JP2019532928A5 - - Google Patents
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- Publication number
- JP2019532928A5 JP2019532928A5 JP2019515241A JP2019515241A JP2019532928A5 JP 2019532928 A5 JP2019532928 A5 JP 2019532928A5 JP 2019515241 A JP2019515241 A JP 2019515241A JP 2019515241 A JP2019515241 A JP 2019515241A JP 2019532928 A5 JP2019532928 A5 JP 2019532928A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- heteroaryl
- pharmaceutically acceptable
- acceptable salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 21
- 125000000623 heterocyclic group Chemical group 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000005843 halogen group Chemical group 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000006677 (C1-C3) haloalkoxy group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 208000035143 Bacterial infection Diseases 0.000 claims 3
- 208000022362 bacterial infectious disease Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 208000015181 infectious disease Diseases 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000006242 amine protecting group Chemical group 0.000 claims 2
- 239000003782 beta lactam antibiotic agent Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- -1 optionally Chemical group 0.000 claims 2
- 208000019206 urinary tract infection Diseases 0.000 claims 2
- 239000002132 β-lactam antibiotic Substances 0.000 claims 2
- 229940124586 β-lactam antibiotics Drugs 0.000 claims 2
- 201000001178 Bacterial Pneumonia Diseases 0.000 claims 1
- 206010060803 Diabetic foot infection Diseases 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010062255 Soft tissue infection Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- LTINZAODLRIQIX-FBXRGJNPSA-N cefpodoxime proxetil Chemical compound N([C@H]1[C@@H]2N(C1=O)C(=C(CS2)COC)C(=O)OC(C)OC(=O)OC(C)C)C(=O)C(=N/OC)\C1=CSC(N)=N1 LTINZAODLRIQIX-FBXRGJNPSA-N 0.000 claims 1
- 229960004797 cefpodoxime proxetil Drugs 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 230000001590 oxidative effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000007094 prostatitis Diseases 0.000 claims 1
- 206010040872 skin infection Diseases 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021203942A JP7281527B2 (ja) | 2016-09-16 | 2021-12-16 | ベータラクタマーゼ阻害剤化合物 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662395464P | 2016-09-16 | 2016-09-16 | |
| US62/395,464 | 2016-09-16 | ||
| US201762456423P | 2017-02-08 | 2017-02-08 | |
| US62/456,423 | 2017-02-08 | ||
| PCT/US2017/051692 WO2018053215A1 (en) | 2016-09-16 | 2017-09-15 | Beta-lactamase inhibitor compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021203942A Division JP7281527B2 (ja) | 2016-09-16 | 2021-12-16 | ベータラクタマーゼ阻害剤化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019532928A JP2019532928A (ja) | 2019-11-14 |
| JP2019532928A5 true JP2019532928A5 (enExample) | 2020-10-01 |
| JP6997178B2 JP6997178B2 (ja) | 2022-02-03 |
Family
ID=60083416
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019515241A Active JP6997178B2 (ja) | 2016-09-16 | 2017-09-15 | ベータラクタマーゼ阻害剤化合物 |
| JP2021203942A Active JP7281527B2 (ja) | 2016-09-16 | 2021-12-16 | ベータラクタマーゼ阻害剤化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021203942A Active JP7281527B2 (ja) | 2016-09-16 | 2021-12-16 | ベータラクタマーゼ阻害剤化合物 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10800778B2 (enExample) |
| EP (1) | EP3512851B1 (enExample) |
| JP (2) | JP6997178B2 (enExample) |
