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公开(公告)号：US07879795B2
公开(公告)日：2011-02-01
申请号：US11832626
申请日：2007-08-01
申请人： Tomasz Glinka , Keith Bostian , Olga Lomovskaya , Mark Surber , Dongxu Sun
发明人： Tomasz Glinka , Keith Bostian , Olga Lomovskaya , Mark Surber , Dongxu Sun
IPC分类号： A61K38/00
CPC分类号： A61K31/165 , A61K31/426 , A61K31/433 , A61K31/47 , A61K31/65
摘要： Disclosed herein are Efflux Pump Inhibitor (EPI) compounds that can be co-administered with antimicrobial agents for the treatment of infections caused by drug resistant pathogens. The EPI compounds are soft drugs which exhibit a reduced propensity for tissue accumulation. It is demonstrated that the EPIs can be used to increase the potency, decrease bacterial resistance and development of bacterial resistance, and increase killing effectivness of tigecycline. Also disclosed are methods of treatment and pharmaceutical compositions for co-administering tigecylcine with an EPI.
摘要翻译： 本文公开了可与抗微生物剂共同施用以治疗由耐药性病原体引起的感染的流出泵抑制剂（EPI）化合物。 EPI化合物是表现出组织积累倾向降低的软性药物。 证明EPI可用于增加效力，降低细菌耐药性和细菌耐药性的发展，并增加替加环素的杀伤效果。 还公开了治疗方法和药物组合物，用于与十二烷基苯共同施用EPI。
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公开(公告)号：US20080076741A1
公开(公告)日：2008-03-27
申请号：US11832626
申请日：2007-08-01
申请人： Tomasz Glinka , Keith Bostian , Olga Lomovskaya , Mark Surber , Dongxu Sun
发明人： Tomasz Glinka , Keith Bostian , Olga Lomovskaya , Mark Surber , Dongxu Sun
IPC分类号： A61K31/65 , A61K31/165 , A61K31/426 , A61P31/04 , A61K31/433 , A61K31/47
CPC分类号： A61K31/165 , A61K31/426 , A61K31/433 , A61K31/47 , A61K31/65
摘要： Disclosed herein are Efflux Pump Inhibitor (EPI) compounds that can be co-administered with antimicrobial agents for the treatment of infections caused by drug resistant pathogens. The EPI compounds are soft drugs which exhibit a reduced propensity for tissue accumulation. It is demonstrated that the EPIs can be used to increase the potency, decrease bacterial resistance and development of bacterial resistance, and increase killing effectivness of tigecycline. Also disclosed are methods of treatment and pharmaceutical compositions for co-administering tigecylcine with an EPI.
摘要翻译： 本文公开了可与抗微生物剂共同施用以治疗由耐药性病原体引起的感染的流出泵抑制剂（EPI）化合物。 EPI化合物是表现出组织积累倾向降低的软性药物。 证明EPI可用于增加效力，降低细菌耐药性和细菌耐药性的发展，并增加替加环素的杀伤效果。 还公开了治疗方法和药物组合物，用于与十二烷基苯共同施用EPI。
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3.发明授权公开(公告)号：US07893020B2
公开(公告)日：2011-02-22
申请号：US11134147
申请日：2005-05-20
申请人： Tomasz Glinka , Keith Bostian , Mark Surber , Olga Lomovskaya , Dongxu Sun
发明人： Tomasz Glinka , Keith Bostian , Mark Surber , Olga Lomovskaya , Dongxu Sun
IPC分类号： A61K38/00
CPC分类号： C07K5/06086 , A61K38/00 , C07K5/0202 , C07K5/0215 , C07K5/06191 , C07K5/0819 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： This invention relates to the field of antimicrobial agents and more specifically it relates to Efflux Pump Inhibitor (EPI) compounds to be co-administered with antimicrobial agents for the treatment of infections caused by drug resistant pathogens. The EPI compounds are soft drugs which exhibit a reduced propensity for tissue accumulation. The invention includes novel compounds useful as efflux pump inhibitors, compositions and devices comprising such efflux pump inhibitors, and therapeutic use of such compounds.
