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1. 发明申请

US20060217361A1 Bicyclic 6-alkylidene-penems as beta-lactamase inhibitors 审中-公开
标题翻译：双环6-亚烷基 - 青霉烯作为β-内酰胺酶抑制剂
公开(公告)号：US20060217361A1
公开(公告)日：2006-09-28
申请号：US11447814
申请日：2006-06-06
申请人： Aranapakam Venkatesan , Tarek Mansour , Takao Abe , Itsuki Yamamura , Tsuyoshi Takasaki , Atul Agarwal , Osvaldo Santos , Fuk-Wah Sum , Yang-I Lin
发明人： Aranapakam Venkatesan , Tarek Mansour , Takao Abe , Itsuki Yamamura , Tsuyoshi Takasaki , Atul Agarwal , Osvaldo Santos , Fuk-Wah Sum , Yang-I Lin
IPC分类号： A61K31/424 , A61K31/43 , C07D499/00
CPC分类号： C07D519/00 , C07D499/861 , C07D499/88 , C07D503/00
摘要： The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
摘要翻译：本发明提供式I化合物，药物组合物及其在有需要的患者中治疗细菌感染或疾病的用途。

2. 发明申请

US20060074064A1 Tricyclic 6-alkylidene-penems as beta-lactamase inhibitors 审中-公开
标题翻译：三环6-亚烷基 - 青霉烯作为β-内酰胺酶抑制剂
公开(公告)号：US20060074064A1
公开(公告)日：2006-04-06
申请号：US11283288
申请日：2005-11-18
申请人： Aranapakam Venkatesan , Tarek Mansour , Takao Abe , Ado Mihira , Atul Agarwal , Hideki Ushirogochi , Yansong Gu , Satoshi Tamai , Fuk-Wah Sum
发明人： Aranapakam Venkatesan , Tarek Mansour , Takao Abe , Ado Mihira , Atul Agarwal , Hideki Ushirogochi , Yansong Gu , Satoshi Tamai , Fuk-Wah Sum
IPC分类号： C07D499/48 , A61K31/43 , A61K31/424
CPC分类号： C07D519/00
摘要： The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
摘要翻译：本发明提供式I化合物，药物组合物及其在有需要的患者中治疗细菌感染或疾病的用途。

3. 发明申请

US20070232582A1 4-substituted or unsubtituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic heteroaryl] substituted-3,6-dicarboxylic acid derivatives as beta-lactamase inhibitors 审中-公开
标题翻译： 4-取代或未取代的7-氢-1,4-硫杂氮-7- [双环或三环杂芳基]取代-3,6-二羧酸衍生物作为β-内酰胺酶抑制剂
公开(公告)号：US20070232582A1
公开(公告)日：2007-10-04
申请号：US11807397
申请日：2007-05-25
申请人： Tarek Mansour , Aranapakam Venkatesan
发明人： Tarek Mansour , Aranapakam Venkatesan
IPC分类号： A61K31/554 , A61K31/426 , A61K31/43 , A61K31/5365 , A61K31/545
CPC分类号： A61K31/426 , A61K31/43 , A61K31/5365 , A61K31/545 , A61K31/554
摘要： The present invention relates to novel, low molecular weight broad spectrum compounds in particular to a class of 4-substituted or unsubstituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic heteroaryl] substituted-3,6-dicarboxylic acid or their derivatives which have β-lactamase inhibitory and antibacterial properties. The compounds are therefore useful in the treatment of antibacterial infections in humans or animals, either alone or in combination with other antibiotics.
摘要翻译：本发明涉及新的低分子量宽谱化合物，特别涉及一类4-取代或未取代的7-氢-1,4-硫杂氮杂-7- [二环或三环杂芳基]取代-3,6-二羧酸酸或其衍生物具有β-内酰胺酶的抑制和抗菌性能。因此，该化合物可用于单独或与其它抗生素联合治疗人或动物中的抗菌感染。

