AR117251A1 - Compuesto macrocíclico como activador de nrf2 - Google Patents

Compuesto macrocíclico como activador de nrf2

Info

Publication number
AR117251A1
AR117251A1 ARP190103549A ARP190103549A AR117251A1 AR 117251 A1 AR117251 A1 AR 117251A1 AR P190103549 A ARP190103549 A AR P190103549A AR P190103549 A ARP190103549 A AR P190103549A AR 117251 A1 AR117251 A1 AR 117251A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
ring
nrf2
alkyl group
hydrogen atom
Prior art date
Application number
ARP190103549A
Other languages
English (en)
Inventor
Tsuyoshi Maekawa
Toshitake Kobayashi
Minoru Ikoma
Satoshi Sasaki
Ayumu Niida
Hideto Fukushi
Naoyoshi Noguchi
Ryoma Hara
Shigemitsu Matsumoto
Original Assignee
Scohia Pharma 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 Scohia Pharma Inc filed Critical Scohia Pharma Inc
Publication of AR117251A1 publication Critical patent/AR117251A1/es

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18—Bridged systems
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4748—Quinolines; Isoquinolines forming part of bridged ring systems
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Compuestos macrocíclicos como activadores de NRF2, composición farmacéutica que los comprende y su uso para el tratamiento de enfermedades mediadas por la activación de NRF2. Reivindicación 1: Un compuesto caracterizado porque es representado por la fórmula (1), donde R¹ es OH, ORʸ o NHRʸ; Rʸ es un grupo C₁₋₆ alquilo opcionalmente sustituido o un grupo cíclico opcionalmente sustituido; R² y R³, que pueden ser iguales o diferentes, son un átomo de hidrógeno o un grupo C₁₋₆ alquilo opcionalmente sustituido, o R² y R³ se unen para formar un grupo C₃₋₆ cicloalquilo; X es C(=O), SO₂ o CRˣ¹Rˣ²; Rˣ¹ y Rˣ², que pueden ser iguales o diferentes, son un átomo de hidrógeno o un grupo C₁₋₆ alquilo opcionalmente sustituido; el anillo A es un anillo benceno que puede tener uno o más sustituyentes adicionales; el anillo B es un anillo benceno que puede tener uno o más sustituyentes adicionales; el anillo C es un anillo aromático de 5 ó 6 miembros opcionalmente sustituido que puede contener uno o más heteroátomos; y L es C₄₋₈ alquileno lineal, saturado o insaturado, opcionalmente sustituido opcionalmente insertado por un heteroátomo; o una sal del mismo.
ARP190103549A 2018-12-05 2019-12-04 Compuesto macrocíclico como activador de nrf2 AR117251A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2018228234 2018-12-05

Publications (1)

Publication Number Publication Date
AR117251A1 true AR117251A1 (es) 2021-07-21

Family

ID=70975488

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP190103549A AR117251A1 (es) 2018-12-05 2019-12-04 Compuesto macrocíclico como activador de nrf2

Country Status (17)

Country Link
US (1) US11518763B2 (es)
EP (1) EP3890738A4 (es)
JP (1) JP2022510736A (es)
KR (1) KR20210099622A (es)
CN (1) CN113164468A (es)
AR (1) AR117251A1 (es)
AU (1) AU2019391942B2 (es)
BR (1) BR112021010704A2 (es)
CA (1) CA3121952A1 (es)
CL (1) CL2021001451A1 (es)
CO (1) CO2021007304A2 (es)
MX (1) MX2021006527A (es)
PH (1) PH12021551262A1 (es)
SG (1) SG11202105125XA (es)
TW (1) TWI820266B (es)
UA (1) UA127872C2 (es)
WO (1) WO2020116660A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3108534A1 (en) 2018-08-20 2020-02-27 Janssen Pharmaceutica Nv Inhibitors of keap1-nrf2 protein-protein interaction
WO2022056448A1 (en) * 2020-09-14 2022-03-17 Sanofi Tetrahydroisoquinoline derivatives for the treatment of red blood disorders and inflammatory diseases

