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1. 发明授权

US08685957B1 Tazobactam arginine compositions 有权
标题翻译：他唑巴坦精氨酸组合物
公开(公告)号：US08685957B1
公开(公告)日：2014-04-01
申请号：US13828534
申请日：2013-03-14
申请人： Jan-Ji Lai , Jian-Qiao Gu , Pradip M. Pathare , Valdas Jurkauskas , Joseph Terracciano , Nicole Miller Damour
发明人： Jan-Ji Lai , Jian-Qiao Gu , Pradip M. Pathare , Valdas Jurkauskas , Joseph Terracciano , Nicole Miller Damour
IPC分类号： A61K31/43 , C07D499/00
CPC分类号： C07D499/897 , A61K9/19 , A61K31/403 , A61K31/4188 , A61K31/43 , A61K31/431 , A61K31/4353 , A61K31/444 , A61K31/496 , A61K31/53 , A61K31/546 , A61K31/675 , C07D499/14 , C07D499/86 , Y02A50/473
摘要： This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions.
摘要翻译：本公开提供了含有固体形式的他唑巴坦精氨酸的组合物，以及制造和使用这些组合物的方法。

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. 发明授权

US07687488B2 2-substituted methyl penam derivatives 有权
标题翻译： 2-取代甲基penam衍生物
公开(公告)号：US07687488B2
公开(公告)日：2010-03-30
申请号：US11822956
申请日：2007-07-11
申请人： Senthilkumar Udayampalayam Palanisamy , Andrew Gnanaprakasam , Panchapakesan Ganapathy , Mukut Gohain , Venkatasubramanian Hariharan , Sriram Rajagopal , Maneesh Paul-Satyaseela , Shakti Singh Solanki , Sathishkumar Devarajan
发明人： Senthilkumar Udayampalayam Palanisamy , Andrew Gnanaprakasam , Panchapakesan Ganapathy , Mukut Gohain , Venkatasubramanian Hariharan , Sriram Rajagopal , Maneesh Paul-Satyaseela , Shakti Singh Solanki , Sathishkumar Devarajan
IPC分类号： A61K31/43 , C07D499/00
CPC分类号： C07D499/86 , Y02P20/55
摘要： Novel 2-substituted methyl penam derivatives include the formula (I), their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them; wherein A=C or N; Het is a three- to seven-membered heterocyclic ring; R1 represents carboxylate anion, or —COOR4 where R4 represents hydrogen, carboxylic acid protecting group or a pharmaceutically acceptable salt; R2 and R3 may be same or different and independently represent hydrogen, halogen, amino, alkyl, protected amino, optionally substituted alkyl, alkenyl, alkynyl and the like; R represents substituted or unsubstituted alkyl, alkenyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heterocyclylalkyl.
摘要翻译：新的2-取代的甲基penam衍生物包括式（I），它们的类似物，它们的互变异构形式，它们的立体异构体，它们的多晶型物，它们的溶剂合物，其药学上可接受的盐和含有它们的药物组合物; 其中A = C或N; Het是一个三至七元的杂环; R1表示羧酸根阴离子，或-COOR4，其中R4表示氢，羧酸保护基或药学上可接受的盐; R2和R3可以相同或不同，并且独立地表示氢，卤素，氨基，烷基，保护的氨基，任选取代的烷基，烯基，炔基等; R代表取代或未取代的烷基，烯基，芳基，芳烷基，环烷基，杂环基或杂环基烷基。

4. 发明申请

US20080015156A1 Novel 2-substituted methyl penam derivatives 有权
标题翻译：新的2-取代的甲基penam衍生物
公开(公告)号：US20080015156A1
公开(公告)日：2008-01-17
申请号：US11822956
申请日：2007-07-11
申请人： Senthilkumar Udayampalayam Palanisamy , Andrew Gnanaprakasam , Panchapakesan Ganapathy , Mukut Gohain , Venkatasubramanian Hariharan , Sriram Rajagopal , Maneesh Paul-Satyaseela , Shakti Solanki , Sathishkumar Devarajan
发明人： Senthilkumar Udayampalayam Palanisamy , Andrew Gnanaprakasam , Panchapakesan Ganapathy , Mukut Gohain , Venkatasubramanian Hariharan , Sriram Rajagopal , Maneesh Paul-Satyaseela , Shakti Solanki , Sathishkumar Devarajan
IPC分类号： A61K31/431 , A61K31/7036 , A61P31/00 , C07D499/00
CPC分类号： C07D499/86 , Y02P20/55
摘要： Novel 2-substituted methyl penam derivatives include the formula (I), their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them; wherein A=C or N; Het is a three- to seven-membered heterocyclic ring; R1 represents carboxylate anion, or —COOR4 where R4 represents hydrogen, carboxylic acid protecting group or a pharmaceutically acceptable salt; R2 and R3 may be same or different and independently represent hydrogen, halogen, amino, alkyl, protected amino, optionally substituted alkyl, alkenyl, alkynyl and the like; R represents substituted or unsubstituted alkyl, alkenyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heterocyclylalkyl.
摘要翻译：新的2-取代的甲基penam衍生物包括式（I），它们的类似物，它们的互变异构形式，它们的立体异构体，它们的多晶型物，它们的溶剂合物，其药学上可接受的盐和含有它们的药物组合物; 其中A = C或N; Het是一个三至七元的杂环; R 1表示羧酸根阴离子或-COOR 4，其中R 4表示氢，羧酸保护基或其药学上可接受的盐; R 2和R 3可以相同或不同，并且独立地表示氢，卤素，氨基，烷基，保护的氨基，任选取代的烷基，烯基，炔基等; R代表取代或未取代的烷基，烯基，芳基，芳烷基，环烷基，杂环基或杂环基烷基。