| KR (2) | KR102667828B1 (enExample) |
| CN (2) | CN109715630B (enExample) |
| AU (1) | AU2017325863B2 (enExample) |
| CA (1) | CA3036557A1 (enExample) |
| DK (1) | DK3512851T3 (enExample) |
| ES (1) | ES2927986T3 (enExample) |
| HR (1) | HRP20221217T1 (enExample) |
| HU (1) | HUE060282T2 (enExample) |
| IL (2) | IL289686B2 (enExample) |
| LT (1) | LT3512851T (enExample) |
| MA (1) | MA46242A (enExample) |
| MX (2) | MX392515B (enExample) |
| PH (1) | PH12019500558B1 (enExample) |
| PL (1) | PL3512851T3 (enExample) |
| PT (1) | PT3512851T (enExample) |
| SG (1) | SG11201901658PA (enExample) |
| SI (1) | SI3512851T1 (enExample) |
| SM (1) | SMT202200397T1 (enExample) |
| TW (1) | TWI773687B (enExample) |
| WO (1) | WO2018053215A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7060245B2 (ja) | 2016-06-30 | 2022-04-26 | キューペックス バイオファーマ， インコーポレイテッド | ボロン酸誘導体およびその治療的使用 |
| SMT202200397T1 (it) * | 2016-09-16 | 2022-11-18 | Entasis Therapeutics Ltd | Composti inibitori di beta-lattamasi |
| PT3630111T (pt) | 2017-05-08 | 2022-03-01 | Entasis Therapeutics Inc | Compostos e métodos de tratamento de infeções bacterianas |
| EP3781576B1 (en) | 2018-04-20 | 2024-06-12 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| DK3833665T3 (da) | 2018-08-09 | 2023-10-09 | Antabio Sas | Diazabicyclooctanoner som hæmmere af serin-beta-lactamaser |
| US11905286B2 (en) | 2018-08-09 | 2024-02-20 | Antabio Sas | Diazabicyclooctanones as inhibitors of serine beta-lactamases |
| CN112209928B (zh) * | 2019-07-10 | 2023-02-17 | 华东理工大学 | 共价键标记丝氨酸类beta-内酰胺酶的试剂及制备和应用 |
| CN110898999A (zh) * | 2019-11-26 | 2020-03-24 | 中国矿业大学 | 一种煤焦油基煤泥浮选药剂及其制备方法 |
| CN111790439B (zh) * | 2020-07-29 | 2022-12-27 | 成都能特科技发展有限公司 | 一种手性二级胺二苯基膦芳甲酰胺双功能催化剂及其制备方法与应用 |
| WO2022047603A1 (en) | 2020-09-01 | 2022-03-10 | Ningxia Academy Of Agriculture And Forestry Sciences | Beta-lactamase inhibitors and their preparation |
| KR20230167077A (ko) * | 2021-04-05 | 2023-12-07 | 큐펙스 바이오파마 인코포레이티드 | 세프티부텐 투여 요법 |
| EP4146651A4 (en) | 2021-05-07 | 2024-06-05 | Ningxia Academy of Agriculture and Forestry Sciences | SULFONYLAMIDINE SUBSTITUTED COMPOUNDS AND THEIR USE AS BETA-LACTAMASE INHIBITORS |
| US11814385B2 (en) * | 2021-06-25 | 2023-11-14 | University Of South Florida | Small molecule inhibitors targeting Clostridioides difficile sporulation |
| WO2023206580A1 (en) | 2022-04-29 | 2023-11-02 | Entasis Therapeutics Limited | Durlobactam crystalline forms |
| US20230398101A1 (en) * | 2022-06-09 | 2023-12-14 | Fleurir Abx Llc | Co-agents as Therapy Against Anaerobic Pathogens |
| CN118271319B (zh) * | 2022-12-30 | 2025-02-28 | 成都四面体药物研究有限公司 | 一种β-内酰胺酶抑制剂含脲双环化合物、其制备方法及其用途 |
| CN118772145B (zh) * | 2023-04-04 | 2025-10-10 | 上海医药工业研究院有限公司 | 一种二氮杂双环辛烯化合物的制备方法 |
| CN116693531A (zh) * | 2023-06-09 | 2023-09-05 | 河南师范大学 | 一种桥联多环内酰胺类化合物的合成方法 |
| WO2025106662A1 (en) * | 2023-11-15 | 2025-05-22 | Entasis Therapeutics, Inc. | Preparation of boronic acid intermediates useful for the preparation of compounds for treating bacterial infections |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4607041A (en) * | 1983-04-27 | 1986-08-19 | Fisons Plc | Antihypertensive 2-phenyl Hantzsch dihydropyridines |
| WO1995018129A1 (en) | 1993-12-29 | 1995-07-06 | Pfizer Inc. | Diazabicyclic neurokinin antagonists |
| FR2812635B1 (fr) | 2000-08-01 | 2002-10-11 | Aventis Pharma Sa | Nouveaux composes heterocycliques, preparation et utilisation comme medicaments notamment comme anti- bacteriens |
