CN103547560A - 稳定的dotap氯化物晶体变体 - Google Patents

稳定的dotap氯化物晶体变体 Download PDF

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Publication number
CN103547560A
CN103547560A CN201280024160.9A CN201280024160A CN103547560A CN 103547560 A CN103547560 A CN 103547560A CN 201280024160 A CN201280024160 A CN 201280024160A CN 103547560 A CN103547560 A CN 103547560A
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China
Prior art keywords
dotap chloride
dotap
chloride
crystals
crystallization
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
CN201280024160.9A
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English (en)
Chinese (zh)
Inventor
M·W·普拉切尔
A·黑丁格尔
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Merck Patent GmbH
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Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Priority to CN201810169562.7A priority Critical patent/CN108285422A/zh
Publication of CN103547560A publication Critical patent/CN103547560A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B43/00—Formation or introduction of functional groups containing nitrogen
    • C07B43/06—Formation or introduction of functional groups containing nitrogen of amide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C219/08—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to an acyclic carbon atom of an acyclic unsaturated carbon skeleton
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A61K31/231—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Liquid Crystal Substances (AREA)
CN201280024160.9A 2011-05-20 2012-05-02 稳定的dotap氯化物晶体变体 Pending CN103547560A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201810169562.7A CN108285422A (zh) 2011-05-20 2012-05-02 稳定的dotap氯化物晶体变体

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161488428P 2011-05-20 2011-05-20
US61/488,428 2011-05-20
PCT/EP2012/001882 WO2012159704A1 (en) 2011-05-20 2012-05-02 Stable crystal modifications of dotap chloride

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201810169562.7A Division CN108285422A (zh) 2011-05-20 2012-05-02 稳定的dotap氯化物晶体变体

Publications (1)

Publication Number Publication Date
CN103547560A true CN103547560A (zh) 2014-01-29

Family

ID=46044632

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201810169562.7A Pending CN108285422A (zh) 2011-05-20 2012-05-02 稳定的dotap氯化物晶体变体
CN201280024160.9A Pending CN103547560A (zh) 2011-05-20 2012-05-02 稳定的dotap氯化物晶体变体

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201810169562.7A Pending CN108285422A (zh) 2011-05-20 2012-05-02 稳定的dotap氯化物晶体变体

Country Status (21)

Country Link
US (1) US10000445B2 (enExample)
EP (1) EP2709981B1 (enExample)
JP (3) JP6290076B2 (enExample)
KR (1) KR101974231B1 (enExample)
CN (2) CN108285422A (enExample)
AU (1) AU2012261276B2 (enExample)
BR (2) BR122021007641B8 (enExample)
CA (1) CA2836499C (enExample)
ES (1) ES2726526T3 (enExample)
HK (1) HK1251217A1 (enExample)
HU (1) HUE042949T2 (enExample)
IL (1) IL229146B (enExample)
MX (1) MX361369B (enExample)
NO (1) NO344225B1 (enExample)
PL (1) PL2709981T3 (enExample)
PT (1) PT2709981T (enExample)
RU (1) RU2627354C2 (enExample)
SG (2) SG10201706859QA (enExample)
TR (1) TR201906107T4 (enExample)
WO (1) WO2012159704A1 (enExample)
ZA (1) ZA201309638B (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107827762A (zh) * 2017-11-14 2018-03-23 苏州东南药业股份有限公司 一种(2, 3‑二油酰基‑丙基)三化甲基氯化铵及其制备方法和用途
CN119371322A (zh) * 2023-07-27 2025-01-28 上海医药工业研究院有限公司 一种1,2-二油酰氧基-3-(二甲氨基)丙烷的制备和纯化方法

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2709981T (pt) * 2011-05-20 2019-05-30 Merck Patent Gmbh Preparação de modificações cristalinas estáveis de cloreto de dotap
KR102583917B1 (ko) * 2014-12-08 2023-10-04 니치유 가부시키가이샤 양이온성 지질을 제조하는 방법