摘要翻译： 本发明涉及抗微生物剂领域，更具体地说，本发明涉及与用于治疗由耐药性病原体引起的感染的抗微生物剂共同施用的流出泵抑制剂（EPI）化合物。 EPI化合物是表现出组织积累倾向降低的软性药物。 本发明包括可用作外排泵抑制剂的新化合物，包含这种外排泵抑制剂的组合物和装置，以及这些化合物的治疗用途。
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4.发明申请公开(公告)号：US20060003944A1
公开(公告)日：2006-01-05
申请号：US11134147
申请日：2005-05-20
申请人： Tomasz Glinka , Keith Bostian , Mark Surber , Olga Lomovskaya , Dongxu Sun
发明人： Tomasz Glinka , Keith Bostian , Mark Surber , Olga Lomovskaya , Dongxu Sun
CPC分类号： C07K5/06086 , A61K38/00 , C07K5/0202 , C07K5/0215 , C07K5/06191 , C07K5/0819 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： This invention relates to the field of antimicrobial agents and more specifically it relates to Efflux Pump Inhibitor (EPI) compounds to be co-administered with antimicrobial agents for the treatment of infections caused by drug resistant pathogens. The EPI compounds are soft drugs which exhibit a reduced propensity for tissue accumulation. The invention includes novel compounds useful as efflux pump inhibitors, compositions and devices comprising such efflux pump inhibitors, and therapeutic use of such compounds.
摘要翻译： 本发明涉及抗微生物剂领域，更具体地说，本发明涉及与用于治疗由耐药性病原体引起的感染的抗微生物剂共同施用的流出泵抑制剂（EPI）化合物。 EPI化合物是表现出组织积累倾向降低的软性药物。 本发明包括可用作外排泵抑制剂的新化合物，包含这种外排泵抑制剂的组合物和装置，以及这些化合物的治疗用途。
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公开(公告)号：US07947741B2
公开(公告)日：2011-05-24
申请号：US11082745
申请日：2005-03-16
申请人： Keith Bostian , Tomasz Glinka , Olga Lomovskaya , Mark Surber
发明人： Keith Bostian , Tomasz Glinka , Olga Lomovskaya , Mark Surber
IPC分类号： A01N37/52 , A61K31/155
CPC分类号： A61K45/06 , A61K31/00 , A61K31/135 , A61K31/421 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483 , A61K2300/00
摘要： This invention provides for efflux pump inhibitors to be co-administered with antimicrobial agents for the treatment of infections caused by drug resistant pathogens, novel efflux pump inhibitors, combined dosage forms of efflux pump inhibitors with an antimicrobial, and novel medical methods.
摘要翻译： 本发明提供了与抗微生物剂共同施用的外排泵抑制剂，用于治疗由耐药性病原体引起的感染，新型外排泵抑制剂，具有抗微生物剂的外排泵抑制剂的组合剂型和新颖的医学方法。
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6.发明授权Bacterial efflux pump inhibitors for the treatment of ophthalmic and otic infections 失效用于治疗眼科和耳部感染的细菌外排泵抑制剂公开(公告)号：US07994225B2
公开(公告)日：2011-08-09
申请号：US11856657
申请日：2007-09-17
申请人： Keith Bostian , Tomasz Glinka , Olga Lomovskaya , Mark Surber , Neil Berkley , David Griffith
发明人： Keith Bostian , Tomasz Glinka , Olga Lomovskaya , Mark Surber , Neil Berkley , David Griffith
IPC分类号： A61K31/13 , A61K31/155
CPC分类号： A61K31/155 , A61K31/17 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/5383 , A61K31/546 , A61K31/655 , A61K31/7036 , A61K45/06 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483 , A61K2300/00
摘要： Efflux pump inhibitors are co-administered with antimicrobial agents for the treatment of ophthalmic or otic infections. The agents may be co-administered directly to the site of infection (e.g., the eye or ear).
