AR108450A1 - Ésteres de oxaborol y sus usos - Google Patents

Ésteres de oxaborol y sus usos

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Publication number
AR108450A1
AR108450A1 ARP170101250A ARP170101250A AR108450A1 AR 108450 A1 AR108450 A1 AR 108450A1 AR P170101250 A ARP170101250 A AR P170101250A AR P170101250 A ARP170101250 A AR P170101250A AR 108450 A1 AR108450 A1 AR 108450A1
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AR
Argentina
Prior art keywords
membered
saturated
nitrogen
oxygen
partially unsaturated
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Application number
ARP170101250A
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English (en)
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Anacor Pharmaceuticals Inc
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Publication date
Application filed by Anacor Pharmaceuticals Inc filed Critical Anacor Pharmaceuticals Inc
Publication of AR108450A1 publication Critical patent/AR108450A1/es

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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/69Boron 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
    • 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
    • A61K31/33Heterocyclic 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
    • A61K31/47Quinolines; 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
    • 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

Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: R¹ es hidrógeno o C₁₋₆ alifático; R¹ᵃ es hidrógeno o C₁₋₆ alifático; o R¹ y R¹ᵃ se toman junto con el átomo de carbono al que están unidos para formar un anillo espiro carbocíclico de 3 a 6 miembros opcionalmente sustituido; cada R² es independientemente hidrógeno, -halógeno, -OR, -NO₂, -CN, -SR, -N(R)₂, -C(O)R, -C(O)OR, -S(O)R, -S(O)₂R, -C(O)N(R)₂, -SO₂N(R)₂, -OC(O)R, -N(R)C(O)R, -N(R)C(O)OR, -N(R)SO₂R, -OC(O)N(R)₂, o un grupo opcionalmente sustituido seleccionado del grupo que consiste en C₁₋₆ alifático y carbociclilo monocíclico saturado o parcialmente insaturado de 3 a 6 miembros; R³ es hidrógeno u C₁₋₆ alifático opcionalmente sustituido; R⁴ es hidrógeno, un grupo de cadena lateral de aminoácido natural o no natural, o un grupo opcionalmente sustituido seleccionado del grupo que consiste en C₁₋₆ alifático, carbociclilo monocíclico saturado o parcialmente insaturado de 3 a 7 miembros, y fenilo; o R³ y R⁴ se toman junto con el átomo de carbono unido a R⁴ y el átomo de nitrógeno unido a R³ para formar un anillo heterociclilo de 3 a 6 miembros opcionalmente sustituido que tiene 0 - 1 heteroátomos adicionales seleccionados de oxígeno, nitrógeno o azufre; R⁵ es hidrógeno o C₁₋₆ alifático opcionalmente sustituido; o R⁴ y R⁵ se toman junto con el átomo de carbono al que están unidos para formar un anillo opcionalmente sustituido seleccionado de un anillo espiro heterocíclico de 3 a 6 miembros que tiene 1 - 2 heteroátomos seleccionados de oxígeno, nitrógeno o azufre y un anillo espiro carbocíclico monocíclico saturado o parcialmente insaturado de 3 a 6 miembros; L es un enlace covalente o una cadena de hidrocarburos, recta o ramificada, C₁₋₁₀ bivalente saturada o insaturada, en donde una, dos o tres unidades de metileno de L son opcionalmente e independientemente reemplazadas por -Cy-, -O-, -SO-, -SO₂-, -C(O)-, -C(O)N(R)-, -S-, -N(R)-, -C(O)O-, -OC(O)-, -N(R)C(O)-, -N(R)SO₂-, o -SO₂N(R)-; en donde cada -Cy- es independientemente un anillo bivalente opcionalmente sustituido seleccionado del grupo consistente en fenileno, carbociclileno monocíclico de 3 a 7 miembros saturado o parcialmente insaturado, heterociclileno monocíclico saturado o parcialmente insaturado de 3 a 7 miembros que tiene 1 - 2 heteroátomos seleccionados de oxígeno, nitrógeno o azufre, heteroarileno de 5 a 6 miembros que tiene 1 - 4 heteroátomos seleccionados de oxígeno, nitrógeno o azufre, carbociclileno bicíclico saturado o parcialmente insaturado de 7 a 10 miembros, arileno bicíclico de 8 a 10 miembros, heterociclileno bicíclico saturado o parcialmente insaturado de 7 a 10 miembros que tiene 1 a 4 heteroátomos seleccionados de oxígeno, nitrógeno o azufre, y heteroarileno bicíclico de 7 a 10 miembros que tiene 1 a 4 heteroátomos seleccionados de oxígeno, nitrógeno o azufre; R⁶ es hidrógeno, -halógeno, -OR, -NO₂, -CN, -SR, -N(R)₂, -C(O)R, -C(O)OR, -S(O)R, -S(O)₂R, -C(O)N(R)₂, -SO₂N(R)₂, -OC(O)R, -N(R)C(O)R, -N(R)C(O)OR, -N(R)SO₂R, -OC(O)N(R)₂, un grupo opcionalmente sustituido seleccionado del grupo consistente en C₁₋₆ alifático, fenilo, carbocíclico monocíclico de 3 a 7 miembros saturado o parcialmente insaturado, heterociclilo monocíclico saturado o parcialmente insaturado de 3 a 7 miembros que tiene 1 - 2 heteroátomos seleccionados de oxígeno, nitrógeno o azufre, heteroarilo de 5 a 6 miembros que tiene 1 - 4 heteroátomos seleccionados de oxígeno, nitrógeno o azufre, carbociclilo bicíclico saturado o parcialmente insaturado de 7 a 10 miembros, arilo bicíclico de 8 a 10 miembros, heterociclilo bicíclico saturado o parcialmente insaturado de 7 a 10 miembros que tiene 1 a 4 heteroátomos seleccionados de oxígeno, nitrógeno o azufre, y heteroarilo bicíclico de 7 a 10 miembros que tiene 1 a 4 heteroátomos seleccionados de oxígeno, nitrógeno o azufre y bicíclico puenteado; cada R es independientemente hidrógeno o C₁₋₆ alifático opcionalmente sustituido; en donde L es un enlace covalente, entonces R⁶ es diferente de -OR, -halógeno, -NO₂, -CN, -SR, -N(R)₂, -S(O)R, -S(O)₂R, -SO₂N(R)₂, -OC(O)R, -N(R)C(O)R, -N(R)C(O)OR, -N(R)SO₂R, o -OC(O)N(R)₂; y en donde L es diferente de un enlace covalente que incluye un átomo de carbono enlazado al oxígeno carboxilo denotado O*.
ARP170101250A 2016-05-12 2017-05-11 Ésteres de oxaborol y sus usos AR108450A1 (es)

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US201662335565P 2016-05-12 2016-05-12

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ARP180103435A AR113543A2 (es) 2016-05-12 2018-11-23 Ésteres de oxaborol y sus usos

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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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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
PE20190119A1 (es) 2019-01-17
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
AR113543A2 (es) 2020-05-13
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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
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US20230132298A1 (en) 2023-04-27

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