公开(公告)号：EP1312607A1

公开(公告)日：2003-05-21

申请号：EP01127296.0

申请日：2001-11-17

申请人： MEDAC GmbH

发明人： Makarov, Vadim, Dr. ,  Möllmann, Ute, Dr.

IPC分类号： C07D239/46 ,  C07D239/56 ,  C07D213/71 ,  C07C333/20 ,  A61K31/506 ,  A61P31/04

CPC分类号： C07D239/56 ,  C07D213/71 ,  C07D239/47

摘要： Compounds of the formula I
wherein X is a bivalent residue selected from the group consisting of


have excellent antibacterial activities and are useful agents for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci.

摘要翻译： 式I 的化合物，其中X是选自 CHEM> CHEM>的二价残基具有优异的抗菌活性，并且是用于治疗或预防哺乳动物（人类）感染性疾病的有用试剂 和动物），由细菌引起的，特别是结核分枝杆菌（TB）和由分支杆菌引起的lepra和由葡萄球菌引起的传染病引起的麻疹。

公开(公告)号：EP1204324A1

公开(公告)日：2002-05-15

申请号：EP00926083.7

申请日：2000-04-18

申请人： Dorn, Gordon L.

发明人： Dorn, Gordon L.

IPC分类号： A01N47/44

CPC分类号： A01N31/16 ,  A01N37/02 ,  A01N47/44 ,  A01N59/14 ,  A01N37/40 ,  A01N31/04 ,  A01N2300/00

摘要： A transport/preservation system has been found which provides safe, effective transport for patient specimens and bodily fluids, and functions as a preservative for biological reagents, therapeutics and personal care products. The transport/preservative formulations can also be used as safe, effective sanitizers on surfaces, equipment, and appliances. The transport preservation formulations comprising a biguanide and one or more other antimicrobial agents are cidal to microorganisms when present in a sample or on a surface to be sanitized.

公开(公告)号：EP1198461A2

公开(公告)日：2002-04-24

申请号：EP00947487.5

申请日：2000-07-17

申请人： Cytoclonal Pharmaceutics, Inc.

发明人： ARAD, Dorit ,  BOLLON, Arthur, P. ,  POLAND, Bradley, W. ,  YOUNG, David, C.

IPC分类号： C07D305/00

CPC分类号： C07C271/22 ,  C07C233/58 ,  C07C233/87 ,  C07C235/14 ,  C07C2602/44

摘要： A method for designing paclitaxel alternative compounds which stabilize the tubulin polymerization process has been found. These compounds in solution possess steric conformational properties of natural paclitaxel and are capable of binding to the tubulin protein at the same site where paclitaxel is known to bind. The compounds of the present invention stabilize tubulin polymerization in a way that is mechanistically equivalent to activity mechanism of paclitaxel. The compounds of the present invention have increased solubility, simpler synthesis, and the possibility for specificity and optimization due to the combinatorial reactions over natural paclitaxel.

摘要翻译： 已经发现了一种设计稳定微管蛋白聚合方法的紫杉醇替代化合物的方法。 溶液中的这些化合物具有天然紫杉醇的空间构象特征，并且能够在已知紫杉醇结合的相同位点处结合微管蛋白。 本发明的化合物以机械方式等同于紫杉醇的活性机理的方式稳定微管蛋白聚合。 由于在天然紫杉醇上的组合反应，本发明的化合物具有增加的溶解性，更简单的合成以及特异性和优化的可能性。