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公开(公告)号：EP1671975B1
公开(公告)日：2011-02-09
申请号：EP04792516.9
申请日：2004-10-08
发明人： TOKUMARU, Yoshihisa, OTSUKA CHEMICAL CO., LTD. , SHIMABAYASHI, Akihiro, OTSUKA CHEMICAL CO., LTD.
IPC分类号： C07D499/00
CPC分类号： C07D499/86
摘要： Novel 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester (TMPB)-acetone crystals for use in producing 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid 1,1-dioxide benzhydryl ester (TAZB); a process for producing TMPB-acetone crystals which comprises (A) the step of concentrating an organic solvent solution containing TMPB, (B) the step of dissolving the resultant concentrate in acetone, and (C) the step of crystallizing TMPB-acetone crystals from the acetone solution obtained; and a process for producing TAZB which comprises the step of reacting TMPB-acetone crystals with an oxidizing agent.
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公开(公告)号：EP1671974A4
公开(公告)日：2007-02-28
申请号：EP04773756
申请日：2004-10-08
发明人： WADA ISAO , KAMEYAMA YUTAKA
IPC分类号： C07D499/00 , C07D499/86
CPC分类号： C07D499/86
摘要： 2β-chloromethyl-2α-methylpenam-3α-carboxylic acid benzhydryl ester (CMPB) crystals having excellent stability; and a process for producing CMPB crystals which comprises (A) the step of concentrating a CMPB-containing solution, (B) the step of subjecting the resultant concentrate to column chromatography, (C) the step of concentrating a CMPB-containing fraction, and (D) the step of dissolving the resultant CMPB-containing concentrate in an ether solvent and subsequently adding a hydrocarbon solvent to this solution to precipitate CMPB crystals.
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公开(公告)号：EP2892903A1
公开(公告)日：2015-07-15
申请号：EP13835071.5
申请日：2013-09-05
发明人： VENUGOPAL, Sivasankaran , ANANDAN, Sakthivel , UDAYAMPALAYAM PALANISAMY, Senthilkumar , RAJAMANICKAM, Kannadhasan , VELRAJ, Loganathan , SINGARAVEL, Mohan
IPC分类号： C07D499/87
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. (Formula I) (I)
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公开(公告)号：EP2046802B1
公开(公告)日：2013-08-21
申请号：EP07804590.3
申请日：2007-07-11
发明人： UDAYAMPALAYAM, Palanisamy, Senthilkumar , GNANAPRAKASAM, Andrew , GANAPATHY, Panchapakesan , MUKUT, Gohain , VENKATASUBRAMANIAN, Hariharan , SRIRAM, Rajagopal , PAUL-SATYASEELA, Maneesh , SOLANKI, Shakti, Singh , DEVARAJAN, Sathishkumar
IPC分类号： C07D499/87 , C07D499/21 , C07D499/28 , C07D499/32 , A61K31/431 , A61P31/00
CPC分类号： C07D499/86 , Y02P20/55
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公开(公告)号：EP2892903A4
公开(公告)日：2016-01-27
申请号：EP13835071
申请日：2013-09-05
申请人： HOSPIRA INC
发明人： VENUGOPAL SIVASANKARAN , ANANDAN SAKTHIVEL , UDAYAMPALAYAM PALANISAMY SENTHILKUMAR , RAJAMANICKAM KANNADHASAN , VELRAJ LOGANATHAN , SINGARAVEL MOHAN
IPC分类号： C07D499/87 , C07D499/06 , C07D499/08
CPC分类号： C07D499/86 , C07D499/00 , C07D499/06 , C07D499/08
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6.发明公开HIGH PENETRATION COMPOSITIONS OR PRODRUGS OF ANTIMICROBIALS AND ANTIMICROBIAL-RELATED COMPOUNDS 审中-公开具有很强的穿透力或前药抗MICRO BIEN和连接与杀伤MICRO BIEN组成
公开(公告)号：EP2440523A1
公开(公告)日：2012-04-18
申请号：EP10785754.2
申请日：2010-06-10
发明人： XU, Lina , CHEN, Yuhua , YAN, Binbing , TU, Shiqian , YU, Chongxi
IPC分类号： C07D205/12 , C07D277/60 , C07D211/26 , C07D211/16 , A61K31/397 , A61K31/43 , A61K31/545 , A61P31/00 , A61P31/04
CPC分类号： C07D499/52 , C07D213/76 , C07D215/233 , C07D471/04 , C07D499/46 , C07D499/62 , C07D499/68 , C07D499/74 , C07D499/76 , C07D499/86 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/59 , C07D503/18
摘要： High penetration comp1ositions (HPCs) or prodrugs (HPPs) of antimicrobials and antimicrobial-related compounds are provided. The HPCs/HPPs are capable of being converted to parent drugs or drug metabolites after crossing the biological barrier and thus can render treatments. Additionally, the HPCs/HPPs are capable of reaching areas that their parent drugs may not be able to access and rendering a sufficient concentration at the target areas and therefore render novel treatments.
