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1. 发明授权

US08865891B2 Optically-detectable enzyme substrates and their method of use 有权
标题翻译：光学上可检测的酶底物及其使用方法
公开(公告)号：US08865891B2
公开(公告)日：2014-10-21
申请号：US13614948
申请日：2012-09-13
申请人： Schuyler Corry , William Downey , Brian Filanoski , Kyle Gee , Lawrence Greenfield , James Hirsch , Iain Johnson , Aleksey Rukavishnikov
发明人： Schuyler Corry , William Downey , Brian Filanoski , Kyle Gee , Lawrence Greenfield , James Hirsch , Iain Johnson , Aleksey Rukavishnikov
IPC分类号： C07D501/36 , C07D501/58 , C07D501/00 , C07F5/02 , C07D503/00 , C07D499/00 , C12Q1/34
CPC分类号： C07F5/022 , C07D499/00 , C07D501/00 , C07D501/58 , C07D501/60 , C07D503/00 , C07D519/00 , C12Q1/34 , C12Q2334/00 , G01N33/581 , G01N2333/986
摘要： The present invention relates to compounds that are substrates for an enzyme, and upon reaction with the enzyme provide a detectable response, such as an optically detectable response. In particular, the compounds have utility in detecting the presence of a β-lactamase in a sample. In addition to the compounds, methods are disclosed for analyzing a sample for the presence of a β-lactamase, for example, as an indicator of expression of a nucleic acid sequence including a sequence coding for a β-lactamase. Kits are disclosed that include the disclosed compounds and additional components, for example, cells, antibodies, a β-lactamase or instructions for using the components in an assay.
摘要翻译：本发明涉及作为酶的底物的化合物，并且在与酶反应时提供可检测的反应，例如可光学检测的反应。特别地，这些化合物可用于检测样品中β-内酰胺酶的存在。除了化合物之外，公开了用于分析样品中β-内酰胺酶的存在的方法，例如，作为包括编码β-内酰胺酶的序列的核酸序列的表达的指示剂。公开了包括所公开的化合物和另外的组分的试剂盒，例如细胞，抗体，β-内酰胺酶或在测定中使用组分的说明书。

2. 发明授权

US07833998B2 Oral neurotherapeutic cephalosporin sulfoxide and sulfone-containing compositions 有权
标题翻译：口服神经治疗性头孢菌素亚砜和含砜组合物
公开(公告)号：US07833998B2
公开(公告)日：2010-11-16
申请号：US10569118
申请日：2004-08-24
申请人： Gary A. Koppel , Michael O. Chaney
发明人： Gary A. Koppel , Michael O. Chaney
IPC分类号： C07D501/36 , A61K31/546 , A61P25/24 , A61P25/22
CPC分类号： A61K31/43 , A61K31/431 , A61K31/545 , A61K31/546 , C07D501/36 , C07D501/60
摘要： The treatment of neurological disorders using cephalosporin sulfoxide-containing and/or cephalosporin sulfone-containing compositions and pharmaceutical compositions including oral dosage forms that include cephalosporin sulfoxide and/or sulfone-containing compositions are described.
摘要翻译：描述了使用含头孢菌素亚砜和/或头孢菌素砜的组合物和包括包括头孢菌素亚砜和/或含砜组合物在内的口服剂型的药物组合物治疗神经障碍。

3. 发明授权

US07452990B2 Intermediates for synthesis of cephalosporins and process for preparation of such intermediates 失效
标题翻译：用于合成头孢菌素的中间体及其制备方法
公开(公告)号：US07452990B2
公开(公告)日：2008-11-18
申请号：US10540770
申请日：2002-12-26
申请人： Debashish Datta , Muralikrishna Dantu , Brijkishore Mishra , Pollepeddi Lakshmi Narayana Sharma
发明人： Debashish Datta , Muralikrishna Dantu , Brijkishore Mishra , Pollepeddi Lakshmi Narayana Sharma
IPC分类号： C07D501/22 , C07D501/24 , C07D501/36 , C07D501/46 , C07D501/34 , C07C305/14
CPC分类号： C07D501/00 , C07C303/24 , C07C305/00 , Y02P20/55
摘要： A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics wherein X is chlorine or bromine; R is hydrogen, C1-4 alkyl group, an easily removable hydroxyl protective group, —CH2COOR5, or —C(CH3)2COOR5, wherein R5 is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV1), wherein X, R and R5 are as defined above, with N,N-dimethylformiminium chloride chlorosulphate of formula (VII) in an organic solvent at a temperature ranging from −30° C. to −15° C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.
摘要翻译：用于制备头孢菌素抗生素的式（I）的新的4-卤代-2-氧亚氨基-3-氧代丁酸-N-，N-二甲基氯化亚硫酸盐，其中X是氯或溴; R为氢，C 1-4烷基，易脱除的羟基保护基，-CH 2 COOR 5或-C（CH 3）其中R 5是氢或易水解的酯基。其中R 5是氢或易水解的酯基。式（I）化合物通过使式（IV ^{）的4-卤代-2-氧亚氨基-3-氧代丁酸（其中X，R和R 5）与式（VII）的N，N-二甲基甲酰亚胺氯化硫酸盐在有机溶剂中在-30℃至-15℃的温度范围内。可从中间体制备的头孢菌素包括头孢地尼头孢匹罗，头孢匹肟，头孢他啶，头孢克肟，头孢匹肟，头孢匹肟，头孢噻肟，头孢噻肟，头孢匹罗，头孢泊肟酯，头孢喹肟，头孢他啶，头孢曲松，头孢噻呋，头孢唑肟，头孢曲松和头孢唑胺。}