5. 发明授权

US07018802B2 Electrochemiluminescent enzyme immunoassay 失效
公开(公告)号：US07018802B2
公开(公告)日：2006-03-28
申请号：US10234874
申请日：2002-09-04
申请人： Mark T. Martin , Rick Saul , Pam Liang
发明人： Mark T. Martin , Rick Saul , Pam Liang
IPC分类号： G01N33/53 , C12Q1/34 , C12N9/86 , C07D499/00
CPC分类号： G01N33/535 , C07F15/0053 , C07K16/44 , G01N33/533
摘要： Electrochemiluminescent-labels and enzyme substrates, which preferably are conjugated, are used in immunoassays and electrochemiluminescence is generated catalytically. In conventional electrochemiluminescence immunoassays, an anti-analyte antibody molecule can give rise to typically 6–8 electrochemiluminescence-active ruthenium atoms, while in the present invention, each enzyme-labeled anti-analyte molecule can give rise to thousands of electrochemiluminescence-active ruthenium atoms per second. An exemplary immunoassay is based on a catalytic process employing β-lactamase-conjugated anti-analytes which enzymatically hydrolyze electrochemiluminescent-labeled substrates, making them strongly electrochemiluminescent. The electrochemiluminescence signal generated by each anti-analyte molecule (i.e., each analyte molecule) is much greater than with the conventional method. Accordingly, greater sensitivity can be gained in the measurement of low concentrations of a given immunoassay analyte.

6. 发明授权

US06979735B1 Agglomerates by crystallization 失效
标题翻译：聚结物通过结晶
公开(公告)号：US06979735B1
公开(公告)日：2005-12-27
申请号：US09937834
申请日：2000-04-03
申请人： Johannes Booij , Ageeth Geertruida Lefferts
发明人： Johannes Booij , Ageeth Geertruida Lefferts
IPC分类号： A61K9/16 , A61K31/424 , A61K31/43 , C07D499/00 , C07D503/00 , C07D503/18
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-lactam compounds. Furthermore, a process for the preparation of said agglomerates, wherein a solution or suspension of at least one β-lactam 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-内酰胺化合物的结晶形式的新型附聚物。此外，已经描述了制备所述附聚物的方法，其中将至少一种β-内酰胺化合物在溶剂中的溶液或悬浮液与一种或多种抗溶剂混合。

7. 发明授权

US06960653B2 Method and kit for detecting, or determining the quantity of, beta-lactam penicillins 有权
标题翻译：用于检测或确定β-内酰胺青霉素数量的方法和试剂盒
公开(公告)号：US06960653B2
公开(公告)日：2005-11-01
申请号：US10211411
申请日：2002-07-31
申请人： Robert Ivan McConnell , Elouard Benchikh , Stephen Peter Fitzgerald , John Victor Lamont
发明人： Robert Ivan McConnell , Elouard Benchikh , Stephen Peter Fitzgerald , John Victor Lamont
IPC分类号： G01N33/53 , C07D499/00 , C07D499/40 , C07K16/14 , C07K16/44 , G01N33/02 , G01N33/536 , G01N33/94 , C07K16/00 , C07D499/44 , G01N33/532
CPC分类号： C07D499/00 , C07K16/44 , G01N33/9446 , G01N2415/00
摘要： The invention provides a hapten comprising a 6-[D-α-aminoacetamido] penicillin derivative crosslinked at the α-amino group with a substituted or unsubstituted phenyldicarbaldehyde. In addition, the invention provides an immunogen comprising the aforementioned hapten coupled to an antigenicity-conferring carrier material, a conjugate comprising the aforementioned hapten coupled to a labelling agent, as well as, antibodies raised against the aforementioned immunogen and capable of binding with at least one structural epitope of an intact β-lactam ring.
摘要翻译：本发明提供了包含在α-氨基与交联的取代或未取代的苯基二甲醛的6- [D-α-氨基乙酰胺基]青霉素衍生物的半抗原。此外，本发明提供了一种免疫原，其包含与产生抗原性的载体材料偶联的上述半抗原，包含与标记试剂偶联的上述半抗原的缀合物，以及针对上述免疫原产生并能够至少结合的抗体完整β-内酰胺环的一个结构表位。

