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1. 发明申请

US20200010432A1 PHENAZINE DERIVATIVES AS ANTIMICROBIAL AGENTS 审中-公开
公开(公告)号：US20200010432A1
公开(公告)日：2020-01-09
申请号：US16486694
申请日：2018-02-17
申请人： University of Florida Research Foundation, Incorporated
发明人： Robert William Huigens, III , Aron Garrison , Yasmeen Abouelhassan , Hongfen Yang , Gena Burch
IPC分类号： C07D241/46 , C07D403/06 , C07H17/02 , C07D501/16 , A61P31/06
摘要： The present invention provides novel phenazine derivatives, such as compounds of Formula (I) (e.g., Formulae (II)-(XIX)), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection or mycobacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium or mycobacterium), killing a microorganism (e.g., a bacterium or mycobacterium), inhibiting the formation and/or growth of a biofilm, reducing or clearing a biofilm, and/or disinfecting a surface.

2. 发明授权

US10450280B2 Tetrazolones as a carboxylic acid bioisosteres 有权
公开(公告)号：US10450280B2
公开(公告)日：2019-10-22
申请号：US15617900
申请日：2017-06-08
申请人： Rigel Pharmaceuticals, Inc.
发明人： Matthew Duncton , Rajinder Singh
IPC分类号： C07D257/04 , A61K31/41 , A61K31/4155 , A61K31/4184 , A61K31/4245 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5383 , A61K31/546 , A61K31/55 , A61K31/58 , C07D403/12 , C07D471/04 , C07D498/06 , C07D401/12 , A61K31/4725 , C07D403/10 , C07D401/14 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/14 , C07D413/10 , C07D487/04 , C07D501/46 , C07J43/00 , C07D401/10 , C07D501/16 , C07J9/00
摘要： The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

3. 发明授权

US09334289B2 Cephem compound having catechol or pseudo-catechol structure 有权
标题翻译：具有儿茶酚或假儿茶酚结构的头孢烯化合物
公开(公告)号：US09334289B2
公开(公告)日：2016-05-10
申请号：US14113459
申请日：2012-04-25
申请人： Yasuhiro Nishitani , Toshiaki Aoki , Jun Sato , Kenji Yamawaki , Katsuki Yokoo , Masayuki Sano
发明人： Yasuhiro Nishitani , Toshiaki Aoki , Jun Sato , Kenji Yamawaki , Katsuki Yokoo , Masayuki Sano
IPC分类号： C07D501/16 , C07D501/60 , C07D501/18 , C07D501/46 , C07D519/06 , C07D519/00
CPC分类号： C07D501/60 , C07D501/18 , C07D501/46 , C07D519/00 , C07D519/06
摘要： The present invention provides a novel compound which has a wide antimicrobial spectrum, and in particular exhibits potent antimicrobial activity against beta-lactamase producing Gram negative bacteria. Specifically, the present invention provides a compound of the formula (I): wherein each symbol is as defined in the specification, or an amino-protected compound when the amino group is present on the ring in the 7-side chain, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
摘要翻译：本发明提供了具有广谱抗菌谱的新型化合物，并且特别表现出对产生β-内酰胺酶的革兰氏阴性菌具有强效的抗微生物活性。具体而言，本发明提供了式（I）化合物：其中各符号如说明书中所定义，或氨基保护的化合物，当氨基存在于7-侧链的环上时，或药学上可接受的盐，以及包含其的药物组合物。