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公开(公告)号：EP1671975A4
公开(公告)日：2007-03-14
申请号：EP04792516
申请日：2004-10-08
IPC分类号： C07D499/00 , C07D499/04 , C07D499/86 , C07D499/87 , C07D499/897
CPC分类号： C07D499/86
摘要： Novel 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester (TMPB)-acetone crystals for use in producing 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid 1,1-dioxide benzhydryl ester (TAZB); a process for producing TMPB-acetone crystals which comprises (A) the step of concentrating an organic solvent solution containing TMPB, (B) the step of dissolving the resultant concentrate in acetone, and (C) the step of crystallizing TMPB-acetone crystals from the acetone solution obtained; and a process for producing TAZB which comprises the step of reacting TMPB-acetone crystals with an oxidizing agent.
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公开(公告)号：EP2046802A4
公开(公告)日：2010-06-02
申请号：EP07804590
申请日：2007-07-11
发明人： UDAYAMPALAYAM PALANISAMY SENTH , GNANAPRAKASAM ANDREW , GANAPATHY PANCHAPAKESAN , MUKUT GOHAIN , VENKATASUBRAMANIAN HARIHARAN , SRIRAM RAJAGOPAL , PAUL-SATYASEELA MANEESH , SOLANKI SHAKTI SINGH , DEVARAJAN SATHISHKUMAR
IPC分类号： C07D499/87 , A61K31/431 , A61P31/00 , C07D499/21 , C07D499/28 , C07D499/32
CPC分类号： C07D499/86 , Y02P20/55
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公开(公告)号：EP2046802A2
公开(公告)日：2009-04-15
申请号：EP07804590.3
申请日：2007-07-11
发明人： UDAYAMPALAYAM, Palanisamy, Senthilkumar , GNANAPRAKASAM, Andrew , GANAPATHY, Panchapakesan , MUKUT, Gohain , VENKATASUBRAMANIAN, Hariharan , SRIRAM, Rajagopal , PAUL-SATYASEELA, Maneesh , SOLANKI, Shakti, Singh , DEVARAJAN, Sathishkumar
IPC分类号： C07D499/87 , C07D499/21 , C07D499/28 , C07D499/32
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.
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10.发明公开
公开(公告)号：EP1671975A1
公开(公告)日：2006-06-21
申请号：EP04792516.9
申请日：2004-10-08
发明人： TOKUMARU, Yoshihisa, OTSUKA CHEMICAL CO., LTD. , SHIMABAYASHI, Akihiro, OTSUKA CHEMICAL CO., LTD.
IPC分类号： C07D499/00
CPC分类号： C07D499/86
摘要： The present invention provides novel 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester (TMPB)-acetone crystals for use in the production of 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid 1,1-dioxide benzhydryl ester (TAZB); a process for producing the TMPB-acetone crystals comprising the steps of (A) concentrating a TMPB-containing organic solvent solution, (B) dissolving the resulting concentrate in acetone, and (C) precipitating TMPB-acetone crystals from the acetone solution thus obtained; and a process for producing TAZB comprising the step of reacting the TMPB-acetone crystals with an oxidizing agent.
摘要翻译： 本发明提供了用于生产2的新的2±甲基-2 - [（1,2,3-三唑-1-基）甲基]己内酰胺-3β-羧酸二苯甲酸酯（TMPB） - 丙酮晶体 ± - 甲基-2 - [（1,2,3-三唑-1-基）甲基] penam-3± - 羧酸1,1-二氧化二苯甲酸酯（TAZB）; 制备TMPB-丙酮晶体的方法包括以下步骤：（A）浓缩含TMPB的有机溶剂溶液，（B）将所得浓缩物溶于丙酮中，和（C）从所得丙酮溶液中沉淀TMPB-丙酮晶体 ; 以及一种制备TAZB的方法，包括使TMPB-丙酮晶体与氧化剂反应的步骤。
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