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1. WO2020138398 - NOVEL COMPOUND INHIBITING LYSINE-SPECIFIC DEMETHYLATING ENZYME 1, METHOD FOR PRODUCING SAME, AND USE OF SAME

Publication Number WO/2020/138398
Publication Date 02.07.2020
International Application No. PCT/JP2019/051371
International Filing Date 27.12.2019
IPC
C07C 217/54 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
54having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
A61K 31/135 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines, e.g. amantadine
135having aromatic rings, e.g. methadone
A61K 31/4045 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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A61K 31/44 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
A61K 31/4409 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
4409only substituted in position 4, e.g. isoniazid, iproniazid
A61K 31/4433 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4433containing a six-membered ring with oxygen as a ring hetero atom
CPC
A61K 31/135
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines
135having aromatic rings ; , e.g. ketamine, nortriptyline
A61K 31/4045
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A61K 31/44
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
44Non condensed pyridines; Hydrogenated derivatives thereof
A61K 31/4409
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
44Non condensed pyridines; Hydrogenated derivatives thereof
4409only substituted in position 4, e.g. isoniazid, iproniazid
A61K 31/4433
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
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4433containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/4439
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
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Applicants
  • 国立研究開発法人理化学研究所 RIKEN [JP]/[JP]
  • 国立大学法人東海国立大学機構 NATIONAL UNIVERSITY CORPORATION TOKAI NATIONAL HIGHER EDUCATION AND RESEARCH SYSTEM [JP]/[JP]
Inventors
  • 梅原 祟史 UMEHARA Takashi
  • 佐藤 心 SATO Shin
  • 山本 博文 YAMAMOTO Hirofumi
  • 甲田 泰子 KODA Yasuko
  • 近藤 豊 KONDO Yutaka
  • 新城 恵子 SHINJO Keiko
Agents
  • 特許業務法人平木国際特許事務所 HIRAKI & ASSOCIATES
Priority Data
2018-24774228.12.2018JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) NOVEL COMPOUND INHIBITING LYSINE-SPECIFIC DEMETHYLATING ENZYME 1, METHOD FOR PRODUCING SAME, AND USE OF SAME
(FR) NOUVEAU COMPOSÉ INHIBITEUR DE L'ENZYME 1 DÉMÉTHYLASE SPÉCIFIQUE DE LA LYSINE, SON PROCÉDÉ DE PRODUCTION ET SON UTILISATION
(JA) リジン特異的脱メチル化酵素1を阻害する新規化合物、その製造方法及びその用途
Abstract
(EN)
The present invention addresses the problem of providing a novel compound exhibiting a high LSD1-inhibiting activity, high selectivity for LSD1 inhibition, and/or having a useful therapeutic effect for various diseases. One embodiment pertains to a compound represented by formula (I) [In the formula, Ar1, n, X2, X3, X4, R25, L and A are as defined in the specification and the claims], a stereoisomer thereof or salts thereof, or solvates thereof. Another embodiment pertains to: methods for producing a compound represented by formula (I), a stereoisomer thereof or salts thereof, or solvates thereof; and an LSD1 inhibitor, a pharmaceutical agent or a pharmaceutical composition that include, as an effective component, said compound, a stereoisomer thereof or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable solvates thereof.
(FR)
La présente invention aborde le problème de la fourniture d'un nouveau composé ayant une activité inhibitrice de LSD1 élevée, une haute sélectivité pour l'inhibition de LSD1, et/ou ayant un effet thérapeutique utile pour diverses maladies. Selon un mode de réalisation, l'invention concerne un composé représenté par la formule (I) [dans la formule, Ar1, n, X2, X3, X4, R25, L et A sont tels que définis dans la description et les revendications], un stéréoisomère de celui-ci ou des sels, ou des solvates de celui-ci. Selon un autre mode de réalisation, l'invention concerne : des procédés de production d'un composé représenté par la formule (I), un stéréoisomère de celui-ci ou des sels, ou des solvates de celui-ci ; et un inhibiteur de LSD1, un agent pharmaceutique ou une composition pharmaceutique qui comprennent, en tant que composant efficace, ledit composé, un stéréoisomère de celui-ci ou des sels pharmaceutiquement acceptables de celui-ci, ou des solvates pharmaceutiquement acceptables de celui-ci.
(JA)
本発明は、高いLSD1阻害活性、LSD1阻害に対する高い選択性、及び/又は様々な疾患に対する有用な治療効果を有する新規化合物を提供することを課題とする。本発明の一態様は、式(I)[式中、Ar1、n、X2、X3、X4、R25、L及びAは、明細書及び特許請求の範囲に記載の意味を有する]で表される化合物、その立体異性体若しくはそれらの塩、又はそれらの溶媒和物に関する。本発明の別の一態様は、式(I)で表される化合物、その立体異性体若しくはそれらの塩、又はそれらの溶媒和物の製造方法、並びに該化合物、その立体異性体若しくはそれらの製薬上許容される塩、又はそれらの製薬上許容される溶媒和物を有効成分として含む、LSD1阻害剤、医薬又は医薬組成物にも関する。
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