4. 发明申请

US20140322739A1 METHODS AND COMPOUNDS FOR DETECTING BETA-LACTAMASE ACTIVITY 审中-公开
标题翻译：用于检测β-乳酸酶活性的方法和化合物
公开(公告)号：US20140322739A1
公开(公告)日：2014-10-30
申请号：US14326215
申请日：2014-07-08
申请人： Nanyang Technological University
发明人： Bengang Xing , Xianfeng Huang , Tingting Jiang , Rongrong Liu
IPC分类号： C12Q1/34 , C07D501/16 , C07D501/04 , C07D519/06
CPC分类号： C12Q1/34 , C07D501/04 , C07D501/16 , C07D501/18 , C07D519/06 , G01N2333/986
摘要： The present invention relates to compounds for and a method of detecting beta-lactamase activity in a sample. The sample is contacted with a nanoparticulate tag. The nanoparticulate tag comprises a metal or a combination of metals, or it comprises a nanotube of a metal, boron nitride and/or carbon. The respective metal is capable of forming one of a covalent bond, a coordinative bond and a non-covalent interaction with a thio or a seleno group. The sample is contacted with a compound of one of general formulas (I)-(III) and (VII)-(IX). At least one beta-lactam moiety of the compound is cleaved by the beta-lactamase activity in the sample. As a result a cleavage moiety Z-A-Z, Z-A-Z—R15, Z-A-Z—R16, Z-A-Z—R17, Z-A-Z—R18 or Z-G-N(R8)R9 is released that is immobilized on the surface of the nanoparticulate tag by a covalent bond via a Z atom. The presence of beta-lactamase activity is determined based on the presence of the cleavage moiety immobilized onto the surface of the nanoparticulate tag.
摘要翻译：本发明涉及用于检测样品中β-内酰胺酶活性的化合物和方法。样品与纳米颗粒标签接触。纳米颗粒标签包括金属或金属的组合，或者它包括金属，氮化硼和/或碳的纳米管。相应的金属能够形成共价键，配位键和与硫代或硒基的非共价相互作用之一。将样品与通式（I） - （III）和（VII） - （IX）之一的化合物接触。化合物的至少一个β-内酰胺部分被样品中的β-内酰胺酶活性切割。结果，通过Z原子通过共价键将解离部分Z-A-Z，Z-A-Z-R15，Z-A-Z-R16，Z-A-Z-R17，Z-A-Z-R18或Z-G-N（R8）R9释放固定在纳米颗粒标签的表面上。基于固定在纳米颗粒标签表面上的切割部分的存在来确定β-内酰胺酶活性的存在。

5. 发明申请

US20100197569A1 CROSS-LINKED GLYCOPEPTIDE-CEPHALOSPORIN ANTIBIOTICS 有权
标题翻译：交联糖蛋白-CEPHALOSPORIN抗生素
公开(公告)号：US20100197569A1
公开(公告)日：2010-08-05
申请号：US12759073
申请日：2010-04-13
申请人： Paul R. Fatheree , Martin S. Linsell , Daniel D. Long , Daniel Marquess , Edmund J. Moran , Matthew B. Nodwell , S. Derek Turner , James Aggen
发明人： Paul R. Fatheree , Martin S. Linsell , Daniel D. Long , Daniel Marquess , Edmund J. Moran , Matthew B. Nodwell , S. Derek Turner , James Aggen
IPC分类号： A61K38/14 , C07K9/00 , C07D501/16 , C07D277/38 , A61P31/04 , A01N37/18 , C07K1/113
CPC分类号： A61K31/545 , A61K38/00 , C07D277/40 , C07D277/42 , C07D407/12 , C07D407/14 , C07D501/00 , C07D501/46 , C07K9/008
摘要： This invention provides cross-linked glycopeptide—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.
摘要翻译：本发明提供可用作抗生素的交联糖肽 - 头孢菌素化合物及其药学上可接受的盐。本发明还提供含有这些化合物的药物组合物; 使用这种化合物治疗哺乳动物细菌感染的方法; 以及可用于制备这些化合物的方法和中间体。