摘要翻译： 流出泵抑制剂与抗微生物剂共同给药以治疗眼部或耳部感染。 药剂可以直接共同施用于感染部位（例如眼睛或耳朵）。
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7.发明申请QUATERNARY ALKYL AMMONIUM BACTERIAL EFFLUX PUMP INHIBITORS AND THERAPEUTIC USES THEREOF 失效季铵盐氨基脲类止痛剂抑制剂及其治疗用途公开(公告)号：US20120165276A1
公开(公告)日：2012-06-28
申请号：US12116164
申请日：2008-05-06
IPC分类号： A61K38/06 , C07D265/16 , A61K31/421 , C07C237/22 , A61P31/04 , A61K31/7056 , C07K5/09 , C07K5/083 , A61K31/536 , A61K38/05 , A61K31/65 , A61K31/7008 , C07K5/068 , A61K38/02
CPC分类号： C07D215/38 , C07C237/22 , C07D277/82 , C07K5/06086
摘要： Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
摘要翻译： 公开了具有至少一个季烷基铵官能团的化合物。 该化合物抑制细菌外排泵抑制剂，并与抗菌剂组合使用以治疗或预防细菌感染。 这些组合可以有效地抵抗通过外排泵机制对抗细菌剂产生抗性的细菌感染。
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8.发明申请公开(公告)号：US20080318957A1
公开(公告)日：2008-12-25
申请号：US12116172
申请日：2008-05-06
IPC分类号： A61K31/47 , C07D215/38 , A61K31/5375 , A61P31/04 , C07D265/30
CPC分类号： C07K5/06086 , A61K38/00 , C07K5/06113 , C07K5/06139 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/483
摘要： Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
摘要翻译： 公开了具有多碱性官能团的化合物。 该化合物抑制细菌外排泵抑制剂，并与抗菌剂组合使用以治疗或预防细菌感染。 这些组合可以有效地抵抗通过外排泵机制对抗细菌剂产生抗性的细菌感染。
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9.发明授权Quaternary alkyl ammonium bacterial efflux pump inhibitors and therapeutic uses thereof 失效季铵烷基铵细菌外排泵抑制剂及其治疗用途公开(公告)号：US08268865B2
公开(公告)日：2012-09-18
申请号：US12116164
申请日：2008-05-06
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07D215/38 , C07C237/22 , C07D277/82 , C07K5/06086
摘要： Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
摘要翻译： 公开了具有至少一个季烷基铵官能团的化合物。 该化合物抑制细菌外排泵抑制剂，并与抗菌剂组合使用以治疗或预防细菌感染。 这些组合可以有效地抵抗通过外排泵机制对抗细菌剂产生抗性的细菌感染。
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10.发明申请BACTERIAL EFFLUX PUMP INHIBITORS FOR THE TREATMENT OF OPHTHALMIC AND OTIC INFECTIONS 失效用于治疗眼睛和眼睛感染的细菌液体泵抑制剂公开(公告)号：US20080132457A1
公开(公告)日：2008-06-05
申请号：US11856657
申请日：2007-09-17
申请人： Keith Bostian , Thomasz Glinka , Olga Lomovskaya , Mark Surber , Neil Berkley , David Griffith
发明人： Keith Bostian , Thomasz Glinka , Olga Lomovskaya , Mark Surber , Neil Berkley , David Griffith
IPC分类号： A61K31/7048 , A61K31/155 , A61K31/655 , A61K31/17 , A61K31/4709 , A61K31/4375 , A61K31/546 , A61K31/496 , A61K31/7036 , A61P31/04 , A61K31/5383
CPC分类号： A61K31/155 , A61K31/17 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/5383 , A61K31/546 , A61K31/655 , A61K31/7036 , A61K45/06 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483 , A61K2300/00
摘要： Efflux pump inhibitors are co-administered with antimicrobial agents for the treatment of ophthalmic or otic infections. The agents may be co-administered directly to the site of infection (e.g., the eye or ear).
摘要翻译： 流出泵抑制剂与抗微生物剂共同给药以治疗眼部或耳部感染。 药剂可以直接共同施用于感染部位（例如眼睛或耳朵）。
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