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1. JP2021046444 - OXYSTEROLS AND METHODS OF USE THEREOF

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Office
Japan
Application Number 2020215040
Application Date 24.12.2020
Publication Number 2021046444
Publication Date 25.03.2021
Publication Kind A
IPC
C07J 9/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
9Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
A61K 31/575
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
575substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
A61K 31/58
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
58containing heterocyclic rings, e.g. aldosterone, danazol, stanozolol, pancuronium, digitogenin
A61P 1/00
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
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
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
CPC
C07J 9/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
9Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
C07J 17/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
17Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
A61P 23/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
23Anaesthetics
A61P 1/00
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
A61P 1/10
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
10Laxatives
A61P 9/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
Applicants SAGE THERAPEUTICS INC
セージ　セラピューティクス，　インコーポレイテッド
Inventors SALITURO FRANCESCO G
フランセスコ　ジー．　サリトゥロ
ALBERT JEAN ROBICHAUD
アルバート　ジーン　ロビチャウド
GABRIEL MARTINEZ BOTELLA
ガブリエル　マルティネス　ボテーラ
BOYD L HARRISON
ボイド　エル．　ハリソン
Agents 山本　秀策
森下　夏樹
飯田　貴敏
石川　大輔
山本　健策
Priority Data 62/189,068 06.07.2015 US
62/332,931 06.05.2016 US
Title
(EN) OXYSTEROLS AND METHODS OF USE THEREOF
(JA) オキシステロールおよびそれらの使用の方法
Abstract
(EN)

PROBLEM TO BE SOLVED: To provide compounds useful for the prevention and treatment of a variety of conditions.

SOLUTION: Provided herein are compounds according to formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; in the formula R1, R2 and R5 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. Provided herein are substituted oxysterols useful for preventing and/or treating a broad range of disorders, including, but not limited to, NMDA-mediated disorders. These compounds are expected to show improved in vivo potency, pharmacokinetic (PK) properties, oral bioavailability, formulation suitability, stability and/or safety compared to other oxysterols. Further provided are pharmaceutical compositions comprising the compounds of the present invention, and methods of their use and treatment.

SELECTED DRAWING: None

COPYRIGHT: (C)2021,JPO&INPIT


(JA)

【課題】種々の症状の予防および処置に有用な化合物を提供すること
【解決手段】 式（Ｉ）

に記載の化合物およびその薬学的に受容可能な塩ならびにその薬学的組成物が提供され；式中、Ｒ１、Ｒ２、およびＲ５は、本明細書中で定義されるとおりである。本発明の化合物は、種々の症状の予防および処置に有用であると予想される。ＮＭＤＡ媒介性障害を含むがこれに限定されない広範囲の障害の予防および／または処置に有用な置換オキシステロールが本明細書中に提供される。これらの化合物は、他のオキシステロールと比べて、改善されたインビボ効力、薬物動態学的（ＰＫ）特性、経口バイオアベイラビリティ、製剤化適性、安定性および／または安全性を示すと予想される。本発明の化合物を含む薬学的組成物ならびにそれらの使用および処置の方法がさらに提供される。
【選択図】なし
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