JPWO2020030761A5 - - Google Patents
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- Publication number
- JPWO2020030761A5 JPWO2020030761A5 JP2021506575A JP2021506575A JPWO2020030761A5 JP WO2020030761 A5 JPWO2020030761 A5 JP WO2020030761A5 JP 2021506575 A JP2021506575 A JP 2021506575A JP 2021506575 A JP2021506575 A JP 2021506575A JP WO2020030761 A5 JPWO2020030761 A5 JP WO2020030761A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- unsubstituted
- substituted
- halogen
- pharmaceutically acceptable
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 102
- 125000001424 substituent group Chemical group 0.000 claims description 64
- 125000005843 halogen group Chemical group 0.000 claims description 51
- 229910052736 halogen Inorganic materials 0.000 claims description 49
- 150000002367 halogens Chemical group 0.000 claims description 49
- 150000001875 compounds Chemical class 0.000 claims description 42
- 150000003839 salts Chemical class 0.000 claims description 36
- 125000000623 heterocyclic group Chemical group 0.000 claims description 29
- 229910052799 carbon Inorganic materials 0.000 claims description 22
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 18
- 125000004429 atom Chemical group 0.000 claims description 18
- 125000004432 carbon atom Chemical group C* 0.000 claims description 18
- 229920006395 saturated elastomer Polymers 0.000 claims description 18
- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- 125000002947 alkylene group Chemical group 0.000 claims description 13
- 230000003115 biocidal effect Effects 0.000 claims description 13
- 239000003795 chemical substances by application Substances 0.000 claims description 13
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 12
- 241000894006 Bacteria Species 0.000 claims description 12
- 208000035143 Bacterial infection Diseases 0.000 claims description 12
- 241000588921 Enterobacteriaceae Species 0.000 claims description 12
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 10
- 241000589289 Moraxellaceae Species 0.000 claims description 9
- 241000947836 Pseudomonadaceae Species 0.000 claims description 9
- 239000003781 beta lactamase inhibitor Substances 0.000 claims description 9
- 229940126813 beta-lactamase inhibitor Drugs 0.000 claims description 9
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 9
- 102000020235 metallo-beta-lactamase Human genes 0.000 claims description 9
- 108060004734 metallo-beta-lactamase Proteins 0.000 claims description 9
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 8
- XQDYOPKCGHWFBY-UHFFFAOYSA-N 1-cyclooctyl-1,3-diazocan-2-one Chemical compound O=C1NCCCCCN1C1CCCCCCC1 XQDYOPKCGHWFBY-UHFFFAOYSA-N 0.000 claims description 7
- 125000003118 aryl group Chemical group 0.000 claims description 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 6
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 6
- 239000003242 anti bacterial agent Substances 0.000 claims description 6
- 229940088710 antibiotic agent Drugs 0.000 claims description 6
- YZBQHRLRFGPBSL-RXMQYKEDSA-N carbapenem Chemical compound C1C=CN2C(=O)C[C@H]21 YZBQHRLRFGPBSL-RXMQYKEDSA-N 0.000 claims description 6
- 229910052801 chlorine Chemical group 0.000 claims description 6
- 239000000460 chlorine Chemical group 0.000 claims description 6
- 229910052731 fluorine Inorganic materials 0.000 claims description 6
- 239000011737 fluorine Substances 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 239000001257 hydrogen Substances 0.000 claims description 6
- 229960002260 meropenem Drugs 0.000 claims description 6
- DMJNNHOOLUXYBV-PQTSNVLCSA-N meropenem Chemical compound C=1([C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)S[C@@H]1CN[C@H](C(=O)N(C)C)C1 DMJNNHOOLUXYBV-PQTSNVLCSA-N 0.000 claims description 6
