CN105744937A - 高效糖皮质激素 - Google Patents

高效糖皮质激素 Download PDF

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Publication number
CN105744937A
CN105744937A CN201480063706.0A CN201480063706A CN105744937A CN 105744937 A CN105744937 A CN 105744937A CN 201480063706 A CN201480063706 A CN 201480063706A CN 105744937 A CN105744937 A CN 105744937A
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CN
China
Prior art keywords
compound
alkyl
group
heteroaryl
aryl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201480063706.0A
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English (en)
Chinese (zh)
Inventor
H·E·徐
Y·何
K·梅尔彻
易伟
施晶晶
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shanghai Institute of Materia Medica of CAS
Van Andel Research Institute
Original Assignee
Shanghai Institute of Materia Medica of CAS
Van Andel Research Institute
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shanghai Institute of Materia Medica of CAS, Van Andel Research Institute filed Critical Shanghai Institute of Materia Medica of CAS
Priority to CN202110799536.4A priority Critical patent/CN113845558A/zh
Publication of CN105744937A publication Critical patent/CN105744937A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0047—Nitrogen only at position 2(3)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Epidemiology (AREA)
CN201480063706.0A 2013-09-25 2014-09-25 高效糖皮质激素 Pending CN105744937A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202110799536.4A CN113845558A (zh) 2013-09-25 2014-09-25 高效糖皮质激素

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361882444P 2013-09-25 2013-09-25
US61/882,444 2013-09-25
PCT/US2014/057497 WO2015048316A1 (en) 2013-09-25 2014-09-25 Highly potent glucocorticoids

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202110799536.4A Division CN113845558A (zh) 2013-09-25 2014-09-25 高效糖皮质激素

Publications (1)

Publication Number Publication Date
CN105744937A true CN105744937A (zh) 2016-07-06

Family

ID=52744465

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201480063706.0A Pending CN105744937A (zh) 2013-09-25 2014-09-25 高效糖皮质激素
CN202110799536.4A Pending CN113845558A (zh) 2013-09-25 2014-09-25 高效糖皮质激素

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202110799536.4A Pending CN113845558A (zh) 2013-09-25 2014-09-25 高效糖皮质激素

Country Status (9)

Country Link
US (1) US9975918B2 (https=)
EP (1) EP3049089B1 (https=)
JP (1) JP2016531852A (https=)
KR (1) KR20160060688A (https=)
CN (2) CN105744937A (https=)
AU (1) AU2014324961A1 (https=)
ES (1) ES2751457T3 (https=)
HK (1) HK1222565A1 (https=)
WO (1) WO2015048316A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110382033A (zh) * 2016-10-14 2019-10-25 范安德尔研究所 用于设计高效力糖皮质激素的结构与机制
CN117024499A (zh) * 2023-07-17 2023-11-10 陕西汉江药业集团股份有限公司 在2位引入亚甲基羟基的甾体化合物制备方法

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3319611T3 (pl) 2015-07-06 2021-07-12 Sage Therapeutics, Inc. Oksysterole i sposoby ich stosowania
MX382122B (es) 2015-07-06 2025-03-13 Sage Therapeutics Inc Oxiesteroles y metodos de uso de los mismos.
EP3436022B1 (en) 2016-04-01 2022-03-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US10752653B2 (en) 2016-05-06 2020-08-25 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
PT3519422T (pt) 2016-09-30 2022-12-05 Sage Therapeutics Inc Oxisteróis substituídos em c7 e métodos como moduladores nmda
CA3041088C (en) 2016-10-18 2024-05-21 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
DK4105223T3 (da) 2016-10-18 2025-07-07 Sage Therapeutics Inc Oxysteroler og fremgangsmåder til anvendelse deraf
CA3166630A1 (en) 2020-01-03 2021-07-08 Berg Llc Polycyclic amides as ube2k modulators for treating cancer
WO2025157225A1 (zh) * 2024-01-24 2025-07-31 浙江柏拉阿图医药科技有限公司 一种高效力糖皮质激素化合物及其制备和用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009044200A1 (en) * 2007-10-04 2009-04-09 Astrazeneca Ab Steroidal [3, 2-c] pyrazole compounds, with glucocorticoid activity
US20100256105A1 (en) * 2009-04-03 2010-10-07 Astrazeneca R&D Novel compounds
CN102834406A (zh) * 2009-06-16 2012-12-19 默沙东公司 作为糖皮质激素受体激动剂的新的[3.2-c]杂芳基甾体、其组合物和用途
US20130237507A1 (en) * 2009-04-03 2013-09-12 Astrazeneca Ab, Intellectual Property Novel Amide Compounds

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4049813A (en) 1976-07-15 1977-09-20 Sandoz, Inc. Substituted isoxazolo pyridinones
CA2451057A1 (en) 2001-06-14 2002-12-27 Banyu Pharmaceutical Co., Ltd. Novel isoxazolopyridone derivatives and use thereof
GB0119911D0 (en) 2001-08-15 2001-10-10 Novartis Ag Organic Compounds
CA2749585A1 (en) 2009-01-13 2010-07-22 Van Andel Research Institute Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009044200A1 (en) * 2007-10-04 2009-04-09 Astrazeneca Ab Steroidal [3, 2-c] pyrazole compounds, with glucocorticoid activity
US20100256105A1 (en) * 2009-04-03 2010-10-07 Astrazeneca R&D Novel compounds
US20130237507A1 (en) * 2009-04-03 2013-09-12 Astrazeneca Ab, Intellectual Property Novel Amide Compounds
CN102834406A (zh) * 2009-06-16 2012-12-19 默沙东公司 作为糖皮质激素受体激动剂的新的[3.2-c]杂芳基甾体、其组合物和用途

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110382033A (zh) * 2016-10-14 2019-10-25 范安德尔研究所 用于设计高效力糖皮质激素的结构与机制
CN110382033B (zh) * 2016-10-14 2022-04-15 范安德尔研究所 用于设计高效力糖皮质激素的结构与机制
CN117024499A (zh) * 2023-07-17 2023-11-10 陕西汉江药业集团股份有限公司 在2位引入亚甲基羟基的甾体化合物制备方法

Also Published As

Publication number Publication date
JP2016531852A (ja) 2016-10-13
EP3049089B1 (en) 2019-08-21
KR20160060688A (ko) 2016-05-30
AU2014324961A8 (en) 2016-04-21
WO2015048316A1 (en) 2015-04-02
CN113845558A (zh) 2021-12-28
EP3049089A4 (en) 2017-08-09
ES2751457T3 (es) 2020-03-31
AU2014324961A1 (en) 2016-04-14
EP3049089A1 (en) 2016-08-03
US20160251393A1 (en) 2016-09-01
US9975918B2 (en) 2018-05-22
HK1222565A1 (zh) 2017-07-07

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