专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2014079497A1 METHOD FOR PREPARING PHENYLOXYMETHYL-NITRO-IMIDAZOLE DERIVATIVES AND USE OF SAME 审中-公开
标题翻译：制备苯基甲基 - 咪唑并咪唑衍生物的方法及其用途
公开(公告)号：WO2014079497A1
公开(公告)日：2014-05-30
申请号：PCT/EP2012/073321
申请日：2012-11-22
申请人： DRUGS FOR NEGLECTED DISEASES INITIATIVE (DNDI)
发明人： PARKANYI, Zsolt , ALATTYANI, Edit , BUGIR, Zoltan , HARSANYI, Marton
IPC分类号： C07D233/94
CPC分类号： C07D233/94
摘要： Fexinidazole is prepared according to a method which comprises the following steps: a) reacting 1-methyl-2-hydroxymethyl-5-nitro-imidazole with methanesulfonyl chloride in the presence of a suspension of powdered alkaline carbonate in an anhydrous organic solvent suitable for performing nucleophile substitution reactions; b) adding to the resulting reaction medium a solution of 4-methyl-mercapto-phenol in the same organic solvent as referred to in step a); c) separating fexinidazole from the reaction mixture as its hydrochloride salt and d) converting said hydrochloride salt into fexinidazole and optionally, purifying the latter.
摘要翻译：根据包括以下步骤的方法制备替硝唑：a）使1-甲基-2-羟甲基-5-硝基 - 咪唑与甲磺酰氯在碱性碳酸碱式粉末的存在下，在无水有机溶剂的存在下反应，亲核取代反应; b）向所得反应介质中加入4-甲基 - 巯基 - 苯酚在与步骤a）中相同的有机溶剂中的溶液; c）从反应混合物中分离出氟硝唑作为其盐酸盐，和d）将所述盐酸盐转化为替尼唑，并任选地将后者纯化。

2. 发明申请

WO2005041853A2 ANTIBACTERIAL AND/OR ANTIPROTOZOAL NITROIMIDAZOLE DERIVATIVE COMPOUNDS WITH UREASE INHIBITOR ACTIVITY, PROCESS FOR PREPARING THESE COMPOUNDS AND USE IN PHARMACEUTICAL COMPOSITIONS AND MEDICINES. 审中-公开
标题翻译：具有尿素抑制剂活性的抗真菌和/或抗真菌硝酸吲哚衍生物，制备这些化合物的方法和用于药物组合物和药物。
公开(公告)号：WO2005041853A2
公开(公告)日：2005-05-12
申请号：PCT/BR2004000210
申请日：2004-10-27
申请人： EMS SA , SILVA ANTONIO , MUNHOZ ANDRESSA , SANTOS JEAN , CAMARGO RODOLFO , CASTRO LUCIA , MENEGON RENATO , VILEGAS WAGNER , FERREIRA ANTONIO , VARANDA ELIANA , CHUNG MAN CHIN
发明人： SILVA ANTONIO , MUNHOZ ANDRESSA , SANTOS JEAN , CAMARGO RODOLFO , CASTRO LUCIA , MENEGON RENATO , VILEGAS WAGNER , FERREIRA ANTONIO , VARANDA ELIANA , CHUNG MAN CHIN
IPC分类号： A61K20060101 , A61K31/4164 , C07D233/94 , A61K
CPC分类号： C07D233/94
摘要： The present application describes nitroimidazolic derivative compounds with antibacterial and/or antiprotozoal activity, which are potent urease inhibitors. It also describes the process for preparing those compounds and their use in pharmaceutical compositions and medicines.
摘要翻译：本申请描述了具有抗细菌和/或抗原虫活性的硝基咪唑衍生物化合物，其是有效的脲酶抑制剂。它还描述了制备这些化合物的方法及其在药物组合物和药物中的应用。

