JP2020117514 SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS

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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

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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

(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

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1	Drugs for disorders of the alimentary tract or the digestive system
04	for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
401	Heterocyclic 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
02	containing two hetero rings
04	directly linked by a ring-member-to-ring- member bond

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1	Drugs for disorders of the alimentary tract or the digestive system
14	Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1	Drugs for disorders of the alimentary tract or the digestive system
16	for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3	Drugs for disorders of the metabolism
08	for glucose homeostasis
10	for hyperglycaemia, e.g. antidiabetics

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1. JP2020117514 - SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495	having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505	Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506	not condensed and containing further heterocyclic rings