公开(公告)号：US20150353536A1

公开(公告)日：2015-12-10

申请号：US14351575

申请日：2014-02-13

申请人： Shangha Ai Qi Ecological Technology Co., Ltd.

发明人： Gong Chen ,  Kunyuan Song

IPC分类号： C07D421/04 ,  C07D311/62 ,  C07C391/00

CPC分类号： C07D421/04 ,  A61K31/095 ,  A61K31/366 ,  C01B19/008 ,  C07C61/13 ,  C07C391/00 ,  C07C2602/42 ,  C07D311/62

摘要： A compound medicine for treating acute and chronic hepatitis B, includes a polyphenolic selenium compound having a functional group of alkali metal ion and selenium coordination complex, which has functions of directly killing HBV and destroying replication template of HBV. Auxiliary formulas thereof include high-purity oxymatrine and glycyrrhizin sulfate. The oxymatrine has an effect of anti-HBV, and is capable of treating acute and chronic hepatitis B, regulating immune system and increasing leukocyte. Serving as a main hepatocyte membrane protective agent, the glycyrrhizin sulfate has not only an effect of anti-inflammation, but also it is capable of regulating immune system and protecting hepatocyte. The compound medicine has no toxicity or side effect.

摘要翻译： 用于治疗急性和慢性乙型肝炎的复方药物包括具有碱金属离子和硒配位络合物官能团的多酚硒化合物，其具有直接杀死HBV和破坏HBV复制模板的功能。 其辅助配方包括高纯度氧化苦参碱和硫酸甘草酸。 氧化苦参碱具有抗HBV的作用，能够治疗急性和慢性乙型肝炎，调节免疫系统和增加白细胞。 作为主要的肝细胞膜保护剂，硫酸甘草酸不仅具有抗炎作用，而且能够调节免疫系统和保护肝细胞。 复方药物无毒副作用。

公开(公告)号：US09023867B2

公开(公告)日：2015-05-05

申请号：US13892576

申请日：2013-05-13

申请人： China Medical University

发明人： Sheng-Chu Kuo ,  Che-Ming Teng ,  Kuo-Hsiung Lee ,  Li-Jiau Huang ,  Li-Chen Chou ,  Chih-Shiang Chang ,  Chung-Ming Sun ,  Tian-Shung Wu ,  Shiow-Lin Pan ,  Tzong-Der Way ,  Jang-Chang Lee ,  Jing-Gung Chung ,  Jai-Sing Yang ,  Chien-Ting Chen ,  Ching-Che Huang ,  Shih-Ming Huang

IPC分类号： C07D421/04 ,  C07F9/6561 ,  C07F9/60 ,  C07D215/233 ,  C07D491/056

CPC分类号： C07F9/6561 ,  C07D215/233 ,  C07D421/04 ,  C07D491/056 ,  C07F9/60

摘要： 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠 盐。 初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。 还合成了2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和N，N-二烷基氨基烷基衍生物。 这些新型中间体显示出显着的抗癌活性。

公开(公告)号：US09023866B2

公开(公告)日：2015-05-05

申请号：US13892522

申请日：2013-05-13

申请人： China Medical University

发明人： Sheng-Chu Kuo ,  Che-Ming Teng ,  Kuo-Hsiung Lee ,  Li-Jiau Huang ,  Li-Chen Chou ,  Chih-Shiang Chang ,  Chung-Ming Sun ,  Tian-Shung Wu ,  Shiow-Lin Pan ,  Tzong-Der Way ,  Jang-Chang Lee ,  Jing-Gung Chung ,  Jai-Sing Yang ,  Chien-Ting Chen ,  Ching-Che Huang ,  Shih-Ming Huang

IPC分类号： C07D421/04 ,  C07F9/6561 ,  C07F9/60 ,  C07D215/233 ,  C07D491/056

CPC分类号： C07F9/6561 ,  C07D215/233 ,  C07D421/04 ,  C07D491/056 ,  C07F9/60

摘要： 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠 盐。 初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。 还合成了2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和N，N-二烷基氨基烷基衍生物。 这些新型中间体显示出显着的抗癌活性。

公开(公告)号：US20140088149A1

公开(公告)日：2014-03-27

申请号：US14088559

申请日：2013-11-25

申请人： Thioredoxin Systems AB

发明人： Arne Holmgren ,  Jun Lu ,  Alexios Vlamis-Gardikas ,  Rong Zhao ,  Karuppasamy Kandasamy ,  Lars Engman ,  Lars Engstrand ,  Sven Hoffner

