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1. WO2022000265 - COCRYSTALS OF AXITINIB AND GLUTARIC ACID, AND PREPARATION METHOD THEREFOR

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Publication Number WO/2022/000265
Publication Date 06.01.2022
International Application No. PCT/CN2020/099269
International Filing Date 30.06.2020
IPC
C07D 401/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/4439 2006.1
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 31/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
CPC
A61K 31/4439
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 401/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • 天津理工大学 TIANJIN UNIVERSITY OF TECHNOLOGY [CN]/[CN]
Inventors
  • 陈嘉媚 CHEN, Jiamei
  • 任伯颖 REN, Boying
Agents
  • 广州嘉权专利商标事务所有限公司 JIAQUAN IP LAW
Priority Data
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) COCRYSTALS OF AXITINIB AND GLUTARIC ACID, AND PREPARATION METHOD THEREFOR
(FR) COCRISTAUX D'AXITINIB ET D'ACIDE GLUTARIQUE, ET LEUR PROCÉDÉ DE PRÉPARATION
(ZH) 一种阿西替尼与戊二酸共晶及其制备方法
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Abstract
(EN) Disclosed in the present invention are cocrystals of axitinib and glutaric acid, and a preparation method therefor. In the cocrystals of axitinib and glutaric acid, the molar ratio of axitinib to glutaric acid is 1:1. The preparation method of the cocrystals of axitinib and glutaric acid features simple technology, an easy-control crystallization process, and good reproducibility, and is suitable for industrial production. Compared with axitinib, the cocrystals of axitinib and glutaric acid have a greater apparent solubility and a faster dissolution rate, and facilitate improving the oral bioavailability of axitinib.
(FR) La présente invention concerne des cocristaux d'axitinib et d'acide glutarique, et leur procédé de préparation. Dans les cocristaux d'axitinib et d'acide glutarique, le rapport molaire entre l'axitinib et l'acide glutarique est de 1 : 1. Le procédé de préparation des co-cristaux d'axitinib et d'acide glutarique a une technologie simple, un procédé de cristallisation facile à commander et une bonne reproductibilité, et est approprié pour une production industrielle. Les co-cristaux d'axitinib et d'acide glutarique, par comparaison avec l'axitinib, ont une solubilité apparente supérieure et une vitesse de dissolution plus rapide, et facilitent l'amélioration de la biodisponibilité orale d'axitinib.
(ZH) 本发明公开了一种阿西替尼与戊二酸共晶及其制备方法。这种阿西替尼与戊二酸共晶中，阿西替尼与戊二酸的摩尔比为1:1。这种阿西替尼与戊二酸共晶的制备方法工艺简单，结晶过程易于控制，重现性好，适用于工业化生产。该阿西替尼与戊二酸共晶较阿昔替尼具有较大的表观溶解度和较快的溶出速率，有利于提高阿昔替尼的口服生物利用度。
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