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11. 发明授权

US07884099B2 Quinolone carboxylic acid-substituted rifamycin derivatives 有权
标题翻译：喹诺酮羧酸取代的利福霉素衍生物
公开(公告)号：US07884099B2
公开(公告)日：2011-02-08
申请号：US12269652
申请日：2008-11-12
申请人： Charles Z. Ding , Yafei Jin , Keith Combrink , In Ho Kim
发明人： Charles Z. Ding , Yafei Jin , Keith Combrink , In Ho Kim
IPC分类号： C07D491/20 , C07D498/16 , A61K31/498 , A61K31/5383
CPC分类号： C07D491/20 , C07D498/16
摘要： The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.
摘要翻译：化合物包括取代的利福霉素衍生物，其中喹诺酮羧酸药效团与苯并恶嗪利福霉素或螺哌啶利多霉素共价键合。利福霉素衍生物可用作抗微生物剂，并且对许多人和兽医革兰氏阳性和革兰氏阴性病原体有效。本发明化合物的优点在于利福霉素和喹诺酮类抗菌药代动力剂与匹配的药代动力学共同输送到感兴趣的靶向病原体。同时向目标病原体递送多个抗菌药代动力，最大限度地实现协同作用，并最大限度地减少给予抗生素的耐药性。

12. 发明申请

US20050209210A1 Rifamycin imino derivatives effective against drug-resistant microbes 有权
标题翻译：对抗耐药性微生物有效的利福霉素亚氨基衍生物
公开(公告)号：US20050209210A1
公开(公告)日：2005-09-22
申请号：US11034279
申请日：2005-01-12
申请人： Charles Ding , Yafei Jin , Jamie Longgood , Zhenkun Ma , Jing Li , In Kim , Keith Minor , Susan Harran
发明人： Charles Ding , Yafei Jin , Jamie Longgood , Zhenkun Ma , Jing Li , In Kim , Keith Minor , Susan Harran
IPC分类号： A61K31/4709 , C07D491/14 , C07D498/08 , C07D519/00
CPC分类号： C07D498/08 , C07D519/00
摘要： The present invention relates to rifamycin 3-iminomethylenyl (—CH═N—) derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. The claimed rifamycin derivative has a rifamycin moiety covalently linked to a linker through an iminomethylenyl (—CH═N—) group at the C-3 carbon of the rifamycin moiety and the linker is, in turn, covalently linked to a quinolone structure or its pharmacophore within the DNA gyrase and topoisomerase IV inhibitor family. The inventive rifamycins are novel and exhibit activity against both rifampin and ciprofloxacin-resistant microorganisms.
摘要翻译：本发明涉及具有抗菌活性的利福霉素3-亚氨基亚甲基（-CH-N-）衍生物，其包括抗药性微生物的活性。所要求的利福霉素衍生物具有通过利莫霉素部分的C-3碳上的亚氨基亚甲基（-CH-N-）基团与连接体共价连接的利福霉素部分，并且连接体又与喹诺酮结构共价连接或其 DNA促旋酶和拓扑异构酶IV抑制剂家族内的药效团。本发明的利福霉素是新颖的，并且表现出抵抗利福平和环丙沙星抗性微生物的活性。

13. 发明申请

US20050118624A1 Fluorescent probes for ribosomes and method of use 审中-公开
标题翻译：核糖体荧光探针及其使用方法
公开(公告)号：US20050118624A1
公开(公告)日：2005-06-02
申请号：US10954996
申请日：2004-09-30
申请人： Zhenkun Ma , Jing Li , In Kim , Yafei Jin , Anthony Lynch , Eric Roche , Doug Beeman
发明人： Zhenkun Ma , Jing Li , In Kim , Yafei Jin , Anthony Lynch , Eric Roche , Doug Beeman
IPC分类号： C07H17/08 , C07H21/04 , C09B11/08 , C09B11/24 , C09B23/01 , C12Q1/68 , G01N33/533 , G01N33/58
CPC分类号： C09B11/08 , C09B11/24 , C09B23/0075 , G01N33/533 , G01N33/582 , G01N2500/00
摘要： Fluorescent probes that have binding affinity to ribosomes. The fluorescent probes are useful tools for identifying small molecules that bind to the 50S or 30S subunits of the bacterial and other ribosomes and serve as novel ribosome inhibitors. These probes are also useful for determining the interactions between a specific ligand and the ribosome.
摘要翻译：对核糖体具有结合亲和力的荧光探针。荧光探针是用于鉴定结合细菌和其他核糖体的50S或30S亚基的小分子并用作新的核糖体抑制剂的有用工具。这些探针也可用于确定特异性配体和核糖体之间的相互作用。

