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

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
    • A61K47/28—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)
  • 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)
  • Saccharide Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Indole 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 (14)

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)
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 (14)

* 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
WO2021132462A1 (ja) 2019-12-26 2021-07-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 補体c5の発現を抑制する二本鎖リボ核酸を含む医薬組成物
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
US20240180954A1 (en) 2021-02-04 2024-06-06 Shionogi & Co., Ltd. Cationic lipid
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
JP2024538582A (ja) * 2021-09-28 2024-10-23 セキラス インコーポレイテッド イオン化可能なカチオン性化合物
CA3241492A1 (en) * 2021-12-23 2023-06-29 Suzhou Abogen Biosciences Co., Ltd. Lipid compound and lipid nanoparticle composition
CN114213346B (zh) * 2022-02-22 2022-05-20 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
KR20250155020A (ko) * 2023-02-09 2025-10-29 세퀴러스 인코포레이티드 이온화 가능한 양이온성 화합물
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

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5777519B2 (ja) 2008-10-09 2015-09-09 テクミラ ファーマシューティカルズ コーポレイション 改良されたアミノ脂質および核酸の送達方法
TR201811076T4 (tr) 2009-06-10 2018-08-27 Arbutus Biopharma Corp Geliştirilmiş lipit formulasyonu.
CA2800401C (en) 2010-06-03 2020-09-15 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.
WO2012061259A2 (en) 2010-11-05 2012-05-10 Merck Sharp & Dohme Corp. Novel low molecular weight cyclic amine containing cationic lipids for oligonucleotide delivery
ES2745373T3 (es) 2011-10-18 2020-03-02 Dicerna Pharmaceuticals Inc Lípidos catiónicos de amina y uso de los mismos
ES3065854T3 (en) 2011-12-07 2026-05-08 Alnylam Pharmaceuticals Inc Biodegradable lipids for the delivery of active agents
NZ630990A (en) * 2012-03-16 2016-04-29 Merck Patent Gmbh Aminoacid lipids
US9402816B2 (en) 2012-04-19 2016-08-02 Sima Therapeutics, Inc. Diester and triester based low molecular weight, biodegradeable cationic lipids for oligonucleotide delivery
TW201726599A (zh) * 2012-07-06 2017-08-01 協和醱酵麒麟有限公司 陽離子性脂質
US9687448B2 (en) 2012-12-07 2017-06-27 Alnylam Pharmaceuticals, Inc. 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
EP3082760A1 (en) 2013-12-19 2016-10-26 Novartis AG LEPTIN mRNA COMPOSITIONS AND FORMULATIONS
CN105916839B (zh) 2014-01-09 2018-09-18 卫材R&D管理有限公司 阳离子性脂质
EP3162794B1 (en) * 2014-06-30 2020-09-16 Kyowa Kirin Co., Ltd. Alkyl substituted azetidines as cationic lipid
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
JPWO2017222016A1 (ja) 2019-04-18
US20190218180A1 (en) 2019-07-18
KR20190021218A (ko) 2019-03-05
CN109311809A (zh) 2019-02-05
WO2017222016A1 (ja) 2017-12-28
EP3476832A1 (en) 2019-05-01
AU2017282459A1 (en) 2018-11-01
CN109311809B (zh) 2022-04-08
US10501416B2 (en) 2019-12-10
IL262574B (en) 2021-10-31
RU2740921C2 (ru) 2021-01-21
SG11201808928YA (en) 2018-11-29
MX2018015236A (es) 2019-04-11
CA3020271A1 (en) 2017-12-28
RU2018143237A3 (es) 2020-07-24
KR102358341B1 (ko) 2022-02-07
TWI745386B (zh) 2021-11-11
AU2017282459B2 (en) 2021-05-06
EP3476832A4 (en) 2020-02-19
ES2948971T3 (es) 2023-09-22
BR112018075123A2 (pt) 2019-06-18
TW201803849A (zh) 2018-02-01
IL262574A (en) 2018-12-31
JP6883034B2 (ja) 2021-06-02
RU2018143237A (ru) 2020-07-24

Similar Documents

Publication Publication Date Title
SG11201808928YA (en) Cationic lipid
EP4310075A3 (en) Ionizable cationic lipid for rna delivery
AU2016343803A8 (en) Novel lipids and lipid nanoparticle formulations for delivery of nucleic acids
ZA202206923B (en) New methylquinazolinone derivatives
EP4458348A3 (en) Pharmaceutical compositions containing substituted polycyclic pyridone derivatives and prodrug thereof
JO3430B1 (ar) مشتقات حمض أميني جديدة، عملية لتحضيرها وتركيبات صيدلية تحتوي عليها
EP4420679A3 (en) Lipids and lipid nanoparticle formulations for delivery of nucleic acids
TN2018000395A1 (en) New (hetero)aryl-substituted-piperidinyl derivatives, a process for their preparation and pharmaceutical compositions containing them
MX2020006800A (es) Lipidos cationicos.
MX381623B (es) Composición limpiadora.
TN2018000424A1 (en) Substituted carbonucleoside derivatives useful as anticancer agents
MA38175A1 (fr) Lactames fusionnés à un aryle et hétéroaryle
MX376833B (es) Oxiesteroles y metodos de uso de los mismos.
WO2014144545A3 (en) Substituted benzoxazoles and methods of use thereof
TN2018000410A1 (en) New piperidinyl derivatives, a process for their preparation and pharmaceutical compositions containing them
WO2018121559A8 (zh) 甘露糖醛二酸的组合物
MX382122B (es) Oxiesteroles y metodos de uso de los mismos.
EA201992771A1 (ru) Ингибитор поверхностного антигена вируса гепатита b
MX2016005993A (es) Anfifilos biscationicos y triscationicos como agentes antimicrobianos.
CR20170134A (es) Método para preparar 2´-o-fucosil-lactosa
MX2021003232A (es) Inhibidores de o-glicoproteina-2-acetamido-2-desoxi-3-d-glucopiran osidasa.
MX2025005209A (es) Compuestos lipídicos y usos de los mismos
AU2020353055A8 (en) Antiviral pyrazolopyridinone compounds
TN2017000342A1 (en) Novel cyclopropabenzofuranyl pyridopyrazinediones
MX386501B (es) Compuestos terapeuticos y sus metodos de uso