4. 发明申请

US20070027130A1 Tricyclic 6-alkylidene-penem beta-lactamase inhibitors and beta-lactam antibiotic combination: a broad spectrum antibiotic 审中-公开
标题翻译：三环6-亚烷基 - 半乳糖β-内酰胺酶抑制剂和β-内酰胺抗生素组合：广谱抗生素
公开(公告)号：US20070027130A1
公开(公告)日：2007-02-01
申请号：US11493331
申请日：2006-07-26
申请人： Tarek Mansour , Aranapakam Venkatesan , Patricia Bradford , Peter Petersen , Steven Projan
发明人： Tarek Mansour , Aranapakam Venkatesan , Patricia Bradford , Peter Petersen , Steven Projan
IPC分类号： A61K31/424 , A61K31/43
CPC分类号： A61K45/06 , A61K31/424 , A61K31/43 , A61K31/431 , A61K2300/00
摘要： The present invention provides a β-lactam antibiotic such as cefepime and a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
摘要翻译：本发明提供β-内酰胺抗生素如头孢吡肟和式I化合物，药物组合物及其用于治疗有需要的患者的细菌感染或疾病的用途。

5. 发明申请

US20080009634A1 Process for synthesizing beta-lactamase inhibitor intermediates 审中-公开
标题翻译： β-内酰胺酶抑制剂中间体的合成方法
公开(公告)号：US20080009634A1
公开(公告)日：2008-01-10
申请号：US11820575
申请日：2007-06-18
申请人： Michael Winkley , Anita Chan , Ivo Jirkovsky , Kenneth Kremer , Joseph Zeldis , Antonia Nikitenko , Henry Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam Venkatesan
发明人： Michael Winkley , Anita Chan , Ivo Jirkovsky , Kenneth Kremer , Joseph Zeldis , Antonia Nikitenko , Henry Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam Venkatesan
IPC分类号： C07D277/60 , C07D487/04
CPC分类号： C07D498/04 , C07D487/04
摘要： There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.
摘要翻译：提供了一种制备具有结构式I的双环杂芳基羧醛的方法，其中X和Y在说明书中定义。双环杂芳基羧醛可用作制备β-内酰胺酶抑制剂的中间体。

6. 发明申请

US20060276445A1 Bicyclic 6-alkylidene-penems as class-D beta-lactamases inhibitors 审中-公开
标题翻译：双环6-亚烷基 - 半乳糖作为D类β-内酰胺酶抑制剂
公开(公告)号：US20060276445A1
公开(公告)日：2006-12-07
申请号：US11444344
申请日：2006-05-31
申请人： Tarek Mansour , Aranapakam Venkatesan
发明人： Tarek Mansour , Aranapakam Venkatesan
IPC分类号： A61K31/43 , A61K31/424
CPC分类号： A61K31/43 , A61K31/424 , A61K31/429 , A61K2300/00
摘要： This invention relates to certain bicyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. In accordance with the present invention there are provided compounds of general formula I or a pharmaceutically acceptable salt or in vivo hydrolyzable ester R5 thereof: wherein: One of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X═O or S.
摘要翻译：本发明涉及作为D类酶抑制剂的某些二环-6-亚烷基半胱氨酸。 β-内酰胺酶水解β-内酰胺抗生素，因此成为细菌耐药的主要原因。当与β-内酰胺抗生素组合时，本发明的化合物将提供有效治疗以防止威胁生命的细菌感染。根据本发明，提供通式I的化合物或其药学上可接受的盐或体内可水解的酯R 5：其中：A和B中的一个表示氢，另一个是任选取代的稠合双环杂芳基; 和X-O或S.