14. 发明申请

US20120077806A1 Deubiquitinase Inhibitors and Methods for Use of the Same 有权
标题翻译：去泛素酶抑制剂及其使用方法
公开(公告)号：US20120077806A1
公开(公告)日：2012-03-29
申请号：US13241802
申请日：2011-09-23
申请人： Nicholas J. Donato , Christiane Wobus , Hollis D. Showalter , Moshe Talpaz , Jeffrey W. Perry , Roderick J. Sorenson , Mary X. O'Riordan , Yafei Jin
发明人： Nicholas J. Donato , Christiane Wobus , Hollis D. Showalter , Moshe Talpaz , Jeffrey W. Perry , Roderick J. Sorenson , Mary X. O'Riordan , Yafei Jin
IPC分类号： A61K31/541 , C12N5/02 , A61K31/5377 , A61K31/53 , A61K31/50 , C07D413/12 , A61K31/496 , A61K31/505 , A61K31/454 , A61K31/4439 , A61K31/44 , A61K31/433 , A61K31/4245 , A61K31/426 , A61K31/42 , A61K31/4164 , A61K31/415 , A61K31/165 , C07D417/12 , C07D253/065 , C07D253/04 , C07D237/06 , C07D239/02 , A61K31/4965 , C07D401/12 , C07D213/57 , C07D285/06 , C07D285/12 , C07D271/10 , C07D277/30 , C07D261/06 , C07D233/90 , C07D231/10 , C07C255/32 , A61P25/28 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/00 , A61P35/00 , C12N9/99
CPC分类号： C07D495/04 , C07C255/43 , C07D213/30 , C07D213/32 , C07D213/61 , C07D213/68 , C07D213/74 , C07D213/75 , C07D231/12 , C07D233/54 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D251/16 , C07D261/08 , C07D271/04 , C07D271/10 , C07D277/30 , C07D285/12 , C07D285/16 , C07D401/12 , C07D417/12 , C12N9/99
摘要： Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.
摘要翻译：本文公开了抑制去泛素酶（DUB），治疗病原体感染（例如病毒，细菌和/或寄生虫）的方法，抑制细胞增殖的方法，治疗神经变性疾病的方法，治疗一种或多种症状的方法的神经变性疾病或遗传性疾病，以及化合物。

15. 发明授权

US08809377B2 Deubiquitinase inhibitors and methods for use of the same 有权
标题翻译：去泛素酶抑制剂及其使用方法
公开(公告)号：US08809377B2
公开(公告)日：2014-08-19
申请号：US13241802
申请日：2011-09-23
申请人： Nicholas J. Donato , Christiane Wobus , Hollis D. Showalter , Moshe Talpaz , Jeffrey W. Perry , Roderick J. Sorenson , Mary X. O'Riordan , Yafei Jin
发明人： Nicholas J. Donato , Christiane Wobus , Hollis D. Showalter , Moshe Talpaz , Jeffrey W. Perry , Roderick J. Sorenson , Mary X. O'Riordan , Yafei Jin
IPC分类号： A61K31/444 , A61K31/4433 , A61K31/4436 , A61K31/4439
CPC分类号： C07D495/04 , C07C255/43 , C07D213/30 , C07D213/32 , C07D213/61 , C07D213/68 , C07D213/74 , C07D213/75 , C07D231/12 , C07D233/54 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D251/16 , C07D261/08 , C07D271/04 , C07D271/10 , C07D277/30 , C07D285/12 , C07D285/16 , C07D401/12 , C07D417/12 , C12N9/99
摘要： Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds, wherein the compound can have a structure of formula (III):
摘要翻译：本文公开了抑制去泛素酶（DUB），治疗病原体感染（例如病毒，细菌和/或寄生虫）的方法，抑制细胞增殖的方法，治疗神经变性疾病的方法，治疗一种或多种症状的方法的神经变性疾病或遗传性疾病，和化合物，其中所述化合物可以具有式（III）的结构：

16. 发明授权

US07432242B2 Inhibitors of RGS proteins 失效
标题翻译： RGS蛋白抑制剂
公开(公告)号：US07432242B2
公开(公告)日：2008-10-07
申请号：US10365840
申请日：2003-02-13
申请人： Henry I. Mosberg , Richard R. Neubig , Yafei Jin , Hauiling Zhong , Roger Sunahara
发明人： Henry I. Mosberg , Richard R. Neubig , Yafei Jin , Hauiling Zhong , Roger Sunahara
IPC分类号： A61K38/12
CPC分类号： A61K38/08 , C07K14/4702 , C07K2319/00 , C07K2319/60 , G01N2500/04 , G01N2500/10
摘要： The present invention relates to novel inhibitors of G-protein signaling. In particular, the present invention provides peptide inhibitors of G protein signaling proteins and methods of using such inhibitors to modulate physiological effects of G protein signaling. The present invention thus provides novel drug targets for a variety of pathologies mediated by defects in G-protein signaling.
摘要翻译：本发明涉及G蛋白信号传导的新型抑制剂。特别地，本发明提供G蛋白信号传导蛋白的肽抑制剂和使用这些抑制剂调节G蛋白信号传导的生理作用的方法。因此，本发明提供了用于由G蛋白信号传导中的缺陷介导的各种病理学的新型药物靶标。

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