SG11201808928YA - Cationic lipid - Google Patents

Cationic lipid

Info

Publication number
SG11201808928YA
SG11201808928YA SG11201808928YA SG11201808928YA SG11201808928YA SG 11201808928Y A SG11201808928Y A SG 11201808928YA SG 11201808928Y A SG11201808928Y A SG 11201808928YA SG 11201808928Y A SG11201808928Y A SG 11201808928YA SG 11201808928Y A SG11201808928Y A SG 11201808928YA
Authority
SG
Singapore
Prior art keywords
carbon atoms
cationic lipid
formulae
formula
independently represent
Prior art date
Application number
SG11201808928YA
Inventor
Yuta Suzuki
Yoshinori Takahashi
Original Assignee
Eisai R&D Man Co Ltd
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 Eisai R&D Man Co Ltd filed Critical Eisai R&D Man Co Ltd
Publication of SG11201808928YA publication Critical patent/SG11201808928YA/en

Links

Classifications

    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/7105—Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • 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
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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—Liposomes
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers

Landscapes

  • 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)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dispersion Chemistry (AREA)
  • Biophysics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Indole Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

The present invention provides a cationic lipid which is able to be used for nucleic acid delivery to the cytoplasm. A cationic lipid according to the present invention is, for example, a compound represented by formula (a) or a pharmaceutically acceptable salt thereof. (In formula (la), each of L 1 and L2 independently represent an alkylene group having 3-10 carbon atoms; each of R 1 and R2 independently represent an alkyl group having 4-22 carbon atoms or an alkenyl group having 4-22 carbon atoms; X i represents a single bond or -CO-O-; and ring P represents one of formulae (P-1) to (P-5).)(In formulae (P-1) to (P-5), R3 represents an alkyl group having 1-3 carbon atoms.) 0 -0-- 0 R 1 ,... , .....---,, 0 L 1 X 1 L2 R ( 1 a) N\"R3 r -----N C\N-R3 H, R3 .\\) cN,,) \,.IsIN__/ \ ,- (PA) (P-2) (P-3) (P-4) (P-5) 123
SG11201808928YA 2016-06-24 2017-06-22 Cationic lipid SG11201808928YA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2016125925 2016-06-24
PCT/JP2017/023051 WO2017222016A1 (en) 2016-06-24 2017-06-22 Cationic lipid

Publications (1)

Publication Number Publication Date
SG11201808928YA true SG11201808928YA (en) 2018-11-29

Family

ID=60784078

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201808928YA SG11201808928YA (en) 2016-06-24 2017-06-22 Cationic lipid

Country Status (15)

Country Link
US (1) US10501416B2 (en)
EP (1) EP3476832B1 (en)
JP (1) JP6883034B2 (en)
KR (1) KR102358341B1 (en)
CN (1) CN109311809B (en)
AU (1) AU2017282459B2 (en)
BR (1) BR112018075123A2 (en)
CA (1) CA3020271A1 (en)
ES (1) ES2948971T3 (en)
IL (1) IL262574B (en)
MX (1) MX2018015236A (en)
RU (1) RU2740921C2 (en)
SG (1) SG11201808928YA (en)
TW (1) TWI745386B (en)
WO (1) WO2017222016A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7164547B2 (en) * 2017-12-27 2022-11-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 cationic lipid
CN110283223B (en) * 2018-03-19 2022-01-04 广州市锐博生物科技有限公司 Cationic lipid molecule and application thereof in nucleic acid delivery
EP3842412B1 (en) * 2018-08-21 2024-04-24 Kabushiki Kaisha Toshiba Biodegradable lipids for delivery of active compounds into tumor cells comprising two or more tertiary amino groups
US10526603B1 (en) * 2018-10-26 2020-01-07 Eisai R&D Management Co., Ltd. Double-stranded ribonucleic acid capable of suppressing expression of complement C5
JP6918197B2 (en) * 2019-12-26 2021-08-11 エーザイ・アール・アンド・ディー・マネジメント株式会社 Pharmaceutical composition containing lipid complex and pharmaceutical composition containing lipid nanoparticles
AU2020413311A1 (en) * 2019-12-26 2022-06-16 Eisai R&D Management Co., Ltd. Pharmaceutical composition containing double-stranded ribonucleic acid inhibiting expression of complement C5
US20240180954A1 (en) 2021-02-04 2024-06-06 Shionogi & Co., Ltd. Cationic lipid
EP4409002A1 (en) * 2021-09-28 2024-08-07 Seqirus Inc. Ionizable cationic compound
CN114874150A (en) * 2022-02-22 2022-08-09 中国科学院基础医学与肿瘤研究所(筹) Bivalent ionizable lipid compound, composition and application thereof

