MX385488B - Lipido cationico. - Google Patents

Lipido cationico.

Info

Publication number
MX385488B
MX385488B MX2018015236A MX2018015236A MX385488B MX 385488 B MX385488 B MX 385488B MX 2018015236 A MX2018015236 A MX 2018015236A MX 2018015236 A MX2018015236 A MX 2018015236A MX 385488 B MX385488 B MX 385488B
Authority
MX
Mexico
Prior art keywords
sub
carbon atoms
cationic lipid
formulae
formula
Prior art date
Application number
MX2018015236A
Other languages
English (en)
Other versions
MX2018015236A (es
Inventor
Yoshinori Takahashi
Yuta Suzuki
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 MX2018015236A publication Critical patent/MX2018015236A/es
Publication of MX385488B publication Critical patent/MX385488B/es

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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
    • A61K47/28—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—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
    • 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
    • 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

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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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

La presente invención se refiere a un compuesto representado por la fórmula (la) a continuación o una sal farmacéuticamente aceptable de este: caracterizado porque L1 y L2 representan independientemente un grupo alquileno que tiene de 3 a 10 átomos de carbono ; R1 y R1 representan independiente un grupo alquilo que tiene de 4 a 22 átomos de carbono o un grupo alquenilo que tiene de 4 z 22 átomos de carbono; X1 representa un enlace sencillo o -CO-O-; y el anillo P representa cualquiera de las fórmulas (P-1) a (P-5) a continuación: donde R3 representa un grupo alquilo que tiene de 1 a 3 átomos de carbono.
MX2018015236A 2016-06-24 2017-06-22 Lipido cationico. MX385488B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2016125925 2016-06-24
PCT/JP2017/023051 WO2017222016A1 (ja) 2016-06-24 2017-06-22 カチオン性脂質

Publications (2)

Publication Number Publication Date
MX2018015236A MX2018015236A (es) 2019-04-11
MX385488B true MX385488B (es) 2025-03-18

Family

ID=60784078

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018015236A MX385488B (es) 2016-06-24 2017-06-22 Lipido cationico.

Country Status (15)

Country Link
US (1) US10501416B2 (es)
EP (1) EP3476832B1 (es)
JP (1) JP6883034B2 (es)
KR (1) KR102358341B1 (es)
CN (1) CN109311809B (es)
AU (1) AU2017282459B2 (es)
BR (1) BR112018075123A2 (es)
CA (1) CA3020271A1 (es)
ES (1) ES2948971T3 (es)
IL (1) IL262574B (es)
MX (1) MX385488B (es)
RU (1) RU2740921C2 (es)
SG (1) SG11201808928YA (es)
TW (1) TWI745386B (es)
WO (1) WO2017222016A1 (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3733647B1 (en) * 2017-12-27 2022-06-15 Eisai R&D Management Co., Ltd. Cationic lipid
CN110283223B (zh) * 2018-03-19 2022-01-04 广州市锐博生物科技有限公司 一种阳离子脂质分子及其在核酸递送中的应用
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
MX2022006514A (es) 2019-12-26 2022-07-11 Eisai R&D Man Co Ltd Composicion farmaceutica que contiene un acido ribonucleico de doble hebra que inhibe la expresion de c5 de complemento.
JP6918197B2 (ja) * 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 脂質複合体を含む医薬組成物及び脂質ナノ粒子を含む医薬組成物
EP4213882A4 (en) * 2020-09-15 2025-02-26 Verve Therapeutics, Inc. LIPID FORMULATIONS FOR GENE EDITING
JPWO2022168884A1 (es) 2021-02-04 2022-08-11
US20250281596A1 (en) * 2021-09-28 2025-09-11 Seqirus Inc. Ionizable cationic compound
JP2024536865A (ja) * 2021-09-28 2024-10-08 セキラス インコーポレイテッド メッセンジャーｒｎａ送達のためのイオン化性カチオン化合物
CN114874150A (zh) * 2022-02-22 2022-08-09 中国科学院基础医学与肿瘤研究所(筹) 一种双价可电离脂质化合物、组合物及其应用
AU2024217713A1 (en) * 2023-02-09 2025-08-14 Seqirus Inc. Ionizable cationic compound
WO2024237214A1 (ja) * 2023-05-12 2024-11-21 エーザイ・アール・アンド・ディー・マネジメント株式会社 脂質複合体

