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1. JP2018076357 - PYRIDINYL TRIAZOLONE DERIVATIVES AND CONDENSED PYRIDINYL TRIAZOLONE DERIVATIVES

Office
Japan
Application Number 2017252294
Application Date 27.12.2017
Publication Number 2018076357
Publication Date 17.05.2018
Grant Number 6462842
Grant Date 11.01.2019
Publication Kind B2
IPC
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
A61K 31/4375
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
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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
A61K 31/4725
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
472Non-condensed isoquinolines, e.g. papaverine
4725containing further heterocyclic rings
A61K 31/519
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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 45/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
CPC
A61K 31/4375
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
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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
A61K 31/4725
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
472Non-condensed isoquinolines, e.g. papaverine
4725containing further heterocyclic rings
A61K 31/519
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
C07D 401/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
Applicants TAKEDA CHEM IND LTD
武田薬品工業株式会社
Inventors JOHN DAVID LAWSON
ローソン、ジョン デイヴィッド
MARK SABAT
サバト、マーク
SCORAH NICHOLAS
スコラー、ニコラス
CHRISTOPHER SMITH
スミス、クリストファー
PHONG H VU
ヴー、フォン エイチ.
WANG HAIXIA
ワン、ハイシャ
Agents 高島 一
土井 京子
鎌田 光宜
田村 弥栄子
小池 順造
當麻 博文
Priority Data 61/776,445 11.03.2013 US
Title
(EN) PYRIDINYL TRIAZOLONE DERIVATIVES AND CONDENSED PYRIDINYL TRIAZOLONE DERIVATIVES
(JA) ピリジニルトリアゾロン誘導体及び縮合ピリジニルトリアゾロン誘導体
Abstract
(EN)

PROBLEM TO BE SOLVED: To provide a compound that is a Bruton's tyrosine kinase (BTK) inhibitor, and a pharmaceutical composition containing the same.

SOLUTION: The present invention provides a compound represented by formula 1 or a pharmaceutically acceptable salt thereof (R1 is H, halogen, CN or the like; R2 and R3 independently represent H, halogen,-CN and the like, or R2 and R3, together with C to which they are attached, form a benzene ring or a pyridine ring; R4 is a (1-acryloylpyrrolidine-3-yl) oxy group, (1-acryloylpyrrolidine-3-yl) amino group, (1-acryloylpyrrolidine-3-yl) methyl group or the like).

SELECTED DRAWING: None

COPYRIGHT: (C)2018,JPO&INPIT

(JA)

【課題】ブルトンチロシンキナーゼ(BTK)の阻害薬である化合物、それを含有する医薬組成物の提供。
【解決手段】式1で表される化合物又は薬学的に許容されるそれらの塩。

(RはH、ハロゲン、CN等;R及びRは各々独立にH、ハロゲン、−CN等、又はR及びRが結合するCと一緒になって、ベンゼン環若しくはピリジン環を形成;Rは(1−アクリロイルピロリジン−3−イル)オキシ基、(1−アクリロイルピロリジン−3−イル)アミノ基、(1−アクリロイルピロリジン−3−イル)メチル基等)
【選択図】なし