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1. 发明申请

US20150246931A1 PROCESS FOR THE PREPARATION OF TAZOBACTAM 审中-公开
标题翻译：制备TAZOBACTAM的方法
公开(公告)号：US20150246931A1
公开(公告)日：2015-09-03
申请号：US14426213
申请日：2013-09-05
申请人： HOSPIRA, INC.
发明人： Senthikumar Udayampalayam Palanisamy , Mohan Singaravel , Sivasankaran Venugopal , Kannadhasan Rajamanickam , Sakthivel Anandan , Loganathan Velraj
IPC分类号： C07D499/86
CPC分类号： C07D499/86 , C07D499/00 , C07D499/06 , C07D499/08
摘要： The present invention relates to an improved process for the preparation of Tazobactam of formula (I) having reduced content of cresol.
摘要翻译：本发明涉及制备具有降低的甲酚含量的式（I）的他唑巴坦的改进方法。

2. 发明申请

US20140057888A1 COMPOUNDS AND THEIR USE 审中-公开
标题翻译：化合物及其用途
公开(公告)号：US20140057888A1
公开(公告)日：2014-02-27
申请号：US13989600
申请日：2011-11-25
申请人： Senthilkumar Udayampalayam Palanisamy , Maneesh Paul-Satyaseela , Shridhar Narayanan , Gopalan Balasubramanian , Aravind Appu , Senthilnathan Manickam , Hariharam Periasamy
发明人： Senthilkumar Udayampalayam Palanisamy , Maneesh Paul-Satyaseela , Shridhar Narayanan , Gopalan Balasubramanian , Aravind Appu , Senthilnathan Manickam , Hariharam Periasamy
IPC分类号： A61K31/431 , C12Q1/44 , A61K31/496 , A61K31/542 , A61K31/4025 , C07D499/00 , A61K31/397
CPC分类号： A61K31/431 , A61K31/397 , A61K31/4025 , A61K31/496 , A61K31/542 , C07D499/00 , C07D499/883 , C12Q1/44
摘要： Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as β-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of β-lactamases. These compounds restore/potentiate the activities of β-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting β-lactamases.Formula (I)
摘要翻译：本文描述的是化合物及其在治疗感染中的用途。本文所述的式（I）化合物，其衍生物，类似物，互变异构体形式，立体异构体，多晶型物，溶剂合物，药学上可接受的盐和药物组合物也可用作β-内酰胺酶抑制剂，其恢复或增强合适的抗生素的抗生素谱代理商式（I）化合物作为β-内酰胺酶的抑制剂。这些化合物恢复/增强β-内酰胺抗生素对碳青霉烯酶的活性。这些化合物可用于检测β-内酰胺酶的诊断方法。式（I）

3. 发明申请

US20120040380A1 OPTICALLY-DETECTABLE ENZYME SUBSTRATES AND THEIR METHOD OF USE 有权
标题翻译：光学检测酶基质及其使用方法
公开(公告)号：US20120040380A1
公开(公告)日：2012-02-16
申请号：US13166627
申请日：2011-06-22
申请人： SCHUYLER BOON CORRY , WILLIAM LOUIS DOWNEY , BRIAN FILANOSKI , KYLE RICHARD GEE , I. LAWRENCE GREENFIELD , JAMES DAVID HIRSCH , IAIN JOHNSON , ALEKSEY RUKAVISHNIKOV
发明人： SCHUYLER BOON CORRY , WILLIAM LOUIS DOWNEY , BRIAN FILANOSKI , KYLE RICHARD GEE , I. LAWRENCE GREENFIELD , JAMES DAVID HIRSCH , IAIN JOHNSON , ALEKSEY RUKAVISHNIKOV
IPC分类号： G01N21/64 , C09B29/36 , 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-lactmase, for example, as an indicator of expression of a nucleic acid sequence including a sequence coding for a β-lactmase. Kits are disclosed that include the disclosed compounds and additional components, for example, cells, antibodies, a β-lactmase 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存在β-乳糖酶的方法，例如，作为包括编码β-乳糖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-乳酸酶或在测定中使用组分的说明书。

