DK2613788T3 - Benzoxaborolderivater til behandling af bakterieinfektioner - Google Patents
Benzoxaborolderivater til behandling af bakterieinfektioner Download PDFInfo
- Publication number
- DK2613788T3 DK2613788T3 DK11758050.6T DK11758050T DK2613788T3 DK 2613788 T3 DK2613788 T3 DK 2613788T3 DK 11758050 T DK11758050 T DK 11758050T DK 2613788 T3 DK2613788 T3 DK 2613788T3
- Authority
- DK
- Denmark
- Prior art keywords
- exemplary embodiment
- unsubstituted
- compound
- mmol
- alkyl
- Prior art date
Links
- 241000894006 Bacteria Species 0.000 title 1
- 208000015181 infectious disease Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 23
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000001246 bromo group Chemical group Br* 0.000 claims 9
- 125000001309 chloro group Chemical group Cl* 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 7
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- -1 methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- 102000004190 Enzymes Human genes 0.000 claims 3
- 108090000790 Enzymes Proteins 0.000 claims 3
- 102000003960 Ligases Human genes 0.000 claims 3
- 108090000364 Ligases Proteins 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 244000005700 microbiome Species 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 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
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 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
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000005920 sec-butoxy group Chemical group 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
- 229910052717 sulfur Inorganic materials 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
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 229910052796 boron Inorganic materials 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000005309 thioalkoxy group Chemical group 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/69—Boron compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (21)
1. Forbindelse, som har en struktur, der er:
hvor R3 er -CH2NO2 eller -CH2NH2; R4 er valgt fra gruppen bestående af halogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy og sec-butoxy; Y er O eller S; og R5 er valgt fra gruppen bestående af substitueret eller usubstitueret alkyl og substitueret eller usubstitueret heteroalkyl; eller et salt, hydrat eller solvat deraf; hvor alkylgrupperne har 10 eller færre carbonatomer, og hvor heteroalkylgrupperne indbefatter mindst ét heteroatom valgt fra gruppen bestående af B, O, N og S; og hvor substituenterne til alkyl- og heteroalkylgrupperne hver er valgt fra gruppen bestående af: -R', -OR', =0, =NR', =N-OR', -NR'R", -SR', -halogen, -SiR'R"R"', OC(0)R', -C(0)R', -C02R', -CONR'R", -0C(0)NR'R", -NR"C(0)R', NR'C(0)NR"R"', -NR"C(0)2R', -NR.....-C(NR'R"R"')=NR"", NR""-C(NR'R")=NR'", -S(0)R', -S(0)2R', -S(0)2NR'R", NR"S02R', -CN, -N02, -N3, -CH(Ph)2, fluor(Ci-C4)-alkoxy og fluor(Ci-C4)-alkyl, i et antal i intervallet fra nul til (2m'+1), hvor m' er det samlede antal carbonatomer i en sådan gruppe; hvor R', R", R"', R"" og R.....hver uafhængigt er hydrogen, usubstituerede heteroalkyl-, usubstituerede aryl-, usubstituerede alkyl-, alkoxy- eller thioalkoxygrupper eller arylalkylgrupper.
2. Forbindelse ifølge krav 1, som har en struktur, der er:
hvor C* er et carbonatom, der er et stereocenter, som har en konfiguration, der er (R) eller (S).
3. Forbindelse ifølge krav 1, som har en struktur, der er
hvor C* er et carbonatom, der er et stereocenter, som har en konfiguration, der er (R) eller (S).
4. Forbindelse ifølge krav 2 eller krav 3, hvor C*-stereocenteret har en (S)-konfiguration.
5. Forbindelse ifølge et hvilket som helst af de foregående krav, hvor R3 er -CH2NH2.
6. Forbindelse ifølge et hvilket som helst af de foregående krav, hvor R4 er valgt fra gruppen bestående af fluor, chlor, brom og iod; idet R4 fortrinsvis er chlor eller brom; og R4 mere fortrinsvis er chlor.
