公开(公告)号：US20080182836A1

公开(公告)日：2008-07-31

申请号：US11700087

申请日：2007-01-31

Applicant: Mao Chen ,  Shaoxuan Zhu ,  Xuebin Liu ,  Chun Luo ,  Shuwen Xu ,  Lizhen Zheng ,  Fang Ye ,  Chenglong Yi ,  Xiaona Zhang

Inventor： Mao Chen ,  Shaoxuan Zhu ,  Xuebin Liu ,  Chun Luo ,  Shuwen Xu ,  Lizhen Zheng ,  Fang Ye ,  Chenglong Yi ,  Xiaona Zhang

IPC: A61K31/546 ,  C07D501/60

CPC classification number: C07D501/36

Abstract: Disclosed herein are a cephalosporin compound comprising a C3 thio-methyl moiety substituted with an N-containing heterocyclic group, and a C7 thiourea acetamido group, the preparation and uses thereof. A method of preparing the cephalosporin compound as disclosed herein comprises reacting a starting cephalosporin comprising a C7 amino group and a C3 thio-methyl moiety substituted with an N-containing heterocyclic group with bromoacetyl bromide and then with a N,N′-bissubstituted thiourea. Methods of treating an infectious disease are also disclosed, comprising administering to a patient in need thereof the pharmaceutical composition disclosed herein.

Abstract translation: 本文公开了包含被含氮杂环基取代的C 3硫代甲基部分和C 7硫脲乙酰氨基的头孢菌素化合物，其制备和用途。 制备本文公开的头孢菌素化合物的方法包括将包含C7氨基的起始头孢菌素和被含氮杂环基取代的C3硫代甲基部分与溴乙酰溴反应，然后与N，N'-双取代的硫脲反应。 还公开了治疗感染性疾病的方法，包括向有需要的患者施用本文公开的药物组合物。

公开(公告)号：US20110118462A1

公开(公告)日：2011-05-19

申请号：US12621237

申请日：2009-11-18

Applicant: Mao CHEN ,  Shaoxuan Zhu ,  Xuebin Liu ,  Lizhen Zheng ,  Liwei Lin ,  Shuwen Xu ,  Yuping Wang ,  Wei Yang ,  Yunfeng Li ,  Fang Ye ,  Xiaona Zhang

Inventor： Mao CHEN ,  Shaoxuan Zhu ,  Xuebin Liu ,  Lizhen Zheng ,  Liwei Lin ,  Shuwen Xu ,  Yuping Wang ,  Wei Yang ,  Yunfeng Li ,  Fang Ye ,  Xiaona Zhang

IPC: C07D501/16

CPC classification number: C07D501/36

Abstract: The invention relates to N-heterocyclic substituent-containing antibiotics, their preparation, and their use. Disclosed are sodium and potassium salts of 7-(α-((N,N′-diisopropylamidino)thio)acetylamino)-3-(((1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio)methyl) cephalosporanic acid as presented by the general structure (I), their preparation, and their use. The antibiotics of the invention can be used to treat diseases caused by Gram-positive or Gram-negative bacteria such as septicaemia, gastrointestinal tract infection, and urinary tract infection. They have increased half-life in blood and lowered toxicity. They can reduce the frequency of drug use and lower medical treatment costs. They have improved stability and can be stored at ambient temperatures. The method of the invention is simple, and it produces high purity products which can meet the requirements of clinical use.

