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1. 发明申请

US20070154948A1 Novel antibacterial agents 审中-公开
公开(公告)号：US20070154948A1
公开(公告)日：2007-07-05
申请号：US11603286
申请日：2006-11-21
申请人： Burton Christensen , Edmund Moran , John Griffin , J. Judice , YongQi Mu , John Pace , Mathai Mammen , James Aggen
发明人： Burton Christensen , Edmund Moran , John Griffin , J. Judice , YongQi Mu , John Pace , Mathai Mammen , James Aggen
IPC分类号： A61K31/545 , A61K38/16 , A61K31/43 , C07D499/44 , C07D487/04
CPC分类号： C07D477/12 , C07D499/32 , C07D499/44 , C07D501/56
摘要： This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

2. 发明申请

US20070265242A1 Novel Carbapenem Compound 审中-公开
标题翻译：新型卡巴培南化合物
公开(公告)号：US20070265242A1
公开(公告)日：2007-11-15
申请号：US11661662
申请日：2005-09-01
申请人： Makoto Sunagawa , Akira Sasaki
发明人： Makoto Sunagawa , Akira Sasaki
IPC分类号： A61K31/397 , A61P31/04 , C07D205/12
CPC分类号： C07D477/12
摘要： A carbapenem compound represented by a following formula [1], wherein R1 is C1 to C3 alkyl or C1 to C3 alkyl substituted by hydroxy. R is hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body, A is a following formula [1a], wherein E is a 5 to 7 membered cyclic ring optionally containing 1 to 3 hetero atoms (excluding benzene ring) which forms a bicyclic ring in corporation with the benzene ring, Y is hydrogen atom, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethoxy, halogen atom or cyano group, or its pharmaceutically acceptable salt.
摘要翻译：由下式[1]表示的碳青霉烯化合物，其中R 1是C 1〜C 3烷基或C 1〜被羟基取代的C 3〜C 3烷基。 R是氢原子或在活体中通过水解再生羧基的基团，A是下式[1a]，其中E是任选含有1〜3个杂原子（苯环除外）的5〜7元环，其与苯环形成双环，Y为氢原子，C 1至C 4烷基，C 1至C 4烷基，三氟甲氧基，卤素原子或氰基，或其药学上可接受的盐。

3. 发明授权

US09840506B2 Crystal of doripenem, and preparation method therefor 有权
公开(公告)号：US09840506B2
公开(公告)日：2017-12-12
申请号：US15307203
申请日：2015-04-15
申请人： JW PHARMACEUTICAL CORPORATION
发明人： Do-Kyu Pyun , Kyoung-Jin O , Sang-A Lee , Ji-Hyun Jung
IPC分类号： C07D477/20 , C07D477/10 , C07D477/12
CPC分类号： C07D477/20 , C07B2200/13 , C07D477/10 , C07D477/12
摘要： This invention relates to a novel doripenem crystal, a solvate thereof, and a preparation method thereof and, more specifically, to a novel doripenem anhydride crystal, a method of preparing the doripenem anhydride crystal using various solvents, and a solvate of doripenem.

4. 发明申请

US20070196859A1 Novel antibacterial agents 审中-公开
标题翻译：新型抗菌剂
公开(公告)号：US20070196859A1
公开(公告)日：2007-08-23
申请号：US11603329
申请日：2006-11-21
申请人： Burton Christensen , Edmund Moran , John Griffin , J. Judice , YongQi Mu , John Pace , Mathai Mammen , James Aggen
发明人： Burton Christensen , Edmund Moran , John Griffin , J. Judice , YongQi Mu , John Pace , Mathai Mammen , James Aggen
IPC分类号： A61K38/14 , A61K31/43 , A61K31/545 , A61K31/407
CPC分类号： C07D477/12 , C07D499/32 , C07D499/44 , C07D501/56
摘要： This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked ) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, penicillinase enzyme, cephalosporinase enzyme, a transglycosylase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
摘要翻译：本发明涉及作为抗菌剂的新型多结合化合物（试剂）。本发明的多相结合化合物包含2-10个配体，其通过连接体或连接体共价连接，其中所述各单体（即，未连接）状态的所述配体具有结合涉及细胞壁生物合成和代谢的酶的能力用于合成细菌细胞壁和/或细菌细胞表面的前体因而干扰细胞壁的合成和/或代谢。特别地，本发明的多相结合化合物包含通过接头或接头共价连接的2-10个配体，其中每个所述配体具有能够结合青霉素结合蛋白的配体结构域，转肽酶，转肽酶的底物， β-内酰胺酶，青霉素酶，头孢菌素酶，转糖基酶或转糖基酶酶底物; 优选地，配体选自β-内酰胺或糖肽类抗菌剂。

5. 发明申请

US20170050969A1 NOVEL CRYSTAL OF DORIPENEM, AND PREPARATION METHOD THEREFOR 有权
标题翻译：多伦多的新水晶及其制备方法
公开(公告)号：US20170050969A1
公开(公告)日：2017-02-23
申请号：US15307203
申请日：2015-04-15
申请人： JW PHARMACEUTICAL CORPORATION
发明人： DO-KYU PYUN , KYOUNG-JIN O , SANG-A LEE , JI-HYUN JUNG
IPC分类号： C07D477/20
CPC分类号： C07D477/20 , C07B2200/13 , C07D477/10 , C07D477/12
摘要： This invention relates to a novel doripenem crystal, a solvate thereof, and a preparation method thereof and, more specifically, to a novel doripenem anhydride crystal, a method of preparing the doripenem anhydride crystal using various solvents, and a solvate of doripenem.
摘要翻译：本发明涉及一种新的多巴培南晶体及其溶剂化物及其制备方法，更具体地说，涉及一种新的多巴培南酐晶体，使用各种溶剂制备多巴培南酐晶体的方法和多里必敏的溶剂合物。

