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1. 发明申请

WO2008017734A8 POLYMYXIN DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：聚亚胺衍生物及其用途
公开(公告)号：WO2008017734A8
公开(公告)日：2009-07-30
申请号：PCT/FI2007050441
申请日：2007-08-10
申请人： NORTHERN ANTIBIOTICS OY , VAARA MARTTI , VAARA TIMO
发明人： VAARA MARTTI , VAARA TIMO
IPC分类号： C07K7/62 , A61K38/12 , A61P31/04 , C12P21/04
CPC分类号： C07K7/62 , A61K38/00
摘要： The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives. The invention further relates to a method for treating, alleviating or ameliorating an infection in a subject, caused by a Gram-negative bacterium by administering a therapeutically effective amount of a derivative according to the present invention to said subject; to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; for reducing the nephrotoxicity, for improving the pharmacokinetic properties of natural polymyxins and octapeptins; and for sensitizing clinically important bacteria to a host defence mechanism complement present in serum. Finally, the invention relates to a process for preparing such polymyxin derivatives.
摘要翻译：本发明涉及多粘菌素衍生物，其中R 1，R 2和R 3是任选的，并且R 1，R 2，R 3，R 5，R 8和R 9是选择的阳离子或中性氨基酸残基，使得在生理pH下的正电荷总数至少为两个但不超过三个; 以及包含至少两种这样的衍生物的组合产品。本发明还涉及通过向所述受试者施用治疗有效量的本发明衍生物来治疗，减轻或改善由革兰氏阴性细菌引起的受试者感染的方法; 涉及将革兰氏阴性细菌对抗菌剂敏感的方法，通过向所述受试者同时或依次施用治疗有效量的所述抗菌剂和本发明衍生物的方法，开发新型抗生素的方法; 用于降低肾毒性，用于改善天然多粘菌素和八肽素的药代动力学性质; 并使临床上重要的细菌对血清中存在的宿主防御机制补体敏感。最后，本发明涉及制备这种多粘菌素衍生物的方法。

2. 发明申请

WO1992007947A1 OLIGOSACCHARIDE MIXTURE, AND PROCEDURE FOR ITS AFTER-TREATMENT 审中-公开
标题翻译：低密度混合物及其后处理程序
公开(公告)号：WO1992007947A1
公开(公告)日：1992-05-14
申请号：PCT/FI1991000240
申请日：1991-08-08
申请人： OY ALKO AB , ROSSI, Marianne , LINKO, Yu-Yen , LINKO, Pekka , VAARA, Timo , TURUNEN, Marja
发明人： OY ALKO AB
IPC分类号： C12P19/20
CPC分类号： C12P19/16 , C12P19/18
摘要： A procedure for after-treatment of an oligosaccharide mixture, wherein glucoamylase and/or yeast is made to act on an oligosaccharide mixture which has been obtained by making cyclomaltodextrin-glucanotransferase (CGTase, E.C.2.4.1.19) act on starch in the presence of acceptor sugar. By this procedure a novel oligosaccharide mixture lower in calories and less cariogenic than before is obtained.
摘要翻译：寡糖混合物的后处理方法，其中葡糖淀粉酶和/或酵母作用于通过制备环糊精 - 葡聚糖转移酶（CGTase，EC2.4.1.19）在受体存在下作用于淀粉而获得的寡糖混合物糖。通过该方法，获得了比以前更低卡路里和较少龋齿的新型低聚糖混合物。

3. 发明申请

WO2009098357A1 SHORT FATTY ACID TAIL POLYMYXIN DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：短脂肪酸尾纤维多糖衍生物及其用途
公开(公告)号：WO2009098357A1
公开(公告)日：2009-08-13
申请号：PCT/FI2009/050093
申请日：2009-02-05
申请人： NORTHERN ANTIBIOTICS OY , VAARA, Martti , VAARA, Timo
发明人： VAARA, Martti , VAARA, Timo
IPC分类号： C07K7/62
CPC分类号： C07K7/62 , A61K38/00 , Y02A50/473
摘要： The present invention relates to a polymyxin derivative wherein the derivative has a total of three positive charges at physiological pH and wherein the terminal moiety (D) of the derivative comprises a total of 1 to 5 carbon atoms; and to a combination product comprising at least two such derivatives. The invention further relates to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; and for sensitizing clinically important bacteria to a host defense mechanism complement present in serum. The invention also relates to a method of treating a subject for a gram-negative bacterial infection by administering a polymyxin derivative of the invention in combination with a second antibacterial agent. Finally, the invention relates to a process for preparing such polymyxin derivatives.
摘要翻译：本发明涉及多粘菌素衍生物，其中衍生物在生理pH下具有总共三个正电荷，并且其中衍生物的末端部分（D）包含总共1至5个碳原子; 以及包含至少两种这样的衍生物的组合产品。本发明还涉及通过以任何顺序将治疗有效量的所述抗菌剂和根据本发明的衍生物给予所述受试者，同时或依次施用革兰氏阴性菌对抗菌剂敏感的方法; 开发新型抗生素的方法; 并使临床上重要的细菌对血清中存在的宿主防御机制补体敏感。本发明还涉及通过将本发明的多粘菌素衍生物与第二抗菌剂组合施用来治疗受试者革兰氏阴性细菌感染的方法。最后，本发明涉及制备这种多粘菌素衍生物的方法。

