HRP20211762T1 - Derivati benzoksaborola za liječenje bakterijskih infekcija - Google Patents
Derivati benzoksaborola za liječenje bakterijskih infekcija Download PDFInfo
- Publication number
- HRP20211762T1 HRP20211762T1 HRP20211762TT HRP20211762T HRP20211762T1 HR P20211762 T1 HRP20211762 T1 HR P20211762T1 HR P20211762T T HRP20211762T T HR P20211762TT HR P20211762 T HRP20211762 T HR P20211762T HR P20211762 T1 HRP20211762 T1 HR P20211762T1
- Authority
- HR
- Croatia
- Prior art keywords
- solvate
- hydrate
- salt
- compound according
- pharmaceutically acceptable
- Prior art date
Links
- GDMJXXLVTYSBBE-UHFFFAOYSA-N 1,2-benzoxaborole Chemical class C1=CC=C2OB=CC2=C1 GDMJXXLVTYSBBE-UHFFFAOYSA-N 0.000 title 1
- 208000035143 Bacterial infection Diseases 0.000 title 1
- 208000022362 bacterial infectious disease Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 239000012453 solvate Substances 0.000 claims 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Chemical group 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
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- -1 methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy Chemical group 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 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
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 206010062207 Mycobacterial infection Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 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
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 229910052740 iodine Chemical group 0.000 claims 1
- 239000011630 iodine Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000027531 mycobacterial infectious disease Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000005920 sec-butoxy group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
Classifications
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (15)
1. Spoj koji ima strukturu koja je:
[image]
u kojoj
R4 je izabran iz grupe koja se sastoji od sljedećih: halogen, metil, etil, propil, izopropil, butil, izobutil, sek-butil, metoksi, etoksi, propoksi, izopropoksi, butoksi, izobutoksi i sek-butoksi; i
gdje a je 2, 3 ili 4; i
R12 je izabran iz grupe koja se sastoji od sljedećih: H, OH, NH2, metil, etil, - NHS(O)2CH3, cijano, -NHC(O)CH3, -NHC(O)NHCH2CH3, -C(O)NH2, -C(O)OH, 4-(metoksi)fenil, benzil, benzoksi, -NHC(O)OCH2Ph, -C(O)NHCH2CH2OH i -C(NH2)(NH);
ili njegova sol, hidrat ili solvat.
2. Spoj prema zahtjevu 1 ili njegova sol, hidrat ili solvat, koji ima strukturu koja je:
[image]
u kojoj C* je stereocentar atoma ugljika koji ima konfiguraciju koja je (R) ili (S).;
3. Spoj prema zahtjevu 2 ili njegova sol, hidrat ili solvat, naznačeno time što C* stereocentar je u (S) konfiguraciji.
4. Spoj prema zahtjevu 1 ili njegova sol, hidrat ili solvat, naznačeno time što R4 je izabran iz grupe koja se sastoji od fluora, klora, broma i joda.
5. Spoj prema zahtjevu 4 ili njegova sol, hidrat ili solvat, naznačeno time što R4 je klor.
6. Spoj prema zahtjevu 1 do 3 ili njegova sol, hidrat ili solvat, naznačeno time što R4 je izabran iz grupe koja se sastoji od sljedećih: metil, etil, propil, izopropil, butil, izobutil, sek-butil.
7. Spoj prema zahtjevu 6 ili njegova sol, hidrat ili solvat, naznačeno time što R4 je metil.
8. Spoj prema bilo kojem od zahtjeva 1 do 6 ili njegova sol, hidrat ili solvat, naznačeno time što a je 2.
9. Spoj prema bilo kojem od zahtjeva 1 do 6 ili njegova sol, hidrat ili solvat, naznačeno time što R12 je OH.
10. Kompozicija koja sadrži:
a) prvi stereoizomer spoja prema bilo kojem od zahtjeva 2 do 9 ili njegovu sol, hidrat ili solvat;
b) najmanje jedan dodatni stereoizomer prvog stereoizomera;
pri čemu je prvi stereoizomer prisutan u enantiomernom višku od najmanje 80% u odnosu na navedeni najmanje jedan dodatni stereoizomer.
11. Kombinacija koja sadrži spoj prema bilo kojem od zahtjeva 1 do 9 ili njegovu farmaceutski prihvatljivu sol, zajedno sa najmanje jednim drugim terapeutski aktivnim sredstvom.
