-03
申请人： Xiaojin Yin , Shibao Yang , Xiaoqiang Li , Zheng Jiang , Jian He , Anyuan Zhang , Xin Huang
发明人： Xiaojin Yin , Shibao Yang , Xiaoqiang Li , Zheng Jiang , Jian He , Anyuan Zhang , Xin Huang
IPC分类号： A61K31/4152 , A61P9/10
CPC分类号： A61K31/045 , A61K31/4152 , C07D231/22
摘要： A pharmaceutical composition comprises 3-methyl-1-phenyl-2-pyrazolin-5-one and borneol, and can be used to prepare the medicine for treating cerebrovascular diseases.
摘要翻译：药物组合物包含3-甲基-1-苯基-2-吡唑啉-5-酮和冰片，可用于制备治疗脑血管疾病的药物。

7. 发明授权

US08986692B2 Anti-VEGF monoclonal antibody and pharmaceutical composition comprising said antibody 有权
标题翻译：抗VEGF单克隆抗体和包含所述抗体的药物组合物
公开(公告)号：US08986692B2
公开(公告)日：2015-03-24
申请号：US13393185
申请日：2010-08-27
申请人： Pierre Li , Yaohuang Ke , Yongke Zhang , Weimin Zhu , Guoliang Yu , Fanxin Ma , Xin Fan
发明人： Pierre Li , Yaohuang Ke , Yongke Zhang , Weimin Zhu , Guoliang Yu , Fanxin Ma , Xin Fan
IPC分类号： A61K39/395 , C07K16/22 , A61K39/00
CPC分类号： C07K16/22 , A61K2039/505 , C07K2317/24 , C07K2317/565 , C07K2317/76 , C07K2317/92
摘要： The present invention provides an anti-VEGF monoclonal antibody, which has the variable region of heavy chain comprising the amino acid sequences of SEQ ID NO:1, SEQ ID NO:2 and SEQ ID NO:3, and/or the variable region of light chain comprising the amino acid sequences of SEQ ID NO:4, SEQ ID NO:5 and SEQ ID NO:6. The antibody can be produced by the cell line with the preservation number of CGMCC NO. 3233. The invention also provides the use of said antibody for the manufacture of medicaments for the treatment of a disease that is relevant to VEGF, wherein further provided are pharmaceutical composition, agents, kits and chips comprising said antibody, as well as the cell line with the preservation number of CGMCC NO. 3233.
摘要翻译：本发明提供了抗VEGF单克隆抗体，其具有包含SEQ ID NO：1，SEQ ID NO：2和SEQ ID NO：3的氨基酸序列的重链可变区和/或轻链，其包含SEQ ID NO：4，SEQ ID NO：5和SEQ ID NO：6的氨基酸序列。该抗体可以通过具有CGMCC NO保存数的细胞系产生。本发明还提供了所述抗体用于制备用于治疗与VEGF相关的疾病的药物的用途，其中还提供了包含所述抗体的药物组合物，试剂，试剂盒和切片以及细胞系保存号码为CGMCC NO。 3233。

8. 发明授权

US08802824B2 Modified recombinant human endostatin and uses thereof 有权
标题翻译：改良的重组人内皮抑素及其用途
公开(公告)号：US08802824B2
公开(公告)日：2014-08-12
申请号：US12676766
申请日：2008-09-04
申请人： Wenbing Yao , Hong Tian , Xiangyang Xu , Hairui Li , Yue Dong , Xiangdong Gao
发明人： Wenbing Yao , Hong Tian , Xiangyang Xu , Hairui Li , Yue Dong , Xiangdong Gao
IPC分类号： A61K38/17 , C07K14/78 , A61K47/48 , A61K38/00
CPC分类号： C07K14/78 , A61K38/00 , A61K47/48215 , A61K47/60
摘要： Provided is a kind of modified recombinant human endostatin that has the structure of CH3O—(CH2CH2O)m—CH2CH2CH2—NαH-Endostar, wherein the average molecular weight of CH3O—(CH2CH2O)m—CH2CH2CH2— is 20-40 kD. The modified recombinant human endostatin enhances the stability in vivo, improves blood drug concentration, prolongs half-life, markedly increases the activity of inhibiting the endothelial cells proliferation, thus reduces drug dosage and decreases administration frequency. Its application for preparing anti-tumor pharmaceutical compositions is also provided.
摘要翻译：提供了一种具有CH3O-（CH2CH2O）m-CH2CH2CH2-NαH-Endostar结构的一种修饰的重组人内皮抑素，其中CH 3 O-（CH 2 CH 2 O）m -CH 2 CH 2 CH 2的平均分子量为20-40kD。修饰的重组人内皮抑素增强体内的稳定性，改善血药浓度，延长半衰期，显着增加抑制内皮细胞增殖的活性，从而降低药物用量，降低给药频率。还提供其制备抗肿瘤药物组合物的应用。

