公开(公告)号：US10201532B2

公开(公告)日：2019-02-12

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 ,  Hariharan Periasamy

发明人： Senthilkumar Udayampalayam Palanisamy ,  Maneesh Paul-Satyaseela ,  Shridhar Narayanan ,  Gopalan Balasubramanian ,  Aravind Appu ,  Senthilnathan Manickam ,  Hariharan Periasamy

IPC分类号： A61K31/431 ,  C07D499/883 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/496 ,  A61K31/542 ,  C07D499/00 ,  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)

公开(公告)号：US20090093423A2

公开(公告)日：2009-04-09

申请号：US11822956

申请日：2007-07-11

申请人： Senthilkumar UDAYAMPALAYAMPALANISAMY ,  Andrew GNANAPRAKASAM ,  Panchapakesan GANAPATHY ,  Mukut GOHAIN ,  Venkatasubramanian HARIHARAN ,  Sriram RAJAGOPAL ,  Maneesh PAUL-SATYASEELA ,  Shakti SINGH SOLANKI ,  Sathishkumar DEVARAJAN

发明人： Senthilkumar UDAYAMPALAYAMPALANISAMY ,  Andrew GNANAPRAKASAM ,  Panchapakesan GANAPATHY ,  Mukut GOHAIN ,  Venkatasubramanian HARIHARAN ,  Sriram RAJAGOPAL ,  Maneesh PAUL-SATYASEELA ,  Shakti SINGH 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; 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。

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）

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。

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。