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1. 发明授权

US5534510A 2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio-carbapenem derivatives 失效
标题翻译： 2- [1-（1,3-噻唑啉-2-基）氮杂环丁烷-3-基]硫代碳代青霉烯衍生物
公开(公告)号：US5534510A
公开(公告)日：1996-07-09
申请号：US267397
申请日：1994-06-29
申请人： Takao Abe , Takeshi Isoda , Chisato Sato , Ado Mihira , Satoshi Tamai , Toshio Kumagai
发明人： Takao Abe , Takeshi Isoda , Chisato Sato , Ado Mihira , Satoshi Tamai , Toshio Kumagai
IPC分类号： C07D477/00 , A61K31/397 , A61K31/425 , A61P31/04 , C07D417/04 , C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20 , C07D417/04
摘要： Novel carbapenem compounds, (1R,5S,6S)-2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio-6-[(R)-1-hydroxyethyl]-1-methyl-carbapen-2-em-3 -carboxyic acid derivatives.These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a [1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), andY is carboxy, --COO.sup..crclbar. or protected carboxy.These compounds are useful antibiotics for prevention and treatment of bacterial infections.
摘要翻译：新的碳青霉烯化合物（1R，5S，6S）-2- [1-（1,3-噻唑烷-2-基）氮杂环丁烷-3-基]硫基-6 - [（R）-1-羟乙基] -1- 甲基 - 碳代青霉-2-烯-3-羧酸衍生物。这些碳青霉烯化合物由在1位引入的β-配位甲基和在2位引入的[1-（1,3-噻唑啉-2-基）氮杂环丁烷-3-基]硫基的下式表示 -位置。在该式中，R是氢; 低级烷基，未取代或被羟基，低级烷氧基或低级烷氧基 - 低级烷氧基取代; 基团-COOR1（R1是氢或低级烷基）; 或基团-CONR 2 R 3（R 2和R 3彼此独立地为氢或低级烷基），Y为羧基，-COO（ - ）或被保护的羧基。这些化合物是预防和治疗细菌感染的有用的抗生素。

2. 发明授权

US07018997B2 Tricyclic 6-alkylidene-penems as β-lactamase inhibitors 失效
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：US07018997B2
公开(公告)日：2006-03-28
申请号：US10427427
申请日：2003-05-01
申请人： Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Takao Abe , Ado Mihira , Atul Agarwal , Hideki Ushirogochi , Yansong Gu , Satoshi Tamai , Fuk-Wah Sum
发明人： Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Takao Abe , Ado Mihira , Atul Agarwal , Hideki Ushirogochi , Yansong Gu , Satoshi Tamai , Fuk-Wah Sum
IPC分类号： C07D499/881 , C07D519/06 , A61K31/43 , A61K31/431 , A61P31/04
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. wherein one of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S.
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。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; 而X是S.

3. 发明授权

US07691842B2 Tricyclic 6-alkylidene-penems as β-lactamase inhibitors 失效
标题翻译：三环6-亚烷基 - 半乳糖和β-内酰胺酶抑制剂
公开(公告)号：US07691842B2
公开(公告)日：2010-04-06
申请号：US12187707
申请日：2008-08-07
申请人： Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Takao Abe , Ado Mihira , Atul Agarwal , Hideki Ushirogochi , Yansong Gu , Satoshi Tamai , Fuk-Wah Sum
发明人： Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Takao Abe , Ado Mihira , Atul Agarwal , Hideki Ushirogochi , Yansong Gu , Satoshi Tamai , Fuk-Wah Sum
IPC分类号： C07D503/10 , C07D519/06 , A61P31/04 , A61K31/424 , A61K31/43 , A61K31/431 , C07D499/881
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, wherein one of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is O.
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，其中A和B之一表示氢，另一个为任选取代的稠合三环杂芳基; 而X是O.

4. 发明申请

US20080318921A1 Tricyclic 6-Alkylidene-Penems as Beta-Lactamase Inhibitors 失效
标题翻译：作为β-内酰胺酶抑制剂的三环6-亚烷基 - 半乳糖
公开(公告)号：US20080318921A1
公开(公告)日：2008-12-25
申请号：US12187707
申请日：2008-08-07
申请人： Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Takao Abe , Ado Mihira , Atul Agarwal , Hideki Ushirogochi , Yansong Gu , Satoshi Tamai , Fuk-Wah Sum
发明人： Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Takao Abe , Ado Mihira , Atul Agarwal , Hideki Ushirogochi , Yansong Gu , Satoshi Tamai , Fuk-Wah Sum
IPC分类号： C07D503/10 , 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。

