JP2013541514A5 - - Google Patents
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- Publication number
- JP2013541514A5 JP2013541514A5 JP2013527375A JP2013527375A JP2013541514A5 JP 2013541514 A5 JP2013541514 A5 JP 2013541514A5 JP 2013527375 A JP2013527375 A JP 2013527375A JP 2013527375 A JP2013527375 A JP 2013527375A JP 2013541514 A5 JP2013541514 A5 JP 2013541514A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- unsubstituted
- alkyl
- ethyl
- chlorine
- 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 41
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 15
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 14
- 229910052801 chlorine Inorganic materials 0.000 claims 14
- 239000000460 chlorine Substances 0.000 claims 14
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 13
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 13
- 229910052794 bromium Inorganic materials 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 238000000034 method Methods 0.000 claims 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 9
- 229910052731 fluorine Inorganic materials 0.000 claims 9
- 239000011737 fluorine Substances 0.000 claims 9
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 7
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 6
- 244000005700 microbiome Species 0.000 claims 5
- 108090000790 Enzymes Proteins 0.000 claims 4
- 102000004190 Enzymes Human genes 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 108090000364 Ligases Proteins 0.000 claims 3
- 102000003960 Ligases Human genes 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 150000001721 carbon Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 230000000813 microbial effect Effects 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 108010071170 Leucine-tRNA ligase Proteins 0.000 claims 1
- 102100023339 Leucine-tRNA ligase, cytoplasmic Human genes 0.000 claims 1
- 241000186359 Mycobacterium Species 0.000 claims 1
- 241000187479 Mycobacterium tuberculosis Species 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 229940121383 antituberculosis agent Drugs 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- -1 methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy Chemical group 0.000 claims 1
- 125000004971 nitroalkyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000005920 sec-butoxy group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- 239000000814 tuberculostatic agent Substances 0.000 claims 1
- 0 **c1c(*O)c(C(*)O)ccc1* Chemical compound **c1c(*O)c(C(*)O)ccc1* 0.000 description 7
- RQBVDAMLFJQLTJ-SSDOTTSWSA-N COc(cc1)c(B(O)O[C@@H]2CN)c2c1Br Chemical compound COc(cc1)c(B(O)O[C@@H]2CN)c2c1Br RQBVDAMLFJQLTJ-SSDOTTSWSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38059610P | 2010-09-07 | 2010-09-07 | |
| US61/380,596 | 2010-09-07 | ||
| PCT/US2011/050728 WO2012033858A2 (en) | 2010-09-07 | 2011-09-07 | Boron-containing small molecules |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016114971A Division JP2016199558A (ja) | 2010-09-07 | 2016-06-09 | 細菌感染治療用のベンゾオキサボロール誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013541514A JP2013541514A (ja) | 2013-11-14 |
| JP2013541514A5 true JP2013541514A5 (enExample) | 2014-10-23 |
