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1. WO2020090971 - TABLET CONTAINING ANTITUMOR AGENT

Publication Number WO/2020/090971
Publication Date 07.05.2020
International Application No. PCT/JP2019/042751
International Filing Date 31.10.2019
IPC
A61K 31/505 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
A61K 9/20 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, lozenges or tablets
A61K 47/12 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
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
08containing oxygen
12Carboxylic acids; Salts or anhydrides thereof
A61K 47/26 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
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/32 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
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • 富士フイルム株式会社 FUJIFILM CORPORATION [JP]/[JP]
Inventors
  • 大浦 泰 OURA Tai
Agents
  • 特許業務法人特許事務所サイクス SIKs & Co.
Priority Data
2018-20485231.10.2018JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) TABLET CONTAINING ANTITUMOR AGENT
(FR) COMPRIMÉ CONTENANT UN AGENT ANTITUMORAL
(JA) 抗腫瘍剤を含む錠剤
Abstract
(EN)
The purpose of the present invention is to provide a tablet which contains succinate of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidine-5-yl)pent-4-yne-1-yl)amino)-1-oxopropane-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide (compound A) which elutes quickly in a weakly acidic test solution. With the present invention, a pharmaceutical composition which contains succinate of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidine-5-yl)pent-4-yne-1-yl)amino)-1-oxopropane-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide (compound A), at least one item selected from a group consisting of sugars and sugar alcohols, and crospovidone is provided.
(FR)
La présente invention a pour objet de fournir un comprimé qui contient du succinate de (S,E)-N-(1-((5-(2-((4-cyanophényl)amino)-4-(propylamino)pyrimidine-5-yl)pent-4-yne-1-yl)amino)-1-oxopropane-2-yl)-4-(diméthylamino)-N-méthylbut-2-énamide (composé A) qui est élué rapidement dans une solution d'essai faiblement acide. La présente invention concerne une composition pharmaceutique qui contient du succinate de (S,E)-N-(1-((5-(2-((4-cyanophényl)amino)-4-(propylamino)pyrimidine-5-yl)pent-4-yne-1-yl)amino)-1-oxopropane-2-yl)-4-(diméthylamino)-N-méthylbut-2-énamide (composé A), au moins un élément sélectionné dans un groupe constitué de sucres et d'alcools de sucre, et de la crospovidone.
(JA)
本発明の課題は、バイオアベイラビィテイの低下を防ぐため、弱酸性溶液において速やかに溶出する(S,E)-N-(1-((5-(2-((4-シアノフェニル)アミノ)-4-(プロピルアミノ)ピリミジン-5-イル)ペント-4-イン-1-イル)アミノ)-1-オキソプロパン-2-イル)-4-(ジメチルアミノ)-N-メチルブト-2-エンアミド(化合物A)のコハク酸塩を含有する錠剤を提供することである。本発明によれば、(S,E)-N-(1-((5-(2-((4-シアノフェニル)アミノ)-4-(プロピルアミノ)ピリミジン-5-イル)ペント-4-イン-1-イル)アミノ)-1-オキソプロパン-2-イル)-4-(ジメチルアミノ)-N-メチルブト-2-エンアミド(化合物A)のコハク酸塩、糖類及び糖アルコールからなる群より少なくとも1種以上並びにクロスポビドンを含有する錠剤が提供される。
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