3. 发明申请

WO2004012648A2 SUBSTITUIERTE DIARYLHETEROCYCLEN, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL 审中-公开
标题翻译：取代DIARYLHETEROCYCLEN，其制造方法相同，它们作为药物
公开(公告)号：WO2004012648A2
公开(公告)日：2004-02-12
申请号：PCT/EP2003/007639
申请日：2003-07-15
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH
发明人： SCHWINK, Lothar , STENGELIS, Siegfried , GOSSEL, Matthias , BOEHME, Thomas , HESSLER, Gerhard , ROSSE, Gerard , WALSER, Armin
IPC分类号： A61K
CPC分类号： C07D233/92 , C07D209/02 , C07D233/32 , C07D233/70 , C07D233/74 , C07D233/94 , C07D243/04 , C07D249/12 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D487/08 , C07D491/10
摘要： Die Erfindung betrifft substituierte Diarylheterocyclen sowie deren physiologisch verträgliche Salze und physiologisch funktionelle Derivate. Es werden Verbindungen der Formel I, worin die Reste die angegebenen Bedeutungen haben, sowie deren physiologisch verträglichen Salze und Verfahren zu deren Herstellung beschrieben. Die Verbindungen eignen sich z.B. als Anorektika.
摘要翻译：本发明涉及取代的Diarylheterocyclen及其生理学上可接受的盐和生理学功能衍生物。是式I，其中的基团具有所述的含义的化合物，和描述它们的生理学可接受的盐和它们的制备方法。的化合物是合适的，例如，是作为食欲抑制剂。

4. 发明申请

WO2012166778A3 CONJUGATES OF NITROIMIDAZOLES AND THEIR USE AS CHEMOTHERAPEUTIC AGENTS 审中-公开
标题翻译：硝基咪唑的结合及其作为化学治疗剂的使用
公开(公告)号：WO2012166778A3
公开(公告)日：2013-03-14
申请号：PCT/US2012039959
申请日：2012-05-30
申请人： UNIV JOHNS HOPKINS , NAT UNIV TSING HUA , HUANG RU CHIH C , MOLD DAVID EDWARD , HWU JIH RU , HSU MING HUA , WU SZU CHUN
发明人： HUANG RU CHIH C , MOLD DAVID EDWARD , HWU JIH RU , HSU MING HUA , WU SZU CHUN
IPC分类号： C07D233/60 , A61K31/4164 , A61P35/00
CPC分类号： A61K31/4164 , A61K45/06 , C07D233/60 , C07D233/91 , C07D233/94
摘要： Novel compounds which are derivatives of tetra-O-methyl nordihydroguaiaretic acid (NDGA), as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof are provided. These NDGA derivatives have a nitroimidazole moiety and these derivatives show preferential toxicity to hypoxic cells as hypoxic cytotoxins. Their cytotoxicity toward hypoxic cells is a result of abstraction of hydrogen from target molecules by free radicals formed in the reduction of the nitro group. This makes the disclosed compounds an effective anti cancer drug because hypoxic cells are generally considered to be more resistant to anti cancer drugs than normal cells. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including hepatocellular carcinoma, breast cancer and prostate cancer, are also provided.
摘要翻译：提供作为四-O-甲基诺二氢愈创木酸（NDGA）的衍生物的新型化合物，以及其药学上可接受的盐，溶剂合物和立体异构体。这些NDGA衍生物具有硝基咪唑部分，并且这些衍生物对缺氧细胞作为缺氧细胞毒素显示优先毒性。它们对缺氧细胞的细胞毒性是通过在还原硝基中形成的自由基从靶分子中抽出氢的结果。这使得所公开的化合物成为有效的抗癌药物，因为低氧细胞通常被认为比正常细胞更耐抗癌药物。还提供了包含这些化合物的药物组合物，以及使用方法和治疗癌症，包括肝细胞癌，乳腺癌和前列腺癌。

5. 发明申请

WO2012166778A2 CONJUGATES OF NITROIMIDAZOLES AND THEIR USE AS CHEMOTHERAPEUTIC AGENTS 审中-公开
标题翻译：硝基咪唑的结合及其作为化学治疗剂的使用
公开(公告)号：WO2012166778A2
公开(公告)日：2012-12-06
申请号：PCT/US2012/039959
申请日：2012-05-30
申请人： THE JOHNS HOPKINS UNIVERSITY , NATIONAL TSING HUA UNIVERSITY , HUANG, Ru Chih C. , MOLD, David Edward , HWU, Jih Ru , HSU, Ming Hua , WU, Szu Chun
发明人： HUANG, Ru Chih C. , MOLD, David Edward , HWU, Jih Ru , HSU, Ming Hua , WU, Szu Chun
IPC分类号： C07D233/60 , A61K31/4164 , A61P35/00
CPC分类号： A61K31/4164 , A61K45/06 , C07D233/60 , C07D233/91 , C07D233/94
摘要： Novel compounds which are derivatives of tetra- O -methyl nordihydroguaiaretic acid (NDGA), as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof are provided. These NDGA derivatives have a nitroimidazole moiety and these derivatives show preferential toxicity to hypoxic cells as hypoxic cytotoxins. Their cytotoxicity toward hypoxic cells is a result of abstraction of hydrogen from target molecules by free radicals formed in the reduction of the nitro group. This makes the disclosed compounds an effective anti cancer drug because hypoxic cells are generally considered to be more resistant to anti cancer drugs than normal cells. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including hepatocellular carcinoma, breast cancer and prostate cancer, are also provided.
摘要翻译：提供作为四-O-甲基诺二氢愈创木酸（NDGA）的衍生物的新型化合物，以及其药学上可接受的盐，溶剂合物和立体异构体。这些NDGA衍生物具有硝基咪唑部分，并且这些衍生物对缺氧细胞作为缺氧细胞毒素显示优先毒性。它们对缺氧细胞的细胞毒性是通过在还原硝基中形成的自由基从靶分子中抽出氢的结果。这使得所公开的化合物成为有效的抗癌药物，因为低氧细胞通常被认为比正常细胞更耐抗癌药物。还提供了包含这些化合物的药物组合物，以及使用方法和治疗癌症，包括肝细胞癌，乳腺癌和前列腺癌。

