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1. 发明申请

US20180186814A1 TRICYCLIC COMPOUND HAVING SULFINYL OR SULFONYL 审中-公开
公开(公告)号：US20180186814A1
公开(公告)日：2018-07-05
申请号：US15740103
申请日：2016-06-30
申请人： Shionogi & Co., Ltd.
发明人： Kenji YAMAWAKI , Hiroki KUSANO
IPC分类号： C07D501/14 , A61P31/04
CPC分类号： C07D501/14 , A61K31/546 , A61P31/04
摘要： The present invention provides a compound exhibiting a strong antimicrobial spectrum against various bacteria, including gram-negative bacteria, or a pharmaceutical composition having an antimicrobial activity carbapenem-resistant bacteria. Provided is a compound represented by formula (I), an ester thereof or a pharmaceutically acceptable salt thereof, or a hydrate thereof. (I) (in the formula, —W— is —S(═O)— or S(═O)2—, -T- is CR4AR4B— or —CR5A—R5B—CR6A—R6B—, each of R2A and R2B is independently a hydrogen atom, etc., or R2A and R2B together form a substituted or unsubstituted methylidene, etc., R3 is a hydrogran atom, etc., R11 is a carboxyl, etc., and each of R7A and R7B is independently a hydrogen atom, etc.)

2. 发明授权

US08329684B2 Cephalosporin derivatives and pharmaceutical compositions thereof 有权
标题翻译：头孢菌素衍生物及其药物组合物
公开(公告)号：US08329684B2
公开(公告)日：2012-12-11
申请号：US13467019
申请日：2012-05-08
申请人： Young Lag Cho , Joung Yul Yun , Sang Eun Chae , Chul Soon Park , Hyang Sook Lee , Kyu Man Oh , Hye Jin Kang , Dae Hyuck Kang , Young Jae Yang , Hyun Jin Kwon , Tae Kyo Park , Sung Ho Woo , Young Zu Kim
发明人： Young Lag Cho , Joung Yul Yun , Sang Eun Chae , Chul Soon Park , Hyang Sook Lee , Kyu Man Oh , Hye Jin Kang , Dae Hyuck Kang , Young Jae Yang , Hyun Jin Kwon , Tae Kyo Park , Sung Ho Woo , Young Zu Kim
IPC分类号： A61K31/545 , C07D501/14
CPC分类号： C07D501/60 , C07D501/24 , C07D501/46
摘要： The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. Compounds of the present invention are effective ingredients for the broad spectrum of antibiotic resistance, exhibit low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
摘要翻译：本发明涉及由化学式1表示的新型头孢菌素衍生物。其中，X，Y，L，R 1和R 2与本发明的描述中所定义相同。本发明还涉及药物抗生素组合物，其包含由化学式1表示的新型胞孢素衍生物，其前药，其水合物，其溶剂合物，其异构体或其药学上可接受的盐作为有效成分。本发明的化合物是广谱抗生素抗性的有效成分，表现出低毒性，特别是在革兰氏阴性细菌中，其可用于强抗微生物活性。

3. 发明申请

US20090075967A1 DEUTERIUM-ENRICHED CEFTRIAXONE 审中-公开
标题翻译：富含DEUTERIUM-ENRICHED CEFTRIAXONE
公开(公告)号：US20090075967A1
公开(公告)日：2009-03-19
申请号：US12196762
申请日：2008-08-22
申请人： Anthony W. Czarnik
发明人： Anthony W. Czarnik
IPC分类号： C07D501/14 , A61K31/546 , A61P31/00 , A61P31/04
CPC分类号： C07D501/14
摘要： The present application describes deuterium-enriched ceftriaxone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
摘要翻译：本申请描述了富含氘的头孢曲松，其药学上可接受的盐形式，以及使用其的治疗方法。

4. 发明申请

US20070213313A1 DIRECT PROCESS FOR THE PRODUCTION OF AN AMINO ACID DIHYDROCHLORIDE 审中-公开
标题翻译：用于生产氨基酸二氯化物的直接方法
公开(公告)号：US20070213313A1
公开(公告)日：2007-09-13
申请号：US11465291
申请日：2006-08-17
申请人： Maurizio Zenoni , Mauro Filippi
发明人： Maurizio Zenoni , Mauro Filippi
IPC分类号： A61K31/545 , C07D501/14
CPC分类号： C07D501/46
摘要： An amino acid in solution is precipitated with concentrated hydrochloric acid and isolated as the dihydrochloride monohydrate. Said dihydrochloride is redissolved and reprecipitated by adding a solvent.
摘要翻译：溶液中的氨基酸用浓盐酸沉淀，分离为二盐酸盐一水合物。所述二盐酸盐再溶解并通过加入溶剂再沉淀。

