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1. 发明授权

US5547978A Derivatives of pyrrolidin-2-ylcarbonylheterocyclic compounds 失效
标题翻译：吡咯烷-2-基羰基杂环化合物的衍生物
公开(公告)号：US5547978A
公开(公告)日：1996-08-20
申请号：US346240
申请日：1994-11-23
申请人： Burton G. Christensen , Takashi Egawa , Yasuyuki Ichimaru , Shokichi Ohuchi , Tsuneo Okonogi , Arthur A. Patchett , Seiji Shibahara , Seiji Tsutsumni
发明人： Burton G. Christensen , Takashi Egawa , Yasuyuki Ichimaru , Shokichi Ohuchi , Tsuneo Okonogi , Arthur A. Patchett , Seiji Shibahara , Seiji Tsutsumni
IPC分类号： A61K31/40 , A61K31/401 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/505 , A61P25/00 , A61P25/28 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04 , C07D207/06 , C07D209/08 , C07D277/06
CPC分类号： C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention relates to derivatives of pyrrolidin-2-ylcarbonylheterocyclic compound of the general formula ##STR1## in which R.sup.1 represents C.sub.1-6 alkyl, C.sub.1-20 cycloalkyl, aryl or heteroaryl,R.sup.2 represents a heterocyclic compound selected from the group consisting of 2-thiazole, 2-oxazole, 2-imidazole, 2-pyrrole, 2-thiophene, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 2-indole, 2-thiazolo[5,4-b]pyridine, 2-oxazolo[4,5-b]pyridine, 2-imidazo[4,5-b]pyridine, 5-thiazole, 2-thiazoline, 2-pyridine, 3-pyridine, 5-pyrimidine, 2-pyrazine, 2-triazole or 2-pyrazole wherein the heterocyclic compound may be unsubstituted or substituted independently with R.sup.4 or R.sup.5 wherein R.sup.4 and R.sup.5 are H, C.sub.1-5 alkyl, aryl or R.sup.4 and R.sup.5 may be ortho substituents on the heterocyclic compounds and connected to form an aryl or heteroaryl ring,A represents a cyclic amino acid, X is oxygen atom, thiomethlene or methylene residue, m is an integer from 1 to 5, to a process for the preparation thereof, to composition containing them, and to the use thereof.
摘要翻译：本发明涉及通式“IMAGE”的吡咯烷-2-基羰基杂环化合物的衍生物，其中R 1表示C 1-6烷基，C 1-20的环烷基，芳基或杂芳基，R 2表示选自下列的杂环化合物：2- 噻唑，2-恶唑，2-咪唑，2-吡咯，2-噻吩，2-苯并噻唑，2-苯并恶唑，2-苯并咪唑，2-吲哚，2-噻唑并[5,4-b]吡啶，2-恶唑并[ 4,5-b]吡啶，2-咪唑并[4,5-b]吡啶，5-噻唑，2-噻唑啉，2-吡啶，3-吡啶，5-嘧啶，2-吡嗪，2-三唑或2- 吡唑，其中杂环化合物可以是未取代的或独立地被R4或R5取代，其中R4和R5是H，C1-5烷基，芳基或R4和R5可以是杂环化合物上的邻位取代基并且连接形成芳基或杂芳基环， A表示环状氨基酸，X为氧原子，巯基或亚甲基残基，m为1〜5的整数，其制备方法为组合物cont 指导他们，以及使用它们。

2. 发明授权

US4534898A 1-Oxa-1-dethia-cephalosporin derivatives 失效
标题翻译： 1-氧杂-1-脱氢头孢菌素衍生物
公开(公告)号：US4534898A
公开(公告)日：1985-08-13
申请号：US515422
申请日：1983-07-20
申请人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Shunzo Fukatsu , Tadashi Wakazawa , Taro Niida , Burton G. Christensen
发明人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Shunzo Fukatsu , Tadashi Wakazawa , Taro Niida , Burton G. Christensen
IPC分类号： C07D498/04 , C07D205/085 , C07D403/12 , C07D505/00 , C07F9/568 , C07D419/14
CPC分类号： C07D403/12 , C07D205/085 , C07D505/00 , C07F9/5683
摘要： This invention relates to 1-oxa-1-dethia-cephalosporins which are useful as anti-biotics.
摘要翻译：本发明涉及可用作抗生物素的1-氧杂-1-脱氢头孢菌素。

