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1. 发明申请

WO2011061272A3 A DI(4-CHLORO-PHENYLDIGUANIDO) DERIVATIVE WHICH IS FREE OF POTENTIAL GENOTOXICITY AND A PROCESS FOR REDUCING THE RESIDUAL AMOUNT OF P-CHLOROANILINE IN SAID DI(4-CHLORO-PHENYLDIGUANIDO) DERIVATIVE 审中-公开
标题翻译：不含潜在致病性的DI（4-氯代苯基）衍生物和用于降低化学式（4-氯 - 苯基）吡啶衍生物中的对氯苯胺残留量的方法
公开(公告)号：WO2011061272A3
公开(公告)日：2011-11-10
申请号：PCT/EP2010067782
申请日：2010-11-18
申请人： MEDICHEM SA , SANCHEZ SALGUERO LAURA , BOU BOSCH RAQUEL , BOSCH I LLADO JORDI , CAMACHO CARRASCO ANTONIO , DURAN LOPEZ ERNESTO , ANDRES MAGNANI PABLO
发明人： SANCHEZ SALGUERO LAURA , BOU BOSCH RAQUEL , BOSCH I LLADO JORDI , CAMACHO CARRASCO ANTONIO , DURAN LOPEZ ERNESTO , ANDRES MAGNANI PABLO
IPC分类号： C07C279/18 , C07C277/08 , C07C279/26
CPC分类号： C07C279/265 , C07C277/08
摘要： The invention relates to a process for reducing the residual amount of p-chloroaniline in chlorhexidine. Also, the invention relates to a process for preparing chlorhexidine, or a pharmaceutically acceptable salt thereof, which is free of potential genotoxicity. In addition, the invention refers to the said chlorhexidine, or a pharmaceutically acceptable salt thereof, which is free of potential genotoxicity. Further, the invention relates to an analytical HPLC method for the determination of potentially genotoxic impurities in samples of chlorhexidine, or of a pharmaceutically acceptable salt thereof. The invention also relates to stabilized chlorhexidine digluconate salt free of potential genotoxicity in aqueous solution, and to a method for stabilizing chlorhexidine digluconate salt free of potential genotoxicity in aqueous solution.
摘要翻译：本发明涉及减少氯己定中对氯苯胺残留量的方法。此外，本发明涉及一种不含潜在遗传毒性的氯己定或其药学上可接受的盐的制备方法。此外，本发明涉及没有潜在遗传毒性的所述氯己定或其药学上可接受的盐。此外，本发明涉及用于测定洗必太或其药学上可接受的盐样品中潜在遗传毒性杂质的分析型HPLC方法。本发明还涉及在水溶液中没有潜在的遗传毒性的稳定的氯己定二葡萄糖酸盐，以及在水溶液中不含潜在遗传毒性的氯己定二葡糖酸盐的稳定化方法。