| JP5952280B2 JP5952280B2 (ja) | 2016-07-13 |
Family
ID=44653589
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013527375A Active JP5952280B2 (ja) | 2010-09-07 | 2011-09-07 | 細菌感染治療用のベンゾオキサボロール誘導体 |
| JP2016114971A Withdrawn JP2016199558A (ja) | 2010-09-07 | 2016-06-09 | 細菌感染治療用のベンゾオキサボロール誘導体 |
| JP2017195759A Active JP6491294B2 (ja) | 2010-09-07 | 2017-10-06 | 細菌感染治療用のベンゾオキサボロール誘導体 |
| JP2019035145A Pending JP2019112431A (ja) | 2010-09-07 | 2019-02-28 | 細菌感染治療用のベンゾオキサボロール誘導体 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016114971A Withdrawn JP2016199558A (ja) | 2010-09-07 | 2016-06-09 | 細菌感染治療用のベンゾオキサボロール誘導体 |
| JP2017195759A Active JP6491294B2 (ja) | 2010-09-07 | 2017-10-06 | 細菌感染治療用のベンゾオキサボロール誘導体 |
| JP2019035145A Pending JP2019112431A (ja) | 2010-09-07 | 2019-02-28 | 細菌感染治療用のベンゾオキサボロール誘導体 |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US8703742B2 (enExample) |
| EP (2) | EP3251678B1 (enExample) |
| JP (4) | JP5952280B2 (enExample) |
| KR (2) | KR101949423B1 (enExample) |
| CN (2) | CN108610356B (enExample) |
| AU (1) | AU2011299243C1 (enExample) |
| BR (1) | BR112013005426B1 (enExample) |
| CA (1) | CA2810021C (enExample) |
| CY (1) | CY1124728T1 (enExample) |
| DK (2) | DK3251678T3 (enExample) |
| EA (2) | EA033311B1 (enExample) |
| ES (2) | ES2635333T3 (enExample) |
| HR (1) | HRP20211762T1 (enExample) |
| HU (1) | HUE059033T2 (enExample) |
| IL (2) | IL225000A (enExample) |
| LT (1) | LT3251678T (enExample) |
| MX (1) | MX338209B (enExample) |
| PL (1) | PL3251678T3 (enExample) |
| PT (1) | PT3251678T (enExample) |
| RS (1) | RS62548B1 (enExample) |
| SG (2) | SG10201507032YA (enExample) |
| SI (1) | SI3251678T1 (enExample) |
| SM (1) | SMT202100643T1 (enExample) |
| WO (1) | WO2012033858A2 (enExample) |
| ZA (1) | ZA201301598B (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7767657B2 (en) | 2005-02-16 | 2010-08-03 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules |
| US9440994B2 (en) | 2009-08-14 | 2016-09-13 | Anacor Pharmaceuticals, Inc. | Boron containing small molecules as antiprotozoal agents |
| WO2011094450A1 (en) | 2010-01-27 | 2011-08-04 | Anacor Pharmaceuticals, Inc | Boron-containing small molecules |
| PT3251678T (pt) * | 2010-09-07 | 2021-11-22 | Anacor Pharmaceuticals Inc | Derivados de benzoxaborol para tratamento de infeções bacterianas |
| US8530452B2 (en) | 2011-12-22 | 2013-09-10 | Micurx Pharmaceuticals, Inc. | Tricyclic boron compounds for antimicrobial therapy |
| US9585396B2 (en) | 2013-01-30 | 2017-03-07 | Agrofresh Inc. | Volatile applications against pathogens |
| US10070649B2 (en) | 2013-01-30 | 2018-09-11 | Agrofresh Inc. | Volatile applications against pathogens |
| KR101666331B1 (ko) | 2013-01-30 | 2016-10-13 | 다우 아그로사이언시즈 엘엘씨 | 육류, 식물, 또는 식물 부분에 대한 휘발성 항미생물제로서의 벤족사보롤의 용도 |
| US11039617B2 (en) | 2013-01-30 | 2021-06-22 | Agrofresh Inc. | Large scale methods of uniformly coating packaging surfaces with a volatile antimicrobial to preserve food freshness |
| US8669207B1 (en) | 2013-01-30 | 2014-03-11 | Dow Agrosciences, Llc. | Compounds and compositions |
| AP2015008638A0 (en) | 2013-02-01 | 2015-08-31 | Anacor Pharmaceuticals Inc | Boron-containing small molecules as antiprotozoal agents |