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5946454B2 (ja) 2010-08-31 2016-07-06 バイオニュア ファーマ， エセ．エレ． ニューロトロフィン受容体のアゴニストおよび医薬としてのその使用
RS58581B1 (sr) 2013-06-21 2019-05-31 Karyopharm Therapeutics Inc 1,2,4-triazoli kao modulatori jedarnog transporta i njihova primena
MX370410B (es) * 2013-12-18 2019-12-11 Glaxosmithkline Ip Dev Ltd Reguladores de nrf2.
PL3307739T3 (pl) 2015-06-15 2021-05-31 Glaxosmithkline Intellectual Property Development Limited Regulatory nrf2
EP3307719A1 (en) 2015-06-15 2018-04-18 GlaxoSmithKline Intellectual Property Development Limited Nrf2 regulators
MA52032A (fr) 2015-06-15 2021-01-20 Astex Therapeutics Ltd Régulateurs de nrf2
WO2017026516A1 (ja) 2015-08-12 2017-02-16 持田製薬株式会社 イソチアゾール誘導体
WO2017060855A1 (en) 2015-10-06 2017-04-13 Glaxosmithkline Intellectual Property Development Limited Arylcyclohexyl pyrazoles as nrf2 regulators
EP3359532A1 (en) 2015-10-06 2018-08-15 GlaxoSmithKline Intellectual Property Development Limited Biaryl pyrazoles as nrf2 regulators
JP2020500919A (ja) 2016-12-12 2020-01-16 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｎｒｆ２レギュレーターとしての３−カルボン酸ピロール
EP3551621A1 (en) 2016-12-12 2019-10-16 GlaxoSmithKline Intellectual Property Development Limited N-aryl pyrazoles as nrf2 regulators
WO2018109643A1 (en) 2016-12-14 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Bisaryl heterocycles as nrf2 acti
US11078216B2 (en) 2016-12-14 2021-08-03 Glaxosmithkline Intellectual Property Development Limited Bisaryl amides as NRF2 activators
ES2848699T3 (es) 2016-12-14 2021-08-11 Glaxosmithkline Ip Dev Ltd Compuestos de 3-oxo-1,4-diazepinilo como activadores de NRF2
EP3555082B1 (en) 2016-12-15 2022-01-26 GlaxoSmithKline Intellectual Property Development Limited Ether linked triazoles as nrf2 regulators
CN110114361B (zh) 2016-12-15 2022-04-12 葛兰素史密斯克莱知识产权发展有限公司 Nrf2化合物
AR110590A1 (es) 2016-12-27 2019-04-10 Biogen Ma Inc Activador de nrf2
WO2018140876A1 (en) 2017-01-30 2018-08-02 Biogen Ma Inc. Nrf2 activator
EP3573963B1 (en) 2017-01-30 2021-09-01 Biogen MA Inc. Nrf2 activator
JP2020097526A (ja) * 2017-03-28 2020-06-25 武田薬品工業株式会社 複素環化合物

Also Published As

Publication number Publication date
MX2021006527A (es) 2021-07-21
PH12021551262A1 (en) 2021-10-25
AU2019391942A1 (en) 2021-06-03
TWI820266B (zh) 2023-11-01
BR112021010704A2 (pt) 2021-08-24
EP3890738A4 (en) 2022-08-17
CA3121952A1 (en) 2020-06-11
WO2020116660A1 (en) 2020-06-11
EP3890738A1 (en) 2021-10-13
US11518763B2 (en) 2022-12-06
AU2019391942B2 (en) 2024-03-21
KR20210099622A (ko) 2021-08-12
CN113164468A (zh) 2021-07-23
US20220119391A1 (en) 2022-04-21
CL2021001451A1 (es) 2021-12-24
JP2022510736A (ja) 2022-01-27
CO2021007304A2 (es) 2021-06-21
UA127872C2 (uk) 2024-01-31
SG11202105125XA (en) 2021-06-29
TW202039494A (zh) 2020-11-01

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