7. Forbindelse ifølge et hvilket som helst af kravene 1 til 5, hvor R3 er -CH2NH2; og R4 er halogen.
8. Forbindelse ifølge et hvilket som helst af de foregående krav, hvor R3 er -CH2NH2; R4 er chlor; Y er O; og R5 er substitueret eller usubstitueret alkyl.
9. Forbindelse ifølge et hvilket som helst af kravene 1 til 5, hvor R4 er valgt fra gruppen bestående af methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy og sec-butoxy; idet R4 fortrinsvis er methoxy eller ethoxy.
10. Forbindelse ifølge et hvilket som helst af de foregående krav, hvor R5 er usubstitueret alkyl; idet R5 fortrinsvis er valgt fra gruppen bestående af methyl, ethyl, propyl, isopropyl, butyl, isobutyl, f-butyl og sec-butyl.
11. Forbindelse ifølge et hvilket som helst af kravene 1 til 9, hvor R5 er:
hvor a er 1, 2, 3, 4, 5, 6, 7, 8, 9 eller 10; hver R10 og hver R11 er uafhængigt valgt fra gruppen bestående af H, substitueret eller usubstitueret alkyl, OFI og NH2; R12 er valgt fra gruppen bestående af H, R7, halogen, cyano, amidino, OR7, NR7R8, SR7, -N(R7)S(0)2R8, -C(0)R7, -C(0)0R7, -C(0)NR7R8, hvor hver R7 og hver R8 er uafhængigt valgt fra gruppen bestående af H, substitueret eller usubstitueret alkyl, substitueret eller usubstitueret heteroalkyl, substitueret eller usubstitueret cycloalkyl, substitueret eller usubstitueret heterocycloalkyl, substitueret eller usubstitueret aryl og substitueret eller usubstitueret heteroaryl; a fortrinsvis er 1, 2, 3, 4 eller 5; a fortrinsvis er 2, 3 eller 4; a fortrinsvis er 3; hver R10 og hver R11 fortrinsvis er uafhængigt valgt fra gruppen bestående af H, substitueret eller usubstitueret alkyl, OH og NH2; idet hver R10 og hver R11 fortrinsvis er H; R12 fortrinsvis er valgt fra gruppen bestående af H, OH, NH2, methyl, ethyl, -NHS(0)2CH3, cyano, -NHC(0)CH3, -NHC(0)NHCH2CH3, -C(0)NH2, -C(0)0H, 4-(methoxy)phenyl, benzyl, benzoxy, -NHC(0)0CH2Ph, -C(0)NHCH2CH20H og -C(NH2)(NH).
12. Forbindelse ifølge et hvilket som helst af kravene 1 til 4, hvor R4 er chlor, R3 er -CH2NH2; og Y er O; R4 er brom, R3 er -CH2NH2; og Y er O; R4 er methyl, R3 er -CH2NH2; og Y er O.
13. Forbindelse ifølge et hvilket som helst af kravene 1 til 11, hvor Y er O.
14. Forbindelse ifølge et hvilket som helst af kravene 1 til 4, hvor R4 er halogen, R3 er -CH2NH2; Y er O; og R5 er methyl; eller R4 er halogen, R3 er -CFI2NFI2; Y er O; og R5 er ethyl; eller R4 er halogen, R3 er -CFI2NFI2; Y er O; og R5 er propyl; eller R4 er halogen, R3 er -CFI2NFI2; Y er O; og R5 er isopropyl; eller R4 er halogen, R3 er -CH2NFI2; Y er O; og R5 er usubstitueret C4-alkyl; eller R4 er halogen, R3 er -CH2NFI2; Y er O; og R5 er usubstitueret Cs-alkyl; eller R4 er halogen, R3 er -CFI2NFI2; Y er O; og R5 er usubstitueret C6-alkyl.
