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1. 发明申请

WO1996004247A1 PROCESS FOR MAKING ANTIMICROBIAL COMPOUNDS 审中-公开
标题翻译：制备抗微生物化合物的方法
公开(公告)号：WO1996004247A1
公开(公告)日：1996-02-15
申请号：PCT/US1995009647
申请日：1995-08-01
申请人： THE PROCTER & GAMBLE COMPANY
发明人： THE PROCTER & GAMBLE COMPANY , RANDALL, Jared, Lynn , GODLEWSKI, Jane, Ellen
IPC分类号： C07D215/56
CPC分类号： C07D501/00 , C07D463/12 , C07D463/20 , C07D463/22
摘要： The present invention provides a process for making a compound having a structure according to formula (I) wherein A , A and A are independently carbon or nitrogen and R , R , R and R are known quinolone substituents; and wherein one of R , R or R may be a lactam-containing moiety; or a protected form, salt, pharmaceutically-acceptable salt, biohydrolyzable ester, or solvate thereof; the process comprising reacting one or more organosilicon compounds with a compound having a structure according to formula (II), wherein A , A and A , R , R , R and R as described above; wherein one of R , R or R may be a lactam-containing moiety; and X is a leaving group; or a protected form, salt, biohydrolyzable ester, or solvate thereof. The compounds prepared according to the processes of the invention are themselves useful as antimicrobials, or they may be used as intermediates for making other quinolone-containing antimicrobials.
摘要翻译：本发明提供了制备具有式（I）结构的化合物的方法，其中A 1，A 2和A 3独立地为碳或氮，R 1，R 3， R 4和R 6是已知的喹诺酮取代基; 并且其中R 1，R 3或R 6中的一个可以是含内酰胺的部分; 或其保护形式，盐，药学上可接受的盐，生物可水解酯或其溶剂化物; 该方法包括使一种或多种有机硅化合物与具有式（II）结构的化合物反应，其中A 1，A 2和A 3，R 1，R 3，R 3， 4>和R 6; 其中R 1，R 3或R 6之一可以是含内酰胺的部分; X为离去群; 或被保护的形式，盐，生物可水解酯或其溶剂合物。根据本发明方法制备的化合物本身可用作抗微生物剂，或者它们可以用作制备其它含喹诺酮的抗微生物剂的中间体。

2. 发明申请

WO2016027262A1 ANTIBACTERIAL SIDEROMYCINS 审中-公开
标题翻译：抗生素治疗
公开(公告)号：WO2016027262A1
公开(公告)日：2016-02-25
申请号：PCT/IB2015/056915
申请日：2015-09-10
申请人： MILLER, Marvin J. , LIN, Yun-ming , GHOSH, Manuka , MILLER, Patricia A. , MÖLLMANN, Ute
发明人： MILLER, Marvin J. , LIN, Yun-ming , GHOSH, Manuka , MILLER, Patricia A. , MÖLLMANN, Ute
IPC分类号： A61K47/48 , A61K31/404 , A61K31/43 , A61K31/435 , A61K31/427 , A61K31/542 , A61K31/295 , C07D209/18 , C07D499/68 , C07D463/20 , C07D417/12 , C07D501/59 , C07C235/60 , C07F15/03 , A61P31/04
CPC分类号： C07F15/03 , A61K31/424 , A61K31/43 , A61K31/431 , A61K45/06 , A61K47/547 , C07C235/60 , C07D209/18 , C07D417/12 , C07D463/22 , C07D499/78 , C07D501/59 , A61K2300/00
摘要： A compound, comprising: an Fe(III)-binding and/or Fe(III)-bound siderophore; one or more optional linker covalently bound to the siderophore; and daptomycin covalently bound to the linker, or, if no linker is present, then to the siderophore; or pharmaceutically acceptable salt or solvate thereof.
摘要翻译：一种化合物，包括：Fe（III）结合和/或Fe（III）键合的铁载体; 与铁载体共价结合的一个或多个任选的接头; 共同结合到连接体上的达托霉素，或者如果不存在连接体，则到载体载体上; 或其药学上可接受的盐或溶剂化物。