4. 发明授权

US07714125B2 Process for producing penam compound useful for preparing tazobactam 有权
标题翻译：制备可用于制备他唑巴坦的penam化合物的方法
公开(公告)号：US07714125B2
公开(公告)日：2010-05-11
申请号：US11665006
申请日：2005-10-25
申请人： Isao Wada , Yoshihisa Tokumaru , Akihiro Shimabayashi
发明人： Isao Wada , Yoshihisa Tokumaru , Akihiro Shimabayashi
IPC分类号： C07D499/04
CPC分类号： C07D499/00
摘要： An object of the invention is to provide an industrially advantageous process capable of remarkably suppressing the generation of an undesirable by-product cepham compound to thereby efficiently produce a desired 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid ester. In the present invention, a diphenylmethyl 2β-bromomethyl-2α-methylpenam-3α-carboxylate (BMPB) is reacted with 1,2,3-triazole in a halogenated hydrocarbon solvent at −5° C. or lower. The reaction in a halogenated hydrocarbon solvent at −5° C. or less can remarkably suppress the generation of an undesirable by-product cepham compound, so that the desired diphenylmethyl 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylate (TMPB) can be efficiently produced.
摘要翻译：本发明的目的是提供一种工业上有利的方法，该方法能够显着抑制不期望的副产物头孢烯化合物的产生，从而有效地产生所需的2α-甲基-2' - [（1,2,3-三唑-1-基） - 基）甲基] penam-3α-羧酸酯。在本发明中，在-5℃或更低的卤代烃溶剂中使二苯基甲基2'-溴甲基-2α-甲基青蒿素-3α-羧酸酯（BMPB）与1,2,3-三唑反应。在-5℃或更低的卤代烃溶剂中的反应可以显着地抑制不期望的副产物头孢烯化合物的产生，从而使所需的二苯基甲基2α-甲基-2' - [（1,2,3-三唑） -1-基）甲基] penam-3α-羧酸酯（TMPB）。

5. 发明申请

US20090170941A1 Pharmaceutical Compounds 失效
标题翻译：药物化合物
公开(公告)号：US20090170941A1
公开(公告)日：2009-07-02
申请号：US12132245
申请日：2008-06-03
申请人： Piero Del SOLDATO
发明人： Piero Del SOLDATO
IPC分类号： A61K31/216 , C07C69/76 , A61P43/00
CPC分类号： C07D295/088 , C07C203/04 , C07C219/22 , C07C219/24 , C07C229/42 , C07C233/25 , C07C317/44 , C07C2602/08 , C07D219/10 , C07D309/30 , C07D401/12 , C07D499/00 , C07F9/3873 , C07H15/252
摘要： Compounds or their salts of general formula (I): A-B—N(O)s wherein: s is an integer equal to 1 or 2; A=R-T1-, wherein R is the drug radical and T1=(CO)t or (X)t′, wherein X=O, S, NR1c, R1c is H or a linear or branched alkyl or a free valence, t and t′ are integers and equal to zero or 1, with the proviso that t=1 when t′=0; t=0 when t′=1; B=-TB-X2—O— wherein TB=(CO) when t=0, TB=X when t′=0, X being as above defined; X2 is equal to R1B—X—R2B radical wherein X is as above defined, R1B and R2B, equal to or different from each other, are linear or branched C1-C6 alkylenes, or X2 is a radical wherein two alkylene chains C1-C4 are linked to nonadjacent positions of a central ring having 4 or 6 atoms, said ring being an unsaturated cycloaliphatic ring, or a saturated or aromatic heterocylic ring, containing one or two heteroatoms, equal or different, selected from O, S, N; wherein the unsaturated cycloaliphatic ring does not have aromatic character according to Huckel's rule.
摘要翻译：通式（I）的化合物或其盐：A-B-N（O）s其中：s为等于1或2的整数; A = R-T1-，其中R是药物基团，T1 =（CO）t或（X）t'，其中X = O，S，NR1c，R1c是H或直链或支链烷基或自由价， t和t'是整数并且等于零或1，条件是当t'= 0时t = 1; 当t'= 1时，t = 0; B = -TB-X2-O-其中当t = 0时TB =（CO），当t'= 0时，TB = X，X如上所定义; X2等于R1B-X-R2B基团，其中X如上所定义，R1B和R2B彼此相同或不同，为直链或支链C1-C6亚烷基，或X2为其中两个亚烷基链C1-C4 连接到具有4或6个原子的中心环的不相邻位置，所述环是不饱和脂环族环或饱和或芳族杂环，其含有一个或两个相同或不同的选自O，S，N的杂原子; 其中不饱和脂环族环根据Huckel的规则不具有芳香性质。