| FR2825705B1 (fr) | 2001-06-08 | 2005-05-20 | Aventis Pharma Sa | Nouveaux composes heterocycliques, leur preparation et leur utilisation comme medicaments, notamment comme anti-bacteriens |
| FR2835186B1 (fr) | 2002-01-28 | 2006-10-20 | Aventis Pharma Sa | Nouveaux composes heterocycliques, actifs comme inhibiteurs de beta-lactamases |
| US7439253B2 (en) | 2002-12-06 | 2008-10-21 | Novexel | Heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors |
| FR2848210B1 (fr) | 2002-12-06 | 2007-10-19 | Aventis Pharma Sa | Nouveaux composes heterocycliques, leur preparation et leur utilisation comme medicaments, notamment comme anti-bacteriens et inhibiteurs de beta-lactamases |
| FR2914923B1 (fr) | 2007-04-12 | 2013-06-14 | Novexel | Nouveaux composes heterocycliques azotes,leur preparation et leur utilisation comme medicaments antibacteriens. |
| JP5038509B2 (ja) * | 2008-01-18 | 2012-10-03 | メルク・シャープ・エンド・ドーム・コーポレイション | β−ラクタマーゼ阻害剤 |
| FR2930553B1 (fr) * | 2008-04-29 | 2010-05-21 | Novexel | Composes azabicycliques, leur preparation et leur utilisation comme medicaments, notamment inhibiteurs de beta-lactamases |
| EP2135959A1 (en) | 2008-06-19 | 2009-12-23 | Novexel | Use of (1R,2S,5R) 1,6-Diazabicyclo [3,2,1]octane-2-carboxamide, 7-oxo-6-(sulfooxy)-, monosodium salt as a diagnostic reagent for detecting serine beta-lactamases |
| FR2936798B1 (fr) | 2008-10-03 | 2012-09-28 | Novexel | Nouveaux composes heterocycliques azotes, leur preparation et leur utilisation comme medicaments antibacteriens. |
| FR2936951B1 (fr) | 2008-10-10 | 2010-12-03 | Novexel | Nouvelles combinaisons de composes heterocycliques azotes antibacteriens avec d'autres composes antibacteriens et leur utilisation comme medicaments |
| FR2937034B1 (fr) | 2008-10-10 | 2012-11-23 | Novexel | Nouveaux composes heterocycliques azotes, leur preparation et leur utilisation comme medicaments antibacteriens |
| FR2951171A1 (fr) | 2009-10-09 | 2011-04-15 | Novexel | Nouveau sel de sodium d'un compose azabicyclique sous forme enantiomere cristallisee et nouvelles formes polymorphes et pseudopolymorphes ainsi que leur preparation |
| TWI543961B (zh) * | 2010-04-20 | 2016-08-01 | 大正製藥股份有限公司 | Novel hydroxamic acid derivatives |
| AU2011373912B2 (en) | 2011-07-26 | 2016-09-29 | Wockhardt Limited | Pharmaceutical compositions comprising beta-lactam antibiotic, sulbactam and beta-lactamase inhibitor |
| JP5808860B2 (ja) | 2011-07-26 | 2015-11-10 | ウォックハート リミテッド | スルバクタム及びベータ−ラクタマーゼインヒビターを含む医薬組成物 |
| RU2636147C1 (ru) * | 2011-08-27 | 2017-11-21 | Вокхардт Лимитед | Производные 1,6-диазабицикло[3,2,1]октан-7-она и их применение при лечении бактериальных инфекционных болезней |
| AU2012303693B2 (en) | 2011-08-30 | 2014-07-03 | Wockhardt Limited | 1,6- diazabicyclo [3,2,1] octan- 7 - one derivatives and their use in the treatment of bacterial infections |
| US8754102B2 (en) | 2011-09-13 | 2014-06-17 | Wockhardt Ltd. | Nitrogen containing compounds and their use |
| US8796257B2 (en) | 2011-12-02 | 2014-08-05 | Naeja Pharmaceutical Inc. | Bicyclic compounds and their use as antibacterial agents and β-lactamase inhibitors |
| EP2814483A2 (en) | 2012-02-15 | 2014-12-24 | Rempex Pharmaceuticals, Inc. | Methods of treating bacterial infections |
| AU2013237869A1 (en) | 2012-03-30 | 2014-10-23 | Cubist Pharmaceuticals, Inc. | Isoxazole beta-lactamase inhibitors |
| WO2013149121A1 (en) | 2012-03-30 | 2013-10-03 | Cubist Pharmaceuticals, Inc. | 1,3,4-oxadiazole and 1,3,4-thiadiazole beta-lactamase inhibitors |