3. 发明申请

WO2010123997A1 CARBACEPHEM BETA-LACTAM ANTIBIOTICS 审中-公开
标题翻译： CARBACEPHEM BETA-LACTAM抗生素
公开(公告)号：WO2010123997A1
公开(公告)日：2010-10-28
申请号：PCT/US2010/031904
申请日：2010-04-21
申请人： ACHAOGEN, INC. , MOSER, Heinz, E. , WAGMAN, Allan, S.
发明人： MOSER, Heinz, E. , WAGMAN, Allan, S.
IPC分类号： C07D463/22 , A61K31/437 , A61P31/04
CPC分类号： C07D463/22
摘要： Carbacephem β-lactam antibiotics having chemical structures (I) and (II) are disclosed: including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar 2 , R 1 , R 2 and R 6 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
摘要翻译：具有化学结构（I）和（II）的碳水化合物β-内酰胺抗生素被公开：包括立体异构体，其药学上可接受的盐，酯和前药，其中Ar 2，R 1，R 2和R 6如本文所定义。这些化合物可用于治疗细菌感染，特别是由耐甲氧西林葡萄球菌引起的细菌感染。

4. 发明申请

WO00032605A1 BI-PYRROLIDINYLVINL (CARBA) CEPHALOSPORINS 审中-公开
标题翻译：二吡咯烷酮（CARBA）CEPHALOSPORINS
公开(公告)号：WO00032605A1
公开(公告)日：2000-06-08
申请号：PCT/EP1999/009120
申请日：1999-11-25
IPC分类号： A61P31/00 , C07D463/00 , C07D501/00 , C07D501/52 , C07D501/56 , A61K31/545
CPC分类号： C07D501/00 , C07D463/22
摘要： The present invention relates to cephalosporin derivatives of general formula (I), wherein R is R -Ys-(CR R )m- or (formula a) R , R are each independently hydrogen or lower alkyl; R is hydrogen, hydroxy-lower alkyl or carbamoylmethyl; Z is phenylene, heterocyclylen or naphthylene; R is halogen, phenyl, benzyl, naphthyl or heterocyclyl, the phenyl, benzyl, naphthyl or heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, lower alkoxy, amino, lower alkylamino, di-lower alkylamino, carboxy, lower alkoxycarbonyl or carbamoyl; Q is S or CH2; Y is S, O, NH or CH2; M is 0 or 1; s is 0 or 1; R , R are each independently hydrogen or lower alkyl; X is CR or N; R is hydrogen, lower alkyl, lower cycloalkyl, formyl, acetyl or pivaloyl; R is hydrogen or halogen; and readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula (I) and of their esters and salts. The invention is further concerned with the manufacture of compounds of formula (I); with their use as pharmaceutically active substances, particularly for the treatment and prophylaxis of infectious diseases, and with pharmaceutical preparations containing a compound of formula (I) for the treatment and prophylaxis of infectious diseases.
摘要翻译：本发明涉及通式（I）的头孢菌素衍生物，其中R是R 4 -Y-（CR 5 R 6）m - 或（式a）R 1，R 2，各自独立地为氢或低级烷基; R 3是氢，羟基 - 低级烷基或氨基甲酰基甲基; Z是亚苯基，亚杂环基或亚萘基; R 4为卤素，苯基，苄基，萘基或杂环基，苯基，苄基，萘基或杂环基任选被至少一个卤素，羟基，任选取代的低级烷基，低级烷氧基，氨基，低级烷基氨基，低级烷基氨基，羧基，低级烷氧基羰基或氨基甲酰基; Q是S或CH2; Y是S，O，NH或CH 2; M为0或1; s为0或1; R 5，R 6各自独立地为氢或低级烷基; X是CR 8或N; R 7是氢，低级烷基，低级环烷基，甲酰基，乙酰基或新戊酰基; R 8是氢或卤素; 和其易水解的酯，所述化合物的药学上可接受的盐和式（I）化合物的水合物及其酯和盐。本发明还涉及式（I）化合物的制备; 其用作药物活性物质，特别是用于治疗和预防感染性疾病，以及含有式（I）化合物的药物制剂用于治疗和预防感染性疾病。

