PE20190119A1 - Esteres de oxaborol y sus usos - Google Patents

Esteres de oxaborol y sus usos

Info

Publication number
PE20190119A1
PE20190119A1 PE2018002055A PE2018002055A PE20190119A1 PE 20190119 A1 PE20190119 A1 PE 20190119A1 PE 2018002055 A PE2018002055 A PE 2018002055A PE 2018002055 A PE2018002055 A PE 2018002055A PE 20190119 A1 PE20190119 A1 PE 20190119A1
Authority
PE
Peru
Prior art keywords
hydrogen
aliphatic
oxaborol
optionally substituted
group
Prior art date
Application number
PE2018002055A
Other languages
English (en)
Inventor
Tsutomu Akama
David Scott Carter
Jason S Halladay
Robert T Jacobs
Yang Liu
Jacob J Plattner
Yong-Kang Zhang
Michael John Witty
Original Assignee
Anacor Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Anacor Pharmaceuticals Inc filed Critical Anacor Pharmaceuticals Inc
Publication of PE20190119A1 publication Critical patent/PE20190119A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02Boron compounds
    • C07F5/027Organoboranes and organoborohydrides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • A61K31/43Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • A61K31/431Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/14Ectoparasiticides, e.g. scabicides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02Boron compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Pyrane Compounds (AREA)

Abstract

Referido a compuestos de ester de oxaborol de formula (I) o una sal farmaceuticamente aceptable del mismo, en donde R1 es hidrogeno C1-6 alifatico, R1a es hidrogeno o C1-6 alifatico; cada R2 es independientemente hidrogeno, -halogeno -OR, -NO2, entre otros, R3 es hidrogeno u opcionalmente C1-6 alifatico sustituido; R4 es hidrogeno, un grupo de cadena lateral de aminoacido natural, o un grupo opcionalmente sustituido seleccionado del grupo que consiste en C1-6 alifatico, entre otros; R5 es hidrogeno o C1-6 alifatico opcionalmente sustituido; L es un enlace covalente o una cadena de hidrocarburos, recta o ramificada, C1-10 bivalente saturada o insaturada; R6 es hidrogeno, - halogeno, -OR, entre otros. Un compuesto seleccionado es 3,4-difluorobencilo(1-hidroxi-7-metilo-1,3-dihidrobenzo[c][1,2]oxaborol-6-carbonilo)-L-valinato. Pueden ser utiles para tratar enfermedades relacionadas con parasitos tales como la enfermedad de Chagas y la tripanosomiasis animal africana.
PE2018002055A 2016-05-12 2017-05-01 Esteres de oxaborol y sus usos PE20190119A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662335565P 2016-05-12 2016-05-12

Publications (1)

Publication Number Publication Date
PE20190119A1 true PE20190119A1 (es) 2019-01-17

Family

ID=58699201

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2019000887A PE20191077A1 (es) 2016-05-12 2017-05-01 Esteres de oxaborol y sus usos
PE2018002055A PE20190119A1 (es) 2016-05-12 2017-05-01 Esteres de oxaborol y sus usos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2019000887A PE20191077A1 (es) 2016-05-12 2017-05-01 Esteres de oxaborol y sus usos

Country Status (31)

Country Link
US (4) US10562921B2 (es)
EP (2) EP3455227A1 (es)
JP (2) JP6715957B2 (es)
KR (2) KR102243775B1 (es)
CN (2) CN109503637B (es)
AR (2) AR108450A1 (es)
AU (2) AU2017263785B2 (es)
BR (2) BR122018076188A2 (es)
CA (1) CA3023490C (es)
CL (2) CL2018003187A1 (es)
CO (1) CO2018012077A2 (es)
CR (2) CR20180502A (es)
DK (1) DK3578562T3 (es)
EA (2) EA036661B1 (es)
EC (2) ECSP18091065A (es)
ES (1) ES2882782T3 (es)
HK (1) HK1258717A1 (es)
HU (1) HUE056320T2 (es)
IL (2) IL262453A (es)
MA (1) MA44968A (es)
MX (2) MX2018013743A (es)
NI (2) NI201801171A (es)
NZ (1) NZ746906A (es)
PE (2) PE20191077A1 (es)
PT (1) PT3578562T (es)
SG (1) SG11201809237RA (es)
TN (2) TN2018000351A1 (es)
TW (1) TWI629279B (es)
UA (2) UA120999C2 (es)
UY (2) UY37236A (es)
WO (1) WO2017195069A1 (es)