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 230000002265 prevention Effects 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 241000588626 Acinetobacter baumannii Species 0.000 claims description 3
- 241000589513 Burkholderia cepacia Species 0.000 claims description 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 3
- 241000588697 Enterobacter cloacae Species 0.000 claims description 3
- 241000588724 Escherichia coli Species 0.000 claims description 3
- 241000588747 Klebsiella pneumoniae Species 0.000 claims description 3
- 241000589517 Pseudomonas aeruginosa Species 0.000 claims description 3
- 125000004450 alkenylene group Chemical group 0.000 claims description 3
- 125000004419 alkynylene group Chemical group 0.000 claims description 3
- 125000002837 carbocyclic group Chemical group 0.000 claims description 3
- 238000011260 co-administration Methods 0.000 claims description 3
- 125000004122 cyclic group Chemical group 0.000 claims description 3
- 230000008030 elimination Effects 0.000 claims description 3
- 238000003379 elimination reaction Methods 0.000 claims description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 3
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical group F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims description 2
- 108010081348 HRT1 protein Hairy Chemical group 0.000 claims description 2
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims description 2
- ZJULYDCRWUEPTK-UHFFFAOYSA-N dichloromethyl Chemical group Cl[CH]Cl ZJULYDCRWUEPTK-UHFFFAOYSA-N 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical group F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- ZBZJXHCVGLJWFG-UHFFFAOYSA-N trichloromethyl(.) Chemical group Cl[C](Cl)Cl ZBZJXHCVGLJWFG-UHFFFAOYSA-N 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 3
- 241000193830 Bacillus <bacterium> Species 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- GCKKZLXJSUOGES-UHNVWZDZSA-N [(2R,5R)-2-fluoro-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] hydrogen sulfate Chemical compound S(=O)(=O)(ON1C(=O)N2C[C@H]1CC[C@H]2F)O GCKKZLXJSUOGES-UHNVWZDZSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- -1 diazabicyclooctanone compound Chemical class 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 230000001580 bacterial effect Effects 0.000 description 3
- 230000001332 colony forming effect Effects 0.000 description 3
- QVRLUCMSCRIFNS-UHNVWZDZSA-N [(2R,5R)-2-chloro-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] hydrogen sulfate Chemical compound S(=O)(=O)(ON1C(=O)N2C[C@H]1CC[C@H]2Cl)O QVRLUCMSCRIFNS-UHNVWZDZSA-N 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 229940123930 Lactamase inhibitor Drugs 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229910000037 hydrogen sulfide Inorganic materials 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18290093.6 | 2018-08-09 | ||
| EP18290093.6A EP3608318A1 (en) | 2018-08-09 | 2018-08-09 | Diaazabicyclooctanone derivatives as antibacterials |
| EP18213635.8A EP3670512A1 (en) | 2018-12-18 | 2018-12-18 | Diazabicyclooctanones as inhibitors of serine beta-lactamases |
| EP18213635.8 | 2018-12-18 | ||
| PCT/EP2019/071370 WO2020030761A1 (en) | 2018-08-09 | 2019-08-08 | Diazabicyclooctanones as inhibitors of serine beta-lactamases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021534095A JP2021534095A (ja) | 2021-12-09 |
| JPWO2020030761A5 true JPWO2020030761A5 (es) | 2022-08-18 |
| JP7429988B2 JP7429988B2 (ja) | 2024-02-09 |
Family
ID=67667824
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021506575A Active JP7429988B2 (ja) | 2018-08-09 | 2019-08-08 | セリンベータ－ラクタマーゼのインヒビターとしてのジアザビシクロオクタノン |