15. Forbindelse ifølge et hvilket som helst af kravene 1 til 4, hvor R4 er fluor, R3 er -CH2NH2; Y er O; og R5 er methyl; eller R4 er chlor, R3 er -CH2NH2; Y er O; og R5 er methyl; eller R4 er brom, R3 er -CH2NH2; Y er O; og R5 er methyl; eller R4 er fluor, R3 er -CFI2NFI2; Y er O; og R5 er ethyl; eller R4 er chlor, R3 er -CH2NH2; Y er O; og R5 er ethyl; eller R4 er brom, R3 er -CH2NH2; Y er O; og R5 er ethyl; eller R4 er fluor, R3 er -CH2NH2; Y er O; og R5 er propyl; R4 er chlor, R3 er -CFI2NH2; Y er O; og R5 er propyl; R4 er brom, R3 er -CFI2NFI2; Y er O; og R5 er propyl; R4 er fluor, R3 er -CFI2NFI2; Y er O; og R5 er isopropyl; R4 er chlor, R3 er -CFI2NH2; Y er O; og R5 er isopropyl; eller R4 er brom, R3 er -CH2NH2; Y er O; og R5 er isopropyl; eller R4 er fluor, R3 er -CFI2NFI2; Y er O; og R5 er usubstitueret C4-alkyl; eller R4 er chlor, R3 er -CFI2NH2; Y er O; og R5 er usubstitueret C4-alkyl; eller R4 er brom, R3 er -CFI2NFI2; Y er O; og R5 er usubstitueret C4-alkyl; R4 er fluor, R3 er -CH2NH2; Y er O; og R5 er usubstitueret Cs-alkyl; eller R4 er chlor, R3 er -CH2NH2; Y er O; og R5 er usubstitueret Cs-alkyl; eller R4 er brom, R3 er -CH2NH2; Y er O; og R5 er usubstitueret Cs-alkyl; eller R4 er fluor, R3 er -CH2NH2; Y er O; og R5 er usubstitueret C6-alkyl; eller R4 er chlor, R3 er -CH2NH2; Y er O; og R5 er usubstitueret C6-alkyl; eller R4 er brom, R3 er -CH2NH2; Y er O; og R5 er usubstitueret C6-alkyl.
16. Forbindelse ifølge et hvilket som helst af kravene 1 til 4, hvor R4 er brom, R3 er -CH2NH2; Y er O; og R5 er methyl.
17. Sammensætning, som omfatter: a) en første stereoisomer af forbindelsen ifølge et hvilket som helst af kravene 2 til 16; b) mindst én yderligere stereoisomer af den første stereoisomer; hvor den første stereoisomer er til stede i et enantiomert overskud på mindst 80% i forhold til den mindst ene yderligere stereoisomer.
18. Kombination, som omfatter forbindelsen ifølge et hvilket som helst af kravene 1 til 16 eller et farmaceutisk acceptabelt salt deraf sammen med mindst ét andet terapeutisk aktivt middel.
19. Farmaceutisk formulering, som omfatter: a) forbindelsen ifølge et hvilket som helst af kravene 1 til 16 eller et farmaceutisk acceptabelt salt deraf; og b) en farmaceutisk acceptabel excipiens.
20. Forbindelse ifølge et hvilket som helst af kravene 1 til 16eller et farmaceutisk acceptabelt salt deraf eller en kombination ifølge krav 18 til anvendelse ved behandling og/eller forebyggelse afen sygdom eller bakterieinfektion hos et dyr; eventuelt hvor sygdommen er tuberkulose; og eventuelt hvor dyret er et menneske.