8. 发明申请

US20050209450A1 Process for producing cyclic compound 有权
标题翻译：环状化合物的制备方法
公开(公告)号：US20050209450A1
公开(公告)日：2005-09-22
申请号：US10508659
申请日：2003-03-26
申请人： Akira Kaneko
发明人： Akira Kaneko
IPC分类号： C07D403/12 , C07D499/00 , C07D499/04 , C07D501/00 , C07D501/02 , C07D503/02 , C07D505/02 , C07D487/08
CPC分类号： C07D403/12 , C07D499/00 , C07D501/00
摘要： The present invention provides a method for preparing a β-lactam compound of the following Formula (3), which comprises the step of reacting a compound of the following Formula (1) with a trialkyl phosphite represented by the formula (R5O)3P (wherein R5 represents an ethyl group, etc.) in an amount of 2 to 5 moles per mole of the compound and the step of heating the resulting reaction mixture in a diluent, wherein said method is characterized by having the step of completely removing unreacted trialkyl phosphite from the reaction mixture prior to the step of heating. (wherein X represents S, etc., Y represents N, etc., n represents 0 or 1, R1 represents an optionally substituted alkyl group containing 1 to 10 carbon atoms, etc., R2 and R3 each represent an optionally substituted alkyl or heterocyclic group, etc., and R4 represents an alkenyloxy group containing 1 to 6 carbon atoms, etc., provided that R1 and R2 may together form a β-lactam ring, etc.)
摘要翻译：本发明提供了制备下式（3）的β-内酰胺化合物的方法，该方法包括下列步骤：使下式（1）的化合物与由式（R 5）表示的亚磷酸三烷基酯反应 O）3％P（其中R 5表示乙基等），每摩尔化合物为2至5摩尔，并且步骤将所得反应混合物加热到稀释剂中，其中所述方法的特征在于具有在加热步骤之前从反应混合物中完全除去未反应的亚磷酸三烷基酯的步骤。（其中X表示S等，Y表示N等，n表示0或1，R 1表示任选取代的含有1至10个碳原子的烷基等，R 0 > 2和R 3各自表示任选取代的烷基或杂环基等，R 4表示含有1至6个碳原子的链烯氧基，等等，条件是R 1和R 2可以一起形成β-内酰胺环等）

9. 发明授权

US6150350A Antimicrobial compositions 失效
标题翻译：抗微生物组合物
公开(公告)号：US6150350A
公开(公告)日：2000-11-21
申请号：US138866
申请日：1998-08-24
申请人： Peter Angehrn , Ingrid Heinze-Krauss , Malcolm Page , Hans G. F. Richter
发明人： Peter Angehrn , Ingrid Heinze-Krauss , Malcolm Page , Hans G. F. Richter
IPC分类号： C07D501/48 , A61K31/00 , A61K31/545 , A61K31/546 , A61K31/79 , A61P31/00 , A61P31/04 , C07D501/54 , C07D501/56 , C07D487/00 , C07D499/00 , C07D501/00
CPC分类号： A61K31/79
摘要： The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from carbapenem antibiotics or with .beta.-lactamase inhibitors, to the use of the compositions for producing a medicament for the treatment and prophylaxis of infectious diseases, including MRSA infections, and to pharmaceutical compositions containing the combination.
摘要翻译：本发明涉及抗微生物组合物，其包含（1）治疗有效量的式I化合物与（2）选自碳青霉烯类抗生素或β-内酰胺酶抑制剂的第二种成分的组合，用于制备用于治疗和预防感染性疾病（包括MRSA感染）的药物和含有该组合的药物组合物。

10. 发明授权

US5750684A Process for the preparatin of .beta.-lactam compounds 失效
标题翻译： β-内酰胺化合物的制备方法
公开(公告)号：US5750684A
公开(公告)日：1998-05-12
申请号：US758433
申请日：1991-08-30
申请人： Herve Geerlandt , Claudine Grand' Henry
发明人： Herve Geerlandt , Claudine Grand' Henry
IPC分类号： C07D463/00 , C07D499/00 , C07D499/04 , C07D499/21 , C07D499/72 , C07D501/04 , C07D501/57 , C07D505/00
CPC分类号： C07D499/00 , C07D505/00
摘要： The present invention provides a process for the substitution of an acylamino .beta.-lactam compound at the carbon atom carrying the acylamino group, which process comprises reacting the .beta.-lactam compound with an halogenating agent and a nucleophilic reagent; characterized in that the acylamino group has an acidic group on the carbon atom adjacent the carbonyl group. In particular the process of this invention comprises reacting a .beta.-lactam of partial structure (I): ##STR1## where X represents an acidic group; with an halogenating agent and a nucleophilic reagent.
摘要翻译：本发明提供了在携带酰基氨基的碳原子上取代酰基氨基β-内酰胺化合物的方法，该方法包括使β-内酰胺化合物与卤化剂和亲核试剂反应; 其特征在于酰氨基在与羰基相邻的碳原子上具有酸性基团。特别地，本发明的方法包括使部分结构（I）的β-内酰胺反应：其中X表示酸性基团; 与卤化剂和亲核试剂。

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