3. 发明授权

US4645769A 1-oxa-1-dethia-cephalosporin compounds and antibacterial agent comprising the same 失效
标题翻译： 1-氧杂-1-脱氢头孢菌素化合物和含有它们的抗菌剂
公开(公告)号：US4645769A
公开(公告)日：1987-02-24
申请号：US705799
申请日：1985-03-01
申请人： Seiji Shibahara , Tsuneo Okonogy , Yasushi Murai , Shunzo Fukatsu , Taro Niida , Burton G. Christensen , Tadashi Wakazawa
发明人： Seiji Shibahara , Tsuneo Okonogy , Yasushi Murai , Shunzo Fukatsu , Taro Niida , Burton G. Christensen , Tadashi Wakazawa
IPC分类号： A61K31/535 , A61P31/04 , C07D498/04 , C07D505/00 , A01N43/90
CPC分类号： C07D505/00
摘要： The subject invention includes a 1-oxa-1-dethia-cephalosporin compound represented by the general formula (1) ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## where R.sup.5 is a methyl group, an ethyl group, a carboxymethyl group or a 2-carboxy isopropyl group, or R.sup.1 is a group of the formula: ##STR3## where R.sup.6 is a hydrogen atom, a 4-ethyl-2,3-dioxopiperazine-1-yl group, a 3,4-dihydroxy phenyl group or a 5- and 6-membered heterocyclic radical having 2 ring nitrogens as the sole hetero substituent in the ring and having at least one hetero group on the carbon adjacent to the ring nitrogens.
摘要翻译：本发明包括由通式（1）表示的1-氧杂-1-脱氧头孢菌素化合物，其中R1是下式的基团：其中R5是甲基，乙基基团，羧甲基或2-羧基异丙基，或R 1是下式的基团：其中R 6是氢原子，4-乙基-2,3-二氧代哌嗪-1-基，3 具有2个环氮原子的5元和6元杂环基作为环中唯一的杂取代基，并且在与环氮相邻的碳上具有至少一个杂基。

4. 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。

5. 发明授权

US5789584A Substituted-pyridinyl cephalosporin antibiotics active against methicillin resistant bacteria 失效
标题翻译：取代的吡啶基头孢菌素抗生素对抗甲氧西林抗性细菌有活性
公开(公告)号：US5789584A
公开(公告)日：1998-08-04
申请号：US415064
申请日：1995-03-29
申请人： Burton G. Christensen , In-Seop Cho , Tomasz W. Glinka , Scott J. Hecker
发明人： Burton G. Christensen , In-Seop Cho , Tomasz W. Glinka , Scott J. Hecker
IPC分类号： A61K31/545 , A61K31/546 , C07D463/00 , C07D477/00 , C07D477/20 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/59 , C07D503/00 , C07D505/00 , C07D513/04 , C07D501/36
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 (7R)-7-(acylamino)-3-(substituted-pyridinyl)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against methicillin-resistant bacteria and are therefore useful as antibacterial agents.
摘要翻译：本发明包括（7R）-7-（酰基氨基）-3-（取代的 - 吡啶基）-3-头孢烯-4-羧酸或其对耐甲氧西林细菌具有抗生素活性的药理学上可接受的盐，因此可用作抗菌剂代理商

6. 发明授权

US5593986A Cephalosporin antibiotics 失效
公开(公告)号：US5593986A
公开(公告)日：1997-01-14
申请号：US415069
申请日：1995-03-29
申请人： Burton G. Christensen , In-Seop Cho , Tomasz W. Glinka , Scott J. Hecker
发明人： Burton G. Christensen , In-Seop Cho , Tomasz W. Glinka , Scott J. Hecker
IPC分类号： A61K31/545 , A61K31/546 , C07D463/00 , C07D477/00 , C07D477/20 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/59 , C07D503/00 , C07D505/00 , C07D513/04 , C07D501/60
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.

7. 发明授权

US4994568A 6- and 4-substituted-1-azabicyclo(3.2.0)heptan-3, 7-dione-2-carboxylates 失效
标题翻译： 6-和4-取代-1-氮杂双环（3.2.0）庚-3,7-二酮-2-羧酸酯
公开(公告)号：US4994568A
公开(公告)日：1991-02-19
申请号：US481715
申请日：1990-02-15
申请人： Burton G. Christensen
发明人： Burton G. Christensen
IPC分类号： C07C1/30 , C07C17/275 , C07C29/147 , C07D205/08 , C07D477/18 , C07F7/10
CPC分类号： C07F7/10 , C07C1/30 , C07C17/275 , C07C29/147 , C07D205/08 , C07D477/18 , Y02P20/55
摘要： Disclosed are 6- and 4-substituted-1-azabicyclo[3.2.0]heptan-3,7-dione-2-carboxylic acid esters and salts (I) which are useful in the preparation of 6-, 1- and 2-substituted carbapenem antibiotics. ##STR1## wherein R.sup.5 is a pharmaceutically acceptable ester moiety or a removable protecting group or an alkali or alkaline earth metal cation such as sodium or potassium and wherein R.sup.1, R.sup.2, Rhu 3 and R.sup.4 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl and aralkyl. Another embodiment disclosed is a group of compounds having the formula ##STR2## where X is a leaving group.
摘要翻译：公开了6-和4-取代-1-氮杂双环[3.2.0]庚烷-3,7-二酮-2-羧酸酯和盐（I），其可用于制备6-，1-和2- 替代的碳青霉烯类抗生素。其中R5是药学上可接受的酯部分或可除去的保护基团或碱金属或碱土金属阳离子如钠或钾，并且其中R 1，R 2，R 3和R 4尤其独立地选自由氢，烷基，芳基和芳烷基组成。所公开的另一个实施方案是一组具有式“IMAGE”的化合物，其中X是离去基团。