IPC分类号： C07D421/04 ,  C07D293/12

CPC分类号： C07D421/04 ,  A61K31/381 ,  A61K31/41 ,  C07D293/12 ,  Y02A50/473

摘要： The mechanism of action of Ebselen differentiates between bacterial and mammalian thioredoxin reductase (TrxR). It displays fast oxidation of mammalian Trx and via the NADPH-TrxR catalyzed turnover of ebselen selenol with hydrogen peroxide, and therefore are mammalian antioxidants. Ebselen, and its diselenide, are strong competitive inhibitors of E. coli TrxR with Ki of 0.14 μM and 0.46 μM, respectively. E. coli mutants lacking glutathione reductase or glutathione were much more sensitive to inhibition by ebselen. Since either glutaredoxin or thioredoxin systems are electron donors to ribonucleotide reductase, ebselen targets primarily glutathione and glutaredoxin-negative bacteria, a class which includes major pathogens. Ebselen, and similar compounds are therefore useful as antibacterial agents, even for multiresistant strains. Two major pathogenic bacteria, which previously had not been known to be sensitive to ebselen, Mycobacterium tuberculosis (tuberculosis) and Helicobacter pylori (stomach ulcer and cancer), were shown to be excellent targets. Helicobacter pylori was also sensitive to ebsulfur.

摘要翻译： Ebselen的作用机制区分细菌和哺乳动物硫氧还蛋白还原酶（TrxR）。 它显示哺乳动物Trx的快速氧化，并且通过NADPH-TrxR催化依次硒硒酚与过氧化氢的周转，因此是哺乳动物抗氧化剂。 依布硒及其二硒化物是大肠杆菌TrxR的强竞争性抑制剂，Ki分别为0.14μM和0.46μM。 缺乏谷胱甘肽还原酶或谷胱甘肽的大肠杆菌突变体对依布硒林的抑制更敏感。 由于谷氧还蛋白或硫氧还蛋白系统是核糖核苷酸还原酶的电子供体，依普硒靶主要是谷胱甘肽和谷氧还蛋白阴性细菌，一类包括主要病原体。 因此，依布硒林和类似化合物可用作抗菌剂，即使对于多抗性菌株也是有用的。 以前不知道对ebselen，结核分枝杆菌（结核分枝杆菌）和幽门螺杆菌（胃溃疡和癌症）敏感的两种主要致病菌被证明是优异的靶标。 幽门螺杆菌对硫化硫也敏感。

公开(公告)号：US20130253006A1

公开(公告)日：2013-09-26

申请号：US13892522

申请日：2013-05-13

申请人： China Medical University

发明人： Sheng-Chu KUO ,  Che-Ming Teng ,  Kuo-Hsiung Lee ,  Li-Jiau Huang ,  Li-Chen Chou ,  Chih-Shiang Chang ,  Chung-Ming Sun ,  Tian-Shung Wu ,  Shiow-Lin Pan ,  Tzong-Der Way ,  Jang-Chang Lee ,  Jing-Gung Chung ,  Jai-Sing Yang ,  Chien-Ting Chen ,  Ching-Che Huang ,  Shih-Ming Huang

IPC分类号： C07D421/04

CPC分类号： C07F9/6561 ,  C07D215/233 ,  C07D421/04 ,  C07D491/056 ,  C07F9/60

摘要： 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠 盐。 初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。 还合成了2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和N，N-二烷基氨基烷基衍生物。 这些新型中间体显示出显着的抗癌活性。

公开(公告)号：US20120178723A1

公开(公告)日：2012-07-12

申请号：US13207696

申请日：2011-08-11

申请人： Masaaki Hirose ,  Zhigen Hu ,  Yongbo Hu ,  Hong Myung Lee ,  Zhan Shi ,  Stepan Vyskocil ,  Tianlin Xu

发明人： Masaaki Hirose ,  Zhigen Hu ,  Yongbo Hu ,  Hong Myung Lee ,  Zhan Shi ,  Stepan Vyskocil ,  Tianlin Xu

IPC分类号： A61K31/437 ,  C07D417/14 ,  A61K31/4439 ,  C07D409/14 ,  C07D495/04 ,  A61K31/4365 ,  A61K31/506 ,  C07D413/14 ,  A61K31/422 ,  C07D409/04 ,  A61K31/501 ,  A61K31/497 ,  A61K31/4725 ,  A61K31/4375 ,  A61K31/496 ,  C07D417/04 ,  A61K31/5377 ,  C07D413/04 ,  A61K31/381 ,  A61K31/4545 ,  C07D491/107 ,  A61K31/498 ,  C07D421/04 ,  A61P35/00 ,  A61P29/00 ,  A61P9/00 ,  A61P37/08 ,  A61P37/06 ,  A61P9/12 ,  A61K31/4436 ,  A61K31/655 ,  A61P7/02 ,  C07D471/04

CPC分类号： C07D277/56 ,  A61K31/4155 ,  A61K31/425 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D277/64 ,  C07D293/06 ,  C07D333/38 ,  C07D333/54 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107 ,  C07D495/04