2. 发明申请

WO2011046267A1 SILVER/POLYDIGUANIDE COMPLEX, PREPARATION METHOD THEREOF, AND ANTIBACTERIAL COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT 审中-公开
标题翻译：银/聚异氰酸酯复合物，其制备方法和含有其作为活性成分的抗菌组合物
公开(公告)号：WO2011046267A1
公开(公告)日：2011-04-21
申请号：PCT/KR2010/000717
申请日：2010-02-05
申请人： SNU R&DB FOUNDATION , SONG, Joon Myong , PAL, Sukdeb
发明人： SONG, Joon Myong , PAL, Sukdeb
IPC分类号： A61K33/38 , A61K31/155 , A61P17/02 , A61P17/00 , C07F1/10
CPC分类号： C07C279/265
摘要： The present invention relates to a silver/polydiguanide complex and derivatives thereof including silver and polydiguanide having at least two biguanide moieties, wherein the silver is stabilized in an oxidation state of an integer of 0 to 4, a mole ratio between the silver and the polydiguanide is 1: 1-4, an average particle diameter of the complex is micrometer or nanometer, and zeta potential of the complex is greater than or equal to zero, a preparation method thereof, and an antibacterial composition for burns or wounds treatment including the same as an active ingredient. A silver/polydiguanide complex according to the present invention is different from conventional silver/polydiguanide complexes in carbon, hydrogen, and nitrogen contents as well as in structure of silver and polydiguanide, and solubility, is a material that exhibits a very good antibacterial activity due to a much lower minimal inhibitory concentration (MIC) value by 10 to 100 folds or more compared to silver sulfadiazine which is a conventional therapeutic agent for burns, and may be usefully used as an antibacterial composition for burns or wounds treatment.
摘要翻译：本发明涉及银/聚二胍复合物及其衍生物，其包含具有至少两个双胍部分的银和聚二胍，其中银以0至4的整数的氧化态稳定，银和聚二胍的摩尔比为1：1-4，络合物的平均粒径为微米或纳米，络合物的ζ电位为大于或等于零，其制备方法以及包含其的烧伤或伤口治疗用抗菌组合物作为活性成分。根据本发明的银/聚二胍复合物与碳，氢和氮含量以及银和聚二胍的结构中的常规银/聚二胍络合物不同，并且溶解度是表现出非常好的抗菌活性的材料与作为常规烧伤治疗剂的磺胺嘧啶磺胺相比，低得多的最小抑制浓度（MIC）值为10〜100倍以上，并且可以有效地用作烧伤或伤口治疗的抗菌组合物。

3. 发明申请

WO2012047630A2 N-ALKYL OR N-ARYL SUBSTITUTED GUANIDE AND BIGUANIDE COMPOUNDS AND METHODS OF THEIR USE 审中-公开
标题翻译： N-烷基或N-芳基取代的胍和双胍化合物及其使用方法
公开(公告)号：WO2012047630A2
公开(公告)日：2012-04-12
申请号：PCT/US2011/053401
申请日：2011-09-27
申请人： TEINTZE, Martin , WILKINSON, Royce A. , LABIB, Mohamed
发明人： TEINTZE, Martin , WILKINSON, Royce A. , LABIB, Mohamed
IPC分类号： A61K31/53
CPC分类号： C07C279/265 , C07C279/04 , C07C279/18 , C07D251/54 , C07D487/18
摘要： The present invention provides N-aryl or N-alkyl guanide and biguanide containing compounds having the structure X. or the structure XI. These compounds may be synthesized by the addition of the respective guanide, biguanide or phenylguanide groups to polyamines containing primary and/or secondary amines. The present invention includes methods of using these compounds for the treatment and/or prevention of bacterial infection, HIV infection, and cancer and for the promotion of stem cell mobilization, wound healing, hematopoiesis, and skin rejuvenation.
摘要翻译：本发明提供具有结构X或结构XI的含N-芳基或N-烷基胍和双胍的化合物。这些化合物可以通过将各自的胍，双胍或苯基胍基团添加到含有伯胺和/或仲胺的多胺来合成。本发明包括使用这些化合物治疗和/或预防细菌感染，HIV感染和癌症以及促进干细胞动员，伤口愈合，造血和皮肤恢复活力的方法。