Country Status (22)
| Country | Link |
|---|---|
| EP (2) | EP3833665B1 (es) |
| JP (1) | JP7429988B2 (es) |
| KR (1) | KR20210055701A (es) |
| CN (2) | CN117384155A (es) |
| AU (1) | AU2019318115B2 (es) |
| BR (1) | BR112021002311A2 (es) |
| CA (1) | CA3110111A1 (es) |
| DK (1) | DK3833665T3 (es) |
| ES (1) | ES2960952T3 (es) |
| FI (1) | FI3833665T3 (es) |
| HR (1) | HRP20231228T1 (es) |
| HU (1) | HUE063324T2 (es) |
| IL (1) | IL280770B2 (es) |
| LT (1) | LT3833665T (es) |
| MX (1) | MX2021001564A (es) |
| PL (1) | PL3833665T3 (es) |
| RS (1) | RS64679B1 (es) |
| SG (1) | SG11202101255UA (es) |
| SI (1) | SI3833665T1 (es) |
| TW (1) | TWI764030B (es) |
| WO (1) | WO2020030761A1 (es) |
| ZA (1) | ZA202100906B (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111943950B (zh) * | 2020-09-10 | 2022-03-29 | 山东安信制药有限公司 | 一种瑞来巴坦的制备方法 |
| CN115605480B (zh) * | 2021-05-07 | 2024-04-05 | 宁夏农林科学院 | 磺酰脒取代的化合物及其作为β-内酰胺酶抑制剂的用途 |
| CN115448920A (zh) * | 2022-10-14 | 2022-12-09 | 广州楷石医药有限公司 | 一种β-内酰胺酶抑制剂及其应用 |
| CN117700415B (zh) * | 2024-02-06 | 2024-04-30 | 成都四面体药物研究有限公司 | 含脲双环化合物、其用途、其制备的药物、其联合用药物及其复方制剂 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2231667T3 (da) * | 2008-01-18 | 2013-12-16 | Merck Sharp & Dohme | Beta-lactamase-hæmmere |
| ES2606059T3 (es) | 2011-08-30 | 2017-03-17 | Wockhardt Limited | Derivados de 1,6-diazabiciclo[3,2,1]octan-7-ona y su uso en el tratamiento de infecciones bacterianas |
| AR090539A1 (es) | 2012-04-02 | 2014-11-19 | Astrazeneca Ab | COMPUESTOS INHIBIDORES DE b LACTAMASA |
| UA111925C2 (uk) | 2012-12-11 | 2016-06-24 | Федора Фармасьютікалз Інк. | БІЦИКЛІЧНІ СПОЛУКИ ТА ЇХ ВИКОРИСТАННЯ ЯК АНТИБАКТЕРІАЛЬНИХ АГЕНТІВ ТА ІНГІБІТОРІВ β-ЛАКТАМАЗИ |
| GB201310542D0 (en) | 2013-06-13 | 2013-07-31 | Antabio Sas | Compounds |
| GB2533136A (en) | 2014-12-11 | 2016-06-15 | Antabio Sas | Compounds |
| KR20200030584A (ko) | 2017-07-21 | 2020-03-20 | 앤타바이오 에스에이에스 | 화합물 |
| CN107501265B (zh) | 2017-10-09 | 2019-05-28 | 台州职业技术学院 | 一种7-氧代-二氮杂二环[3,2,1]辛烷衍生化合物及其制备方法和应用 |
| WO2019093450A1 (ja) | 2017-11-10 | 2019-05-16 | 塩野義製薬株式会社 | ジアザビシクロオクタン誘導体 |
-
2019
- 2019-08-08 KR KR1020217007060A patent/KR20210055701A/ko active Search and Examination
- 2019-08-08 ES ES19755850T patent/ES2960952T3/es active Active
- 2019-08-08 DK DK19755850.5T patent/DK3833665T3/da active
- 2019-08-08 EP EP19755850.5A patent/EP3833665B1/en active Active
- 2019-08-08 CA CA3110111A patent/CA3110111A1/en active Pending
- 2019-08-08 PL PL19755850.5T patent/PL3833665T3/pl unknown
- 2019-08-08 SI SI201930627T patent/SI3833665T1/sl unknown
- 2019-08-08 BR BR112021002311-9A patent/BR112021002311A2/pt unknown
- 2019-08-08 HU HUE19755850A patent/HUE063324T2/hu unknown
- 2019-08-08 JP JP2021506575A patent/JP7429988B2/ja active Active
- 2019-08-08 EP EP23180712.4A patent/EP4272831A3/en active Pending
- 2019-08-08 WO PCT/EP2019/071370 patent/WO2020030761A1/en active Application Filing
- 2019-08-08 LT LTEPPCT/EP2019/071370T patent/LT3833665T/lt unknown
- 2019-08-08 AU AU2019318115A patent/AU2019318115B2/en active Active
- 2019-08-08 FI FIEP19755850.5T patent/FI3833665T3/fi active
- 2019-08-08 MX MX2021001564A patent/MX2021001564A/es unknown
- 2019-08-08 CN CN202311024006.8A patent/CN117384155A/zh active Pending
- 2019-08-08 IL IL280770A patent/IL280770B2/en unknown
- 2019-08-08 SG SG11202101255UA patent/SG11202101255UA/en unknown
- 2019-08-08 HR HRP20231228TT patent/HRP20231228T1/hr unknown
- 2019-08-08 CN CN201980014933.7A patent/CN111954671B/zh active Active
- 2019-08-08 TW TW108128294A patent/TWI764030B/zh active
- 2019-08-08 RS RS20230929A patent/RS64679B1/sr unknown
-
2021
- 2021-02-10 ZA ZA2021/00906A patent/ZA202100906B/en unknown
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