4. 发明授权

US07098329B2 Process for the preparation of a cephalosporin antibiotic 失效
标题翻译：制备头孢菌素抗生素的方法
公开(公告)号：US07098329B2
公开(公告)日：2006-08-29
申请号：US10867723
申请日：2004-06-16
申请人： Pandurang Balwant Deshpande , Prabhat Kumar Sahoo , Anandam Vempali , Srinivasu Ghanta
发明人： Pandurang Balwant Deshpande , Prabhat Kumar Sahoo , Anandam Vempali , Srinivasu Ghanta
IPC分类号： C07D501/36
CPC分类号： C07D501/00
摘要： An improved process for the preparation of ceftriaxone sodium comprising the steps of: i) reacting the 3-cephem derivative of formula (II) with halo acid derivative of formula (III) wherein X represents halogen and Y represent halogen in the presence of silylating agent and methylene chloride at −25 to 10° C., to produce (IV), ii) quenching the reaction by pouring the reaction mixture into water or in a aqueous solution of sodium carbonate, iii) preparing sodium salt solution of (IV) by adding sodium carbonate and separating the organic layer, iv) cyclizing the sodium salt of (IV) in the aqueous solution with thiourea at a temperature in the range of 0 to 30° C., v) adjusting the pH to 1.5 to 2.5 to precipitate the ceftriaxone free acid, vi) converting the ceftriaxone free acid to sodium salt using sodium-2-ethyl hexanoate in water and vii) precipitating and isolating the ceftriaxone sodium.
摘要翻译：一种用于制备头孢曲松钠的改进方法，包括以下步骤：i）使式（II）的3-头孢烯衍生物与式（III）的卤酸衍生物反应，其中X代表卤素，Y代表甲硅烷基化剂存在下的卤素和二氯甲烷在-25至10℃下反应，以产生（Ⅳ），ⅱ）通过将反应混合物倒入水中或在碳酸钠水溶液中淬灭反应，ⅲ）制备（Ⅳ）的钠盐溶液加入碳酸钠并分离有机层，iv）在0至30℃的温度范围内，用硫脲环化水溶液中的（Ⅳ）的钠盐，v）将pH调节至1.5至2.5以沉淀头孢曲松游离酸，vi）使用2-乙基己酸钠在水中将头孢曲松游离酸转化为钠盐，和vii）沉淀并分离头孢曲松钠。