4. 发明申请

WO2007021839A3 POLYAMINES USEFUL AS ANTI-PARASITIC AND ANTI-CANCER THERAPEUTICS AND AS LYSINE-SPECIFIC DEMETHYLASE INHIBITORS 审中-公开
标题翻译：用作抗寄生虫和抗癌治疗剂以及作为赖氨酸特异性二甲基酶抑制剂的聚酰胺
公开(公告)号：WO2007021839A3
公开(公告)日：2007-06-14
申请号：PCT/US2006031198
申请日：2006-08-10
申请人： UNIV JOHNS HOPKINS , UNIV WAYNE STATE , WOSTER PATRICK M , BONCHER TRACEY , CASERO ROBERT A
发明人： WOSTER PATRICK M , BONCHER TRACEY , CASERO ROBERT A
IPC分类号： C07C211/09 , A61K31/132 , A61K31/155 , A61P33/00 , A61P35/00 , C07C279/04
CPC分类号： C07C279/18 , C07C211/09 , C07C211/18 , C07C211/22 , C07C211/36 , C07C211/49 , C07C215/14 , C07C233/38 , C07C247/12 , C07C279/04 , C07C279/12 , C07C279/265 , C07C323/25 , C07C381/00 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/20 , C07C2603/50 , C07F9/3264
摘要： Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.
摘要翻译：公开了多胺，多胺/胍基和多胺/双胍化合物。这些化合物可用作抗癌和抗寄生虫治疗。该化合物也可用作赖氨酸特异性脱甲基酶-1的抑制剂。

5. 发明申请

WO2007021839A2 POLYAMINES USEFUL AS ANTI-PARASITIC AND ANTI-CANCER THERAPEUTICS AND AS LYSINE-SPECIFIC DEMETHYLASE INHIBITORS 审中-公开
标题翻译：聚氨酯有效地作为抗癌和抗癌治疗药物和特定的脱乙酰酶抑制剂
公开(公告)号：WO2007021839A2
公开(公告)日：2007-02-22
申请号：PCT/US2006/031198
申请日：2006-08-10
申请人： JOHNS HOPKINS UNIVERSITY , WAYNE STATE UNIVERSITY , WOSTER, Patrick, M. , BONCHER, Tracey , CASERO, Robert, A.
发明人： WOSTER, Patrick, M. , BONCHER, Tracey , CASERO, Robert, A.
IPC分类号： C07C211/09 , C07C279/04 , A61K31/132 , A61K31/155 , A61P35/00 , A61P33/00
CPC分类号： C07C279/18 , C07C211/09 , C07C211/18 , C07C211/22 , C07C211/36 , C07C211/49 , C07C215/14 , C07C233/38 , C07C247/12 , C07C279/04 , C07C279/12 , C07C279/265 , C07C323/25 , C07C381/00 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/20 , C07C2603/50 , C07F9/3264
摘要： Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.
摘要翻译：公开了多胺，多胺/胍基和多胺/双胍化合物。该化合物可用作抗癌和抗寄生虫治疗。该化合物也可用作酶赖氨酸特异性脱甲基酶-1的抑制剂。

6. 发明申请

WO2015042495A2 METFORMIN SALTS TO TREAT TYPE2 DIABETES 审中-公开
标题翻译： METFORMIN盐治疗2型糖尿病
公开(公告)号：WO2015042495A2
公开(公告)日：2015-03-26
申请号：PCT/US2014/056700
申请日：2014-09-20
申请人： JIVA PHARMA, INC.
发明人： GOEL, Om P
IPC分类号： A61K31/4439 , C07D417/12
CPC分类号： C07C279/265 , A61K31/155 , A61K31/4439 , C07D277/34 , C07D417/12 , A61K2300/00
摘要： Metformin salts of 2,4-thiazolidinediones are described for the treatment of diabetes mellitus Type2, gestational diabetes, polycystic ovary syndrome, non-alcoholic fatty liver disease, coronary artery disease, pancreatic cancer, premature puberty, and other diseases which manifest insulin resistance.
摘要翻译：描述了2,4-噻唑烷二酮的二甲双胍盐用于治疗2型糖尿病，妊娠糖尿病，多囊卵巢综合征，非酒精性脂肪肝疾病，冠状动脉疾病，胰腺癌，青春期早产，和其他表现出胰岛素抵抗的疾病。