5. 发明申请

US20070191331A1 Crystalline forms of cefdinir potassium salt 审中-公开
标题翻译：头孢地尼钾盐的结晶形式
公开(公告)号：US20070191331A1
公开(公告)日：2007-08-16
申请号：US11591217
申请日：2006-10-31
申请人： Vinod Kansal , Dhirenkumar Mistry , Saurabh Pandey , Rakesh Patel , Shlomit Wizel , Jean Hildesheim
发明人： Vinod Kansal , Dhirenkumar Mistry , Saurabh Pandey , Rakesh Patel , Shlomit Wizel , Jean Hildesheim
IPC分类号： A61K31/545 , C07D501/14
CPC分类号： C07D501/22 , C07D501/00
摘要： The present invention encompasses the solid state chemistry of cefdinir potassium salt.
摘要翻译：本发明包括头孢地尼钾盐的固态化学。

6. 发明授权

US07157575B2 Substrates for β-lactamase and uses thereof 有权
标题翻译： β-内酰胺酶底物及其用途
公开(公告)号：US07157575B2
公开(公告)日：2007-01-02
申请号：US10280482
申请日：2002-10-24
申请人： Roger Y. Tsien , Gregor Zlokarnik
发明人： Roger Y. Tsien , Gregor Zlokarnik
IPC分类号： C07D501/14
CPC分类号： C07D501/36 , C07D501/00 , C07D505/00 , C07D519/00 , C12N9/86 , C12N15/85 , C12N2800/90 , C12N2830/002 , C12P17/184 , C12P17/188 , C12P35/00 , C12Q1/18 , C12Q1/34 , C12Q1/6897 , C12Q2334/00 , G01N2333/986 , G01N2415/00 , Y10S435/805
摘要： Substrates for β-lactamase of the general formula I in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R′ is selected from the group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH2)nOH, in which n is 0 or an integer from 1 to 5; R″ is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, —CHR2OCO(CH2)nCH3, —CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z′ and Z″ are linkers for the fluorescent donor and quencher moieties. Methods of assaying β-lactamase activity and monitoring expression in systems using β-lactamase as a reporter gene also are disclosed.
摘要翻译：通式I的β-内酰胺酶底物，其中X和Y中的一个是荧光供体部分，另一个是猝灭剂（其可以或不再发射）; R'选自H，低级（即1至约5个碳原子的烷基）和（CH 2 CH 2）n OH，其中n是 0或1〜5的整数; R“选自H，生理学上可接受的金属和铵阳离子，-CHR 2 OCO（CH 2）n CH 酰基硫基甲基，酰氧基-α-苄基，三氟甲磺酸酯，三氟甲磺酸酯，丁基内酰胺，甲氧基羰氧基甲基，苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基，酰氧基烷基，二烷基氨基羰氧基甲基和脂族基，其中R 2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; Z'和Z“是荧光供体和猝灭剂部分的接头。公开了使用β-内酰胺酶作为报道基因的体内测定β-内酰胺酶活性和监测表达的方法。

7. 发明申请

US20060258636A1 CRYSTALLINE SOLVATE OF CEFUROXIME ACID 有权
标题翻译： CEFUROXIME ACID的水溶性溶剂
公开(公告)号：US20060258636A1
公开(公告)日：2006-11-16
申请号：US11379132
申请日：2006-04-18
申请人： Maurizio ZENONI , Angelo Cattaneo
发明人： Maurizio ZENONI , Angelo Cattaneo
IPC分类号： A61K31/545 , C07D501/14
CPC分类号： C07D501/00
摘要： Crystalline Solvate of cefuroxime acid, useful for preparing the antibiotic cefuroxime sodium salt.
摘要翻译：头孢呋辛酸的结晶溶剂化物，可用于制备抗生素头孢呋辛钠盐。