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PL2350043T3 (en) 2008-10-09 2014-09-30 Tekmira Pharmaceuticals Corp Improved amino lipids and methods for the delivery of nucleic acids
PL3431076T3 (en) 2009-06-10 2022-01-31 Arbutus Biopharma Corporation Improved lipid formulation
KR20190039347A (en) 2010-06-03 2019-04-10 알닐람 파마슈티칼스 인코포레이티드 Biodegradable lipids for the delivery of active agents
KR101878361B1 (en) 2010-09-20 2018-08-20 시르나 쎄러퓨틱스 인코퍼레이티드 Novel low molecular weight cationic lipids for oligonucleotide delivery
DK2635265T3 (en) 2010-11-05 2018-07-16 Sirna Therapeutics Inc New low molecular weight cyclic amine-containing cationic lipids for oligonucleotide delivery
AU2012325997C1 (en) 2011-10-18 2018-07-05 Dicerna Pharmaceuticals, Inc. Amine cationic lipids and uses thereof
WO2013086354A1 (en) * 2011-12-07 2013-06-13 Alnylam Pharmaceuticals, Inc. Biodegradable lipids for the delivery of active agents
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EP2838877B1 (en) 2012-04-19 2018-09-12 Sirna Therapeutics, Inc. Novel diester and triester based low molecular weight, biodegradable cationic lipids for oligonucleotide delivery
TW201408625A (en) * 2012-07-06 2014-03-01 Kyowa Hakko Kirin Co Ltd Cationic lipid
CA2891911C (en) 2012-12-07 2023-03-07 Alnylam Pharmaceuticals, Inc. Improved nucleic acid lipid particle formulations
TW201534578A (en) * 2013-07-08 2015-09-16 Daiichi Sankyo Co Ltd Novel lipid
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CA2935914C (en) * 2014-01-09 2022-02-08 Eisai R&D Management Co., Ltd. Cationic lipid
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EP3239132B1 (en) 2014-12-26 2019-03-06 Eisai R&D Management Co., Ltd. Cationic lipid

Also Published As

Publication number Publication date
EP3476832B1 (en) 2023-04-19
WO2017222016A1 (en) 2017-12-28
TWI745386B (en) 2021-11-11
EP3476832A1 (en) 2019-05-01
JPWO2017222016A1 (en) 2019-04-18
KR20190021218A (en) 2019-03-05
RU2018143237A3 (en) 2020-07-24
KR102358341B1 (en) 2022-02-07
US10501416B2 (en) 2019-12-10
RU2018143237A (en) 2020-07-24
EP3476832A4 (en) 2020-02-19
ES2948971T3 (en) 2023-09-22
US20190218180A1 (en) 2019-07-18
TW201803849A (en) 2018-02-01
JP6883034B2 (en) 2021-06-02
MX2018015236A (en) 2019-04-11
AU2017282459B2 (en) 2021-05-06
RU2740921C2 (en) 2021-01-21
AU2017282459A1 (en) 2018-11-01
CN109311809A (en) 2019-02-05
IL262574B (en) 2021-10-31
CN109311809B (en) 2022-04-08
CA3020271A1 (en) 2017-12-28
IL262574A (en) 2018-12-31
BR112018075123A2 (en) 2019-06-18

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