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11. 发明授权

US06825199B2 7-Substituted quinazolin-2,4-diones useful as antibacterial agents 失效
标题翻译： 7-取代喹唑啉-2,4-二酮可用作抗菌剂
公开(公告)号：US06825199B2
公开(公告)日：2004-11-30
申请号：US09971343
申请日：2001-10-04
申请人： John Michael Domagala , Edmund Lee Ellsworth , Liren Huang , Thomas Eric Renau , Rajeshwar Singh , Michael Andrew Stier
发明人： John Michael Domagala , Edmund Lee Ellsworth , Liren Huang , Thomas Eric Renau , Rajeshwar Singh , Michael Andrew Stier
IPC分类号： C07D23996
CPC分类号： C07D403/04 , C07D239/96 , C07D471/04 , C07D471/06
摘要： The invention is a series of 7-substituted quinazolin-2,4-diones useful as antibacterial agents, processes for the preparation of the compounds, and a pharmaceutical composition containing one or more of the compounds.
摘要翻译：本发明是用作抗菌剂的一系列7-取代喹唑啉-2,4-二酮，用于制备化合物的方法和含有一种或多种化合物的药物组合物。

12. 发明授权

US06177423B1 Isoquinolones 失效
标题翻译：异喹诺酮类
公开(公告)号：US06177423B1
公开(公告)日：2001-01-23
申请号：US09254645
申请日：1999-03-12
申请人： Albert Kudzoi Amegadzie , Maureen Elizabeth Carey , John Michael Domagala , Liren Huang , Ronald George Micetich , Joseph Peter Sanchez , Rajeshwar Singh , Michael Andrew Stier , Arkadii Vaisburg
发明人： Albert Kudzoi Amegadzie , Maureen Elizabeth Carey , John Michael Domagala , Liren Huang , Ronald George Micetich , Joseph Peter Sanchez , Rajeshwar Singh , Michael Andrew Stier , Arkadii Vaisburg
IPC分类号： A61K31535
CPC分类号： C07D221/14 , C07D401/04 , C07D491/06 , Y02P20/55
摘要： Benzo[de]isoquinoline-1,3-dione of Formula or a pharmaceutically acceptable salt thereof wherein R is hydrogen or a protecting group typically used in the art for protecting alcohols and R1-R5 are each independently chosen from H, Cl, Br, F, straight or branched alkyl C1-C8 alkyl, C3-C8 cycloalkyl, heterocycle or bridged heterocycle of 4-9 atoms containing 1-3 heteroatoms, —(CR′2)nOR6, —(CR′2)nN(R6)2, —(CR′2)nNR6COR7, —(CR′2)nNR6SO2OR7, —(CR′2)nNR6SO2 N(R6)2, —(CR′2)nOSO2 N(R6)2, —(CR′2)nCN, —(CR′2)n(NOR6)R7, NO2, CF3, —(CR′2)nSOmR7, —(CR′2)nSOmR7, —(CR′2)nCO2R6, —(CR′2)nCON(R6)2, Ph, and any two of R1-R5 may form a substituted or unsubstituted ring of 5-7 total atoms having 0-2 heteroatoms are claimed which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents. Methods for their preparation and formulation as well as novel intermediates useful in the preparation of the final products are also claimed.
摘要翻译：配方的苯并[de]异喹啉-1,3-二酮其药学上可接受的盐，其中R为氢或本领域通常用于保护醇和R 1 -R 5的保护基各自独立地选自H，Cl，Br，F ，含有1-3个杂原子的4-9个原子的直链或支链烷基C1-C8烷基，C3-C8环烷基，杂环或桥连杂环， - （CR'2）nOR6， - （CR'2）nN（R6）2， - （CR'2）nNR6COR7， - （CR'2）nNR6SO2OR7， - （CR'2）nNR6SO2N（R6）2， - （CR'2）nOSO2 N（R6）2， - （CR'2） - （CR'2）n（NOR6）R7，NO2，CF3， - （CR'2）nSOmR7， - （CR'2）nSOmR7， - （CR'2）nCO2R6， - （CR'2）nCON（R6） 2，Ph和R 1 -R 5中的任何两个可以形成5-7个总原子的取代或未取代的环，其具有0-2个杂原子，其是细菌DNA促旋酶的选择性抑制剂和可用于抗菌剂的DNA拓扑异构酶。还要求保护其制备和制剂的方法以及用于制备最终产品的新型中间体。