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WO2010042877A1 (en) 2008-10-09 2010-04-15 Tekmira Pharmaceuticals Corporation Improved amino lipids and methods for the delivery of nucleic acids
KR20230098713A (ko) 2009-06-10 2023-07-04 알닐람 파마슈티칼스 인코포레이티드 향상된 지질 조성물
NZ605079A (en) 2010-06-03 2015-08-28 Alnylam Pharmaceuticals Inc Biodegradable lipids for the delivery of active agents
MX349088B (es) 2010-09-20 2017-07-10 Merck Sharp & Dohme Lípidos catiónicos novedosos de bajo peso molecular para la entrega de oligonucleótidos.
DK2635265T3 (en) 2010-11-05 2018-07-16 Sirna Therapeutics Inc New low molecular weight cyclic amine-containing cationic lipids for oligonucleotide delivery
WO2013059496A1 (en) 2011-10-18 2013-04-25 Dicerna Pharmaceuticals, Inc. Amine cationic lipids and uses thereof
CA2856742A1 (en) 2011-12-07 2013-06-13 Alnylam Pharmaceuticals, Inc. Biodegradable lipids for the delivery of active agents
BR112014022847B1 (pt) * 2012-03-16 2022-08-23 Merck Patent Gmbh Lipídios aminoácidos, composição vesicular, e kit
AU2013249548A1 (en) 2012-04-19 2014-11-06 Sirna Therapeutics, Inc. Novel diester and triester based low molecular weight, biodegradable cationic lipids for oligonucleotide delivery
TW201726600A (zh) * 2012-07-06 2017-08-01 協和醱酵麒麟有限公司 陽離子性脂質
CA2891911C (en) 2012-12-07 2023-03-07 Alnylam Pharmaceuticals, Inc. Improved nucleic acid lipid particle formulations
TW201534578A (zh) * 2013-07-08 2015-09-16 Daiichi Sankyo Co Ltd 新穎脂質
WO2015095346A1 (en) 2013-12-19 2015-06-25 Novartis Ag Lipids and lipid compositions for the delivery of active agents
JP2017500865A (ja) 2013-12-19 2017-01-12 ノバルティス アーゲー レプチンｍＲＮＡの組成物および製剤
JP6389477B2 (ja) * 2014-01-09 2018-09-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 カチオン性脂質
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CN107207413B (zh) 2014-12-26 2019-04-30 卫材R&D管理有限公司 阳离子性脂质

Also Published As

Publication number Publication date
IL262574A (en) 2018-12-31
KR102358341B1 (ko) 2022-02-07
ES2948971T3 (es) 2023-09-22
AU2017282459A1 (en) 2018-11-01
US20190218180A1 (en) 2019-07-18
WO2017222016A1 (ja) 2017-12-28
TWI745386B (zh) 2021-11-11
CA3020271A1 (en) 2017-12-28
BR112018075123A2 (pt) 2019-06-18
RU2018143237A3 (es) 2020-07-24
CN109311809A (zh) 2019-02-05
RU2740921C2 (ru) 2021-01-21
MX2018015236A (es) 2019-04-11
EP3476832A4 (en) 2020-02-19
SG11201808928YA (en) 2018-11-29
TW201803849A (zh) 2018-02-01
CN109311809B (zh) 2022-04-08
EP3476832B1 (en) 2023-04-19
JP6883034B2 (ja) 2021-06-02
JPWO2017222016A1 (ja) 2019-04-18
KR20190021218A (ko) 2019-03-05
AU2017282459B2 (en) 2021-05-06
IL262574B (en) 2021-10-31
US10501416B2 (en) 2019-12-10
EP3476832A1 (en) 2019-05-01
RU2018143237A (ru) 2020-07-24

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