Processing

Please wait...

Settings

Settings

Goto Application

1. WO2022214025 - PEGYLATED LIPID, LIPOSOME MODIFIED THEREBY, PHARMACEUTICAL COMPOSITION CONTAINING LIPOSOME, PREPARATION THEREOF, AND USE THEREOF

Publication Number WO/2022/214025
Publication Date 13.10.2022
International Application No. PCT/CN2022/085526
International Filing Date 07.04.2022
IPC
C07C 219/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
219Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
02having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
06having the hydroxy groups esterified by carboxylic acids having the esterifying carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms of an acyclic saturated carbon skeleton
C07C 217/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
02having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
06having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
08the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
C07C 229/16 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
06having only one amino and one carboxyl group bound to the carbon skeleton
10the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
16to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
C07C 229/26 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
26having more than one amino group bound to the carbon skeleton, e.g. lysine
C07C 235/10 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
04the carbon skeleton being acyclic and saturated
10having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 323/25 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
23containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
24having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
25the carbon skeleton being acyclic and saturated
CPC
A61K 31/7088
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
A61K 31/7105
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
7105Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 31/713
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
713Double-stranded nucleic acids or oligonucleotides
A61K 45/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
A61K 47/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
16containing nitrogen, ; e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
A61K 47/20
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
20containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
Applicants
  • 厦门赛诺邦格生物科技股份有限公司 XIAMEN SINOPEG BIOTECH CO., LTD [CN]/[CN]
Inventors
  • 翁文桂 WENG, Wengui
  • 刘超 LIU, Chao
  • 王爱兰 WANG, Ailan
  • 林聪明 LIN, Congming
  • 王琳琳 WANG, Linlin
Priority Data
202110379685.508.04.2021CN
202110780188.609.07.2021CN
202110839008.723.07.2021CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PEGYLATED LIPID, LIPOSOME MODIFIED THEREBY, PHARMACEUTICAL COMPOSITION CONTAINING LIPOSOME, PREPARATION THEREOF, AND USE THEREOF
(FR) LIPIDE PEGYLÉ, LIPOSOME AINSI MODIFIÉ, COMPOSITION PHARMACEUTIQUE CONTENANT UN LIPOSOME, PRÉPARATION ET UTILISATION ASSOCIÉES
(ZH) 一种聚乙二醇化脂质及其修饰的脂质体、含该脂质体的药物组合物及其制剂和应用
Abstract
(EN) Disclosed in the present invention are a pegylated lipid, a preparation method therefor, a liposome containing the pegylated lipid, a pharmaceutical composition containing the liposome, a preparation thereof, and the use thereof, belonging to the field of drug delivery. The pegylated lipid of the present invention can be used for modifying a liposome, and the pegylated lipid can also be further modified and coupled with a targeting group and then used for modifying a liposome to obtain a liposome having the targeting group. Due to the presence of a long-chain PEG and the targeting group on the pegylated lipid, the modified liposome can not only effectively avoid being removed by the reticuloendothelial system in a human body, but can also realize a targeting function. Therefore, when the pegylated lipid-modified liposome delivers an active drug to cells or a patient, especially when delivering a nucleic acid drug and anti-tumor drug, the liposome can not only realize long circulation in vivo and improve a drug transportation rate, but also has a targeting function, so that the therapeutic effect of a drug is improved under a synergistic effect.
(FR) La présente invention concerne un lipide pegylé, son procédé de préparation, un liposome contenant le lipide pegylé, une composition pharmaceutique contenant le liposome, une préparation et une utilisation associées, appartenant au domaine de l'administration de médicament. Le lipide pegylé selon la présente invention peut être utilisé pour modifier un liposome, et le lipide pegylé peut également être encore modifié et couplé à un groupe de ciblage et ensuite utilisé pour modifier un liposome afin d'obtenir un liposome ayant le groupe de ciblage. Du fait de la présence d'un PEG à longue chaîne et du groupe de ciblage sur le lipide pegylé, le liposome modifié peut non seulement éviter efficacement d'être éliminé par le système réticulo-endothélial dans un corps humain, mais peut également réaliser une fonction de ciblage. Par conséquent, lorsque le liposome modifié par un lipide pegylé délivre un médicament actif à des cellules ou à un patient, en particulier lors de l'administration d'un médicament à base d'acide nucléique et d'un médicament antitumoral, le liposome peut non seulement réaliser une longue circulation in vivo et améliorer un taux de transport de médicament, mais a également une fonction de ciblage, de telle sorte que l'effet thérapeutique d'un médicament est amélioré sous un effet synergique.
(ZH) 本发明公开了一种聚乙二醇化脂质及其制备方法、含该聚乙二醇化脂质的脂质体、含该脂质体的药物组合物及其制剂和应用,属于药物递送领域。本发明的聚乙二醇化脂质可以用于修饰脂质体,也可以将聚乙二醇化脂质进一步修饰偶联上靶向基团再用于修饰脂质体得到带有靶向基团的脂质体。由于聚乙二醇化脂质上的长链PEG和靶向基团的存在,所修饰的脂质体不仅可以有效避免人体内网状内皮系统对脂质体的清除,还可以实现靶向功能。因此,在聚乙二醇化脂质修饰的脂质体将活性药物递送至细胞或患者中时,尤其是递送核酸类药物和抗肿瘤药物时,脂质体在体内不仅可以实现长循环,提高药物转运率,还兼具靶向功能,协同作用下提高药物的治疗效果。
Latest bibliographic data on file with the International Bureau