6. 发明申请

US20090111737A1 Novel antibacterial agents 审中-公开
标题翻译：新型抗菌剂
公开(公告)号：US20090111737A1
公开(公告)日：2009-04-30
申请号：US12082666
申请日：2008-04-11
申请人： Burton G. Christensen , Edmund J. Moran , John H. Griffin , J. Kevin Judice , YongQi Mu , John L. Pace , Mathai Mammen , James Aggen
发明人： Burton G. Christensen , Edmund J. Moran , John H. Griffin , J. Kevin Judice , YongQi Mu , John L. Pace , Mathai Mammen , James Aggen
IPC分类号： A61K38/14 , C07K7/00 , A61P43/00
CPC分类号： C07D477/12 , C07D499/32 , C07D499/44 , C07D501/56
摘要： This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
摘要翻译：本发明涉及作为抗菌剂的新型多结合化合物（试剂）。本发明的多相结合化合物包含2-10个配体，其通过连接体或连接体共价连接，其中所述各单体（即，未连接）状态的所述配体具有结合涉及细胞壁生物合成和代谢的酶的能力用于合成细菌细胞壁和/或细菌细胞表面的前体因而干扰细胞壁的合成和/或代谢。特别地，本发明的多相结合化合物包含通过接头或接头共价连接的2-10个配体，其中每个所述配体具有能够结合青霉素结合蛋白的配体结构域，转肽酶，转肽酶的底物， β-内酰胺酶，pencillinase酶，头孢菌素酶，转糖基酶或转糖基酶酶底物; 优选地，配体选自β-内酰胺或糖肽类抗菌剂。

7. 发明授权

US5703017A 3-(Het) arylcarboxylic acid derivatives, their preparation and intermediates for their preparation 失效
标题翻译： 3-（Het）芳基羧酸衍生物，其制备方法及其制备中间体
公开(公告)号：US5703017A
公开(公告)日：1997-12-30
申请号：US537843
申请日：1995-10-19
申请人： Ernst Baumann , Joachim Rheinheimer , Uwe Josef Vogelbacher , Matthias Bratz , Hans Theobald , Matthias Gerber , Karl-Otto Westphalen , Helmut Walter , Wilhelm Rademacher
发明人： Ernst Baumann , Joachim Rheinheimer , Uwe Josef Vogelbacher , Matthias Bratz , Hans Theobald , Matthias Gerber , Karl-Otto Westphalen , Helmut Walter , Wilhelm Rademacher
IPC分类号： C07D251/22 , A01N43/54 , A01N43/64 , A01N43/72 , A01P13/00 , A01P21/00 , C07C45/58 , C07C47/198 , C07C47/277 , C07C59/125 , C07C67/31 , C07C69/708 , C07C69/734 , C07C205/28 , C07C323/22 , C07C323/50 , C07D239/26 , C07D239/30 , C07D239/34 , C07D239/38 , C07D239/60 , C07D251/24 , C07D251/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D411/12 , C07D413/12 , C07D477/12 , C07D491/048 , A01N43/66 , C07D251/30
CPC分类号： C07D401/12 , A01N43/54 , C07C69/708 , C07C69/734 , C07D239/60 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D477/12
摘要： 3-(Het)arylcarboxylic acid derivatives of the formula I ##STR1## where R is formyl, CO.sub.2 H or a radical hydrolyzable to COOH and the other substituents have the following meanings: R.sup.2 and R.sup.3 are each halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; X is nitrogen or CR.sup.14, where R.sup.14 is hydrogen or, together with R.sup.3, forms an alkylene or alkenylene chain, in each of which a methylene group is replaced by oxygen; R.sup.4 is phenyl or naphthyl, each of which is unsubstituted or substituted or an unsubstituted or substituted five-membered or six-membered heteroaromatic structure containing one to three nitrogen atoms or one sulfur or oxygen atom; R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, alkoxyalkyl, alkylthioalkyl or phenyl; R.sup.6 is C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or C.sub.3 -C.sub.4 -cyclo-alkyl, each of which may be mono- or polysubstituted; Y is sulfur, oxygen or a single bond; and Z is sulfur or oxygen; with the proviso that R.sup.6 is not unsubstituted C.sub.1 -C.sub.4 -alkyl when R.sup.4 is unsubstituted phenyl, Z is oxygen and simultaneously R.sup.5 is methyl or hydrogen.
摘要翻译： PCT No.PCT / EP94 / 01141 Sec。 371 1995年10月19日日期 102（e）1995年10月19日PCT PCT 1994年4月13日PCT公布。公开号WO94 / 25442 日期：1943年11月10日 - （Het）式I的芳基羧酸衍生物其中R是甲酰基，CO 2 H或可水解成COOH的基团，其它取代基具有以下含义：R 2和R 3各自为卤素，烷基，卤代烷基，烷氧基，卤代烷氧基或烷硫基; X是氮或CR14，其中R14是氢或与R3一起形成亚烷基或亚烯基链，其中每个亚甲基被氧代替; R4是苯基或萘基，其各自为未取代或取代的，或未取代或取代的含有1-3个氮原子或一个硫或氧原子的五元或六元杂芳族结构; R5是氢，烷基，烯基，炔基，环烷基，卤代烷基，烷氧基烷基，烷硫基烷基或苯基; R6是C1-C8-烷基，C3-C6-烯基，C3-C6-炔基或C3-C4-环烷基，其中每一个可以是单取代或多取代的; Y是硫，氧或单键; Z为硫或氧; 条件是当R 4为未取代的苯基时，R 6为未取代的C 1 -C 4 - 烷基，Z为氧，同时R 5为甲基或氢。

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