21. In v/fro-fremgangsmåde til: (A) at hæmme et enzym, hvilket omfatter: at bringe enzymet i kontakt med forbindelsen ifølge et hvilket som helst af kravene 1 til 16, hvorved enzymet hæmmes; (B) at dræbe en mikroorganisme og/eller forhindre dens vækst, hvilket omfatter: at bringe mikroorganismen i kontakt med en effektiv mængde af forbindelsen ifølge et hvilket som helst af kravene 1 til 16, hvorved mikroorganismen dræbes, og/eller dens vækst forhindres; eller (C) at hæmme redigeringsdomænet afen t-RNA-syntetase, hvilket omfatter: at bringe syntetasen i kontakt med en effektiv mængde af en forbindelse ifølge et hvilket som helst af kravene 1 til 16 eller et farmaceutisk acceptabelt salt deraf, hvorved syntetasen hæmmes.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38059610P | 2010-09-07 | 2010-09-07 | |
| PCT/US2011/050728 WO2012033858A2 (en) | 2010-09-07 | 2011-09-07 | Boron-containing small molecules |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2613788T3 true DK2613788T3 (da) | 2017-08-07 |
Family
ID=44653589
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK11758050.6T DK2613788T3 (da) | 2010-09-07 | 2011-09-07 | Benzoxaborolderivater til behandling af bakterieinfektioner |
| DK17176654.6T DK3251678T3 (da) | 2010-09-07 | 2011-09-07 | Benzoxaborolderivater til behandling af bakterieinfektioner |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK17176654.6T DK3251678T3 (da) | 2010-09-07 | 2011-09-07 | Benzoxaborolderivater til behandling af bakterieinfektioner |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US8703742B2 (da) |
| EP (2) | EP3251678B1 (da) |
| JP (4) | JP5952280B2 (da) |
| KR (2) | KR101949423B1 (da) |
| CN (2) | CN103140228A (da) |
| AU (1) | AU2011299243C1 (da) |
| BR (1) | BR112013005426B1 (da) |
| CA (1) | CA2810021C (da) |
| CY (1) | CY1124728T1 (da) |
| DK (2) | DK2613788T3 (da) |
| EA (2) | EA028743B1 (da) |
| ES (2) | ES2635333T3 (da) |
| HR (1) | HRP20211762T1 (da) |
| HU (1) | HUE059033T2 (da) |
| IL (2) | IL225000A (da) |
| LT (1) | LT3251678T (da) |
| MX (1) | MX338209B (da) |
| PL (1) | PL3251678T3 (da) |
| PT (1) | PT3251678T (da) |
| RS (1) | RS62548B1 (da) |
| SG (2) | SG10201507032YA (da) |
| SI (1) | SI3251678T1 (da) |
| SM (1) | SMT202100643T1 (da) |
| WO (1) | WO2012033858A2 (da) |
| ZA (1) | ZA201301598B (da) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106008583A (zh) | 2005-12-30 | 2016-10-12 | 安纳考尔医药公司 | 含硼的小分子 |
| AP4039A (en) | 2009-08-14 | 2017-02-28 | Daitao Chen | Boron-containing small molecules as antiprotozoal agents |
| WO2011094450A1 (en) | 2010-01-27 | 2011-08-04 | Anacor Pharmaceuticals, Inc | Boron-containing small molecules |
| MX338209B (es) | 2010-09-07 | 2016-04-07 | Anacor Pharmaceuticals Inc | Derivados de benzoxaborol para tratar infecciones bacterianas. |
| KR20140114380A (ko) | 2011-12-22 | 2014-09-26 | 미큐알엑스 파마슈티칼스, 인크. | 항미생물 요법용 트리시클릭 붕소 화합물 |
| US8669207B1 (en) | 2013-01-30 | 2014-03-11 | Dow Agrosciences, Llc. | Compounds and compositions |
| 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 |
| 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 |
| WO2014121124A1 (en) | 2013-02-01 | 2014-08-07 | 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 |
| SG11201600787PA (en) | 2013-08-09 | 2016-03-30 | Glaxosmithkline Ip No 2 Ltd | 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 |
| TW201625649A (zh) * | 2014-07-01 | 2016-07-16 | 第一三共股份有限公司 | 作爲抗菌劑的三環化合物 |
| MA41494B1 (fr) | 2015-02-12 | 2020-10-28 | Glaxosmithkline Ip No 2 Ltd | Composés benzoxaborole substitués en position 4 et utilisations associées |
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