8. 发明授权

US4839352A N-acyl derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-酰基衍生物
公开(公告)号：US4839352A
公开(公告)日：1989-06-13
申请号：US90400
申请日：1987-08-27
申请人： Louis Barash , Burton G. Christensen , John Hannah , William J. Leanza , David H. Shih
发明人： Louis Barash , Burton G. Christensen , John Hannah , William J. Leanza , David H. Shih
IPC分类号： C07D205/08 , C07D477/20 , C07D498/04
CPC分类号： C07D477/20 , C07D205/08
摘要： Disclosed are N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen and acyl. Such derivatives and their pharmaceutically acceptable salts, are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
摘要翻译：公开了具有以下结构式的抗生素硫霉素的N-酰基衍生物：其中R 1和R 2独立地选自氢和酰基。这些衍生物及其药学上可接受的盐可用作抗生素。还公开了制备这种衍生物的方法，包含这种衍生物的药物组合物，以及治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

9. 发明授权

US4833167A 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 失效
标题翻译： 2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸
公开(公告)号：US4833167A
公开(公告)日：1989-05-23
申请号：US743139
申请日：1985-06-10
申请人： Burton G. Christensen , John C. Chabala , Ronald W. Ratcliffe
发明人： Burton G. Christensen , John C. Chabala , Ronald W. Ratcliffe
IPC分类号： C07D477/22 , C07F9/6561
CPC分类号： C07F9/65611 , C07D477/22 , Y02P20/55
摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, diaklylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译：公开了2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐，酯，酸酐和酰胺衍生物，其可用作抗生素。还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β-甲基 ; R6和R7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，被保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基取代条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

10. 发明授权

US4725594A Carbapenems having an internally or externally alkylated mono- or bicyclic 2-quaternary heteroarylalxyl heteromethyl substituent 失效
标题翻译：具有内部或外部烷基化单环或双环2-季杂芳基甲基取代基的碳青霉烯
公开(公告)号：US4725594A
公开(公告)日：1988-02-16
申请号：US681344
申请日：1984-12-13
申请人： Burton G. Christensen , James V. Heck , Ronald W. Ratcliffe , Thomas N. Salzmann
发明人： Burton G. Christensen , James V. Heck , Ronald W. Ratcliffe , Thomas N. Salzmann
IPC分类号： C07D487/04 , A61K31/40 , A61P31/04 , C07D477/14
CPC分类号： C07D477/14
摘要： Carbapenems having the formula: ##STR1## wherein: R.sup.1 is H;R.sup.4 and R.sup.5 are independently H, CH.sub.3 --, CH.sub.3 CH.sub.2 --, (CH.sub.3).sub.2 CH--, HOCH.sub.2 --, CH.sub.3 CH(OH)--, (CH.sub.3).sub.2 C(OH)--, FCH.sub.2, F.sub.2 CH--, F.sub.3 C--, CH.sub.3 CH(F)--, CH.sub.3 CF.sub.2 --, (CH.sub.3).sub.2 C(F)--; X is --S--, --SO--, --SO.sub.2 --, --O-- or --NH; L is a bridging group comprising substituted or unsubstituted C.sub.1 --C.sub.4 straight, C.sub.2 -C.sub.6 branched or C.sub.3 -C.sub.7 cycloalkyl groups wherein the substituents are selected from C.sub.1 -C.sub.6 alkyl, O--C.sub.1 -C.sub.6 alkyl, S--C.sub.1 -C.sub.6 alkyl, CF.sub.3, N(C.sub.1 -C.sub.6 alkyl).sub.2 ; Y is a carboxy-containing substituent; Het is internally alkylated heteroarylium, ##STR2## or externally alkylated heteroarylium, ##STR3## their preparation and antibiotic use are disclosed.
摘要翻译：具有下式的碳青霉烯类：其中：R1是H; （CH 3）2 CH-，HOCH 2 - ，CH 3 CH（OH） - ，（CH 3）2 C（OH） - ，FCH 2，F 2 CH-，F 3 C - ，CH 3 CH（F） - ，CH 3 CF 2 - ，（CH 3）2 C（F） - ; X是-S - ， - SO - ， - SO 2 - ， - O-或-NH; L是包含取代或未取代的C 1 -C 4直链，C 2 -C 6支链或C 3 -C 7环烷基的桥连基团，其中取代基选自C 1 -C 6烷基，O-C 1 -C 6烷基，S-C 1 -C 6烷基，CF 3 ，N（C 1 -C 6烷基）2; Y是含羧基的取代基; Het是内部烷基化杂芳族化合物，图像或外部烷基化杂芳基，其公开了它们的制备和抗生素用途。

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