13. 发明申请

US20110136763A1 TRISUBSTITUTED BORON-CONTAINING MOLECULES 有权
标题翻译：含有分子量的含硼分子
公开(公告)号：US20110136763A1
公开(公告)日：2011-06-09
申请号：US12844748
申请日：2010-07-27
申请人： Yi Xia , Michael Richard Kevin Alley , Yasheen Zhou , Rajeshwar Singh , Charles Ding , Kathy Cao , Jacob J. Plattner , Ligong Ou , Guofeng Jia , Neerja Saraswat , Sreekanth Ramachandran , Ding Zhou
发明人： Yi Xia , Michael Richard Kevin Alley , Yasheen Zhou , Rajeshwar Singh , Charles Ding , Kathy Cao , Jacob J. Plattner , Ligong Ou , Guofeng Jia , Neerja Saraswat , Sreekanth Ramachandran , Ding Zhou
IPC分类号： A61K31/69 , C07F5/04 , A01N55/08 , C12N9/99 , A01P1/00 , A61P31/04
CPC分类号： C07F5/025 , A61K31/69 , A61K45/06 , A61K2300/00
摘要： This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections.
摘要翻译：本发明主要涉及3,4,6-三取代苯并恶唑化合物及其用于治疗细菌感染的用途。

14. 发明申请

US20090239824A1 HYDROLYTICALLY-RESISTANT BORON-CONTAINING THERAPEUTICS AND METHODS OF USE 有权
标题翻译：含抗水解硼含量的治疗方法及使用方法
公开(公告)号：US20090239824A1
公开(公告)日：2009-09-24
申请号：US12270636
申请日：2008-11-13
申请人： Ving Lee , Jacob J. Plattner , Stephen J. Benkovic , Stephen J. Baker , Kirk R. Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio A. Sauro
发明人： Ving Lee , Jacob J. Plattner , Stephen J. Benkovic , Stephen J. Baker , Kirk R. Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio A. Sauro
IPC分类号： A61K31/69 , C07F5/02 , A61P31/04
CPC分类号： C07F5/025
摘要： Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
摘要翻译：公开了用于治疗由细菌或病毒引起的疾病的治疗剂的硼烷衍生物，包括苯并恶唑，苯并唑并苯并噻唑的组合物和方法，以及合成所述试剂及其组合物的方法。

15. 发明申请

US20090227541A1 BORON-CONTAINING SMALL MOLECULES 有权
标题翻译：含硼的小分子
公开(公告)号：US20090227541A1
公开(公告)日：2009-09-10
申请号：US12142692
申请日：2008-06-19
申请人： Stephen J. Baker , Vincent S. Hernandez , Rashmi Sharma , James A. Nieman , Tsutomu Akama , Yong-Kang Zhang , Jacob J. Plattner , Michael Richard Kevin Alley , Rajeshwar Singh , Fernando Rock
发明人： Stephen J. Baker , Vincent S. Hernandez , Rashmi Sharma , James A. Nieman , Tsutomu Akama , Yong-Kang Zhang , Jacob J. Plattner , Michael Richard Kevin Alley , Rajeshwar Singh , Fernando Rock
IPC分类号： A61K31/69 , C07F5/02 , C12N9/99 , C12N1/36 , A61P31/04
CPC分类号： C07F5/025 , A61K31/69 , Y02A50/387
摘要： This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
摘要翻译：本发明尤其提供了可用于治疗细菌感染的新化合物，含有这些化合物的药物组合物，以及这些化合物与至少一种另外的治疗有效药物的组合。

16. 发明申请

US20070265226A1 Hydrolytically-Resistant Boron-Containing Therapeutics And Methods Of Use 有权
标题翻译：耐水解硼含量治疗剂及其使用方法
公开(公告)号：US20070265226A1
公开(公告)日：2007-11-15
申请号：US11743665
申请日：2007-05-02
申请人： Ving Lee , Jacob Plattner , Stephen Benkovic , Stephen Baker , Kirk Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro
发明人： Ving Lee , Jacob Plattner , Stephen Benkovic , Stephen Baker , Kirk Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro
IPC分类号： A61K31/69 , C07F5/02
CPC分类号： C07F5/025
摘要： Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
摘要翻译：公开了用于治疗由真菌，酵母，细菌或病毒引起的疾病的治疗剂的硼衍生物，包括苯并恶唑，苯并唑并苯并噻唑的组合物和方法，以及合成所述试剂及其组合物的方法。