5. 发明授权

US06906187B2 Manufacture of cefalosporins and intermediates 失效
标题翻译：头孢菌素和中间体的制造
公开(公告)号：US06906187B2
公开(公告)日：2005-06-14
申请号：US10374723
申请日：2003-02-27
申请人： Giordano Lesma
发明人： Giordano Lesma
IPC分类号： C07D501/00 , C07D501/14 , C07D501/36 , C07D501/22 , C07D501/59
CPC分类号： C07D501/00
摘要： There is described a process for the preparation of 3-disubstituted cepham-4-carboxylic acid derivatives of formula I wherein R″ is 4-methoxybenzyl, X is the residue of a thioether and Z is a residue of a nucleophilic compound, such as 2-furoylthio, acetoxy or 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-ylthio, by reaction of a functional derivative of α-(2-chloroacetamido)thiazol-4-yl-α-methoxyiminoacetic acid with 7β-amino-3-methylenecepham-4-carboxylic acid 4-methoxybenzyl ester, subsequent treatment of the obtained 4-methoxybenzyl 7β-[α-(2-chloroacetamido)thiazol-4-yl-α-methoxyimino]acetamido-3-methylenecepham-4-carboxylate with a S-chloromercaptan of formula X—S—Cl, such as methanesulfenyl chloride, and final treatment of the corresponding 4-methoxybenzyl 7β-[α-(2-chloroacetamido)thiazol-4-yl-α-methoxyimino]acetamido-3-thio-3-chloromethylcepham-4-carboxylate thus obtained of formula V wherein R″ and X are as defined above, with a compound of formula M-Z, in which M is an alkaline metal or a hydrogen atom and Z is as defined above. These novel intermediates may be converted into the corresponding 3-cephem derivatives by oxidative cleavage of the mercaptan X—SH. By suitable deprotection, these 3-cephem derivatives afford cephalosporins such as ceftiofur, cefotaxime and ceftriaxone.
摘要翻译：描述了制备式I的3-二取代的头孢烯-4-羧酸衍生物的方法，其中R“是4-甲氧基苄基，X是硫醚的残基，Z是亲核化合物的残基，例如 2-呋喃硫基，乙酰氧基或1,2,5,6-四氢-2-甲基-5,6-二氧代-1,2,4-三嗪-3-基硫基，通过α-（2- 氯代乙酰氨基）噻唑-4-基-α-甲氧基亚氨基乙酸与7-氨基-3-亚甲基头孢-4-羧酸4-甲氧基苄基酯反应，随后处理所获得的4-甲氧基苄基的7a-（2-氯乙酰氨基） 4-甲氧基亚氨基]乙酰氨基-3-甲氧基亚氨基-4-羧酸甲酯与式XS-Cl的S-氯代硫醇如甲亚磺酰氯反应，最后处理相应的4-甲氧基苄基的7β-（α- 氯乙酰胺基）噻唑-4-基-α-甲氧基亚氨基]乙酰氨基-3-硫代-3-氯甲基头孢-4-羧酸酯，其中R“和X如上所定义，与式 nd的式M-Z，其中M是碱金属或氢原子，Z如上定义。这些新型中间体可以通过硫醇X-SH的氧化裂解转化为相应的3-头孢烯衍生物。通过适当的脱保护，这些3-头孢烯衍生物提供头孢菌素如头孢噻呋，头孢噻肟和头孢曲松。

6. 发明授权

US5856502A Method for manufacture of cephalosporin and intermediates thereof 失效
标题翻译：头孢菌素的制造方法及其中间体
公开(公告)号：US5856502A
公开(公告)日：1999-01-05
申请号：US995074
申请日：1997-12-19
申请人： Debashish Datta , Vinod George , Bishwa Prakash Rai
发明人： Debashish Datta , Vinod George , Bishwa Prakash Rai
IPC分类号： C07D257/04 , C07D277/20 , C07D501/00 , C07D501/34 , C07D501/36 , C07D277/587
CPC分类号： C07D257/04 , C07D277/587 , C07D501/00
摘要： This invention relates to reactive derivatives of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid and 1H-tetrazol-1-acetic acid of the following general formula I, ##STR1## wherein ##STR2## as well as to use thereof in the manufacture of cephalosporin antibiotics such as cefotaxime, ceftriaxone and cefazolin.
摘要翻译：本发明涉及以下通式I的2-（2-氨基噻唑-4-基）-2-甲氧基亚氨基乙酸和1H-四唑-1-乙酸的反应性衍生物，其中以及其在制造头孢菌素抗生素如头孢噻肟，头孢曲松和头孢唑啉中的用途。

7. 发明授权

US5741902A 7-acyl-3-(substituted carbamoyloxy) cephem compounds and process for their preparation 失效
公开(公告)号：US5741902A
公开(公告)日：1998-04-21
申请号：US464341
申请日：1995-06-05
申请人： Shigeto Negi , Motosuke Yamanaka , Kanemasa Katsu , Isao Sugiyama , Yuuki Komatu , Atsushi Kamata , Akihiko Tsuruoka , Yoshimasa Machida
发明人： Shigeto Negi , Motosuke Yamanaka , Kanemasa Katsu , Isao Sugiyama , Yuuki Komatu , Atsushi Kamata , Akihiko Tsuruoka , Yoshimasa Machida
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/18 , C07D501/26 , C07D501/28 , C07D501/34 , C07D501/36 , C07D501/40
CPC分类号： C07D501/00
摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

