CN109415406A - 羊毛甾醇前药化合物及其制备方法和应用 - Google Patents

羊毛甾醇前药化合物及其制备方法和应用 Download PDF

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CN109415406A
CN109415406A CN201880002549.0A CN201880002549A CN109415406A CN 109415406 A CN109415406 A CN 109415406A CN 201880002549 A CN201880002549 A CN 201880002549A CN 109415406 A CN109415406 A CN 109415406A
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alkyl
pharmaceutically acceptable
acceptable salt
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CN109415406B (zh
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刘奕志
王延东
李小林
罗志
沈良
候丽娟
文欣欣
贺海鹰
黎健
陈曙辉
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Runer Eye Medicine Guangzhou Co ltd
Guangzhou Ocusun Ophthalmic Biotechnology Co Ltd
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Zhongshan Ophthalmic Center
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0038—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an androstane skeleton, including 18- or 19-substituted derivatives, 18-nor derivatives and also derivatives where position 17-beta is substituted by a carbon atom not directly bonded to a further carbon atom and not being part of an amide group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—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
    • C07J9/005—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 containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

一种羊毛甾醇前药化合物、药学上可接受的盐及其异构体，以及包含羊毛甾醇前药化合物的药物组合物，及其在制备治疗白内障药物上的应用。羊毛甾醇前药化合物与羊毛甾醇相比具有更好的渗透性。

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN201880002549.0A 2017-01-25 2018-01-25 羊毛甾醇前药化合物及其制备方法和应用 Active CN109415406B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201710061039 2017-01-25
CN2017100610398 2017-01-25
CN2017108682746 2017-09-22
CN201710868274 2017-09-22
PCT/CN2018/074120 WO2018137683A1 (zh) 2017-01-25 2018-01-25 羊毛甾醇前药化合物及其制备方法和应用

Publications (2)

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CN109415406A true CN109415406A (zh) 2019-03-01
CN109415406B CN109415406B (zh) 2019-08-06

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US (1) US10738076B2 (zh)
EP (1) EP3536698B1 (zh)
JP (1) JP6704535B2 (zh)
KR (1) KR102267924B1 (zh)
CN (1) CN109415406B (zh)
AU (1) AU2018212270B2 (zh)
DK (1) DK3536698T3 (zh)
ES (1) ES2890667T3 (zh)
RU (1) RU2720677C1 (zh)
WO (1) WO2018137683A1 (zh)
ZA (1) ZA201904124B (zh)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3078680A1 (en) * 2017-11-17 2019-05-23 Mahmood Piraee Combinations of lanosterol or 25-hydroxycholesterol including derivatives thereof useful in the treatment of lens disorders
KR20210038596A (ko) * 2018-07-25 2021-04-07 광저우 오쿠순 옵탈믹 바이오테크놀로지 캄파니 리미티드 라노 스테롤 전구 약물 화합물의 결정 형태 및 이의 용도
WO2020177714A1 (zh) * 2019-03-04 2020-09-10 中山大学中山眼科中心 一种羊毛甾醇前药化合物的组合物及其制备方法和应用
WO2021172359A1 (ja) * 2020-02-25 2021-09-02 大日本住友製薬株式会社 Ｃｄｋ９阻害剤プロドラッグ及びそれを内封するリポソーム
TW202320798A (zh) * 2021-08-18 2023-06-01 大陸商廣州潤爾眼科生物科技有限公司 甾體化合物在製備預防和/或治療飛蚊症的藥物中的應用
WO2023078252A1 (en) 2021-11-02 2023-05-11 Flare Therapeutics Inc. Pparg inverse agonists and uses thereof
WO2023143452A1 (zh) * 2022-01-28 2023-08-03 广州润尔眼科生物科技有限公司 甾体化合物在预防和/或治疗白内障中的应用
WO2023147640A1 (en) * 2022-02-07 2023-08-10 GERVÁSIO ALVES DA SILVA, Társis Preparation of novel triterpene alcohol derivatives with enhanced bioavailability for cancer, inflammation and pain treatment
WO2023173846A1 (zh) * 2022-03-14 2023-09-21 广州润尔眼科生物科技有限公司 一种甾体化合物及其制备方法与应用
TW202404608A (zh) * 2022-04-15 2024-02-01 大陸商廣州潤爾眼科生物科技有限公司 甾體化合物在製備預防和／或治療老花眼的藥物的用途
WO2023222116A1 (zh) * 2022-05-20 2023-11-23 广州润尔眼科生物科技有限公司 甾体化合物的应用
WO2024017315A1 (zh) * 2022-07-21 2024-01-25 广州润尔眼科生物科技有限公司 甾体化合物在制备预防和/或治疗眼科疾病药物中的应用

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WO2016029197A1 (en) * 2014-08-22 2016-02-25 Kang Zhang Compositions and methods to treat and/or prevent vision disorders of the lens of the eye
CN106074568A (zh) * 2015-09-02 2016-11-09 盛世泰科生物医药技术(苏州)有限公司 一种用于预防和治疗白内障的眼用制剂及其制备方法

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JP4995334B2 (ja) * 2010-08-27 2012-08-08 キヤノン株式会社 アゾ化合物、該アゾ化合物を含有する顔料分散剤、顔料組成物、顔料分散体及びトナー
JP5748430B2 (ja) * 2010-08-27 2015-07-15 キヤノン株式会社 色素化合物、該色素化合物を含有する顔料分散剤、顔料組成物、顔料分散体及びトナー
CN104203970B (zh) * 2012-01-12 2016-08-17 和光纯药工业株式会社 液晶取向剂
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CN111529481B (zh) * 2014-08-22 2023-09-15 广州康睿生物医药科技股份有限公司 用于治疗视觉障碍的组合物和方法
US10155788B2 (en) * 2014-10-07 2018-12-18 Brigham Young University Cationic steroidal antimicrobial prodrug compositions and uses thereof
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CA3078680A1 (en) 2017-11-17 2019-05-23 Mahmood Piraee Combinations of lanosterol or 25-hydroxycholesterol including derivatives thereof useful in the treatment of lens disorders

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016029197A1 (en) * 2014-08-22 2016-02-25 Kang Zhang Compositions and methods to treat and/or prevent vision disorders of the lens of the eye
CN106074568A (zh) * 2015-09-02 2016-11-09 盛世泰科生物医药技术(苏州)有限公司 一种用于预防和治疗白内障的眼用制剂及其制备方法

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Publication number Publication date
EP3536698B1 (en) 2021-08-04
AU2018212270A1 (en) 2019-05-23
KR20190057378A (ko) 2019-05-28
KR102267924B1 (ko) 2021-06-21
EP3536698A1 (en) 2019-09-11
ES2890667T3 (es) 2022-01-21
ZA201904124B (en) 2021-05-26
US10738076B2 (en) 2020-08-11
JP2020503379A (ja) 2020-01-30
AU2018212270B2 (en) 2020-07-02
RU2720677C1 (ru) 2020-05-12
BR112019013598A2 (pt) 2020-01-07
US20190256548A1 (en) 2019-08-22
EP3536698A4 (en) 2019-11-27
WO2018137683A1 (zh) 2018-08-02
JP6704535B2 (ja) 2020-06-03
CN109415406B (zh) 2019-08-06
DK3536698T3 (da) 2021-09-27

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