CN110049992A - 一类水溶性别孕烯醇酮衍生物及其用途 - Google Patents

一类水溶性别孕烯醇酮衍生物及其用途 Download PDF

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CN110049992A
CN110049992A CN201780075016.0A CN201780075016A CN110049992A CN 110049992 A CN110049992 A CN 110049992A CN 201780075016 A CN201780075016 A CN 201780075016A CN 110049992 A CN110049992 A CN 110049992A
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compound
pharmaceutically acceptable
acid
polymorph
acceptable salt
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CN110049992B (zh
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李勤耕
王涛
陈刚
任亮
刘新
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Jiangsu Nhwaluokang Pharmceutical Research And Development Co ltd
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Jiangsu Nhwaluokang Pharmceutical Research And Development Co ltd
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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
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system 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
    • A—HUMAN NECESSITIES
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    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/62—Quaternary ammonium compounds
    • C07C211/63—Quaternary ammonium compounds having quaternised nitrogen atoms bound to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/62—Quaternary ammonium compounds
    • C07C211/64—Quaternary ammonium compounds having quaternised nitrogen atoms bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07J41/005—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 only two carbon atoms, e.g. pregnane 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
    • 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
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)

Abstract

Description

PCT国内申请，说明书已公开。

Claims (12)

  1. PCT国内申请，权利要求书已公开。
CN201780075016.0A 2016-12-05 2017-12-05 一类水溶性别孕烯醇酮衍生物及其用途 Active CN110049992B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201611101726.XA CN108148106A (zh) 2016-12-05 2016-12-05 一类水溶性别孕烯醇酮衍生物及其用途
CN201611101726X 2016-12-05
PCT/CN2017/114590 WO2018103626A1 (zh) 2016-12-05 2017-12-05 一类水溶性别孕烯醇酮衍生物及其用途

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CN110049992A true CN110049992A (zh) 2019-07-23
CN110049992B CN110049992B (zh) 2022-05-27

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US (1) US20190322698A1 (zh)
EP (1) EP3549945A4 (zh)
JP (1) JP2019536821A (zh)
KR (1) KR20190092466A (zh)
CN (2) CN108148106A (zh)
AU (1) AU2017372251A1 (zh)
CA (1) CA3045955A1 (zh)
EA (1) EA201991374A1 (zh)
WO (1) WO2018103626A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113368084A (zh) * 2020-03-10 2021-09-10 上海喀露蓝科技有限公司 含有大麻二酚，丙泊酚前药和别孕烯醇酮前药化合物的药物组合物及其在医药上的应用

Families Citing this family (6)

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Publication number Priority date Publication date Assignee Title
CZ309617B6 (cs) * 2019-04-05 2023-05-24 Ústav organické chemie a biochemie AV ČR, v. v. i 3α5ß-Neuroaktivní steroidy pro léčbu epilepsie a záchvatových onemocnění
CN112341511A (zh) * 2019-08-09 2021-02-09 南京诺瑞特医药科技有限公司 3-羟基-5-孕烷-20-酮衍生物及其用途
CN112824426B (zh) * 2019-11-21 2022-02-11 上海喀露蓝科技有限公司 一种别孕烯醇酮膦酰胺衍生物、其制备方法及其在医药上的用途
CN114907436A (zh) * 2021-02-08 2022-08-16 南京诺瑞特医药科技有限公司 3-羟基-5-孕烷-20-酮衍生物的晶型及其制备方法和用途
KR20240050372A (ko) * 2021-09-14 2024-04-18 난징 미노바 파마슈티컬 컴퍼니, 리미티드 수용성 알로프레그나놀론 유도체 및 이의 제조 방법과 용도
CN117801047A (zh) * 2023-01-19 2024-04-02 北京华睿鼎信科技有限公司 神经甾体衍生物及其用途

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WO2009108804A2 (en) * 2008-02-26 2009-09-03 Emory University Steroid analogues for neuroprotection

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US2708651A (en) * 1955-01-07 1955-05-17 Pfizer & Co C Water-soluble esters of pregnanolones
US6623933B1 (en) * 1999-08-31 2003-09-23 Trustees Of Boston University Methods for identifying a subunit specific modulator of N-methyl-D-asparate receptor
CZ303037B6 (cs) * 2009-05-28 2012-03-07 Ústav organické chemie a biochemie, Akademie ved CR, v. v. i. Deriváty pregnanolonu substituované v poloze 3alfa, zpusob jejich výroby a jejich použití
US20130245253A1 (en) * 2010-03-26 2013-09-19 Department Of Veterans Affairs Conjugated Neuroactive Steroid Compositions And Methods Of Use
CZ303443B6 (cs) * 2011-02-15 2012-09-12 Ústav organické chemie a biochemie Akademie ved CR, v.v.i. Deriváty pregnanolonu substituované v poloze 3alfa kationickou skupinou, zpusob jejich výroby, jejich použití a prostredek je obsahující
NZ627781A (en) 2012-01-23 2016-10-28 Sage Therapeutics Inc Neuroactive steroid formulations and methods of treating cns disorders

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Publication number Priority date Publication date Assignee Title
WO2009108804A2 (en) * 2008-02-26 2009-09-03 Emory University Steroid analogues for neuroprotection

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113368084A (zh) * 2020-03-10 2021-09-10 上海喀露蓝科技有限公司 含有大麻二酚，丙泊酚前药和别孕烯醇酮前药化合物的药物组合物及其在医药上的应用

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US20190322698A1 (en) 2019-10-24
EP3549945A4 (en) 2020-05-27
WO2018103626A1 (zh) 2018-06-14
EP3549945A1 (en) 2019-10-09
AU2017372251A1 (en) 2019-07-25
JP2019536821A (ja) 2019-12-19
EA201991374A1 (ru) 2019-11-29
CN110049992B (zh) 2022-05-27
CA3045955A1 (en) 2018-06-14
CN108148106A (zh) 2018-06-12
KR20190092466A (ko) 2019-08-07

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