7. 发明申请

US20060276446A1 Tricyclic 6-alkylidene-penems as class-D beta-lactamases inhibitors 审中-公开
标题翻译：作为D类β-内酰胺酶抑制剂的三环6-亚烷基 - 青霉烯
公开(公告)号：US20060276446A1
公开(公告)日：2006-12-07
申请号：US11444346
申请日：2006-05-31
申请人： Tarek Mansour , Aranapakam Venkatesan
发明人： Tarek Mansour , Aranapakam Venkatesan
IPC分类号： A61K31/43 , A61K31/424
CPC分类号： A61K31/424 , A61K31/43 , Y02A50/473
摘要： This invention relates to certain tricyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. In accordance with the present invention there are provided compounds of formula I which are useful for treatment of bacterial infections having class-D enzymes associated therewith: wherein: One of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S or O.
摘要翻译：本发明涉及作为D类酶抑制剂的某些三环6-亚烷基半胱氨酸。 β-内酰胺酶水解β-内酰胺抗生素，因此成为细菌耐药的主要原因。当与β-内酰胺抗生素组合时，本发明的化合物将提供有效治疗以防止威胁生命的细菌感染。根据本发明，提供了可用于治疗与其相关的D类酶的细菌感染的式I化合物：其中：A和B之一表示氢，另一个表示任选取代的稠合三环杂芳基; X为S或O.

8. 发明申请

US20070129344A1 Bicyclic 6-alkylidene-penem beta-lactamase inhibitors and beta-lactam antibiotic combination: a broad spectrum antibiotic 审中-公开
标题翻译：双环6-亚烷基 - 半乳糖β-内酰胺酶抑制剂和β-内酰胺抗生素组合：广谱抗生素
公开(公告)号：US20070129344A1
公开(公告)日：2007-06-07
申请号：US11493178
申请日：2006-07-26
申请人： Tarek Mansour , Aranapakam Venkatesan , Patricia Bradford , Peter Petersen , Steven Projan
发明人： Tarek Mansour , Aranapakam Venkatesan , Patricia Bradford , Peter Petersen , Steven Projan
IPC分类号： A61K31/424 , A61K31/43
CPC分类号： A61K31/424 , A61K31/429 , A61K31/43 , A61K31/546 , Y02A50/473 , A61K2300/00
摘要： The present invention provides a β-lactam antibiotic such as cefepime and a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
摘要翻译：本发明提供β-内酰胺抗生素如头孢吡肟和式I化合物，药物组合物及其用于治疗有需要的患者的细菌感染或疾病的用途。

