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1. CN108135911 - OXYSTEROLS AND METHODS OF USE THEREOF

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China

Application Number 201680050744.1

Application Date 06.07.2016

Publication Number 108135911

Publication Date 08.06.2018

Grant Number 108135911

Grant Date 25.06.2021

Publication Kind B

IPC

A61K 31/567

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
56	Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
565	not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
567	substituted in position 17 alpha, e.g. mestranol, norethandrolone

A61K 31/566

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
56	Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
565	not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
566	having an oxo group in position 17, e.g. oestrone

A61K 31/567

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
56	Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
565	not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
567	substituted in position 17 alpha, e.g. mestranol, norethandrolone

A61K 31/566

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
56	Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
565	not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
566	having an oxo group in position 17, e.g. oestrone

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CPC

C07J 9/00

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
9	Normal 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

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
17	Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton

A61P 23/00

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
23	Anaesthetics

A61P 1/00

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

A61P 1/10

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
10	Laxatives

A61P 9/14

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9	Drugs for disorders of the cardiovascular system
14	Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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C07J 9/00

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
9	Normal 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

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
17	Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton

A61P 23/00

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
23	Anaesthetics

A61P 1/00

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

A61P 1/10

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
10	Laxatives

A61P 9/14

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9	Drugs for disorders of the cardiovascular system
14	Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

A61P 35/00

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35	Antineoplastic agents

A61P 29/00

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29	Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)

A61P 3/10

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

A61P 25/00

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system

A61P 25/22

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
22	Anxiolytics

A61P 25/28

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
28	for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

A61P 25/18

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
18	Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

A61P 25/04

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
04	Centrally acting analgesics, e.g. opioids

A61P 25/08

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
08	Antiepileptics; Anticonvulsants

A61P 25/14

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
14	for treating abnormal movements, e.g. chorea, dyskinesia

A61P 25/16

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
14	for treating abnormal movements, e.g. chorea, dyskinesia
16	Anti-Parkinson drugs

A61P 27/02

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27	Drugs for disorders of the senses
02	Ophthalmic agents

A61P 27/16

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27	Drugs for disorders of the senses
16	Otologicals

A61P 9/10

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9	Drugs for disorders of the cardiovascular system
10	for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

A61P 25/24

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
24	Antidepressants

C07J 7/002

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
7	Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
0005	not substituted in position 21
001	substituted in position 20 by a keto group
0015	not substituted in position 17 alfa
002	not substituted in position 16

C07J 9/005

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
9	Normal 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
005	containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

C07J 13/007

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
13	Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
007	with double bond in position 17 (20)

C07J 31/006

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
31	Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
006	not covered by C07J31/003

C07J 41/0061

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
41	Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
0033	not covered by C07J41/0005
0055	the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
0061	one of the carbon atoms being part of an amide group

C07J 13/005

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
13	Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
005	with double bond in position 16 (17)

A61P 3/00

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

A61P 25/20

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system
20	Hypnotics; Sedatives

C07J 21/00

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
J	STEROIDS
21	Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton

A61K 31/575

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
56	Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
575	substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol

A61K 31/58

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
56	Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
58	containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin

A61P 1/04

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

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Applicants SAGE THERAPEUTICS INC.
萨奇治疗股份有限公司

Inventors SALITURO FRANCESCO G
F.G.萨利图罗
ROBICHAUD ALBERT JEAN
A.J.罗比乔德
MARTINEZ BOTELLA GABRIEL
G.马丁内斯博特拉
HARRISON BOYD L
B.L.哈里森

Agents 北京市柳沈律师事务所 11105
北京市柳沈律师事务所 11105

Priority Data 62/189,068 06.07.2015 US
62/332,931 06.05.2016 US

Title

(EN) OXYSTEROLS AND METHODS OF USE THEREOF

(ZH) 氧甾醇及其使用方法

Abstract

(EN) Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, and R3 are as defined herein. Compounds of the invention are contemplated useful for the prevention and treatment of a variety of conditions.

(ZH) 本文提供式(I)化合物及其药学上可接受的盐和包含其的药物组合物；其中R1、R2和R3如本文所定义。本发明化合物预期用于预防和治疗多种病症。

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1. CN108135911 - OXYSTEROLS AND METHODS OF USE THEREOF