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WO2017155879A1 (en) 2016-03-07 2017-09-14 Agrofresh Inc. Synergistic methods of using benzoxaborole compounds and preservative gases as an antimicrobial for crops
KR102243775B1 (ko) * 2016-05-12 2021-04-22 아나코르 파마슈티칼스 인코포레이티드 옥사보롤 에스터 및 이의 용도
MX2020005464A (es) 2017-11-30 2020-12-03 Boragen Inc Compuestos de benzoxaborol y formulaciones de los mismos.
JP2020180170A (ja) * 2019-04-23 2020-11-05 東ソー株式会社 ハロゲン含有ポリエーテルポリオール組成物

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KR102243775B1 (ko) * 2016-05-12 2021-04-22 아나코르 파마슈티칼스 인코포레이티드 옥사보롤 에스터 및 이의 용도

Also Published As

Publication number Publication date
MX2018015410A (es) 2019-05-27
TWI629279B (zh) 2018-07-11
CL2018003187A1 (es) 2019-01-11
US20210101916A1 (en) 2021-04-08
DK3578562T3 (da) 2021-07-12
KR102231489B1 (ko) 2021-03-23
KR20190002695A (ko) 2019-01-08
PE20191077A1 (es) 2019-08-20
US20200017531A1 (en) 2020-01-16
US10882872B2 (en) 2021-01-05
HUE056320T2 (hu) 2022-02-28
JP2019081770A (ja) 2019-05-30
SG11201809237RA (en) 2018-11-29
ECSP18091065A (es) 2019-07-31
UA121354C2 (uk) 2020-05-12
US20170327519A1 (en) 2017-11-16
UY37236A (es) 2018-01-02
UY37980A (es) 2020-06-30
IL262453A (en) 2018-12-31
IL263161B (en) 2022-05-01
CN109153688A (zh) 2019-01-04
NZ746906A (en) 2020-06-26
AU2018264116B2 (en) 2020-03-12
PT3578562T (pt) 2021-08-05
MX2018013743A (es) 2019-05-02
CR20180560A (es) 2019-01-25
AU2017263785A1 (en) 2018-10-25
TN2018000351A1 (en) 2020-06-15
TN2019000106A1 (en) 2020-10-05
EA036661B1 (ru) 2020-12-04
CA3023490A1 (en) 2017-11-16
BR122018076188A2 (pt) 2019-09-10
EP3455227A1 (en) 2019-03-20
CN109503637B (zh) 2021-03-16
EA201892475A1 (ru) 2019-04-30
HK1258717A1 (zh) 2019-11-15
CA3023490C (en) 2021-06-08
TW201808968A (zh) 2018-03-16
KR20190005982A (ko) 2019-01-16
NI201801171A (es) 2019-04-10
ECSP19026702A (es) 2019-06-30
CO2018012077A2 (es) 2018-11-22
MA44968A (fr) 2019-03-20
ES2882782T3 (es) 2021-12-02
CN109503637A (zh) 2019-03-22
WO2017195069A1 (en) 2017-11-16
US10562921B2 (en) 2020-02-18
AR108450A1 (es) 2018-08-22
AR113543A2 (es) 2020-05-13
CR20180502A (es) 2018-12-21
JP6715957B2 (ja) 2020-07-01
EP3578562A1 (en) 2019-12-11
JP2019520326A (ja) 2019-07-18
US11578087B2 (en) 2023-02-14
JP6715966B2 (ja) 2020-07-01
KR102243775B1 (ko) 2021-04-22
EP3578562B1 (en) 2021-06-23
BR122023022427A2 (pt) 2023-12-26
AU2017263785B2 (en) 2019-10-03
NI201801172A (es) 2019-04-10
AU2018264116A1 (en) 2018-12-06
CL2018003377A1 (es) 2019-01-11
IL263161A (en) 2018-12-31
BR112018071931A2 (pt) 2019-02-05
UA120999C2 (uk) 2020-03-10
EA034415B1 (ru) 2020-02-05
EA201892203A1 (ru) 2019-04-30
US20230132298A1 (en) 2023-04-27

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