6. 发明申请

US20090047692A1 OPTICALLY-DETECTABLE ENZYME SUBSTRATES AND THEIR METHOD OF USE 审中-公开
标题翻译：光学检测酶基质及其使用方法
公开(公告)号：US20090047692A1
公开(公告)日：2009-02-19
申请号：US12099085
申请日：2008-04-07
申请人： Schuyler Boon CORRY , William Louis Downey , Brian Filanoski , Kyle Richard Gee , I. Lawrence Greenfield , James David Hirsch , Iain Johnson , Aleksey Rukavishnikov
发明人： Schuyler Boon CORRY , William Louis Downey , Brian Filanoski , Kyle Richard Gee , I. Lawrence Greenfield , James David Hirsch , Iain Johnson , Aleksey Rukavishnikov
IPC分类号： G01N33/53 , C07D501/60 , C07D498/04 , 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-lactmase, for example, as an indicator of expression of a nucleic acid sequence including a sequence coding for a β-lactmase. Kits are disclosed that include the disclosed compounds and additional components, for example, cells, antibodies, a β-lactmase 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存在β-内酰胺酶的方法，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。

7. 发明申请

US20090012287A1 Process for Producing Penam Compound 有权
标题翻译：生产Penam化合物的方法
公开(公告)号：US20090012287A1
公开(公告)日：2009-01-08
申请号：US11665006
申请日：2005-10-25
申请人： Isao Wada , Yoshihisa Tokumaru , Akihiro Shimabayashi
发明人： Isao Wada , Yoshihisa Tokumaru , Akihiro Shimabayashi
IPC分类号： C07D499/04
CPC分类号： C07D499/00
摘要： An object of the invention is to provide an industrially advantageous process capable of remarkably suppressing the generation of an undesirable by-product cepham compound to thereby efficiently produce a desired 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid ester. In the present invention, a diphenylmethyl 2β-bromomethyl-2α-methylpenam-3α-carboxylate (BMPB) is reacted with 1,2,3-triazole in a halogenated hydrocarbon solvent at −5° C. or lower. The reaction in a halogenated hydrocarbon solvent at −5° C. or less can remarkably suppress the generation of an undesirable by-product cepham compound, so that the desired diphenylmethyl 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylate (TMPB) can be efficiently produced.
摘要翻译：本发明的目的是提供一种工业上有利的方法，该方法能够显着地抑制不期望的副产物头孢烯化合物的产生，从而有效地产生所需的2α-甲基-2aeta - [（1,2,3-三唑-1-基）吡啶-3-基）甲基] penam-3α-羧酸酯。在本发明中，在-5℃或更低的卤代烃溶剂中使二苯基甲基2ba-溴甲基-2α-甲基青蒿素-3α-羧酸酯（BMPB）与1,2,3-三唑反应。在-5℃或更低的卤代烃溶剂中的反应可以显着地抑制不合需要的副产物头孢烯化合物的产生，使得所需的二甲基二甲基-2α-甲基-2β-[（1,2,3-三唑-2-基）（TMPB））可以有效地制备。