7. 发明申请

WO2007000590A8 ANTIMICROBIAL BIGUANIDE METAL COMPLEXES 审中-公开
标题翻译：抗微生物双金属金属复合物
公开(公告)号：WO2007000590A8
公开(公告)日：2008-05-02
申请号：PCT/GB2006002364
申请日：2006-06-27
申请人： SMITH & NEPHEW , GREENER BRYAN
发明人： GREENER BRYAN
IPC分类号： C07F1/10
CPC分类号： C07C279/265 , A01N59/16 , C07C279/26 , A01N47/44 , A01N25/22 , A01N2300/00
摘要： A compound comprising a metal species and a biologically acceptable llgand, wherein the biologically acceptable ligand comprises a biguanide moiety, and wherein the biologically acceptable ligand forms a complex with the metal species in which the metal species is stabilised in an oxidation state greater than 1+. Compositions and medical devices comprising the compound. A method for the treatment or prophylaxis of microbial, including bacterial, infections, comprising the use of such compounds, compositions or medical devices.
摘要翻译：一种包含金属物质和生物可接受的化合物的化合物，其中所述生物可接受的配体包含双胍部分，并且其中所述生物学上可接受的配体与金属物质形成复合物，其中所述金属物质在大于1+ 。包含该化合物的组合物和医疗装置。用于治疗或预防微生物，包括细菌感染的方法，包括使用这些化合物，组合物或医疗装置。

8. 发明申请

WO1987000437A1 METHODS FOR DESINFECTING AND PRESERVING CONTACT LENSES 审中-公开
标题翻译：消除和保存接触镜的方法
公开(公告)号：WO1987000437A1
公开(公告)日：1987-01-29
申请号：PCT/US1985001393
申请日：1985-07-22
申请人： BAUSCH & LOMB INCORPORATED
发明人： BAUSCH & LOMB INCORPORATED , OGNUBIYI, Lai , SCOTT, Francis, L. , SMITH, Francis, X.
IPC分类号： A61L02/18
CPC分类号： C07C279/265 , A01N47/44 , A61L12/141
摘要： Improved methods of disinfecting and/or preserving contact lenses comprises treating said lenses with an effective concentration of a solution comprising a biguanide or a water soluble salt of formula (I), wherein R1 and R3 are selected hydrogen, halogen, alkyl, alkoxy, nitro, -SO2R4, carboxyl or hydroxyl where R4 is -NH2, -NHR', -NR'R'', -OR' or -O-aryl in which R' and R'' are alkyl or alkoxy; R2 is hydrogen or halogen and X is hydrogen or alkyl, provided that when R2 is halogen then both R1 and R3 are hydrogen and X is alkyl. The method provides for disinfecting and/or preserving contact lenses wherein the monomeric biguanide-containing solutions offer a wide spectrum of antimicrobial activity with nominal binding and concentrating onto lens surfaces and low levels of eye tissue irritation or inflammation.
摘要翻译：改进的消毒和/或保存隐形眼镜的方法包括用有效浓度的包含式（I）的双胍或水溶性盐的溶液处理所述镜片，其中R1和R3选自氢，卤素，烷基，烷氧基，硝基，-SO 2 R 4，羧基或羟基，其中R 4是-NH 2，-NHR'，-NR'R“，-OR'或-O-芳基，其中R'和R”是烷基或烷氧基; R2是氢或卤素，X是氢或烷基，条件是当R 2是卤素时，R 1和R 3都是氢，X是烷基。该方法提供消毒和/或保存隐形眼镜，其中单体含双胍的溶液提供广泛的抗菌活性，具有标称结合并集中在镜片表面上，并且低水平的眼组织刺激或炎症。

