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1. 发明专利

CA2910593C ANTIMICROBIAL POTENTIATORS 未知
公开(公告)号：CA2910593C
公开(公告)日：2018-09-04
申请号：CA2910593
申请日：2014-05-03
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , NGUYEN SON T , KWASNY STEVEN M , DING XIAOYUAN
IPC分类号： A61K31/436 , A61K31/444 , A61K31/5377 , A61K31/551 , A61K31/553 , A61P31/04 , C07D491/052
摘要： Novel compounds are disclosed having the structure of Formula I: wherein, n is an integer from 1 to 5; X is -CN, -F, -CI, -Br, -I, -N02; W is S, SO, S02, O, NH, or NR5; R5 is alkyl, aralkyl, alkenyl, or alkynyl; Y is O, S; Z is NR1R2 or heterocycloalkyl; R1, R2 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups; R3 and R4 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups, and may together form a cyclic structure; and Ar is mono-, di-, or tri-substituted phenyl or heteroaryl, a pharmaceutically acceptable salts thereof. The compounds are potent bacterial efflux pump inhibitors (EPIs). Such compounds are useful to potentiate the antimicrobial activity of antimicrobial compounds such as beta-lactam antibiotics and quinolone antibiotics against Gram-negative bacteria.

2. 发明专利

AU2014259608C1 Antimicrobial potentiators 未知
公开(公告)号：AU2014259608C1
公开(公告)日：2017-08-17
申请号：AU2014259608
申请日：2014-05-03
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , NGUYEN SON T , KWASNY STEVEN M , DING XIAOYUAN
IPC分类号： A61K31/436
摘要： Novel compounds are disclosed having the structure of Formula I. The compounds are potent bacterial efflux pump inhibitors (EPis). Such compounds are useful to potentiate the antimicrobial activity of antimicrobial compounds such as beta-lactam antibiotics and quinolone antibiotics against Gram-negative bacteria. These novel compounds are effective as antibiotic or antimicrobial potentiators. Structures of these compounds are distinctive from other reported efflux pump inhibitors and antibiotic potentiators. Also disclosed are methods for inhibiting bacterial efflux pumps with the novel compounds described herein. In another embodiment, the present invention discloses the use of these novel compounds for the inhibition of bacterial efflux pumps. In yet another embodiment, the present invention discloses the use of these novel compounds for treating or inhibiting bacterial infection.

3. 发明专利

AU2013209355A1 Inhibitors of bacterial biofilm formation 未知
公开(公告)号：AU2013209355A1
公开(公告)日：2013-08-15
申请号：AU2013209355
申请日：2013-07-26
申请人： MICROBIOTIX INC
发明人： KHAN ATIYYA R , WILLIAMS JOHN D , OPPERMAN TIMOTHY J , KWASNY STEVEN M , PEET NORTON P
IPC分类号： A01N43/78
摘要： INHIBITORS OF BACTERIAL BIOFILM FORMATION Organic compounds are described for use in inhibiting or preventing formation of bacterial biofilms.

4. 发明公开

EP2296476A4 INHIBITORS OF BACTERIAL BIOFILM FORMATION 审中-公开
标题翻译：细菌生物膜教育的抑制剂
公开(公告)号：EP2296476A4
公开(公告)日：2013-11-06
申请号：EP09750951
申请日：2009-05-19
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , WILLIAMS JOHN D , PEET NORTON P , KHAN ATIYYA R , KWASNY STEVEN M
IPC分类号： A01N43/78
CPC分类号： A01N43/78 , A01N43/50

5. 发明专利

CA3072103A1 METABOLICALLY STABLE N-ACYLAMINOOXADIAZOLES USEFUL AS ANTIBACTERIAL AGENTS 未知
公开(公告)号：CA3072103A1
公开(公告)日：2019-02-28
申请号：CA3072103
申请日：2018-08-21
申请人： MICROBIOTIX INC , PENN STATE RES FOUND
发明人： ARON ZACHARY D , KWASNY STEVEN M , TORHAN MATTHEW C , BARBOR JAY P , CARDINALE STEVEN C , BUTLER MICHELLE M , OPPERMAN TIMOTHY J , KEILER KENNETH C
IPC分类号： C07D271/10 , C07D271/107 , C07D271/113
摘要： The present invention is related to the development of therapeutics and prophylactics for the treatment and/or prevention of bacterial infections in humans and other mammals. A new class of small molecules is disclosed that inhibits the bacterial trans-translation/ribosome rescue mechanism and thus blocks infection of host cells by bacteria. Also disclosed are methods of using the small molecule inhibitors in the treatment/prevention of bacterial infections.