Abstract translation: 本发明涉及含有N-杂环取代基的抗生素，其制备及其应用。 公开了7-（α - （（N，N'-二异丙基脒基）硫基）乙酰氨基）-3 - （（（1,2,5,6-四氢-2-甲基-5,6-二氧代 -1,2,4-三嗪-3-基）硫基）甲基）头孢烷酸，其总体结构（I），它们的制备及其用途。 本发明的抗生素可用于治疗由革兰氏阳性或革兰氏阴性菌引起的疾病，例如败血症，胃肠道感染和尿路感染。 它们增加了血液中的半衰期，降低了毒性。 它们可以减少使用药物的频率，降低医疗费用。 它们具有改善的稳定性并且可以在环境温度下储存。 本发明的方法简单，产生可满足临床用途要求的高纯度产品。

公开(公告)号：US20110028444A1

公开(公告)日：2011-02-03

申请号：US12936088

申请日：2009-04-02

Applicant: Mao Chen ,  Shaoxuan Zhu ,  Lizhen Zheng ,  Xuebin Liu ,  Yuping Wang ,  Shuwen Xu

Inventor： Mao Chen ,  Shaoxuan Zhu ,  Lizhen Zheng ,  Xuebin Liu ,  Yuping Wang ,  Shuwen Xu

IPC: A61K31/397 ,  C07D513/04 ,  A61P31/00

CPC classification number: C07D513/04

Abstract: The invention discloses the pharmaceutically acceptable salts of an optically active quinolone compound useful against infection, specifically the pharmaceutically acceptable salts of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid. The pharmaceutically acceptable salts of the present invention are stable and have improved water solubility. They possess higher biological activity, less toxicity for kidney and no irritation to skin and muscle.

Abstract translation: 本发明公开了用于抗感染的光学活性喹诺酮化合物的药学上可接受的盐，特别是（S）-6-氟-1-甲基-4-氧代-7-（1-哌嗪基）-1H，4H - [1,3]噻唑并[3,2-a]喹啉-3-羧酸。 本发明的药学上可接受的盐是稳定的并且具有改善的水溶性。 它们具有较高的生物活性，对肾脏毒性较小，对皮肤和肌肉无刺激性。

公开(公告)号：US20140128359A1

公开(公告)日：2014-05-08

申请号：US13667266

申请日：2012-11-02

Applicant: Mao Chen ,  Shaoxuan Zhu ,  Xuebin Liu ,  Lizhen Zheng ,  Liwei Lin ,  Shuwen Xu ,  Yuping Wang ,  Wei Yang ,  Yunfeng Li ,  Fang Ye ,  Xiaona Zhang

Inventor： Mao Chen ,  Shaoxuan Zhu ,  Xuebin Liu ,  Lizhen Zheng ,  Liwei Lin ,  Shuwen Xu ,  Yuping Wang ,  Wei Yang ,  Yunfeng Li ,  Fang Ye ,  Xiaona Zhang

IPC: C07D501/36 ,  C07D501/04

CPC classification number: C07D501/36

Abstract: The invention relates to N-heterocyclic substituent-containing antibiotics, their preparation, and their use. Disclosed are sodium and potassium salts of 7-(α-((N,N′-diisopropylamidino)thio)acetylamino)-3-(((1,2,5,6-tetrahydro-2-methyl-5,6-diox o-1,2,4-triazin-3-yl)thio)methyl) cephalosporanic acid as presented by the general structure (I), their preparation, and their use. The antibiotics of the invention can be used to treat diseases caused by Gram-positive or Gram-negative bacteria such as septicaemia, gastrointestinal tract infection, and urinary tract infection. They have increased half-life in blood and lowered toxicity. They can reduce the frequency of drug use and lower medical treatment costs. They have improved stability and can be stored at ambient temperatures. The method of the invention is simple, and it produces high purity products which can meet the requirements of clinical use.

Abstract translation: 本发明涉及含有N-杂环取代基的抗生素，其制备及其应用。 公开了7-（α - （（N，N'-二异丙基脒基）硫基）乙酰氨基）-3 - （（（1,2,5,6-四氢-2-甲基-5,6-二氧杂） o-1,2,4-三嗪-3-基）硫基）甲基）头孢烷酸，其总体结构（I），它们的制备及其用途。 本发明的抗生素可用于治疗由革兰氏阳性或革兰氏阴性菌如败血病，胃肠道感染和尿路感染引起的疾病。 它们增加了血液中的半衰期，降低了毒性。 它们可以减少使用药物的频率，降低医疗费用。 它们具有改善的稳定性并且可以在环境温度下储存。 本发明的方法简单，产生可满足临床用途要求的高纯度产品。