8. 发明申请

US20060172987A1 Amoxicillin trihydrate 审中-公开
标题翻译：阿莫西林三水合物
公开(公告)号：US20060172987A1
公开(公告)日：2006-08-03
申请号：US10548189
申请日：2004-03-19
申请人： Jan Groenendaal , Everardus Johannus Leenderts , Thomas Does
发明人： Jan Groenendaal , Everardus Johannus Leenderts , Thomas Does
IPC分类号： A61K31/43 , C07D499/26
CPC分类号： A61K9/4866 , A61K9/2054 , C07D499/00
摘要： The present invention relates to a product of amoxicillin trihydrate, having a free water content of less than 0.1 wt. %, preferably less than 0.07 wt. %, more preferably less than 0.05 wt. %, measured at an equilibrium relative humidity of 30% and at a temperature of 25° C. The product is advantageously used in mixture with clavulanic acid. The invention also relates to a process for the preparation of the new product.
摘要翻译：本发明涉及游离水含量小于0.1重量％的阿莫西林三水合物的产品。％，优选小于0.07wt。％，更优选小于0.05wt。％，在30％的平衡相对湿度和25℃的温度下测量。该产品有利地与克拉维酸混合使用。本发明还涉及一种制备新产品的方法。

9. 发明授权

US07041820B2 Process for producing (dioxolenon-4-yl)methyl ester derivative 失效
标题翻译：（二氧噻吩-4-基）甲酯衍生物的制备方法
公开(公告)号：US07041820B2
公开(公告)日：2006-05-09
申请号：US10473297
申请日：2002-03-29
申请人： Toshiyuki Watai , Mitsuru Takase , Takahiro Sagae , Shigeo Mori , Noriaki Kawahara
发明人： Toshiyuki Watai , Mitsuru Takase , Takahiro Sagae , Shigeo Mori , Noriaki Kawahara
IPC分类号： C07D499/08
CPC分类号： C07D499/88 , C07D317/40 , C07D499/00
摘要： There is provided a method by which various compounds (1) having a carboxyl group in the molecule have the carboxyl group converted to a (dioxolenon-4-yl)methyl ester at low cost, in a simple way and at high yield.The process for producing compounds of formula (3) according to the reaction scheme shown below comprises reacting carboxylic acids of formula (1) with 4-chloromethyldioxolenone compounds of formula (2) in a solvent in the presence of both a phase transfer catalyst and a metal iodide: [where Q represents an organic group, M represents a hydrogen atom, an alkali metal, an alkaline earth metal or a transition metal, R1 and R2 represent a hydrogen atom, an optionally substituted (C1-6 alkyl group or phenyl group)].
摘要翻译：提供了以简单的方式和高产率，分子中具有羧基的各种化合物（1）以低成本将羧基转化为（二氧戊环-4-基）甲酯的方法。根据下述反应路线制备式（3）化合物的方法包括使式（1）的羧酸与式（2）的4-氯甲基二氧戊烯酮化合物在溶剂中在相转移催化剂和金属碘化物：[其中Q表示有机基团，M表示氢原子，碱金属，碱土金属或过渡金属，R 1和R 2表示氢原子，任选取代的（C 1-6烷基或苯基）]。

10. 发明申请

US20060079496A1 Agglomerates by crystallisation 审中-公开
标题翻译：通过结晶聚集
公开(公告)号：US20060079496A1
公开(公告)日：2006-04-13
申请号：US11290185
申请日：2005-11-30
申请人： Johannes Booij , Geertruida Lefferts
发明人： Johannes Booij , Geertruida Lefferts
IPC分类号： A61K31/43 , A61K31/407 , C07D487/08
CPC分类号： C07D503/00 , A61K9/1688 , A61K31/424 , A61K31/43 , C07D499/00 , Y10T428/2982 , A61K31/42 , A61K2300/00
摘要： The present invention describes novel agglomerates in crystalline form of β-lactum compounds, Furthermore, a process for the preparation of said agglomerates, wherein a solution or suspension of at least one β-lactum compound in a solvent is mixed with one or more anti-solvents has been described.
摘要翻译：本发明描述了β-内酯化合物的结晶形式的新型附聚物。此外，制备所述附聚物的方法，其中将至少一种β-内酯化合物在溶剂中的溶液或悬浮液与一种或多种抗坏血酸混合，已经描述了溶剂。

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