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1. WO2018136002 - HYPERSTABILIZED LIPOSOMES INCREASE TARGETING OF MITOTIC CELLS

Publication Number WO/2018/136002
Publication Date 26.07.2018
International Application No. PCT/SG2018/050026
International Filing Date 17.01.2018
IPC
A61K 9/127 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
127Liposomes
A61K 31/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
A61K 47/00 2006.01
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
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/517
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
517ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 47/02
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
02Inorganic compounds
A61K 47/12
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
08containing oxygen, ; e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
12Carboxylic acids; Salts or anhydrides thereof
A61K 9/1271
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
127Liposomes
1271Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
A61K 9/1278
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
127Liposomes
1277Processes for preparing; Proliposomes
1278Post-loading, e.g. by ion or pH gradient
Applicants
  • TEMASEK LIFE SCIENCES LABORATORY LIMITED [SG]/[SG]
Inventors
  • NG, Chang Zhi Adrian
  • CHEONG, Shen-Yi Ian
Agents
  • MATTEUCCI, Gianfranco
Priority Data
62/447,49818.01.2017US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) HYPERSTABILIZED LIPOSOMES INCREASE TARGETING OF MITOTIC CELLS
(FR) LIPOSOMES HYPERSTABILISÉS AUGMENTANT LE CIBLAGE DE CELLULES MITOTIQUES
Abstract
(EN)
Hyperstable liposome comprising an anti-mitotic agent, one or more anions and one or more cations entrapped in the inner milieu, wherein the entrapped anti-mitotic drug is released at a slow rate that is less than 0.6% in 12 hours or less than 5% in 8 hours when the liposomes are suspended in 600mM sucrose. These liposomes are useful in the treatment of cancer. In particular, HEPC:Chol:DSPE-PEG2000 (50:45:5) liposomes comprising BI 2536 and citrate:phosphate in a ratio of 1 :3.
(FR)
L'invention concerne un liposome hyperstable qui comprend un agent antimitotique, un ou plusieurs anions et un ou plusieurs cations piégés dans le milieu interne, le médicament antimitotique piégé étant libéré à une vitesse lente qui est inférieure à 0,6 % en 12 heures ou inférieure à 5 % en 8 heures lorsque les liposomes sont en suspension dans du saccharose à 600 mM. Ces liposomes sont utiles dans le traitement du cancer. Il s'agit en particulier des liposomes HEPC:Chol:DSPE-PEG2000 (50:45:5) comprenant du BI 2536 et un rapport citrate:phosphate de 1:3.
Latest bibliographic data on file with the International Bureau