RU2627354C2 - Устойчивые кристаллические модификации хлорида dotap - Google Patents

Устойчивые кристаллические модификации хлорида dotap Download PDF

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RU2627354C2
RU2627354C2 RU2013156477A RU2013156477A RU2627354C2 RU 2627354 C2 RU2627354 C2 RU 2627354C2 RU 2013156477 A RU2013156477 A RU 2013156477A RU 2013156477 A RU2013156477 A RU 2013156477A RU 2627354 C2 RU2627354 C2 RU 2627354C2
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Prior art keywords
chloride
dotap
crystalline
values
theta
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RU2013156477A
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English (en)
Russian (ru)
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RU2013156477A (ru
Inventor
Михаэль Вильхельм ПЛАЧЕР
Альфред ХЕДИНГЕР
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Мерк Патент Гмбх
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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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (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)
RU2013156477A 2011-05-20 2012-05-02 Устойчивые кристаллические модификации хлорида dotap RU2627354C2 (ru)

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

Publications (2)

Publication Number Publication Date
RU2013156477A RU2013156477A (ru) 2015-06-27
RU2627354C2 true RU2627354C2 (ru) 2017-08-07

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RU2013156477A RU2627354C2 (ru) 2011-05-20 2012-05-02 Устойчивые кристаллические модификации хлорида dotap

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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) SG194957A1 (enExample)
TR (1) TR201906107T4 (enExample)
WO (1) WO2012159704A1 (enExample)
ZA (1) ZA201309638B (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108285422A (zh) * 2011-05-20 2018-07-17 默克专利股份有限公司 稳定的dotap氯化物晶体变体
WO2016093205A1 (ja) * 2014-12-08 2016-06-16 日油株式会社 カチオン性脂質の製造方法
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
CN119371322B (zh) * 2023-07-27 2026-08-11 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

Citations (4)

* 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
RU2179549C2 (ru) * 1995-06-14 2002-02-20 Роше Диагностикс Гмбх Новые катионные и поликатионные амфифильные соединения, содержащие их реагенты и их применение
WO2005049549A1 (en) * 2003-11-12 2005-06-02 Chemi Spa Process for the synthesis of cationic lipids
WO2006056312A1 (de) * 2004-11-26 2006-06-01 Merck Patent Gmbh Stabile kristallmodifikationen von dotap chlorid

Family Cites Families (5)

* 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
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
CN108285422A (zh) * 2011-05-20 2018-07-17 默克专利股份有限公司 稳定的dotap氯化物晶体变体

Patent Citations (4)

* 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
RU2179549C2 (ru) * 1995-06-14 2002-02-20 Роше Диагностикс Гмбх Новые катионные и поликатионные амфифильные соединения, содержащие их реагенты и их применение
WO2005049549A1 (en) * 2003-11-12 2005-06-02 Chemi Spa Process for the synthesis of cationic lipids
WO2006056312A1 (de) * 2004-11-26 2006-06-01 Merck Patent Gmbh Stabile kristallmodifikationen von dotap chlorid

Also Published As

Publication number Publication date
SG194957A1 (en) 2013-12-30
ZA201309638B (en) 2015-04-29
SG10201706859QA (en) 2017-09-28
PL2709981T3 (pl) 2019-07-31
IL229146A0 (en) 2013-12-31
JP2017075166A (ja) 2017-04-20
US10000445B2 (en) 2018-06-19
TR201906107T4 (tr) 2019-05-21
IL229146B (en) 2019-08-29
AU2012261276B2 (en) 2017-05-25
AU2012261276A1 (en) 2014-01-09
EP2709981B1 (en) 2019-02-13
MX361369B (es) 2018-12-05
CA2836499C (en) 2019-01-15
CN103547560A (zh) 2014-01-29
KR101974231B1 (ko) 2019-04-30
JP2018203776A (ja) 2018-12-27
NZ619175A (en) 2015-08-28
ES2726526T3 (es) 2019-10-07
JP6290076B2 (ja) 2018-03-07
NO20131703A1 (no) 2013-12-18
CN108285422A (zh) 2018-07-17
JP2014520085A (ja) 2014-08-21
HUE042949T2 (hu) 2019-07-29
US20140093558A1 (en) 2014-04-03
BR122021007641B1 (pt) 2021-11-09
BR122021007641B8 (pt) 2021-12-07
RU2013156477A (ru) 2015-06-27
WO2012159704A1 (en) 2012-11-29
BR112013029588B1 (pt) 2021-10-26
WO2012159704A8 (en) 2013-09-12
NO344225B1 (no) 2019-10-14
HK1251217A1 (zh) 2019-01-25
BR112013029588A2 (pt) 2020-11-17
EP2709981A1 (en) 2014-03-26
PT2709981T (pt) 2019-05-30
MX2013013403A (es) 2013-12-10
KR20140032451A (ko) 2014-03-14
CA2836499A1 (en) 2012-11-29

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