5. 发明申请

WO1985005620A1 CEPHEM COMPOUNDS 审中-公开
标题翻译： CEPHEM化合物
公开(公告)号：WO1985005620A1
公开(公告)日：1985-12-19
申请号：PCT/JP1984000270
申请日：1984-05-25
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD. , MIYAKE, Akio , KONDO, Masahiro , FUJINO, Masahiko
IPC分类号： C07D519/00
CPC分类号： C07D277/587 , C07D463/22 , C07D471/04 , C07D505/00
摘要： Novel cephem compounds of the general formula (I), wherein R1 represents an optionally protected amino group, R2 represents a hydrogen atom or a halogen atom, R3 represents a hydrogen atom or an optionally substituted hydrocarbon residue, R4 represents a hydrogen atom or a methoxy group, A represents an optionally substituted imidazol-1-yl group forming a fused ring at positions 2 and 3 or 3 and 4, and n represents 0 or 1. They have an excellent antibacterial activity.
摘要翻译：通式（I）的新型头孢烯化合物，其中R 1表示任选保护的氨基，R 2表示氢原子或卤素原子，R 3表示氢原子或任选取代的烃基，R 4表示氢原子或甲氧基基团，A表示任选取代的咪唑-1-基，其在位置2和3或3和4上形成稠环，n表示0或1.它们具有优异的抗菌活性。

6. 发明申请

WO1985004878A1 BETA-LACTAM DERIVATIVES, PREPARATION, COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： BETA-LACTAM衍生物，制备，它们的组合物
公开(公告)号：WO1985004878A1
公开(公告)日：1985-11-07
申请号：PCT/GB1985000161
申请日：1985-04-12
申请人： BEECHAM GROUP P.L.C. , TAYLOR, Andrew, William , COOK, Richard, Thomas
发明人： BEECHAM GROUP P.L.C.
IPC分类号： C07D499/68
CPC分类号： C07D499/00 , C07D231/20 , C07D463/22 , C07D505/00
摘要： Compounds of general formula (I), their pharmaceutically acceptable salts and in-vivo hydrolysable esters are antibacterial agents; in which R is optionally substituted phenyl or optionally substituted 5 or 6-membered heterocyclyl; R is substituted amino; R is H or alkyl; R is H, CH3 or CH3COO; R is H, -OCH3 or -NHCO; Y is in formula (II), Y is -O-, -S-, or -CH2-; and Z is H, halogen or organic.
摘要翻译：通式（I）的化合物，其药学上可接受的盐和体内可水解的酯是抗菌剂; 其中R 1是任选取代的苯基或任选取代的5或6元杂环基; R 2是取代的氨基; R 3是H或烷基; R 4是H，CH 3或CH 3 COO; R 5是H，-OCH 3或-NHCO; Y在式（II）中，Y 1是-O-，-S-或-CH 2 - ; Z为H，卤素或有机基。

7. 发明申请

WO2010030810A1 CARBACEPHEM BETA-LACTAM ANTIBIOTICS 审中-公开
标题翻译： CARBACEPHEM BETA-LACTAM抗生素
公开(公告)号：WO2010030810A1
公开(公告)日：2010-03-18
申请号：PCT/US2009/056554
申请日：2009-09-10
申请人： ACHAOGEN, INC. , WAGMAN, Allan, Scott , MOSER, Heinz, Ernst
发明人： WAGMAN, Allan, Scott , MOSER, Heinz, Ernst
IPC分类号： C07D463/22 , A61K31/4353 , A61P31/04
CPC分类号： C07D463/22
摘要： Carbacephem β-lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar 2 , X, R 1 and R 2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
摘要翻译：公开了具有结构（I）的碳纤维β-内酰胺抗生素，包括立体异构体，其药学上可接受的盐，酯和前药，其中Ar 2，X，R 1和R 2如本文所定义。这些化合物可用于治疗细菌感染，特别是由耐甲氧西林葡萄球菌引起的细菌感染。