8. 发明申请

US20060189802A1 Process for the preparation of cephradine 有权
标题翻译：制备头孢拉定的方法
公开(公告)号：US20060189802A1
公开(公告)日：2006-08-24
申请号：US10562345
申请日：2004-07-01
申请人： Dennis Heemskerk , Anja Gerarda Hogenboom , Carlos Lenhardt , Harold Moody , Theodorus Johannes Godfried Maria Dooren
发明人： Dennis Heemskerk , Anja Gerarda Hogenboom , Carlos Lenhardt , Harold Moody , Theodorus Johannes Godfried Maria Dooren
IPC分类号： C07D501/14
CPC分类号： C07D501/00 , C12P35/04
摘要： The present invention describes a process for preparing cephradine, said process comprising reacting 7-aminodesacetoxy cephalosporanic acid (7-ADCA) with D-dihydrophenylglycine in activated form (DHa) in the presence of an enzyme in a reaction mixture to form cephradine, resulting in a conversion of 7-ADCA into cephradine of at least 70%, wherein the concentration D-dihydrophenylglycine (DH) in the reaction mixture is below 2 wt.%, wherein the conversion of 7-ADCA into cephradine & equals; (nCEF/n7-ADCA)*100%, wherein nCEF=quantity of cephradine formed (in mole); and n7-ADCA=total quantity of 7-ADCA added to reaction mixture (in mole). The invention also describes a process for the preparation of cephradine hydrate characterised in that the process comprises: —reacting 7-amino acid desacetoxy cephalosporanic acid (7-ADCA) with DHa in the presence of an enzyme in a reaction mixture to form cephradine; —preparing an aqueous solution comprising at least part of the cephradine; and crystallising the cephradine from said aqueous solution. The invention further describes cephradine hydrate obtainable by a process according to invention. The invention also describes cephradine hydrate with an absorbance at 450 nm of below 0.050.
摘要翻译：本发明描述了一种制备头孢拉定的方法，所述方法包括使7-氨基二乙酰氧基头孢菌酸（7-ADCA）与活化形式的二氢苯基甘氨酸（DHa）在酶的存在下在反应混合物中反应形成头孢拉定，得到将7-ADCA转化为至少70％的头孢拉定，其中反应混合物中D-二氢苯基甘氨酸（DH）的浓度低于2重量％，其中7-ADCA转化成头孢拉定等于; （％CEF / n 7-ADCA）* 100％，其中n CEF =形成的头孢拉定量（以摩尔计）; 和n 7-ADCA =加入到反应混合物中的7-ADCA的总量（以摩尔计）。本发明还描述了一种制备头孢拉定水合物的方法，其特征在于该方法包括：在反应混合物中，在酶的存在下，用7-氨基酸脱乙酰氧基头孢菌酸（7-ADCA）与DHa反应形成头孢拉定; - 制备包含至少一部分头孢拉定的水溶液; 并从所述水溶液中结晶头孢拉定。本发明还描述了通过根据本发明的方法获得的头孢拉定水合物。本发明还描述了在450nm处的吸光度低于0.050的头孢拉定水合物。

9. 发明申请

US20060122165A1 Crystalline cefdinir 审中-公开
标题翻译：结晶头孢地尼
公开(公告)号：US20060122165A1
公开(公告)日：2006-06-08
申请号：US11294116
申请日：2005-12-05
申请人： Otto Daemon , Klaus Hartmann , Johannes Raneburger
发明人： Otto Daemon , Klaus Hartmann , Johannes Raneburger
IPC分类号： A61K31/545 , C07D501/14
CPC分类号： C07D501/00
摘要： The present invention relates to a new crystalline form of cefdinir and processes for the preparation thereof. Furthermore, the present invention relates to pharmaceutical compositions comprising said new crystalline form of cefdinir and to processes for preparing these compositions.
摘要翻译：本发明涉及头孢地尼的新结晶形式及其制备方法。此外，本发明涉及包含所述新型结晶形式的头孢地尼的药物组合物以及制备这些组合物的方法。

10. 发明申请

US20060025586A1 Cefdinir intermediate 失效
标题翻译：头孢地尼中间体
公开(公告)号：US20060025586A1
公开(公告)日：2006-02-02
申请号：US10524397
申请日：2003-08-12
申请人： Peter Kremminger , Siegfried Wolf , Johannes Ludescher
发明人： Peter Kremminger , Siegfried Wolf , Johannes Ludescher
IPC分类号： C07D501/14
CPC分类号： C07D501/00
摘要： 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula I in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula I in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.
摘要翻译：具有结晶盐形式的式I的7- [2-（2-氨基噻唑-4-基）-2-（甲基羰氧基亚氨基）乙酰氨基] -3-乙烯基头孢烯-4-羧酸及其用途，在制备纯头孢地尼。在另一方面，本发明涉及任选呈结晶形式的盐形式的式I化合物，其中盐选自磷酸盐，磷酸氢盐，甲磺酸盐，甲苯磺酸盐，硫酸盐，硫酸氢盐和氨基磺酸盐。

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