摘要： This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

摘要翻译： 本发明提供式IA-a或IB-a及其子集的化合物：其中Z，HY，R1，R2，G1，W，n和A及其子集如说明书中所述。 这些化合物是PI3K的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

公开(公告)号：US20030028015A1

公开(公告)日：2003-02-06

申请号：US10061480

申请日：2002-02-01

发明人： Ching-Jer Chang ,  Curtis L. Ashendel ,  Darrick Kim

IPC分类号： C07D421/04 ,  A61K031/33

CPC分类号： C07D421/14 ,  A61K31/34 ,  A61K31/381 ,  A61K31/4025 ,  C07D307/46 ,  C07D333/22 ,  C07D345/00 ,  C07F7/0838

摘要： Novel selenophene compounds useful as anti-tumor agents are described. Preferred compounds include compounds of formula I: 1 wherein R1 and R2 are independently selected from the group consisting of, 2 H, CHO, CH2OH and CH2NH2; and X and Y are independently selected from the group consisting of Se, S, O, NCH3 and NH. Pharmaceutical compositions and a method for treating patients having tumors utilizing the disclosed selenophene compounds are also described.

摘要翻译： 描述了可用作抗肿瘤剂的新型硒吩类化合物。 优选的化合物包括式I化合物：其中R 1和R 2独立地选自H，CHO，CH 2 OH和CH 2 NH 2; X和Y独立地选自Se，S，O，NCH 3和NH。 还描述了药物组合物和利用所公开的硒吩化合物治疗患有肿瘤的患者的方法。

公开(公告)号：US6071922A

公开(公告)日：2000-06-06

申请号：US44558

申请日：1998-03-19

申请人： Raymond F. Schinazi ,  Chung K. Chu ,  Jinfa Du

发明人： Raymond F. Schinazi ,  Chung K. Chu ,  Jinfa Du

IPC分类号： C07D421/04 ,  C07D473/00 ,  C07D473/18 ,  C07F9/6558 ,  C07F9/6561 ,  A61K31/505 ,  C07D239/02

CPC分类号： C07D473/00 ,  C07D421/04 ,  C07D473/18 ,  C07F9/65586 ,  C07F9/65616

摘要： A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

公开(公告)号：US5075322A

公开(公告)日：1991-12-24

申请号：US613149

申请日：1990-11-14

申请人： Pierre Braquet ,  Colette Broquet

发明人： Pierre Braquet ,  Colette Broquet

IPC分类号： A61K31/445 ,  A61K31/55 ,  A61P11/00 ,  A61P37/08 ,  A61P43/00 ,  C07D421/04

CPC分类号： C07D421/04

摘要： The invention relates to new selenophen derivatives of the formulae, ##STR1## to a preparation process of said compounds and to therapeutic compositions containing the same.

摘要翻译： 本发明涉及所述化合物的制备方法和含有该化合物的治疗组合物的新颖的具有下式的硒吩衍生物： 。

公开(公告)号：US4886625A

公开(公告)日：1989-12-12

申请号：US114011

申请日：1987-10-29

申请人： James P. Albarella ,  J. Oakey Noell ,  Paul O. Vogelhut ,  deceased, Frederick E. Ward

发明人： James P. Albarella ,  J. Oakey Noell ,  Paul O. Vogelhut ,  deceased, Frederick E. Ward

IPC分类号： C12Q1/26 ,  C07D333/40 ,  C07D409/04 ,  C07D409/14 ,  C07D419/14 ,  C07D421/04 ,  C07D421/14 ,  C07D521/00 ,  C08G61/10 ,  C08G61/12 ,  C12Q1/00 ,  C12Q1/54 ,  G01N33/532 ,  G01N33/543 ,  H01B1/12

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D409/04 ,  C07D409/14 ,  C08G61/123 ,  C12Q1/002 ,  C12Q1/54 ,  G01N33/532 ,  H01B1/127

摘要： Electrically conducting homo- and/or copolymers and/or tripolymers can be produced from novel monomers, such as a 3-substituted 2,5-di(2-thienyl)pyrrole. The polymers exhibit unexpectedly high stability and conductivities, and can be functionalized, such as with an enzyme, like glucose oxidase, or an ion-specific binding site, like a crown ether, or an antigen, without adversely affecting the conductivity of the polymer. The functionalized, conducting polymer can be used in a diagnostic device to determine the presence and concentration of a specific analyte in a liquid medium. For example, the presence and concentration of glucose is determined by measuring the conductivity change in the polymer caused by the vibrational excitation induced in the enzyme, glucose oxidase, from its reaction with the glucose and/or by measuring a secondary effect of the enzyme/substrate reaction, such as the change in the conductivity of the conducting polymer caused by the generation of hydrogen peroxide during the glucose-glucose oxidase reaction.