JP2019507768A5 - - Google Patents
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- Publication number
- JP2019507768A5 JP2019507768A5 JP2018546678A JP2018546678A JP2019507768A5 JP 2019507768 A5 JP2019507768 A5 JP 2019507768A5 JP 2018546678 A JP2018546678 A JP 2018546678A JP 2018546678 A JP2018546678 A JP 2018546678A JP 2019507768 A5 JP2019507768 A5 JP 2019507768A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- heta
- cycloalkyl
- substituted
- 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
- 150000003839 salts Chemical group 0.000 claims 33
- 229910052757 nitrogen Inorganic materials 0.000 claims 28
- 150000001875 compounds Chemical class 0.000 claims 25
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 239000001257 hydrogen Substances 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 150000002367 halogens Chemical class 0.000 claims 19
- 229910052760 oxygen Inorganic materials 0.000 claims 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims 16
- 229910052717 sulfur Inorganic materials 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 125000002950 monocyclic group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 208000035143 Bacterial infection Diseases 0.000 claims 6
- 208000022362 bacterial infectious disease Diseases 0.000 claims 6
- 235000019000 fluorine Nutrition 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 241001169527 Morganella sp. (in: Fungi) Species 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- HZZVJAQRINQKSD-UHFFFAOYSA-N Clavulanic acid Natural products OC(=O)C1C(=CCO)OC2CC(=O)N21 HZZVJAQRINQKSD-UHFFFAOYSA-N 0.000 claims 3
- 229940123930 Lactamase inhibitor Drugs 0.000 claims 3
- NDCUAPJVLWFHHB-UHNVWZDZSA-N avibactam Chemical compound C1N2[C@H](C(N)=O)CC[C@@]1([H])N(OS(O)(=O)=O)C2=O NDCUAPJVLWFHHB-UHNVWZDZSA-N 0.000 claims 3
- 229960002379 avibactam Drugs 0.000 claims 3
- 239000003781 beta lactamase inhibitor Substances 0.000 claims 3
- 229940126813 beta-lactamase inhibitor Drugs 0.000 claims 3
- HZZVJAQRINQKSD-PBFISZAISA-N clavulanic acid Chemical compound OC(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21 HZZVJAQRINQKSD-PBFISZAISA-N 0.000 claims 3
- 229960003324 clavulanic acid Drugs 0.000 claims 3
- 229960005256 sulbactam Drugs 0.000 claims 3
- FKENQMMABCRJMK-RITPCOANSA-N sulbactam Chemical compound O=S1(=O)C(C)(C)[C@H](C(O)=O)N2C(=O)C[C@H]21 FKENQMMABCRJMK-RITPCOANSA-N 0.000 claims 3
- 229960003865 tazobactam Drugs 0.000 claims 3
- LPQZKKCYTLCDGQ-WEDXCCLWSA-N tazobactam Chemical compound C([C@]1(C)S([C@H]2N(C(C2)=O)[C@H]1C(O)=O)(=O)=O)N1C=CN=N1 LPQZKKCYTLCDGQ-WEDXCCLWSA-N 0.000 claims 3
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 claims 3
- 241000589291 Acinetobacter Species 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 241000588923 Citrobacter Species 0.000 claims 2
- 241000588914 Enterobacter Species 0.000 claims 2
- 241000588722 Escherichia Species 0.000 claims 2
- 241000588748 Klebsiella Species 0.000 claims 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims 2
- 241000589774 Pseudomonas sp. Species 0.000 claims 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 2
- 241000607720 Serratia Species 0.000 claims 2
- 238000007792 addition Methods 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- VFRSADQPWYCXDG-LEUCUCNGSA-N ethyl (2s,5s)-5-methylpyrrolidine-2-carboxylate;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.CCOC(=O)[C@@H]1CC[C@H](C)N1 VFRSADQPWYCXDG-LEUCUCNGSA-N 0.000 claims 2
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- -1 oxadiazolonyl Chemical group 0.000 claims 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 1
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 1
- 238000010276 construction Methods 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- UTCSSFWDNNEEBH-UHFFFAOYSA-N imidazo[1,2-a]pyridine Chemical compound C1=CC=CC2=NC=CN21 UTCSSFWDNNEEBH-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662304447P | 2016-03-07 | 2016-03-07 | |
| US62/304,447 | 2016-03-07 | ||
| PCT/US2017/020303 WO2017155765A1 (en) | 2016-03-07 | 2017-03-02 | Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019507768A JP2019507768A (ja) | 2019-03-22 |
| JP2019507768A5 true JP2019507768A5 (https=) | 2020-04-02 |
| JP7034929B2 JP7034929B2 (ja) | 2022-03-14 |
Family
ID=59789685
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018546678A Active JP7034929B2 (ja) | 2016-03-07 | 2017-03-02 | 二環式アリールモノバクタム化合物及び細菌感染症を治療するためにそれらを使用する方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10407421B2 (https=) |
| EP (1) | EP3426248B1 (https=) |
