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31.发明授权3-(Heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids derivatives as antibacterial agents 失效3-（杂芳基乙酰氨基）-2-氧代 - 氮杂环丁烷-1-磺酸衍生物作为抗菌剂公开(公告)号：US06916803B2
公开(公告)日：2005-07-12
申请号：US10363222
申请日：2001-09-14
Applicant: Ronald George Micetich , Samarendra Maiti , Charles Fiakpui , George Thomas , Andhe V. Narender Reddy , Sameeh M. Salama , Rajeshwar Singh
Inventor： Ronald George Micetich , Samarendra Maiti , Charles Fiakpui , George Thomas , Andhe V. Narender Reddy , Sameeh M. Salama , Rajeshwar Singh
IPC: A61K31/4439 , A61P31/04 , C07D417/14 , C07D227/087
CPC classification number: C07D417/14 , Y02A50/473
Abstract: The present invention relates to novel Syn isomers of racemates and optical isomers of 3-(heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids of the following formula: and their use in treating infections caused by gram-negative pathogenic bacteria.
Abstract translation: 本发明涉及下式的3-（杂芳基乙酰氨基）-2-氧代 - 氮杂环丁烷-1-磺酸的外消旋体和旋光异构体的新型Syn异构体及其在治疗由革兰氏阴性致病菌引起的感染中的用途。
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公开(公告)号：US20050070503A1
公开(公告)日：2005-03-31
申请号：US10867465
申请日：2004-06-14
Applicant: Ving Lee , Stephen Benkovic , Stephen Baker , Kirk Maples , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro , Chetan Pandit , Zhuoyi Su , Zhixiang Yang
Inventor： Ving Lee , Stephen Benkovic , Stephen Baker , Kirk Maples , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro , Chetan Pandit , Zhuoyi Su , Zhixiang Yang
CPC classification number: C07F5/025
Abstract: The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.
Abstract translation: 公开了包含硼酸络合物的抗生素的结构和制备，特别是羟基喹啉，咪唑和吡啶甲酸衍生物，以及这些抗生素的组合物以及使用抗生素和组合物作为杀菌和杀真菌剂的方法以及用于治疗 细菌和真菌引起的疾病。
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公开(公告)号：US06635621B1
公开(公告)日：2003-10-21
申请号：US10048396
申请日：2002-01-30
Applicant: Rajeshwar Singh , Nian Zhou , Andhe V. N. Reddy , George Thomas , Qizhu Ding , Jadwiga Kaleta , Ronald George Micetich , Mark Whittaker
Inventor： Rajeshwar Singh , Nian Zhou , Andhe V. N. Reddy , George Thomas , Qizhu Ding , Jadwiga Kaleta , Ronald George Micetich , Mark Whittaker
IPC: C07D29512
CPC classification number: C07D295/125 , A61K38/00 , C07D207/14 , C07D333/38 , C07K5/06043 , C07K5/06078
Abstract: This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is described or a pharmaceutically acceptable salt, hydrate or solvate thereof. Pharmaceutically acceptable salts of the compounds of this invention include the sodium, potassium, magnesium, calcium, hydrogen chloride, tartaric acid, succinic acid, fumaric acid and p-toluenesulfonic acid salts.
Abstract translation: 本发明涉及α-氨基酸酰胺的衍生物，含有这些化合物的药物组合物，以及它们在医学上作为半胱氨酸蛋白酶特别是组织蛋白酶抑制剂的用途。 描述式（I）化合物或其药学上可接受的盐，水合物或溶剂合物。 本发明化合物的药学上可接受的盐包括钠，钾，镁，钙，氯化氢，酒石酸，琥珀酸，富马酸和对甲苯磺酸盐。
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34.发明授权3-Substituted-4-oxa-1-azabicyclo �3,2,0!heptan-7-one as cysteine protease inhibitors 失效3-取代-4-氧杂-1-氮杂双环[3,2,0]庚-7-酮作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US5925633A
公开(公告)日：1999-07-20
申请号：US611946
申请日：1996-03-06
Applicant: Rajeshwar Singh , Nian E. Zhou , Deqi Guo , Jadwiga Kaleta , Ronald George Micetich
Inventor： Rajeshwar Singh , Nian E. Zhou , Deqi Guo , Jadwiga Kaleta , Ronald George Micetich
IPC: A61K31/424 , A61K38/05 , A61K38/55 , A61K31/395
CPC classification number: A61K38/55 , A61K31/424 , A61K38/05
Abstract: The use of certain 3-substituted-4-oxa-1-azabicyclo�3,2,0! heptan-7-one derivatives of general formula I, ##STR1## or physiologically acceptable salts thereof or isomers thereof, as active ingredients for the preparation of pharmaceutical composition and treatment of different diseases associated with deregulation of cysteine proteases is disclosed.