9. 发明申请

WO2012047630A3 N-ALKYL OR N-ARYL SUBSTITUTED GUANIDE AND BIGUANIDE COMPOUNDS AND METHODS OF THEIR USE 审中-公开
标题翻译： N-烷基或N-芳基取代的保护基和双胍化合物及其使用方法
公开(公告)号：WO2012047630A3
公开(公告)日：2012-06-21
申请号：PCT/US2011053401
申请日：2011-09-27
申请人： TEINTZE MARTIN , WILKINSON ROYCE A , LABIB MOHAMED
发明人： TEINTZE MARTIN , WILKINSON ROYCE A , LABIB MOHAMED
IPC分类号： A61L9/01 , C08G73/00
CPC分类号： C07C279/265 , C07C279/04 , C07C279/18 , C07D251/54 , C07D487/18
摘要： The present invention provides N-aryl or N-alkyl guanide and biguanide containing compounds having the structure X. or the structure XI. These compounds may be synthesized by the addition of the respective guanide, biguanide or phenylguanide groups to polyamines containing primary and/or secondary amines. The present invention includes methods of using these compounds for the treatment and/or prevention of bacterial infection, HIV infection, and cancer and for the promotion of stem cell mobilization, wound healing, hematopoiesis, and skin rejuvenation.
摘要翻译：本发明提供具有结构X或结构XI的N-芳基或N-烷基胍和含双胍的化合物。这些化合物可以通过将各自的胍，双胍或苯胍基加成到含有伯胺和/或仲胺的多胺中来合成。本发明包括使用这些化合物治疗和/或预防细菌感染，HIV感染和癌症以及促进干细胞动员，伤口愈合，造血和皮肤年轻化的方法。

10. 发明申请

WO2011061272A2 A DI(4-CHLORO-PHENYLDIGUANIDO) DERIVATIVE WHICH IS FREE OF POTENTIAL GENOTOXICITY AND A PROCESS FOR REDUCING THE RESIDUAL AMOUNT OF P-CHLOROANILINE IN SAID DI(4-CHLORO-PHENYLDIGUANIDO) DERIVATIVE 审中-公开
标题翻译：一种不具有潜在的基因毒性的DI（4-氯 - 苯基二胍基）衍生物和一种降低所述二氯苯基二甲基锗衍生物中氯代苯胺残留量的方法
公开(公告)号：WO2011061272A2
公开(公告)日：2011-05-26
申请号：PCT/EP2010/067782
申请日：2010-11-18
申请人： MEDICHEM S.A. , SANCHEZ SALGUERO, Laura , BOU BOSCH, Raquel , BOSCH I LLADÓ, Jordi , CAMACHO CARRASCO, Antonio , DURAN LOPEZ, Ernesto , ANDRES MAGNANI, Pablo
发明人： SANCHEZ SALGUERO, Laura , BOU BOSCH, Raquel , BOSCH I LLADÓ, Jordi , CAMACHO CARRASCO, Antonio , DURAN LOPEZ, Ernesto , ANDRES MAGNANI, Pablo
IPC分类号： C07C279/18 , C07C277/08
CPC分类号： C07C279/265 , C07C277/08
摘要： The invention relates to a process for reducing the residual amount of p -chloroaniline in chlorhexidine. Also, the invention relates to a process for preparing chlorhexidine, or a pharmaceutically acceptable salt thereof, which is free of potential genotoxicity. In addition, the invention refers to the said chlorhexidine, or a pharmaceutically acceptable salt thereof, which is free of potential genotoxicity. Further, the invention relates to an analytical HPLC method for the determination of potentially genotoxic impurities in samples of chlorhexidine, or of a pharmaceutically acceptable salt thereof. The invention also relates to stabilized chlorhexidine digluconate salt free of potential genotoxicity in aqueous solution, and to a method for stabilizing chlorhexidine digluconate salt free of potential genotoxicity in aqueous solution.
摘要翻译：本发明涉及一种减少氯己定中对氯苯胺残留量的方法。而且，本发明涉及制备无潜在遗传毒性的氯己定或其药学上可接受的盐的方法。另外，本发明涉及所述没有潜在遗传毒性的氯己定或其药学上可接受的盐。此外，本发明涉及用于测定氯己定或其药学上可接受的盐样品中潜在遗传毒性杂质的分析HPLC方法。本发明还涉及在水溶液中无潜在遗传毒性的稳定的氯己定二葡糖酸盐，以及稳定在水溶液中无潜在遗传毒性的氯己定二葡糖酸盐的方法。

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