| KR101636431B1 (ko) | 2013-07-30 | 2016-07-05 | 동아에스티 주식회사 | 트리사이클릭 벤즈옥사보롤 화합물, 이의 제조방법 및 용도 |
| EP4029870A1 (en) | 2013-08-09 | 2022-07-20 | GlaxoSmithKline Intellectual Property (No.2) Limited | Tricyclic benzoxaborole compounds and uses thereof |
| EA038093B1 (ru) * | 2013-12-20 | 2021-07-05 | Глаксосмитклайн Интеллекчуал Проперти (№2) Лимитед | Способ лечения заболевания, вызванного инфекцией комплекса mycobacterium tuberculosis, с использованием (s)-(3-хлор-7,8-дигидро-2h-1,6,9-триокса-9a-борабензо[cd]азулен-2-ил)метанамина или его фармацевтически приемлемой соли |
| WO2016001834A1 (en) | 2014-07-01 | 2016-01-07 | Daiichi Sankyo Company, Limited | Tricyclic benzoxaboroles as antibacterial agents |
| MA41494B1 (fr) * | 2015-02-12 | 2020-10-28 | Glaxosmithkline Ip No 2 Ltd | Composés benzoxaborole substitués en position 4 et utilisations associées |
| NZ745681A (en) | 2016-03-07 | 2022-05-27 | Agrofresh Inc | Synergistic methods of using benzoxaborole compounds and preservative gases as an antimicrobial for crops |
| EP3609504A4 (en) | 2017-03-01 | 2021-03-03 | Anacor Pharmaceuticals, Inc. | NEW OXABOROLE ANALOGUES AND USES OF THE LATEST |
| US11834466B2 (en) | 2017-11-30 | 2023-12-05 | 5Metis, Inc. | Benzoxaborole compounds and formulations thereof |
| CN108727176B (zh) * | 2018-07-26 | 2021-05-18 | 荆楚理工学院 | 一种制备5-卤-2,3-二羟基苯甲醛的方法 |
| BR112021003037A2 (pt) | 2018-08-18 | 2021-05-11 | Boragen, Inc. | formas sólidas de benzoxaborol substituído e composições do mesmo |
| AR119515A1 (es) * | 2019-07-30 | 2021-12-22 | Boragen Inc | Proceso de reacción de flujo para la fabricación de agroquímicos que contienen boro |
| CN110664756B (zh) * | 2019-10-09 | 2020-11-17 | 吉林大学 | 一种小儿外伤喷雾剂及其制备方法 |
| US20230340530A1 (en) | 2020-08-31 | 2023-10-26 | Pfizer Inc. | Methods of Protecting RNA |
| CA3239097A1 (en) | 2022-06-23 | 2023-12-28 | Shanghai Micurx Pharmaceutical Co., Ltd. | Prodrugs of boron compounds and their use in treating bacterial infections |
| CN119233823A (zh) * | 2022-06-23 | 2024-12-31 | 上海盟科药业股份有限公司 | 硼化合物治疗非结核分枝杆菌感染的方法和用途及用于治疗相同疾病的药物组合物 |
| CN115572218B (zh) * | 2022-08-29 | 2024-04-16 | 江阴勒森生物科技有限公司 | 一种2-溴-3-羟基苯甲醛及其相关化学发光底物中间体的制备方法 |
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| US20100256092A1 (en) | 2008-05-12 | 2010-10-07 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules |
| WO2010028005A1 (en) | 2008-09-04 | 2010-03-11 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules |
| WO2010045505A1 (en) | 2008-10-15 | 2010-04-22 | Anacor Pharmaceuticals, Inc | Boron-containing small molecules as anti-protozoal agents |
| WO2010045503A1 (en) | 2008-10-15 | 2010-04-22 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules as anti-protozoal agents |
| CN102256494A (zh) | 2008-12-17 | 2011-11-23 | 阿纳科制药公司 | (s)-3-氨甲基-7-(3-羟基-丙氧基)-3h-苯并[c][1,2]氧杂硼杂环戊-1-醇的多晶型物 |
| JP2013500974A (ja) | 2009-07-28 | 2013-01-10 | アナコール ファーマシューティカルズ，インコーポレイテッド | 三置換ホウ素含有分子 |
| PT3251678T (pt) * | 2010-09-07 | 2021-11-22 | Anacor Pharmaceuticals Inc | Derivados de benzoxaborol para tratamento de infeções bacterianas |
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