6. 发明授权

US5750682A Glutaryl 7-ACA derivatives and processes for obtaining them 失效
标题翻译： Glutaryl 7-ACA衍生物和获得它们的方法
公开(公告)号：US5750682A
公开(公告)日：1998-05-12
申请号：US605135
申请日：1996-03-13
申请人： Loris Sogli , Davide Longoni , Giovanni Pozzi , Enrico Siviero , Daniele Mario Terrassan , Ermanno Bernasconi , Francisco Salto
发明人： Loris Sogli , Davide Longoni , Giovanni Pozzi , Enrico Siviero , Daniele Mario Terrassan , Ermanno Bernasconi , Francisco Salto
IPC分类号： C07D501/04 , C07D501/00 , C07D501/14 , C07D501/16 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/28 , C07D501/59 , C07D501/60
CPC分类号： C07D501/00
摘要： There are disclosed new compounds of formula (I), wherein R is: a hydrogen atom: a linear or branched C1-C4 alkyl group, unsubstituted or substituted by at least a phenyl group or at least a hydrogen atom: a benzyl group substituted by at least a linear or branched C1-C4 alkyl or alkoxy group or a nitro group; a silyl substituted by at least a linear or branched, unsubstituted or substituted C1-C4 alkyl group; n is 0 or 1; and Y is a radical of formula (II), wherein A is H, OH, Cl, CH2, CH2X, where X is F, Cl, Br, I, OH or OR' and R' is COCH3 or a linear or branched, unsubstituted or substituted C1-C4 alkyl group and . . . represents a single or a double bond, with the proviso that when n=0 and R is H, R' is not a methyl group; and processes for obtaining them.
摘要翻译： PCT No.PCT / EP95 / 02802 Sec。 371日期：1996年3月13日 102（e）1996年3月13日PCT 1995年7月17日PCT公布。 WO95 / 35020PC PCT出版物日期1995年12月28日公开了新的式（I）化合物，其中R是：氢原子：未被取代或被至少一个苯基或至少一个氢原子取代的直链或支链C 1 -C 4烷基：被至少一个直链或支链的C 1 -C 4烷基或烷氧基或硝基取代的苄基; 由至少一个直链或支链的未取代或取代的C 1 -C 4烷基取代的甲硅烷基; n为0或1; 并且Y是式（II）的基团，其中A是H，OH，Cl，CH 2，CH 2 X，其中X是F，Cl，Br，I，OH或OR'，R'是COCH 3或直链或支链的，未取代或取代的C 1 -C 4烷基和+ E，。 + EE表示单键或双键，条件是当n = 0且R为H时，R'不为甲基; 以及获得它们的过程。

7. 发明授权

US5359058A Cephem derivatives 失效
标题翻译： Cephem衍生物
公开(公告)号：US5359058A
公开(公告)日：1994-10-25
申请号：US874738
申请日：1992-04-27
申请人： Jan Verweij , Henri G. J. Hirs , Hendrik A. Witkamp , Everardus J. A. M. Leenderts , Jan J. Dekoning , Herman H. Grootveld
发明人： Jan Verweij , Henri G. J. Hirs , Hendrik A. Witkamp , Everardus J. A. M. Leenderts , Jan J. Dekoning , Herman H. Grootveld
IPC分类号： A61K31/545 , C07D20060101 , C07D499/00 , C07D501/00 , C07D501/04 , C07D501/16 , C07D501/18 , C07D501/46
CPC分类号： C07D501/04 , C07D499/00 , C07D501/18
摘要： A cephalosporin compound substituted in the 7-position with a (cyclo)alkylideneammonio group of formula (II) ##STR1## wherein X' is an anion from an acid HX, R.sub.1 and R.sub.2 are individually a C.sub.1 -C.sub.16 alkyl group, or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a cycloalkylidene ring with up to 8 carbon atoms and a process for the preparation which compounds are useful intermediates.
摘要翻译：在7-位上用式（II）的（环）亚烷基氨基取代的头孢菌素化合物其中X'是酸HX的阴离子，R1和R2分别是C1-C16烷基，或R 1和R 2与它们所连接的碳原子一起形成具有至多8个碳原子的亚环烷基环，以及这些化合物是有用的中间体的方法。