6. 发明专利

AU2017204761A1 Antimicrobial potentiators 未知
公开(公告)号：AU2017204761A1
公开(公告)日：2017-07-27
申请号：AU2017204761
申请日：2017-07-11
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , NGUYEN SON T , KWASNY STEVEN M , DING XIAOYUAN
IPC分类号： A61K31/436
摘要： R 3 '1 W I Ar n Novel compounds are disclosed having the structure of Formula I: wherein, n is an integer from 1 to 5; X is -CN, -F,-CI, -Br, -I, -N0 2 ; W is S, SO, SO 2, 0, NH, or NR5; R5 is alkyl, aralkyl, alkenyl, or alkynyl; Y is 0, S; Z is NR'R 2 or heterocycloalkyl; R', R2 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups; R3 and R4 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups, and may together form a cyclic structure; and Ar is mono-, di-, or tri-substituted phenyl or heteroaryl, a pharmaceutically acceptable salts thereof. The compounds are potent bacterial efflux pump inhibitors (EPIs). Such compounds are useful to potentiate the antimicrobial activity of antimicrobial compounds such as beta lactam antibiotics and quinolone antibiotics against Gram-negative bacteria.

7. 发明专利

AU2014259608A1 Antimicrobial potentiators 未知
公开(公告)号：AU2014259608A1
公开(公告)日：2015-11-12
申请号：AU2014259608
申请日：2014-05-03
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , NGUYEN SON T , KWASNY STEVEN M , DING XIAOYUAN
IPC分类号： C07D491/04 , A61K31/551
摘要： Novel compounds are disclosed having the structure of Formula I: wherein, n is an integer from 1 to 5; X is -CN, -F, -CI, -Br, -I, -N0

8. 发明申请

WO2014179784A3 ANTIMICROBIAL POTENTIATORS 审中-公开
标题翻译：抗微生物电位
公开(公告)号：WO2014179784A3
公开(公告)日：2015-11-19
申请号：PCT/US2014036712
申请日：2014-05-03
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , NGUYEN SON T , KWASNY STEVEN M , DING XIAOYUAN
IPC分类号： A61K31/436
CPC分类号： C07D491/052 , A01N43/90 , A01N47/44 , A61K31/436 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/541 , A61K31/551 , A61K31/553 , A61K45/06 , C07D493/04 , C07D513/04 , A61K2300/00
摘要： Novel compounds are disclosed having the structure of Formula I. The compounds are potent bacterial efflux pump inhibitors (EPis). Such compounds are useful to potentiate the antimicrobial activity of antimicrobial compounds such as beta-lactam antibiotics and quinolone antibiotics against Gram-negative bacteria. These novel compounds are effective as antibiotic or antimicrobial potentiators. Structures of these compounds are distinctive from other reported efflux pump inhibitors and antibiotic potentiators. Also disclosed are methods for inhibiting bacterial efflux pumps with the novel compounds described herein. In another embodiment, the present invention discloses the use of these novel compounds for the inhibition of bacterial efflux pumps. In yet another embodiment, the present invention discloses the use of these novel compounds for treating or inhibiting bacterial infection.
摘要翻译：公开了具有式I结构的新型化合物。该化合物是有效的细菌外排泵抑制剂（EPis）。这些化合物可用于增强抗菌化合物如β-内酰胺抗生素和喹诺酮抗生素对革兰氏阴性菌的抗微生物活性。这些新型化合物作为抗生素或抗微生物增效剂是有效的。这些化合物的结构与其他报道的外排泵抑制剂和抗生素增强剂不同。还公开了用本文所述的新型化合物抑制细菌外排泵的方法。在另一个实施方案中，本发明公开了这些新型化合物用于抑制细菌外排泵的用途。在另一个实施方案中，本发明公开了这些新化合物用于治疗或抑制细菌感染的用途。

9. 发明专利

CA3011999A1 ANTIMICROBIAL POTENTIATORS 未知
公开(公告)号：CA3011999A1
公开(公告)日：2014-11-06
申请号：CA3011999
申请日：2014-05-03
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , NGUYEN SON T , KWASNY STEVEN M , DING XIAOYUAN
IPC分类号： A61K31/436 , A61K31/444 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P31/04 , C07D491/052
摘要： The compounds are potent bacterial efflux pump inhibitors (EPIs). Such compounds are useful to potentiate the antimicrobial activity of antimicrobial compounds such as beta-lactam antibiotics and quinolone antibiotics against Gram-negative bacteria.

10. 发明专利

CA2910593A1 ANTIMICROBIAL POTENTIATORS 未知
公开(公告)号：CA2910593A1
公开(公告)日：2014-11-06
申请号：CA2910593
申请日：2014-05-03
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , NGUYEN SON T , KWASNY STEVEN M , DING XIAOYUAN
IPC分类号： A61K31/436 , A61K31/444 , A61K31/5377 , A61K31/551 , A61K31/553 , A61P31/04 , C07D491/052
摘要： Novel compounds are disclosed having the structure of Formula I: wherein, n is an integer from 1 to 5; X is -CN, -F, -CI, -Br, -I, -N02; W is S, SO, S02, O, NH, or NR5; R5 is alkyl, aralkyl, alkenyl, or alkynyl; Y is O, S; Z is NR1R2 or heterocycloalkyl; R1, R2 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups; R3 and R4 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups, and may together form a cyclic structure; and Ar is mono-, di-, or tri-substituted phenyl or heteroaryl, a pharmaceutically acceptable salts thereof. The compounds are potent bacterial efflux pump inhibitors (EPIs). Such compounds are useful to potentiate the antimicrobial activity of antimicrobial compounds such as beta-lactam antibiotics and quinolone antibiotics against Gram-negative bacteria.

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