5. 发明授权

US5783703A Sulfur-containing compounds method for their use and prodction 失效
标题翻译：含硫化合物的使用和生产方法
公开(公告)号：US5783703A
公开(公告)日：1998-07-21
申请号：US795428
申请日：1997-02-05
申请人： Kazuhiko Hayashi , Chisato Sato , Satoshi Tamai , Takao Abe , Takeshi Isoda , Ado Mihira , Toshio Kumagai
发明人： Kazuhiko Hayashi , Chisato Sato , Satoshi Tamai , Takao Abe , Takeshi Isoda , Ado Mihira , Toshio Kumagai
IPC分类号： C07D417/04
CPC分类号： C07D417/04
摘要： A first embodiment of the invention relates to novel carbapenem compounds, (1R, 5S, 6S)-2-�1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-6-�(R)-1-hydroxy-ethyl!-1-methylcarbapen-2-em-3-carboxyic acid derivatives. These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a �1-(1,3-thia-zolin-2-yl)azetidin-3-yl!thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), and Y is carboxy, --COO.sup..crclbar. or protected carboxy. These compounds are useful antibiotics for prevention and treatment of bacterial infections. The second embodiment of the invention relates to 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine represented by the following formula and its acid addition salts ##STR2## and to the production process therefor. The above compounds are useful as intermediates for preparing carbapenem compounds, which have strong antibacterial activity, with convenience and high yield.
摘要翻译：本发明的第一个实施方案涉及新的碳青霉烯化合物，（1R，5S，6S）-2- [1-（1,3-噻唑烷-2-基）氮杂环丁烷-3-基]硫基-6 - [（R） -1-羟基 - 乙基] -1-甲基碳代青霉-2-烯-3-羧酸衍生物。这些碳青霉烯类化合物由下式表示：在1-位引入的β-配位甲基和[1-（1,3-硫杂 - 唑啉-2-基）氮杂环丁烷-3-基]硫基引入到 2位。在该式中，R是氢; 低级烷基，未取代或被羟基，低级烷氧基或低级烷氧基 - 低级烷氧基取代; 基团-COOR1（R1是氢或低级烷基）; 或基团-CONR 2 R 3（R 2和R 3彼此独立地为氢或低级烷基），Y为羧基，-COO（ - ）或被保护的羧基。这些化合物是预防和治疗细菌感染的有用的抗生素。本发明的第二个实施方案涉及由下式表示的3-巯基-1-（1,3-噻唑啉-2-基）氮杂环丁烷及其酸加成盐及其制备方法。上述化合物可用作制备碳青霉烯类化合物的中间体，其具有强的抗菌活性，方便性和高产率。

6. 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。

7. 发明授权

US5679790A 2-�1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-carbapenem derivatives 失效
标题翻译： 2- [1-（1,3-噻唑啉-2-基）氮杂环丁烷-3-基]硫代碳代青霉烯衍生物
公开(公告)号：US5679790A
公开(公告)日：1997-10-21
申请号：US631224
申请日：1996-04-12
申请人： Takao Abe , Takeshi Isoda , Chisato Sato , Ado Mihira , Satoshi Tamai , Toshio Kumagai
发明人： Takao Abe , Takeshi Isoda , Chisato Sato , Ado Mihira , Satoshi Tamai , Toshio Kumagai
IPC分类号： C07D477/00 , A61K31/397 , A61K31/425 , A61P31/04 , C07D417/04 , C07D477/20 , C07D487/04
CPC分类号： C07D477/20 , C07D417/04
摘要： Novel carbapenem compounds, (1R,5S,6S)-2-�1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-6-�(R)-1-hydroxyethyl!-1-methyl-carbapen-2-em-3-carboxyic acid derivatives. These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a �1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), and Y is carboxy, --COO.sup..crclbar. or protected carboxy. These compounds are useful antibiotics for prevention and treatment of bacterial infections.
摘要翻译：新型碳青霉烯化合物（1R，5S，6S）-2- [1-（1,3-噻唑烷-2-基）氮杂环丁烷-3-基]硫基-6 - [（R）-1-羟基乙基] -1 - 甲基 - 碳代青霉-2-烯-3-羧酸衍生物。这些碳青霉烯化合物由在1位引入的β-配位甲基和在2位引入的[1-（1,3-噻唑啉-2-基）氮杂环丁烷-3-基]硫基的下式表示 -位置。在该式中，R是氢; 低级烷基，未取代或被羟基，低级烷氧基或低级烷氧基 - 低级烷氧基取代; 基团-COOR1（R1是氢或低级烷基）; 或基团-CONR 2 R 3（R 2和R 3彼此独立地为氢或低级烷基），Y为羧基，-COO（ - ）或被保护的羧基。这些化合物是预防和治疗细菌感染的有用的抗生素。

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