8. 发明申请

WO2004037163A3 STERICALLY-AWKWARD beta-LACTAMASE INHIBITORS 审中-公开
标题翻译： STERICALLY-AWKWARDβ-LACTAMASE抑制剂
公开(公告)号：WO2004037163A3
公开(公告)日：2005-02-24
申请号：PCT/US0315140
申请日：2003-05-14
申请人： UNIV NORTHWESTERN
发明人： SHOICHET BRIAN K , BLASZCZAK LARRY C
IPC分类号： A61K31/397 , A61K31/43 , A61P31/04 , C07D463/00 , C07D463/22 , C07D499/00 , C07D499/64 , C07D499/70 , C07D499/80 , C07D501/14 , A61K31/431 , A61K31/4353
CPC分类号： C07D499/00 , A61K31/397 , A61K31/43 , C07D463/22
摘要： 6(7)-beta-substituted beta-lactam compounds as inhibitors of beta-lactamase activity.
摘要翻译： 6（7）β-取代的β-内酰胺化合物作为β-内酰胺酶活性的抑制剂。

9. 发明申请

WO2004046142A1 MONOHYDRATE SOLVATES OF LORACARBEF 审中-公开
标题翻译：单硫酸氢钠溶液
公开(公告)号：WO2004046142A1
公开(公告)日：2004-06-03
申请号：PCT/IB2003/005331
申请日：2003-11-21
申请人： RANBAXY LABORATORIES LIMITED , KUMAR, Yatendra , TEWARI, Neera , MEERAN, Hashim, Nizar, Poovanathi, Nagoor , RAI, Bishwa, Prakash , SINGH, Shailendra, Kumar
发明人： KUMAR, Yatendra , TEWARI, Neera , MEERAN, Hashim, Nizar, Poovanathi, Nagoor , RAI, Bishwa, Prakash , SINGH, Shailendra, Kumar
IPC分类号： C07D463/00
CPC分类号： C07D463/22
摘要： This invention relates to monohydrate solvates of loracarbef. The invention also relates to processes for preparing solvates of loracarbef, crystalline monohydrate of loracarbef from said solvates and pharmaceutical compositions that include the crystalline monohydrate of loracarbef.
摘要翻译：本发明涉及劳拉卡贝的一水合物溶剂化物。本发明还涉及从所述溶剂化物制备劳拉卡品溶液的溶剂化物，劳拉卡的结晶一水合物的方法以及包括劳拉卡氏菌的一水合物的药物组合物。

10. 发明申请

WO1995026966A1 CEPHALOSPORIN ANTIBIOTICS 审中-公开
标题翻译： CEPHALOSPORIN抗生素
公开(公告)号：WO1995026966A1
公开(公告)日：1995-10-12
申请号：PCT/US1995003976
申请日：1995-03-29
申请人： MICROCIDE PHARMACEUTICALS, INC.
发明人： MICROCIDE PHARMACEUTICALS, INC. , CHRISTENSEN, Burton, G. , CHO, In-Seop , GLINKA, Tomasz, W. , HECKER, Scott, J. , LEE, Ving, J. , ZHANG, Zhijia, J.
IPC分类号： C07D501/59
CPC分类号： C07D477/00 , C07D463/18 , C07D463/22 , C07D477/20 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to beta -lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.
摘要翻译：本发明包括新的（7R）-7-（酰基氨基）-3-（芳硫基）-3-头孢烯-4-羧酸或其药理学上可接受的盐，其对广谱生物体表现出抗生素活性，包括对 β-内酰胺抗生素，可用作抗菌剂。本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

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