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1. WO2020116660 - MACROCYCLIC COMPOUND AND USE THEREOF

Publication Number WO/2020/116660
Publication Date 11.06.2020
International Application No. PCT/JP2019/048593
International Filing Date 04.12.2019
IPC
A61K 31/4748 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
4748forming part of bridged ring systems
A61K 31/5386 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5386spiro-condensed or forming part of bridged ring systems
A61P 1/16 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 7/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
06Antianaemics
A61P 9/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
CPC
A61K 31/4748
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
4748forming part of bridged ring systems
A61K 31/5386
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5386spiro-condensed or forming part of bridged ring systems
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
Applicants
  • SCOHIA PHARMA, INC. [JP]/[JP]
Inventors
  • MATSUMOTO, Shigemitsu
  • HARA, Ryoma
  • NOGUCHI, Naoyoshi
  • FUKUSHI, Hideto
  • NIIDA, Ayumu
  • SASAKI, Satoshi
  • IKOMA, Minoru
  • KOBAYASHI, Toshitake
  • MAEKAWA, Tsuyoshi
Agents
  • KOBAYASHI, Hiroshi
Priority Data
2018-22823405.12.2018JP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) MACROCYCLIC COMPOUND AND USE THEREOF
(FR) COMPOSÉ MACROCYCLIQUE ET SON UTILISATION
Abstract
(EN)
A compound represented by the following formula (I): wherein each symbol in the formula is as described herein or a salt thereof has an NRF2 activating activity, and is expected to be useful as a preventive or therapeutic agent for diseases associated with oxidative stress, in particular, hepatic disease (for example, non-alcoholic steatohepatitis (NASH)), cardiovascular disease (for example, heart failure or pulmonary arterial hypertension), lung disease (for example, chronic obstructive pulmonary disease (COPD)), kidney disease (for example, chronic kidney disease (CKD) or acute kidney injury (AKI)), central nervous system disease (for example, Parkinson's disease), mitochondrial disease (for example, Friedreich motor ataxia, mitochondrial myopathy), inflammatory disease (for example, multiple sclerosis (MS), inflammatory bowel disease (IBD)), sickle cell disease, cancer, or the like.
(FR)
La présente invention concerne un composé représenté par la formule (I) suivante : dans laquelle chaque symbole dans la formule est tel que décrit ou un sel de ce dernier a une activité d'activation de NRF2, et est supposé être utile en tant qu'agent préventif ou thérapeutique pour des maladies associées au stress oxydatif, en particulier, une maladie hépatique (par exemple, une stéatohépatite non alcoolique (NASH)), une maladie cardiovasculaire (par exemple, une insuffisance cardiaque ou une hypertension artérielle pulmonaire), une maladie pulmonaire (par exemple, une bronchopneumopathie chronique obstructive (BPCO)), une maladie rénale (par exemple, une insuffisance rénale chronique (IRN) ou une insuffisance rénale aiguë (IRA)), une maladie du système nerveux central (par exemple, la maladie de Parkinson), une maladie mitochondriale (par exemple l'ataxie de Friedreich, la myopathie mitochondriale), une maladie inflammatoire (par exemple, la sclérose en plaques (SEP), une maladie inflammatoire chronique de l'intestin (MICI)), la drépanocytose, le cancer ou similaire.
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