公开(公告)号：US20130183343A1

公开(公告)日：2013-07-18

申请号：US13635075

申请日：2011-03-15

Applicant: Brian J. Czerniecki ,  Shuwen Xu ,  Gary K. Koski ,  Brian McDevitt

Inventor： Brian J. Czerniecki ,  Ursula Koldovsky ,  Shuwen Xu ,  Gary K. Koski

IPC: C12N5/0784 ,  A61K39/02 ,  A61K39/00

CPC classification number: C12N5/0639 ,  A61K39/00 ,  A61K39/0011 ,  A61K39/02 ,  A61K2039/5154

Abstract: The present invention provides compositions and methods for generating and cryopreserving dendritic cells with superior functionality in producing stronger signals to T cells, resulting in a more potent DC-based anti-tumor vaccine. The present invention includes mature, antigen loaded DCs activated by Toll-like receptor agonists that induce clinically effective immune responses, preferably when used earlier in the disease process. The DCs of the present invention produce desirable levels of cytokines and chemokines, and further have the capacity to induce apoptosis of tumor cells. The cells can be cryopreserved and thawed for later use, thereby reducing the need for repeated pheresis and elutriation processes during vaccine production. These methods can also be utilized to directly target molecules involved in carcinogenetic signaling pathways and cancer stem cells.

Abstract translation: 本发明提供用于产生和冷冻保存树突状细胞的组合物和方法，其具有在向T细胞产生更强信号方面具有优异的功能性，导致更有效的基于DC的抗肿瘤疫苗。 本发明包括诱导临床有效免疫应答的Toll样受体激动剂激活的成熟的抗原负载DC，优选在疾病过程中较早使用时。 本发明的DC产生所需水平的细胞因子和趋化因子，并且还具有诱导肿瘤细胞凋亡的能力。 细胞可以冷冻保存和解冻以供以后使用，从而减少在疫苗生产过程中反复进行血液分离和淘析过程的需要。 这些方法也可以用于直接靶向参与致癌信号通路和癌症干细胞的分子。

公开(公告)号：US07700581B2

公开(公告)日：2010-04-20

申请号：US11700087

申请日：2007-01-31

Applicant: Mao Chen ,  Shaoxuan Zhu ,  Xuebin Liu ,  Chun Luo ,  Shuwen Xu ,  Lizhen Zheng ,  Fang Ye ,  Chenglong Yi ,  Xiaona Zhang

Inventor： Mao Chen ,  Shaoxuan Zhu ,  Xuebin Liu ,  Chun Luo ,  Shuwen Xu ,  Lizhen Zheng ,  Fang Ye ,  Chenglong Yi ,  Xiaona Zhang

IPC: C07D501/36 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04

CPC classification number: C07D501/36

Abstract: Disclosed herein are a cephalosporin compound of formula I, wherein R1 is selected from the following groups: wherein R2 is selected from the following groups: the preparation and uses thereof. A method of preparing the cephalosporin compound as disclosed herein comprises reacting a starting cephalosporin comprising a C7 amino group and a C3 thio-methyl moiety substituted with an N-containing heterocyclic group with bromoacetyl bromide and then with a N,N′-bissubstituted thiourea. Methods of treating an infectious disease are also disclosed, comprising administering to a patient in need thereof the pharmaceutical composition disclosed herein.

Abstract translation: 本文公开的是式I的头孢菌素化合物，其中R 1选自以下基团：其中R 2选自以下基团：其制备和用途。 制备本文公开的头孢菌素化合物的方法包括将包含C7氨基的起始头孢菌素和被含氮杂环基取代的C3硫代甲基部分与溴乙酰溴反应，然后与N，N'-双取代的硫脲反应。 还公开了治疗感染性疾病的方法，包括向有需要的患者施用本文公开的药物组合物。