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1. JP2020117514 - SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS

Office
Japan
Application Number 2020054551
Application Date 25.03.2020
Publication Number 2020117514
Publication Date 06.08.2020
Grant Number 6982376
Grant Date 24.11.2021
Publication Kind B2
IPC
A61P 1/04
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
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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
A61P 1/14
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
14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 5/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
14of the thyroid hormones, e.g. T3, T4
CPC
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
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 405/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
C07D 409/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
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
Applicants AURIGENE DISCOVERY TECHNOLOGIES LTD
オーリジーン ディスカバリー テクノロジーズ リミテッド
Inventors RAVI KOTRABASAIAH UJJINAMATADA
コトラバサイア ウッジナマタダ,ラヴィ
CHETAN PANDIT
パンディット,チェタン
Agents 清原 義博
Priority Data 2448/CHE/2015 15.05.2015 IN
Title
(EN) SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS
(JA) RORガンマ調節物質としての置換型テトラヒドロキノリン化合物
Abstract
(EN)

PROBLEM TO BE SOLVED: To provide a method of producing 6-(2,6-dimethylpyrimidin-4-yl)-N-(4-(ethylsulfonyl)benzyl)-6-methyl-5-oxo-5,6,7,8-tetrahydroquinoline-2-carboxamide, which is a retinoic acid receptor-related orphan receptor (ROR) modulator, effective for an immune or inflammatory disease.

SOLUTION: There is provided a process of preparing a compound according to the following scheme, which includes coupling a carboxylic acid with an amine in the presence of a base and a coupling agent, and isolating a desired product from the reaction mixture, and may additionally include chiral separation of the compound for isolating an enantiomer.

SELECTED DRAWING: None

COPYRIGHT: (C)2020,JPO&INPIT


(JA)

【課題】免疫疾患や炎症性疾患に有効な、レチノイン酸受容体関連オーファン受容体(ROR)調節物質である、6−(2,6−ジメチルピリミジン−4−イル)−N−(4−(エチルスルホニル)ベンジル)−6−メチル−5−オキソ−5,6,7,8−テトラヒドロキノリン−2−カルボキサミドの製造方法の提供。
【解決手段】以下のスキームに従って化合物を調製するプロセスであって、塩基及びカップリング剤の存在下でカルボン酸をアミンとカップリングする工程、及び反応混合物から所望の生成物の単離する工程を含む、プロセス。エナンチオマーを単離するために化合物のキラル分離の追加の工程を含んでいても良い。

【選択図】なし


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