12. Farmaceutska formulacija koja sadrži:
a) spoj prema bilo kojem od zahtjeva 1 do 9 ili njegovu farmaceutski prihvatljivu sol; i
b) farmaceutski prihvatljiv ekscipijent.
13. Spoj ili njegova farmaceutski prihvatljiva sol, hidrat ili solvat, kako je definirano u bilo kojem od zahtjeva 1 do 9, za uporabu u terapiji.
14. Spoj ili njegova farmaceutski prihvatljiva sol, hidrat ili solvat, kako je definirano u bilo kojem od zahtjeva 1 do 9, za uporabu u liječenju bolesti izazvane infekcijom mikobakterijom.
15. Spoj ili njegova farmaceutski prihvatljiva sol, hidrat ili solvat, kako je definirano u bilo kojem od zahtjeva 1 do 9, za uporabu u liječenju tuberkuloze.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38059610P | 2010-09-07 | 2010-09-07 | |
| EP17176654.6A EP3251678B1 (en) | 2010-09-07 | 2011-09-07 | Benzoxaborole derivatives for treating bacterial infections |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211762T1 true HRP20211762T1 (hr) | 2022-02-18 |
Family
ID=44653589
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211762TT HRP20211762T1 (hr) | 2010-09-07 | 2011-09-07 | Derivati benzoksaborola za liječenje bakterijskih infekcija |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US8703742B2 (hr) |
| EP (2) | EP3251678B1 (hr) |
| JP (4) | JP5952280B2 (hr) |
| KR (2) | KR102152901B1 (hr) |
| CN (2) | CN108610356B (hr) |
| AU (1) | AU2011299243C1 (hr) |
| BR (1) | BR112013005426B1 (hr) |
| CA (1) | CA2810021C (hr) |
| CY (1) | CY1124728T1 (hr) |
| DK (2) | DK3251678T3 (hr) |
| EA (2) | EA033311B1 (hr) |
| ES (2) | ES2635333T3 (hr) |
| HK (1) | HK1247841A1 (hr) |
| HR (1) | HRP20211762T1 (hr) |
| HU (1) | HUE059033T2 (hr) |
| IL (2) | IL225000A (hr) |
| LT (1) | LT3251678T (hr) |
| MX (1) | MX338209B (hr) |
| PL (1) | PL3251678T3 (hr) |
| PT (1) | PT3251678T (hr) |
| RS (1) | RS62548B1 (hr) |
| SG (2) | SG187969A1 (hr) |
| SI (1) | SI3251678T1 (hr) |
| WO (1) | WO2012033858A2 (hr) |
| ZA (1) | ZA201301598B (hr) |
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| RU2008131324A (ru) | 2005-12-30 | 2010-02-10 | Анакор Фармасьютикалз, Инк. (Us) | Борсодержащие малые молекулы |
| US9440994B2 (en) * | 2009-08-14 | 2016-09-13 | Anacor Pharmaceuticals, Inc. | Boron containing small molecules as antiprotozoal agents |
| US8716478B2 (en) | 2010-01-27 | 2014-05-06 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules |
| CN108610356B (zh) * | 2010-09-07 | 2021-02-26 | 阿纳科制药公司 | 苯并氧杂硼杂环戊二烯衍生物用于治疗细菌感染 |
| JP6031122B2 (ja) * | 2011-12-22 | 2016-11-24 | ミクウルク ファーマシューティカルズ，インコーポレイテッド | 抗微生物療法のための三環式ホウ素化合物 |
| 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 |
| 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 |
| CN105101791B (zh) | 2013-01-30 | 2017-11-17 | 美国陶氏益农公司 | 苯硼酸半酯作为挥发性抗微生物剂在肉类、植物或植物部分上的用途 |
| 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 |
| HRP20220384T1 (hr) * | 2013-08-09 | 2022-07-22 | Glaxosmithkline Intellectual Property (No. 2) Limited | Triciklički benzoksaborol spojevi i njihove uporabe |
| 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 |
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| 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 |
| CN111655035A (zh) | 2017-11-30 | 2020-09-11 | 博瑞金股份有限公司 | 苯并氧杂硼杂环戊烯化合物和其制剂 |
| 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 |
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| US20220275007A1 (en) * | 2019-07-30 | 2022-09-01 | Boragen, Inc. | Flow reaction process for manufacture of boron-containing agrochemicals |
| 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 |
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