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。

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.

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.

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。

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。

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。

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。