9. 发明授权

US09018242B2 Salt form of tyrosine kinase inhibitor 有权
标题翻译：盐形式的酪氨酸激酶抑制剂
公开(公告)号：US09018242B2
公开(公告)日：2015-04-28
申请号：US14023486
申请日：2013-09-11
申请人： Jiangsu Simcere Pharmaceutical R&D Co., Ltd
发明人： Feng Tang , Qiu Jin , Wei Li , Tian Zhu , Yang Hu , Feng Shao
IPC分类号： A61K31/4045 , C07D209/42
CPC分类号： A61K31/4045 , C07D209/42
摘要： Provided are acid addition salts of (Z)—N-[2-(diethylamino)ethyl]-2-methyl-7-(1,2 -dihydro-5-fluoro-2-oxo-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indol-3-carboxamide, wherein the salt comprising at least one of a number of salts including L-malate, hydrochloride, phosphate, L-tartrate, benzenesulfonate, sulfate, methanesulfonate, succinate, citrate, fumarate, p-toluenesulfonate, hydrobromate, L-mandelate, lactate, acetate or maleate salt. Also provided is a pharmaceutical composition comprising the salt compounds, and a method of treatment by administering a therapeutically effective amount of the salt compounds as preparation of medicaments.
摘要翻译：提供（Z）-N- [2-（二乙基氨基）乙基] -2-甲基-7-（1,2-二氢-5-氟-2-氧代-3H-吲哚-3-亚基） -4,5,6,7-四氢-1H-吲哚-3-甲酰胺，其中所述盐包括多种盐，包括L-苹果酸盐，盐酸盐，磷酸盐，L-酒石酸盐，苯磺酸盐，硫酸盐，甲磺酸盐，琥珀酸盐，柠檬酸盐，富马酸盐，对甲苯磺酸盐，氢溴酸盐，L-扁桃酸盐，乳酸盐，乙酸盐或马来酸盐。还提供了包含盐化合物的药物组合物，以及通过施用治疗有效量的盐化合物作为药物制剂的治疗方法。

10. 发明申请

US20100160318A1 3-Pyrrolo[b]Cyclohexylene-2-Dihydroindolinone Derivatives and Uses Thereof 有权
标题翻译： 3-吡咯并[b]环己基-2-二氢吲哚啉酮衍生物及其用途
公开(公告)号：US20100160318A1
公开(公告)日：2010-06-24
申请号：US12517351
申请日：2007-12-03
申请人： Feng Tang , Han Shen , Qiu Jin , Lei Ding , Jie Yang , Xiaojin Yin , Shiyue Lu
发明人： Feng Tang , Han Shen , Qiu Jin , Lei Ding , Jie Yang , Xiaojin Yin , Shiyue Lu
IPC分类号： A61K31/404 , C07D209/42 , C07D413/12 , C07D401/12 , C07D403/12 , C07D405/08 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4439 , C07D401/14 , C07D403/14 , A61K31/4545 , A61P35/00 , A61P17/00 , A61P9/00 , A61P9/10 , A61P3/10 , A61P19/02 , A61P37/00 , A61P29/00 , A61P27/02
CPC分类号： C07D209/42 , C07D401/14 , C07D403/14
摘要： 3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.
摘要翻译：式（I）的3-吡咯并[b]亚环己基-2-二氢 - 二氢吲哚酮衍生物或其药学上可接受的盐和用途。用于制备上述化合物的式（II）的中间体。生物测定显示，上述化合物及其药学上可接受的盐可调节蛋白激酶（PK）的活性，抑制酪氨酸激酶（PTK）的活性并抑制多种肿瘤细胞。

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