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5264618A (en) * 1990-04-19 1993-11-23 Vical, Inc. Cationic lipids for intracellular delivery of biologically active molecules
WO2005049549A1 (en) * 2003-11-12 2005-06-02 Chemi Spa Process for the synthesis of cationic lipids
CN101065350A (zh) * 2004-11-26 2007-10-31 默克专利股份有限公司 稳定的dotap氯化物晶形

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4013632A1 (de) 1990-04-27 1991-10-31 Max Planck Gesellschaft Liposomen mit positiver ueberschussladung
DE19521412A1 (de) * 1995-06-14 1996-12-19 Boehringer Mannheim Gmbh Neue kationische und polykationische Amphiphile, diese enthaltende Reagenzien und deren Verwendung
US5869715A (en) 1995-09-27 1999-02-09 The Reagents Of The University Of California Polyfunctional cationic cytofectins
US20030129223A1 (en) 2000-10-11 2003-07-10 Targesome, Inc. Targeted multivalent macromolecules
AU2002953285A0 (en) * 2002-12-12 2003-01-02 Protech Research Pty Ltd Yeast treatment
PT2709981T (pt) * 2011-05-20 2019-05-30 Merck Patent Gmbh Preparação de modificações cristalinas estáveis de cloreto de dotap

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5264618A (en) * 1990-04-19 1993-11-23 Vical, Inc. Cationic lipids for intracellular delivery of biologically active molecules
WO2005049549A1 (en) * 2003-11-12 2005-06-02 Chemi Spa Process for the synthesis of cationic lipids
CN101065350A (zh) * 2004-11-26 2007-10-31 默克专利股份有限公司 稳定的dotap氯化物晶形

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107827762A (zh) * 2017-11-14 2018-03-23 苏州东南药业股份有限公司 一种(2, 3‑二油酰基‑丙基)三化甲基氯化铵及其制备方法和用途
CN107827762B (zh) * 2017-11-14 2020-10-02 苏州东南药业股份有限公司 一种(2,3-二油酰基-丙基)三甲基氯化铵及其制备方法和用途
CN119371322A (zh) * 2023-07-27 2025-01-28 上海医药工业研究院有限公司 一种1,2-二油酰氧基-3-(二甲氨基)丙烷的制备和纯化方法

Also Published As

Publication number Publication date
RU2627354C2 (ru) 2017-08-07
BR112013029588B1 (pt) 2021-10-26
IL229146A0 (en) 2013-12-31
ZA201309638B (en) 2015-04-29
SG194957A1 (en) 2013-12-30
EP2709981A1 (en) 2014-03-26
CA2836499A1 (en) 2012-11-29
CN108285422A (zh) 2018-07-17
WO2012159704A1 (en) 2012-11-29
JP2018203776A (ja) 2018-12-27
NO344225B1 (no) 2019-10-14
JP2017075166A (ja) 2017-04-20
JP2014520085A (ja) 2014-08-21
AU2012261276A1 (en) 2014-01-09
NZ619175A (en) 2015-08-28
BR122021007641B1 (pt) 2021-11-09
US10000445B2 (en) 2018-06-19
BR122021007641B8 (pt) 2021-12-07
SG10201706859QA (en) 2017-09-28
KR20140032451A (ko) 2014-03-14
BR112013029588A2 (pt) 2020-11-17
AU2012261276B2 (en) 2017-05-25
CA2836499C (en) 2019-01-15
JP6290076B2 (ja) 2018-03-07
RU2013156477A (ru) 2015-06-27
US20140093558A1 (en) 2014-04-03
MX361369B (es) 2018-12-05
MX2013013403A (es) 2013-12-10
EP2709981B1 (en) 2019-02-13
PT2709981T (pt) 2019-05-30
IL229146B (en) 2019-08-29
KR101974231B1 (ko) 2019-04-30
WO2012159704A8 (en) 2013-09-12
PL2709981T3 (pl) 2019-07-31
HUE042949T2 (hu) 2019-07-29
NO20131703A1 (no) 2013-12-18
HK1251217A1 (zh) 2019-01-25
ES2726526T3 (es) 2019-10-07
TR201906107T4 (tr) 2019-05-21

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