| US8916709B2 (en) | 2012-03-30 | 2014-12-23 | Cubist Pharmaceuticals, Inc. | 1,2,4-oxadiazole and 1,2,4-thiadiazole β-lactamase inhibitors |
| US8969570B2 (en) | 2012-03-30 | 2015-03-03 | Cubist Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| AR090539A1 (es) * | 2012-04-02 | 2014-11-19 | Astrazeneca Ab | COMPUESTOS INHIBIDORES DE b LACTAMASA |
| TWI565707B (zh) | 2012-05-30 | 2017-01-11 | 明治製菓藥業股份有限公司 | 新穎β－內醯胺酶抑制劑及其製造方法 |
| EP2961751B1 (en) | 2012-08-25 | 2018-03-21 | Wockhardt Limited | 1,6- diazabicyclo [3,2,1]octan- 7- one derivatives and their use in the treatment of bacterial infections |
| CN104768547A (zh) | 2012-09-03 | 2015-07-08 | 沃克哈特有限公司 | 抗菌组合物 |
| CA2897446A1 (en) | 2013-02-06 | 2014-08-14 | Astrazeneca Ab | Combination therapy for the treatment of nosocomial pneumonia |
| WO2014141132A1 (en) | 2013-03-14 | 2014-09-18 | Naeja Pharmaceutical Inc. | NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS |
| US9968593B2 (en) | 2014-11-17 | 2018-05-15 | Entasis Therapeutics Limited | Combination therapy for treatment of resistant bacterial infections |
| WO2016156348A1 (en) * | 2015-03-31 | 2016-10-06 | Mutabilis | Novel heterocyclic compounds and their use in preventing or treating bacterial infections |
| SMT202200397T1 (it) * | 2016-09-16 | 2022-11-18 | Entasis Therapeutics Ltd | Composti inibitori di beta-lattamasi |
| KR20230007830A (ko) * | 2021-07-06 | 2023-01-13 | 현대자동차주식회사 | 고강성 저선팽창 열가소성 수지 조성물 및 이를 포함하는 성형체 |
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2017
- 2017-09-15 SM SM20220397T patent/SMT202200397T1/it unknown
- 2017-09-15 AU AU2017325863A patent/AU2017325863B2/en active Active
- 2017-09-15 EP EP17784063.4A patent/EP3512851B1/en active Active
- 2017-09-15 PT PT177840634T patent/PT3512851T/pt unknown
- 2017-09-15 HR HRP20221217TT patent/HRP20221217T1/hr unknown
- 2017-09-15 CA CA3036557A patent/CA3036557A1/en active Pending
- 2017-09-15 DK DK17784063.4T patent/DK3512851T3/da active
- 2017-09-15 CN CN201780057302.4A patent/CN109715630B/zh active Active
- 2017-09-15 JP JP2019515241A patent/JP6997178B2/ja active Active
- 2017-09-15 HU HUE17784063A patent/HUE060282T2/hu unknown
- 2017-09-15 MX MX2021010077A patent/MX392515B/es unknown
- 2017-09-15 KR KR1020237017457A patent/KR102667828B1/ko active Active
- 2017-09-15 ES ES17784063T patent/ES2927986T3/es active Active
- 2017-09-15 LT LTEPPCT/US2017/051692T patent/LT3512851T/lt unknown
- 2017-09-15 KR KR1020197010376A patent/KR102537340B1/ko active Active
- 2017-09-15 PL PL17784063.4T patent/PL3512851T3/pl unknown
- 2017-09-15 WO PCT/US2017/051692 patent/WO2018053215A1/en not_active Ceased
- 2017-09-15 PH PH1/2019/500558A patent/PH12019500558B1/en unknown
- 2017-09-15 MX MX2019003060A patent/MX385507B/es unknown
- 2017-09-15 CN CN202210161577.5A patent/CN114591223B/zh active Active
- 2017-09-15 SI SI201731232T patent/SI3512851T1/sl unknown
- 2017-09-15 TW TW106131860A patent/TWI773687B/zh active
- 2017-09-15 US US16/333,900 patent/US10800778B2/en active Active
- 2017-09-15 IL IL289686A patent/IL289686B2/en unknown
- 2017-09-15 SG SG11201901658PA patent/SG11201901658PA/en unknown
- 2017-09-15 MA MA046242A patent/MA46242A/fr unknown
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2019
- 2019-03-11 IL IL265276A patent/IL265276B/en unknown
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2021
- 2021-12-16 JP JP2021203942A patent/JP7281527B2/ja active Active