9. 发明授权

US06649756B2 PROCESS IMPROVEMENT IN THE PREPARATION OF (4R, 5S, 6S)-3-[[(2R,3R)-2-[[[(S)-2-AMINO-3-METHYL-1-OXOBUTYL]AMINO]METHYL]TETRAHYDRO-3-FURANYL]THIO]-6-[(R)-1-HYDROXYETHYL]-4-METHYL-7-OXO-1-AZABICYCLO[3.2.0]HEPT-2-ENE-2-CARBOXYLIC ACID 失效
标题翻译：（4R，5S，6S）-3 - [[（2R，3R）-2 - [[（S）-2-氨基-3-甲基-1-氧代丁基]氨基]甲基]四氢呋喃的制备中的工艺改进 -3-FURANYL] THIO] -6 - [（R）-1-羟基乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0] HEPT-2-环己基-2-羧酸
公开(公告)号：US06649756B2
公开(公告)日：2003-11-18
申请号：US09901335
申请日：2001-07-09
申请人： Tarek Mansour , Phaik-Eng Sum , Yang-I Lin , Zhong Li
发明人： Tarek Mansour , Phaik-Eng Sum , Yang-I Lin , Zhong Li
IPC分类号： C07D47720
CPC分类号： C07D477/20 , C07D477/08
摘要： The invention is a process improvement for producing the carbapenem antibacterial agent (4R, 5S, 6S)-3-[[2R,3R)-2-[[[(S)-2-amino-3-methyl-1-oxobutyl]amino]methyl]tetrahydro-3-furanyl]thio]-6-[R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid by hydrogenation of 4-nitrobenzyl (4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-3-{[2R,3R)-2-({[(2S)-3-methyl-2-({[4-nitrobenzyl)oxy]carbonyl}amino)butanoyl]amino}methyl)-tetrahydrofuran-3-yl]thio}-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate in a biphasic solvent mixture comprising a water portion and an organic solvent portion, not containing an acid acceptor. The water portion is separated from the organic solvent portion and (4R,5S,6S)-3-[[(2R,3R)-2-[[[(S)-2-amino-3-methyl-1-oxobutyl]amino]methyl]tetrahydro-3-furanyl]thio]-6-[R-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid is isolated from the separated water portion by lyophilization or reverse osmosis.
摘要翻译：本发明是用于生产碳青霉烯类抗菌剂（4R，5S，6S）-3 - [[2R，3R）-2 - [[[（S）-2-氨基-3-甲基-1-氧代丁基] 氨基]甲基]四氢-3-呋喃基]硫基] -6- [R）-1-羟乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸通过氢化（4R，5S，6S）-6 - [（1R）-1-羟乙基] -4-甲基-3 - {[2R，3R）-2 - （{[（2S）-3- 甲基-2 - （{[4-硝基苄基）氧基]羰基}氨基）丁酰基]氨基}甲基） - 四氢呋喃-3-基]硫代} -7-氧代-1-氮杂双环[3.2.0]庚-2-烯 -2-羧酸酯在包含水部分和不含酸受体的有机溶剂部分的双相溶剂混合物中。将水部分与有机溶剂部分分离，和（4R，5S，6S）-3 - [[（2R，3R）-2 - [[[（S）-2-氨基-3-甲基-1-氧代丁基] 氨基]甲基]四氢-3-呋喃基]硫基] -6- [R-羟乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸从分离的水部分通过冻干或反渗透。

10. 发明授权

US5693787A Intermediates in the synthesis of 1,3-oxathiolanyl cytosine nucleoside analogues 失效
标题翻译：中间体合成1,3-氧硫杂环戊烷胞嘧啶核苷类似物
公开(公告)号：US5693787A
公开(公告)日：1997-12-02
申请号：US464317
申请日：1995-06-05
申请人： Tarek Mansour , Haolun Jin , Allan H. L. Tse , M. Arshad Siddiqui
发明人： Tarek Mansour , Haolun Jin , Allan H. L. Tse , M. Arshad Siddiqui
IPC分类号： C07H19/00 , A61K31/513 , A61P31/12 , B01J31/02 , C07B53/00 , C07B61/00 , C07C13/10 , C07D20060101 , C07D207/00 , C07D231/04 , C07D233/02 , C07D261/02 , C07D263/04 , C07D275/02 , C07D277/04 , C07D285/04 , C07D291/04 , C07D307/04 , C07D307/16 , C07D307/18 , C07D307/24 , C07D317/08 , C07D317/24 , C07D317/32 , C07D317/34 , C07D323/02 , C07D327/04 , C07D333/48 , C07D339/02 , C07D339/06 , C07D341/00 , C07D403/04 , C07D405/04 , C07D407/04 , C07D409/04 , C07D411/04 , C07D411/12 , C07D411/14 , C07D413/04 , C07D419/04 , C07D471/00 , C07D473/00 , C07D473/06 , C07D473/30 , C07D473/34 , C07H19/04 , C07H19/06 , C07H19/16 , C07D333/36 , C07D333/42
CPC分类号： C07D405/04 , C07D307/24 , C07D317/32 , C07D317/34 , C07D327/04 , C07D339/06 , C07D409/04 , C07D411/04 , C07H19/04 , C07H19/06 , C07H19/16
摘要： The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes.
摘要翻译：本发明涉及用于生产高光学纯度的顺式核苷和核苷类似物和衍生物的高度非对映选择性方法以及在这些方法中有用的中间体。

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