6. 发明申请

WO2012046062A1 USE OF PRODRUGS TO AVOID GI MEDIATED ADVERSE EVENTS 审中-公开
标题翻译：使用产品避免GI介入的不良事件
公开(公告)号：WO2012046062A1
公开(公告)日：2012-04-12
申请号：PCT/GB2011/051911
申请日：2011-10-05
申请人： SHIRE, LLC , FRANKLIN, Richard , QUIBELL, Martin , TYSON, Robert , GOLDING, Bernard
发明人： FRANKLIN, Richard , QUIBELL, Martin , TYSON, Robert , GOLDING, Bernard
IPC分类号： A61K47/48 , A61P31/04 , A61P9/06 , A61P3/00 , A61P25/28 , A61P19/02 , A61P25/24 , A61P35/00 , A61P19/10 , A61P31/12 , A61P3/10
CPC分类号： C07F9/3873 , A61K47/542 , C07C233/46 , C07C233/54 , C07C279/26 , C07C2601/14 , C07D211/20 , C07D233/94 , C07D285/135 , C07D307/20 , C07D403/12 , C07D473/30 , C07D501/59
摘要： The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side–effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
摘要翻译：本发明涉及各种药物的前药和含有这些前药的药物组合物。还提供了用于使局部介导的（来自肠内腔）最小化与未发病药物相关的不良胃肠道事件和用上述前药增加血浆药物水平的维持的方法。因此，本发明涉及广泛多样的药物（阿片样物质除外）的前体药物使用以使其短暂失活，并因此降低在给予母体化合物后通常明显的局部介导的不良胃肠道（GI）副作用。此外，这样的前药可以赋予改善的药代动力学。

7. 发明申请

WO2009046804A1 IMIDAZOLDERIVATE 审中-公开
标题翻译：咪唑衍生物
公开(公告)号：WO2009046804A1
公开(公告)日：2009-04-16
申请号：PCT/EP2008/007367
申请日：2008-09-09
申请人： MERCK PATENT GMBH , SCHULTZ, Melanie , SCHIEMANN, Kai , BOTTON, Gérard , BLAUKAT, Andree , KOBER, Ingo
发明人： SCHULTZ, Melanie , SCHIEMANN, Kai , BOTTON, Gérard , BLAUKAT, Andree , KOBER, Ingo
IPC分类号： C07D233/94 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D417/12 , A61K31/4178
CPC分类号： C07D233/94 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D417/12
摘要： Verbindungen der Formel (I), worin R 1 , D, E, L, Q, X und q die in Anspruch 1 angegebenen Bedeutungen haben, können und zur Behandlung von Tumoren eingesetzt werden.
摘要翻译：式（I）化合物，其中R 1，D，E，L，Q，X和q具有权利要求1中给出的含义，并且可用于治疗肿瘤。

8. 发明申请

WO2007067727A2 METRONIDAZOLE COCRYSTALS AND IMIPRAMINE COCRYSTALS 审中-公开
标题翻译：甲磺酸盐和木糖醇
公开(公告)号：WO2007067727A2
公开(公告)日：2007-06-14
申请号：PCT/US2006046824
申请日：2006-12-08
申请人： SSCI INC , CHILDS SCOTT LAWRENCE
发明人： CHILDS SCOTT LAWRENCE
IPC分类号： A61K31/4166
CPC分类号： C07D233/94 , C07D223/28
摘要： Cocrystals of metronidazole are described herein. Such cocrystals are a cocrystal of metronidazole with gentisic acid and a cocrystal of metronidazole with gallic acid. Cocrystals of imipramine hydrochloride are also described. Such cocrystals are a cocrystal of imipramine hydrochloride with (+)-camphoric acid, a cocrystal of imipramine hydrochloride with fumaric acid, and a cocrystal of imipramine hydrochloride with 1-hydroxy-2-naphthoic acid.
摘要翻译：本文描述了甲硝唑的晶体。这种共晶体是甲硝唑与龙胆酸的共结晶体和甲硝唑与没食子酸的共结晶体。也描述了盐酸丙咪嗪的Cystystals。这种共晶体是盐酸丙咪嗪与（+） - 樟脑酸，盐酸丙咪嗪与富马酸的共结晶和盐酸丙咪嗪与1-羟基-2-萘甲酸的共结晶。