8. 发明授权

US4908444A Method of producing cephem compounds 失效
标题翻译：头孢烯化合物的制备方法
公开(公告)号：US4908444A
公开(公告)日：1990-03-13
申请号：US3286
申请日：1987-01-14
申请人： Kenzo Naito , Yukio Ishibashi
发明人： Kenzo Naito , Yukio Ishibashi
IPC分类号： C07D501/04 , A61K31/545 , C07D501/06 , C07D501/16 , C07D501/18 , C07D501/24 , C07D501/26 , C07D501/28 , C07D501/34 , C07D501/57
CPC分类号： C07D501/04 , C07D501/34
摘要： A method of producing 3-alkanoyloxymethyl-3-cephem-4-carboxylic acids, which are useful as antibiotics or as intermediates in the synthesis of antibiotics, by reacting a 3-hydroxymethyl-3-cephem-4-carboxylic acid with a saturated fatty acid anhydride in an aqueous medium in the presence of an acid-acceptor base and a 4-(tertiary amino)pyridine.
摘要翻译：通过使3-羟甲基-3-头孢烯-4-羧酸与饱和脂肪酸反应，制备3-烷酰氧基甲基-3-头孢烯-4-羧酸的方法，其可用作抗生素或合成抗生素中的中间体酸酐在酸性受体碱和4-（叔氨基）吡啶的存在下在水性介质中反应。

9. 发明授权

US4870168A 3-Unsaturated alkyl cephems from 3-triflyl cephems 失效
标题翻译： 3-不饱和的烷基头孢菌素，来自3-三叶草
公开(公告)号：US4870168A
公开(公告)日：1989-09-26
申请号：US19396
申请日：1987-02-26
申请人： Stephen R. Baker , Vittorio Farina , Chester Sapino, Jr.
发明人： Stephen R. Baker , Vittorio Farina , Chester Sapino, Jr.
IPC分类号： C07D501/18 , A61K31/545 , A61K31/546 , A61K31/695 , A61P31/04 , B01J27/13 , B01J31/04 , B01J31/22 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/16 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/38 , C07D501/46 , C07D501/59 , C07F7/10
CPC分类号： C07D501/00 , C07D501/04 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/59
摘要： There is disclosed a process for the production of certain 3-hydrocarbyl-3-cephem derivatives wherein the hydrocarbyl group is selected from 1-alkenyl and conjugated and unconjugated 1-polyalkenyl, 1-alkynl, carbocyclic and heterocyclic aryl, and carbocyclic and heterocyclic arylmethyl and, in the case of the 1-alkenyl and conjugated 1-polyalkenyl derivatives, with substantially complete stereospecificity, by coupling a 3-triflyloxy cephem with a hydrocarbyltributylstannane in the presence of bis(dibenzylideneacetonyl)-palladium, a phosphine, and a metal halide such as, for example, zinc chloride. The 3-unsaturated alkyl-3-cephem derivatives so-produced are useful as broad-spectrum antibacterial agents.
摘要翻译：公开了生产某些3-烃基-3-头孢烯衍生物的方法，其中烃基选自1-烯基和共轭和未共轭的1-聚烯基，1-炔烃，碳环和杂环芳基，以及碳环和杂环芳基甲基并且在1-烯基和共轭的1-聚烯基衍生物的情况下，具有基本上完全的立体定向性，通过在双（二亚苄基丙酰基） - 钯，膦和金属卤化物的存在下将3-三氟氧基头孢烯与烃基三丁基锡烷偶联例如氯化锌。所产生的3-不饱和烷基-3-头孢烯衍生物可用作广谱抗菌剂。

10. 发明授权

US4800199A 3-[2-thiazoloamino]-8-oxo-7-substituted-5-thia-1-a zabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and salts thereof and diphenylmethyl esters thereof 失效
标题翻译： 3- [2-噻唑基氨基] -8-氧代-7-取代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸及其盐及其二苯甲基酯
公开(公告)号：US4800199A
公开(公告)日：1989-01-24
申请号：US920397
申请日：1986-10-20
申请人： Robert Babine , Ving J. Lee
发明人： Robert Babine , Ving J. Lee
IPC分类号： C07D499/00 , C07D501/16 , A61K31/545
CPC分类号： C07D499/00
摘要： Cephalosporins active as antibacterial agents, and processes for synthesis of such agents, are disclosed.
摘要翻译：公开了作为抗菌剂活性的头孢菌素和这些药剂的合成方法。

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