8. 发明授权

US5739346A Dimethyl formiminium chloride chlorosulphate derivatives useful as intermediates for producing cephalosporins 失效
标题翻译：氯化二甲基氯化亚锡盐酸盐衍生物可用作生产头孢菌素的中间体
公开(公告)号：US5739346A
公开(公告)日：1998-04-14
申请号：US624737
申请日：1996-03-26
申请人： Debashish Datta , Vinod George , Bishwa Prakash Rai
发明人： Debashish Datta , Vinod George , Bishwa Prakash Rai
IPC分类号： C07D257/04 , C07D277/20 , C07D501/00 , C07D501/34 , C07D501/36 , C07D277/587
CPC分类号： C07D257/04 , C07D277/587 , C07D501/00
摘要： This invention relates to reactive derivatives of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid and 1H-tetrazol-1-acetic acid of the following general formula I, ##STR1## wherein R.sub.3 = ##STR2## as well as to use thereof in the manufacture of cephalosporin antibiotics such as cefotaxime, ceftriaxone and cefazolin.
摘要翻译：本发明涉及以下通式I的2-（2-氨基噻唑-4-基）-2-甲氧基亚氨基乙酸和1H-四唑-1-乙酸的反应性衍生物，其中R3 = 的头孢菌素类抗生素如头孢噻肟，头孢曲松和头孢唑啉。

9. 发明授权

US5734047A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5734047A
公开(公告)日：1998-03-31
申请号：US761738
申请日：1996-12-05
申请人： Choung U. Kim , Muzammil M. Mansuri , Peter F. Misco , John A. Wichtowski
发明人： Choung U. Kim , Muzammil M. Mansuri , Peter F. Misco , John A. Wichtowski
IPC分类号： C07D501/00 , C07D501/36 , A61K31/545
CPC分类号： C07D501/00
摘要： Novel cephem derivatives represented by the general formula ##STR1## wherein Ar is an optionally substituted lipophilic phenyl, naphthyl, benzthiazolyl or pyridyl group; R.sup.1 represents a group of the formula ##STR2## in which R.sup.8 and R.sup.9 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl or (C.sub.1 -C.sub.6)alkoxycarbonyl, said C.sub.1 -C.sub.6 alkyl group being optionally substituted by 1-5 hydroxy or C.sub.1 -C.sub.6 alkoxy groups; m is either 0 or 1; A is a C.sub.2 -C.sub.10 alkyl group optionally substituted by 1-5 hydroxy groups; and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.
摘要翻译：由通式 + TR 表示的新型头孢烯衍生物，其中Ar是任选取代的亲脂性苯基，萘基，苯并噻唑基或吡啶基; R 1表示式（VIII）的基团，其中R 8和R 9各自独立地为氢，C 1 -C 6烷基或（C 1 -C 6）烷氧基羰基，所述C 1 -C 6烷基任选被1-5个羟基或C 1 -C 6 烷氧基 m为0或1; A是任选被1-5个羟基取代的C 2 -C 10烷基; 且R 2和R 3各自独立地为氢或C 1 -C 6烷基。衍生物是革兰氏阳性抗菌剂，特别适用于治疗耐甲氧西林金黄色葡萄球菌引起的疾病。

10. 发明授权

US5668284A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5668284A
公开(公告)日：1997-09-16
申请号：US644751
申请日：1996-05-08
申请人： Choung U. Kim , Peter F. Misco, Jr. , John A. Wichtowski , Yasutsugu Ueda , Thomas W. Hudyma , John D. Matiskella , Stanley V. D'Andrea , Shelley E. Hoeft , Raymond F. Miller , Muzammil M. Mansuri , Joanne J. Bronson
发明人： Choung U. Kim , Peter F. Misco, Jr. , John A. Wichtowski , Yasutsugu Ueda , Thomas W. Hudyma , John D. Matiskella , Stanley V. D'Andrea , Shelley E. Hoeft , Raymond F. Miller , Muzammil M. Mansuri , Joanne J. Bronson
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/36 , C07D211/84 , C07F9/58
CPC分类号： C07D501/00
摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).
摘要翻译：由通式表示的新型头孢烯衍生物，其中酰基取代基是式IMA的组，其中Ar是亲脂性任选取代的苯基，萘基，吡啶基或苯并噻唑基; R1选自某些任选取代的脂族，芳族，芳基脂族或糖部分，R2和R3各自独立地为氢，烷基或氨基烷基羰基氨基是革兰氏阳性抗菌剂，特别可用于治疗由耐甲氧西林金黄色葡萄球菌引起的感染性疾病（ MRSA）。

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