| JP (1) | JP7034929B2 (https=) |
| KR (1) | KR102408800B1 (https=) |
| CN (1) | CN108778273B (https=) |
| AU (1) | AU2017228870B2 (https=) |
| BR (1) | BR112018067930B1 (https=) |
| CA (1) | CA3016341A1 (https=) |
| MA (1) | MA43811A (https=) |
| MX (1) | MX2018010878A (https=) |
| RU (1) | RU2733402C2 (https=) |
| WO (1) | WO2017155765A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3016341A1 (en) | 2016-03-07 | 2017-09-14 | Merck Sharp & Dohme Corp. | Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections |
| EP3601259B1 (en) | 2017-03-30 | 2022-02-23 | F. Hoffmann-La Roche AG | Isoquinolines as inhibitors of hpk1 |
| EP3691639B1 (en) * | 2017-10-02 | 2023-11-15 | Merck Sharp & Dohme LLC | Chromane monobactam compounds for the treatment of bacterial infections |
| WO2019144969A1 (zh) * | 2018-01-29 | 2019-08-01 | 南京明德新药研发股份有限公司 | 用于治疗细菌感染的单环β-内酰胺化合物 |
| TW202019905A (zh) | 2018-07-24 | 2020-06-01 | 瑞士商赫孚孟拉羅股份公司 | 異喹啉化合物及其用途 |
| TW202024053A (zh) | 2018-10-02 | 2020-07-01 | 美商建南德克公司 | 異喹啉化合物及其用途 |
| US11612606B2 (en) | 2018-10-03 | 2023-03-28 | Genentech, Inc. | 8-aminoisoquinoline compounds and uses thereof |
| KR20210083285A (ko) * | 2018-11-13 | 2021-07-06 | 난징 산홈 팔마세우티칼 컴퍼니 리미티드 | 모노박탐 화합물 및 그의 사용 |
| WO2020125670A1 (zh) * | 2018-12-18 | 2020-06-25 | 南京明德新药研发有限公司 | 单环β-内酰胺化合物在制药中的应用 |
| CN110963967B (zh) * | 2019-11-25 | 2021-02-12 | 武汉智顿科技发展有限公司 | 一种2-甲基-4-氨基喹啉的制备方法 |
| CN111018777B (zh) * | 2019-11-25 | 2021-02-12 | 武汉智顿科技发展有限公司 | 一种地喹氯铵的制备方法 |
| CN111303144B (zh) * | 2019-12-13 | 2020-11-27 | 苏州信诺维医药科技有限公司 | 一种治疗细菌感染的化合物 |
| CN114828850B (zh) * | 2019-12-19 | 2024-08-13 | 深圳嘉科生物科技有限公司 | 化合物在制药中的应用 |
| EP4146650B1 (en) | 2020-09-01 | 2026-01-21 | Ningxia Academy of Agriculture and Forestry Sciences | Beta-lactamase inhibitors and their preparation |
| EP4685147A3 (en) | 2021-03-31 | 2026-04-15 | Fedora Pharmaceuticals Inc. | Lactivicin compounds, their preparation and use as antibacterial agents |
| US12410166B2 (en) | 2021-05-07 | 2025-09-09 | Ningxia Academy Of Agriculture And Forestry Sciences | Sulfonylamidine substituted compounds and their use as beta-lactamase inhibitors |
| AU2021473165B2 (en) * | 2021-11-09 | 2025-05-22 | Guangzhou HC New Drug Research Co., Ltd. | PHARMACEUTICAL COMPOSITION CONTAINING β-LACTAM COMPOUND AND USE THEREOF |
| IL320644A (en) * | 2022-11-07 | 2025-07-01 | Univ Kyoto | Quinazoline derivatives |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4684722A (en) | 1986-01-06 | 1987-08-04 | E. R. Squibb & Sons, Inc. | Monosulfactams |
| US5250691A (en) * | 1991-09-09 | 1993-10-05 | E. R. Squibb & Sons, Inc. | Heteroaryl derivatives of monocyclic beta-lactam antibiotics |
| MY127641A (en) | 1995-10-12 | 2006-12-29 | Essential Therapeutics Inc | Cephalosporin antibiotics |
| RU2269525C2 (ru) * | 2000-08-10 | 2006-02-10 | Бритиш Биотех Фармасьютикалс Лимитед | Антибактериальные агенты |
| CA2783572C (en) | 2005-12-07 | 2016-08-09 | Basilea Pharmaceutica Ag | Useful combinations of monobactam antibiotics with beta-lactamase inhibitors |
| TWI519508B (zh) * | 2007-06-12 | 2016-02-01 | Achaogen Inc | 抗菌劑 |
| DK2646436T3 (en) | 2010-11-29 | 2015-06-29 | Pfizer | monobactams |
| UY34585A (es) | 2012-01-24 | 2013-09-02 | Aicuris Gmbh & Co Kg | Compuestos b-lactámicos sustituidos con amidina, su preparación y uso |
| US20140275007A1 (en) | 2013-03-14 | 2014-09-18 | Rempex Pharmaceuticals, Inc. | Oxamazin antibiotics |
| MX373444B (es) | 2014-03-24 | 2020-04-30 | Novartis Ag | Compuestos organicos de monobactam para el tratamiento de infecciones bacterianas. |
| CA3016341A1 (en) | 2016-03-07 | 2017-09-14 | Merck Sharp & Dohme Corp. | Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections |
-
2017
- 2017-03-02 CA CA3016341A patent/CA3016341A1/en active Pending
- 2017-03-02 RU RU2018134948A patent/RU2733402C2/ru active
- 2017-03-02 EP EP17763763.4A patent/EP3426248B1/en active Active
- 2017-03-02 MA MA043811A patent/MA43811A/fr unknown
- 2017-03-02 AU AU2017228870A patent/AU2017228870B2/en active Active
- 2017-03-02 WO PCT/US2017/020303 patent/WO2017155765A1/en not_active Ceased
- 2017-03-02 MX MX2018010878A patent/MX2018010878A/es unknown
- 2017-03-02 JP JP2018546678A patent/JP7034929B2/ja active Active
- 2017-03-02 KR KR1020187028417A patent/KR102408800B1/ko active Active
- 2017-03-02 US US16/076,781 patent/US10407421B2/en active Active
- 2017-03-02 CN CN201780015430.2A patent/CN108778273B/zh active Active
- 2017-03-02 BR BR112018067930-5A patent/BR112018067930B1/pt active IP Right Grant
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