4. 发明申请

WO2008017734A1 POLYMYXIN DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：聚亚胺衍生物及其用途
公开(公告)号：WO2008017734A1
公开(公告)日：2008-02-14
申请号：PCT/FI2007/050441
申请日：2007-08-10
申请人： NORTHERN ANTIBIOTICS OY , VAARA, Martti , VAARA, Timo
发明人： VAARA, Martti , VAARA, Timo
IPC分类号： C07K7/62 , A61K38/12 , C12P21/04 , A61P31/04
CPC分类号： C07K7/62 , A61K38/00 , Y02A50/473
摘要： The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives. The invention further relates to a method for treating, alleviating or ameliorating an infection in a subject, caused by a Gram-negative bacterium by administering a therapeutically effective amount of a derivative according to the present invention to said subject; to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; for reducing the nephrotoxicity, for improving the pharmacokinetic properties of natural polymyxins and octapeptins; and for sensitizing clinically important bacteria to a host defence mechanism complement present in serum. Finally, the invention relates to a process for preparing such polymyxin derivatives.
摘要翻译：本发明涉及多粘菌素衍生物，其中R 1，R 2和R 3是任选的，并且R 1，R 2，R 3，R 5，R 8和R 9是选择的阳离子或中性氨基酸残基，使得在生理pH下的正电荷总数至少为两个但不超过三个; 以及包含至少两种这样的衍生物的组合产品。本发明还涉及通过向所述受试者施用治疗有效量的本发明衍生物来治疗，减轻或改善由革兰氏阴性细菌引起的受试者感染的方法; 涉及将革兰氏阴性细菌对抗菌剂敏感的方法，通过向所述受试者同时或依次施用治疗有效量的所述抗菌剂和本发明衍生物的方法，开发新型抗生素的方法; 用于降低肾毒性，用于改善天然多粘菌素和八肽素的药代动力学性质; 并使临床上重要的细菌对血清中存在的宿主防御机制补体敏感。最后，本发明涉及制备这种多粘菌素衍生物的方法。

5. 发明申请

WO1992006602A1 YEAST FIBER COMPOSITION AND PROCESS FOR THE PRODUCTION THEREOF 审中-公开
标题翻译： YEAST纤维组合物及其生产方法
公开(公告)号：WO1992006602A1
公开(公告)日：1992-04-30
申请号：PCT/FI1991000316
申请日：1991-10-15
申请人： ALKO LTD. , PENTTILÄ, Liisa , VAARA, Timo
发明人： ALKO LTD.
IPC分类号： A23L01/28
CPC分类号： A23K10/16 , A23L33/14 , A23L33/145 , A23L33/21
摘要： The invention relates to yeast cell compositions and to processes for the production therefor. According to the invention, in a mild flavored, smooth textured composition of yeast cells, more than 50 % of the yeast cells comprise whole yeast cell walls. The composition comprises at least about 40 % by weight of fibre and less than about 1.6 % by weight of nucleic acid. It is prepared via extraction comprising a heating step.

6. 发明申请

WO1992003565A1 OLIGOSACCHARIDE MIXTURE, AND PROCEDURE FOR ITS MANUFACTURING 审中-公开
标题翻译：低聚物混合物及其制造方法
公开(公告)号：WO1992003565A1
公开(公告)日：1992-03-05
申请号：PCT/FI1991000239
申请日：1991-08-08
申请人： OY ALKO AB , ROSSI, Marianne , LINKO, Yu-Yen , LINKO, Pekka , VAARA, Timo , TURUNEN, Marja
发明人： OY ALKO AB
IPC分类号： C12P19/18
CPC分类号： C12P19/18
摘要： A procedure for manufacturing an oligosaccharide mixture, in which cyclomaltodextrin-glucanotransferase (CGTase; E.C. 2.4.1.19) acts on starch in the presence of acceptor sugar (trehalose or cellobiose), whereby oligosaccharides containing trehalose and cellobiose, and unique of their sugar composition, are produced.
摘要翻译：制备寡糖混合物的方法，其中环糊精 - 葡聚糖转移酶（CGTase; EC 2.4.1.19）在受体糖（海藻糖或纤维二糖）存在下作用于淀粉，由此含有海藻糖和纤维二糖的寡糖，并且它们的糖组成独特，被生产。

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