9. 发明申请

WO1991000858A1 PHARMACEUTICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：药物活性化合物
公开(公告)号：WO1991000858A1
公开(公告)日：1991-01-24
申请号：PCT/US1990003694
申请日：1990-07-06
申请人： SCHERING CORPORATION , GIRIJAVALLABHAN, Viyyoor, M. , GANGULY, Ashit, K. , PINTO, Patrick, A. , VERSACE, Richard, W.
发明人： SCHERING CORPORATION
IPC分类号： C07D233/60
CPC分类号： C07D213/30 , C07D213/70 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/70 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D249/08 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/088 , C07D307/20 , C07D401/06 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/32 , C07D473/34 , C07D487/04 , C07D493/04
摘要： The disclosed invention relates to compounds represented by the formula (I): Z-X-Q-Y-W, (II): Z-X-Q-Y-W'-Y-Q-X-Z and pharmaceutically acceptable salts thereof, wherein each Z is independently tertiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, or 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining member of the ring being at least one carbon, and optionally sulfur or oxygen; X and Y are each independently a bond, -O-, -S-, -SO2-, (a), (b), (c), (d), (e), (f), (g), (h) or -CH2-O-; each Q is independently a divalent substituted or unsubstituted, straight or branched chain lower alkanediyl, lower alkanediyl-cycloalkanediyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofurandiyl, loweralkanediyl-dihydrofurandiyl-loweralkanediyl, tetrahydrofurandiyl, tetrahydropyrandiyl, loweralkanediyl-tetrahydropyrandiyl-loweralkanediyl or, loweralkanediyl-tetrahydrofurandiyl-loweralkanediyl, wherein the substituents are one or more of hydroxy, ketalized adjacent hydroxys, epoxy, fluorine, chlorine, azide, or amino; W is a monovalent substituted or unsubstituted aryl group or a heterocyclic single or fused ring, at least one hetero atom of which is a nitrogen atom and the remaining ring atoms being at least one carbon and optionally sulfur or oxygen, with the proviso that W cannot be substituted or unsubstituted isoxazolyl, and with the further proviso that when Z is 2-chloro-4-methoxyphenyl, X is -O-, Q is C5-C7 alkanediyl and Y is a bond, W is not imidazolyl substituted at positions 2, 4 and 5 with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyloweralkyl, nitro, loweralkoxycarbonyl, lower alkyl and amino methylene; W' is divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.

10. 发明申请

WO2015198107A1 SYNTHESIS OF METRONIDAZOLE 审中-公开
标题翻译：甲硝唑的合成
公开(公告)号：WO2015198107A1
公开(公告)日：2015-12-30
申请号：PCT/IB2014/064597
申请日：2014-09-17
申请人： KIANY FARD, Taghi
发明人： KIANY FARD, Taghi , KIANIFARD, Toktam , SARVI, Iraj , KOWSAR, Kasra
IPC分类号： C07D233/94
CPC分类号： C07D233/94
摘要： The producers utilize costly and unique active ingredients to produce metronidazole synthesis which has to be imported from other countries; consequently the cost of its production rises greatly. Furthermore, this drug has side effect in the present methods of production. Overusing usual samples leads to kidney stone in the patient's body. The purpose of this invention is to remove the mentioned defects. Producing metronidazole using the new method does not require utilizing costly and unique active ingredients for the producer and production process can be done with a lower cost. In addition, its production using the new method has fewer side effects rather than the previous methods.
摘要翻译：生产者利用昂贵和独特的活性成分来生产必须从其他国家进口的甲硝唑合成; 其生产成本大幅上升。此外，该药物在目前的生产方法中具有副作用。过度使用通常的样品会导致患者体内的肾结石。本发明的目的是去除所述缺陷。使用新方法生产甲硝唑不需要为生产者使用昂贵且独特的活性成分，并且可以以较低的成本进行生产过程。此外，使用新方法的生产具有较少的副作用，而不是以前的方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式