MX2018015236A - Lipido cationico. - Google Patents

Lipido cationico.

Info

Publication number
MX2018015236A
MX2018015236A MX2018015236A MX2018015236A MX2018015236A MX 2018015236 A MX2018015236 A MX 2018015236A MX 2018015236 A MX2018015236 A MX 2018015236A MX 2018015236 A MX2018015236 A MX 2018015236A MX 2018015236 A MX2018015236 A MX 2018015236A
Authority
MX
Mexico
Prior art keywords
carbon atoms
cationic lipid
formulae
formula
alkyl group
Prior art date
Application number
MX2018015236A
Other languages
English (en)
Inventor
Takahashi Yoshinori
Suzuki Yuta
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

Links

Classifications

    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (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)
  • Biophysics (AREA)
  • Dispersion Chemistry (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 proporciona un lípido catiónico que es apto para usarse en el suministro de ácidos nucleicos al citoplasma. Un lípido catiónico de acuerdo con la presente invención es, por ejemplo, un compuesto representado por la fórmula (1a) o una sal farmacéuticamente aceptable de este. (En la fórmula (1a), cada uno de L1 y L2 representa independientemente un grupo alquileno que tiene 3-10 átomos de carbono; cada uno de R1 y R2 representa independientemente un grupo alquilo que tiene 4-22 átomos de carbono o un grupo alquenilo que tiene 4-22 átomos de carbono; X1 representa un enlace sencillo o -CO-O-; y el anillo P representa una de las fórmulas (P-1) a (P-5)). (En las fórmulas (P-1) a (P-5), R3 representa un grupo alquilo que tiene 1-3 átomos de carbono). (ver Fórmulas).
MX2018015236A 2016-06-24 2017-06-22 Lipido cationico. MX2018015236A (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 (1)

Publication Number Publication Date
MX2018015236A true MX2018015236A (es) 2019-04-11

Family

ID=60784078

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018015236A MX2018015236A (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) MX2018015236A (es)
RU (1) RU2740921C2 (es)
SG (1) SG11201808928YA (es)
TW (1) TWI745386B (es)
WO (1) WO2017222016A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7164547B2 (ja) * 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 カチオン性脂質
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
CN111164068B (zh) 2018-08-21 2023-11-14 株式会社东芝 生物降解性化合物、脂质粒子、含有脂质粒子的组合物、及试剂盒
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
EP4289814A1 (en) 2021-02-04 2023-12-13 Shionogi & Co., Ltd Cationic lipid
AU2022358609A1 (en) * 2021-09-28 2024-05-02 Seqirus Inc. Ionizable cationic compound
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

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2475065T3 (es) 2008-10-09 2014-07-10 Tekmira Pharmaceuticals Corporation Aminol�pidos mejorados y métodos para la administración de ácidos nucleicos
TR201811076T4 (tr) 2009-06-10 2018-08-27 Arbutus Biopharma Corp Geliştirilmiş lipit formulasyonu.
CN103096875B (zh) 2010-06-03 2016-08-17 阿尔尼拉姆医药品有限公司 用于递送活性剂的生物可降解脂质
JP5961170B2 (ja) 2010-09-20 2016-08-02 サーナ・セラピューティクス・インコーポレイテッドＳｉｒｎａ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． オリゴヌクレオチドの送達のための新規な低分子量カチオン性脂質
WO2012061259A2 (en) 2010-11-05 2012-05-10 Merck Sharp & Dohme Corp. Novel low molecular weight cyclic amine containing cationic lipids for oligonucleotide delivery
KR102011048B1 (ko) 2011-10-18 2019-08-14 다이서나 파마수이티컬, 인크. 아민 양이온성 지질 및 그것의 용도
AU2012347637B2 (en) 2011-12-07 2017-09-14 Alnylam Pharmaceuticals, Inc. Biodegradable lipids for the delivery of active agents
ES2700742T3 (es) * 2012-03-16 2019-02-19 Merck Patent Gmbh Lípidos aminoácidos
JP6232416B2 (ja) 2012-04-19 2017-11-15 サーナ・セラピューティクス・インコーポレイテッドＳｉｒｎａ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． オリゴヌクレオチド送達のための、新規なジエステルおよびトリエステルベースの低分子量、生分解性カチオン性脂質
TW201408625A (zh) * 2012-07-06 2014-03-01 Kyowa Hakko Kirin Co Ltd 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
EP3083579B1 (en) 2013-12-19 2022-01-26 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
AU2015285279A1 (en) * 2014-06-30 2017-02-16 Kyowa Hakko Kirin Co., Ltd. Cationic lipid
CA2969664C (en) 2014-12-26 2022-06-21 Eisai R&D Management Co., Ltd. Cationic lipid

Also Published As

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

Similar Documents

Publication Publication Date Title
MX2018015236A (es) Lipido cationico.
EP4310075A3 (en) Ionizable cationic lipid for rna delivery
AU2016343803A8 (en) Novel lipids and lipid nanoparticle formulations for delivery of nucleic acids
MX2021002978A (es) Lactamas biciclicas y metodos de uso de las mismas.
MX2018011831A (es) Antagonistas solubles de receptor de c5aa(c5ar).
PH12017500281A1 (en) Pyrrolopyrimidine compounds used as tlr7 agonist
NZ720174A (en) Ionizable cationic lipid for rna delivery
PH12016501633B1 (en) Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
TN2017000524A1 (en) New bicyclic derivatives, a process for their preparation and pharmaceutical compositions containing them
EP3828186A3 (en) Pyrimidinones as factor xia inhibitors
TN2017000521A1 (en) New aminoacid derivatives, a process for their preparation and pharmaceutical compositions containing them
TN2018000395A1 (en) New (hetero)aryl-substituted-piperidinyl derivatives, a process for their preparation and pharmaceutical compositions containing them
MY196413A (en) Substituted Carbonucleoside Derivatives Useful as Anticancer Agents
WO2014144545A3 (en) Substituted benzoxazoles and methods of use thereof
MX2018008095A (es) Compuestos heterociclicos triciclicos condensados como inhibidores de integrasa del vih.
CR20220251A (es) Nuevos derivados de metilquinazolinona
TW201613864A (en) Novel compounds
MX2017016030A (es) Derivado de dihidropirrolopirazol sustituido.
CL2017002354A1 (es) Compuestos derivados de heteroarilos bicíclicos fusionados con actividad como inhibidores de phd.
AU2017269673A1 (en) Pyridine dicarboxamide derivatives as bromodomain inhibitors
MX2019013815A (es) Inhibidor de antigenos de superficie del virus de la hepatitis b.
MX2016005993A (es) Anfifilos biscationicos y triscationicos como agentes antimicrobianos.
BR112017000246A2 (pt) composto, sal farmaceuticamente aceitável de um composto, composição farmacêutica, e, uso de um composto ou de um sal
NZ721780A (en) Heterocyclic modulators of lipid synthesis for use against cancer and viral infections
MX2021005462A (es) Lipidos cationicos que contienen silicio.