17. 发明申请

US20060183762A1 3-AMINOQUINAZOLIN-2,4-DIONE ANTIBACTERIAL AGENTS 有权
标题翻译： 3-氨基喹唑啉-2,4-二酮抗菌剂
公开(公告)号：US20060183762A1
公开(公告)日：2006-08-17
申请号：US10182221
申请日：2000-12-12
申请人： Paul Bird , Edmund Ellsworth , Dai Nguyen , Joseph Sanchez , Howard Showalter , Rajeshwar Singh , Michael Stier , Tuan Tran , Brian Watson , Judy Yip
发明人： Paul Bird , Edmund Ellsworth , Dai Nguyen , Joseph Sanchez , Howard Showalter , Rajeshwar Singh , Michael Stier , Tuan Tran , Brian Watson , Judy Yip
IPC分类号： A61K31/517 , C07D403/02 , C07D239/96
CPC分类号： C07D401/04 , C07D239/96 , C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04 , C07D487/10
摘要： Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R1 and R3 include alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclic, and heteroaryl; R5, R6, and R8 include H, alkyl, alkoxy, halo, NO2, CN, NH2, alkyl and dialkylamino; R7 includes hydrogen, alkyl, cycloalkyl, heterocyclic, fused heterocyclic, aryl and fused aryl; J and K are C or N; and pharmaceutically acceptable salts thereof.
摘要翻译：抗菌3-氨基喹唑啉-2,4-二酮具有式（I），其中：R 1和R 3包括烷基，烯基，炔基，环烷基，芳基，杂环和杂芳基; R 5，R 6和R 8包括H，烷基，烷氧基，卤素，NO 2，CN ，NH 2，烷基和二烷基氨基; R 7包括氢，烷基，环烷基，杂环，稠合杂环，芳基和稠合芳基; J和K是C或N; 及其药学上可接受的盐。

18. 发明授权

US5561126A 4-oxa-1-azabicyclo [3,2,0] heptan-7-one derivatives as antitumor agents 失效
标题翻译： 4-氧杂-1-氮杂双环[3,2,0]庚-7-酮衍生物作为抗肿瘤剂
公开(公告)号：US5561126A
公开(公告)日：1996-10-01
申请号：US362490
申请日：1995-03-16
申请人： Toshio Otani , Shinji Oie , Hiroshi Matsumoto , Mark Tempest , Ronald Micetich , Rajeshwar Singh , Tomohiro Yamashita
发明人： Toshio Otani , Shinji Oie , Hiroshi Matsumoto , Mark Tempest , Ronald Micetich , Rajeshwar Singh , Tomohiro Yamashita
IPC分类号： C07D503/00 , A61K31/42 , A61P35/00 , H61K31/395
CPC分类号： A61K31/42
摘要： The present invention relates to the use of 4-oxa-1-azabicyclo [3,2,0] heptan-7-one derivatives of formula (I) or a pharmaceutically acceptable salt thereof, as antitumor agents. ##STR1## Wherein R is --OCOR.sub.1 group wherein R.sub.1 is hydrogen atom, a C.sub.1-9 alkyl group which may be substituted by either one or two substituents selected together from halogen atom, hydroxy, carboxy group or (3RS,5SR)-(4-oxo-1-azabicyclo[3,2,0]heptan-7-one-3-yl) methyloxycarbonyl, a C.sub.2-17 alkenyl group, which may be substituted by carboxy group or (3RS,5SR)-(4-oxa-1-azabicyclo [3,2,0]heptan-7-one-3-yl)methyloxycarbonyl, A C.sub.2-4 alkynyl group, a C.sub.3-6 cycloalkyl group which may be substituted by carboxy group or phenyl group which may have 1, 2 or 3 substituents selected from the group consisting of cyano group, halogen atom, C.sub.1-6 alkoxy group which may be substituted by carboxy group, C.sub.1-6 alkyl group, amino group or hydroxy group.--OR.sub.2 wherein R.sub.2 is a hydrogen atom or benzyl group which may be substituted by 1 or 2 C.sub.1-6 alkoxy group.--S(O).sub.n R.sub.3 wherein R.sub.3 is phenyl group or a benzyl group which may be substituted by C.sub.1-6 alkyl group, n is 0, 1, or 2;or --CH.sub.2 OH.
摘要翻译： PCT No.PCT / GB93 / 01435 Sec。 371日期1995年3月16日 102（e）1995年3月16日PCT PCT 1993年7月8日PCT公布。公开号WO94 / 01109 1994年1月20日的日本本发明涉及式（I）的4-氧杂-1-氮杂双环[3,2,0]庚-7-酮衍生物或其药学上可接受的盐作为抗肿瘤剂。（I）其中R是-OCOR1基团，其中R1是氢原子，可以被一个或两个选自卤原子，羟基，羧基或（3RS，5SR）的取代基取代的C1-9烷基， - （4-氧代-1-氮杂双环[3,2,0]庚-7-酮-3-基）甲氧基羰基，可被羧基取代的C 2-7烯基或（3RS，5SR） - （ 4-氧杂-1-氮杂双环[3,2,0]庚-7-酮-3-基）甲氧基羰基，C 2-4炔基，可被羧基或苯基取代的C 3-6环烷基，可以具有1,2或3个选自氰基，卤素原子，可被羧基，C 1-6烷基，氨基或羟基取代的C 1-6烷氧基的取代基。 -OR 2，其中R 2是可被1或2个C 1-6烷氧基取代的氢原子或苄基。 -S（O）n R 3，其中R 3是苯基或可被C 1-6烷基取代的苄基，n是0,1或2; 或-CH 2 OH。