Abstract translation: 使用通式I的某些3-取代-4-氧杂-1-氮杂双环[3,2,0]庚-7-酮衍生物或其生理学上可接受的盐或其异构体作为制备药物的活性成分 公开了与半胱氨酸蛋白酶失调相关的不同疾病的组合和治疗。
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公开(公告)号：US08343944B2
公开(公告)日：2013-01-01
申请号：US12844748
申请日：2010-07-27
Applicant: 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
Inventor： 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
CPC classification number: C07F5/025 , A61K31/69 , A61K45/06 , A61K2300/00
Abstract: This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections.
Abstract translation: 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。
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Patent Agency Ranking
公开(公告)号：US20120214765A1
公开(公告)日：2012-08-23
申请号：US13236543
申请日：2011-09-19
Applicant: Tsutomu Akama , Yong-Kang Zhang , Charles Z. Ding , Jacob J. Plattner , Kirk R. Maples , Yvonne Freund , Virginia Sanders , Yi Xia , Stephen J. Baker , James A. Nieman , Xiaosong Lu , Marcelo Sales , Rashmi Sharma , Rajeshwar Singh , Robert T. Jacobs , Daitao Chen , Michael Richard Kevin Alley
Inventor： Tsutomu Akama , Yong-Kang Zhang , Charles Z. Ding , Jacob J. Plattner , Kirk R. Maples , Yvonne Freund , Virginia Sanders , Yi Xia , Stephen J. Baker , James A. Nieman , Xiaosong Lu , Marcelo Sales , Rashmi Sharma , Rajeshwar Singh , Robert T. Jacobs , Daitao Chen , Michael Richard Kevin Alley
CPC classification number: C07F5/025 , A61K31/69 , C07F5/04 , Y02A50/411
Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.
Abstract translation: 公开了治疗抗炎症状的化合物和方法。
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公开(公告)号：US08039450B2
公开(公告)日：2011-10-18
申请号：US12399015
申请日：2009-03-05
Applicant: Tsutomu Akama , Yong-Kang Zhang , Charles Z. Ding , Jacob J. Plattner , Kirk R. Maples , Yvonne Freund , Virginia Sanders , Yi Xia , Stephen J. Baker , James A. Nieman , Xiaosong Lu , Marcelo Sales , Rashmi Sharma , Rajeshwar Singh , Robert Jacobs , Daitao Chen , Michael Richard Kevin Alley
Inventor： Tsutomu Akama , Yong-Kang Zhang , Charles Z. Ding , Jacob J. Plattner , Kirk R. Maples , Yvonne Freund , Virginia Sanders , Yi Xia , Stephen J. Baker , James A. Nieman , Xiaosong Lu , Marcelo Sales , Rashmi Sharma , Rajeshwar Singh , Robert Jacobs , Daitao Chen , Michael Richard Kevin Alley
CPC classification number: C07F5/025 , A61K31/69 , C07F5/04 , Y02A50/411
Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.
Abstract translation: 公开了治疗抗炎症状的化合物和方法。
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38.发明授权公开(公告)号：US07968752B2
公开(公告)日：2011-06-28
申请号：US12270636
申请日：2008-11-13
Applicant: 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
Inventor： 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: C07F9/02
CPC classification number: C07F5/025
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20100292504A1
公开(公告)日：2010-11-18
申请号：US12848051
申请日：2010-07-30
Applicant: 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
Inventor： 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: C07F5/02
CPC classification number: C07F5/025 , A61K31/69 , Y02A50/387
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US07816344B2
公开(公告)日：2010-10-19
申请号：US12142692
申请日：2008-06-19
Applicant: 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
Inventor： 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: A61K31/69 , C07D493/00
CPC classification number: C07F5/025 , A61K31/69 , Y02A50/387
Abstract: This invention provides, among other things, novel oxaboroles which are monosubstituted at the 3-, 6-, or 7-position, or disubstituted at the 3-/6- or 3-/7- positions, which are useful for treating bacterial infections, pharmaceutical compositions containing such oxaboroles, as well as combinations of these oxaboroles with at least one additional therapeutically effective agent.
Abstract translation: 本发明尤其提供了在3-，6-或7-位单取代的或在3- / 6-或3- / 7-位二取代的新的恶唑烷，其可用于治疗细菌感染 ，含有这种恶唑烷的药物组合物，以及这些恶唑烷与至少一种另外的治疗有效药剂的组合。
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