19. 发明授权

US08895534B2 Boron containing small molecules 有权
标题翻译：硼含有小分子
公开(公告)号：US08895534B2
公开(公告)日：2014-11-25
申请号：US12848051
申请日：2010-07-30
申请人： Stephen J. Baker , Vincent S. Hernandez , Rashmi Sharma , James A. Nieman , Tsutomu Akama , Yong-Kang Zhang , Jacob J. Plattner , Michael Richard Kevin Alley , Rajeshwar Singh , Fernando Rock
发明人： Stephen J. Baker , Vincent S. Hernandez , Rashmi Sharma , James A. Nieman , Tsutomu Akama , Yong-Kang Zhang , Jacob J. Plattner , Michael Richard Kevin Alley , Rajeshwar Singh , Fernando Rock
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , A61K31/69 , Y02A50/387
摘要： Novel monosubstituted and disubstutituted oxaboroles and pharmaceutical compositions containing such oxaboroles are provided, which are useful for treating bacterial infections, as well as combinations of these oxaboroles with at least one additional therapeutically effective agent.
摘要翻译：提供了新的单取代和二取代的奥沙伏醇和含有这种恶唑烷的药物组合物，其可用于治疗细菌感染，以及这些恶唑烷与至少一种另外的治疗有效药剂的组合。

20. 发明申请

US20100256092A1 BORON-CONTAINING SMALL MOLECULES 审中-公开
标题翻译：含硼的小分子
公开(公告)号：US20100256092A1
公开(公告)日：2010-10-07
申请号：US12464829
申请日：2009-05-12
申请人： Yi Xia , Michael Richard Kevin Alley , Yasheen Zhou , Vincent S. Hernandez , Jacob J. Plattner , Charles Z. Ding , Kathy Cao , Yong-Kang Zhang , Andrew Benowitz , Tsutomu Akama , Jessica Sligar , Guofeng Jia , Ligong Ou , Neerja Saraswat , Sreekanth Ramachandran , Chris Diaper , Yanchen Zhang , Goverdhan Reddy Banda , James A. Nieman , Mehdi Keramane , Rahim Mohammed , Rajendra Subedi , Hong Liang , Rajeshwar Singh
发明人： Yi Xia , Michael Richard Kevin Alley , Yasheen Zhou , Vincent S. Hernandez , Jacob J. Plattner , Charles Z. Ding , Kathy Cao , Yong-Kang Zhang , Andrew Benowitz , Tsutomu Akama , Jessica Sligar , Guofeng Jia , Ligong Ou , Neerja Saraswat , Sreekanth Ramachandran , Chris Diaper , Yanchen Zhang , Goverdhan Reddy Banda , James A. Nieman , Mehdi Keramane , Rahim Mohammed , Rajendra Subedi , Hong Liang , Rajeshwar Singh
IPC分类号： A61K31/69 , C07F5/02 , A61P31/04 , A01N55/08 , A01P1/00 , C12N9/99
CPC分类号： A61K31/33 , A61K31/43 , A61K45/06 , C07F5/025 , Y02A50/401 , Y02A50/411 , A61K2300/00
摘要： This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.
摘要翻译：本发明涉及6-取代的苯并恶唑化合物及其用于治疗细菌感染的用途。

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