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1. WO2017016514 - PYRIDINE SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR CRYSTAL

Publication Number WO/2017/016514
Publication Date 02.02.2017
International Application No. PCT/CN2016/092269
International Filing Date 29.07.2016
IPC
C07D 401/14 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
14containing three or more hetero rings
A61K 31/496 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/496
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
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07D 401/14
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
14containing three or more hetero rings
Applicants
  • 正大天晴药业集团股份有限公司 CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. [CN]/[CN]
  • 连云港润众制药有限公司 LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD. [CN]/[CN]
  • 北京赛林泰医药技术有限公司 CENTAURUS BIOPHARMA CO., LTD. [CN]/[CN]
Inventors
  • 龚峰 GONG, Feng
  • 李新路 LI, Xinlu
  • 赵锐 ZHAO, Rui
  • 张喜全 ZHANG, Xiquan
  • 许新合 XU, Xinhe
  • 刘希杰 LIU, Xijie
  • 校登明 XIAO, Dengming
  • 韩永信 HAN, Yongxin
Agents
  • 北京三友知识产权代理有限公司 BEIJING SANYOU INTELLECTUAL PROPERTY AGENCY LTD.
Priority Data
201510458524.X30.07.2015CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PYRIDINE SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR CRYSTAL
(FR) CRYSTAL DE 2-AMINOPYRIDINE SUBSTITUÉ PAR LA PYRIDINE À ACTION INHIBITRICE DE PROTÉINE KINASES
(ZH) 吡啶取代的2-氨基吡啶类蛋白激酶抑制剂的结晶
Abstract
(EN)
Disclosed is a pyridine substituted 2-aminopyridine protein kinase inhibitor crystal, in particular relating to 5-((R)-1-(2,6-dichloro -3-fluorophenyl)ethoxyl)-4'-methoxyl-6'-((S)-2-methylpiperazin-1-yl)-3,3'-bipyridyl-6-amine citrate crystal, a preparation method thereof, a crystal composition and a pharmaceutical composition. Also disclosed is a use of a citrate crystal of a compound of formula I in diseases associated with protein kinases. The citrate crystal of the present invention is superior to 5-((R)-1-(2,6-dichloro -3-fluorophenyl)ethoxyl)-4'-methoxyl-6'-((S)-2-methylpiperazin-1-yl)-3,3'-bipyridyl-6-amine or other salts of 5-((R)-1-(2,6-dichloro -3-fluorophenyl)ethoxyl)-4'-methoxyl-6'-((S)-2-methylpiperazin-1-yl)-3,3'-bipyridyl-6-amine in at least one of bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation and the like.
(FR)
L'invention concerne un crystal de 2-aminopyridine substitué par la pyridine à action inhibitrice de protéine kinases, en particulier un crystal de 5-((R)-1-(2,6-dichloro-3-fluorophényl)éthoxyl)-4'-méthoxyl-6'-((S)-2-méthylpipérazine-1-yl)-3,3'-bipyridyl-6-amine citrate, une méthode de préparation de celui-ci, une composition à base de ce crystal et une composition pharmaceutique. L'invention concerne également une utilisation d'un cristal de citrate d'un composé de formule I dans des maladies associées à des protéine kinases. Le cristal de citrate de la présente invention est supérieur au 5-((R)-1-(2,6-dichloro-3-fluorophényl)éthoxyl)-4'-méthoxyl-6'-((S)-2-méthylpipérazine-1-yl)-3,3'-bipyridyl-6-amine ou autres sels du 5-((R)-1-(2,6-dichloro-3-fluorophényl)éthoxyl)-4'-méthoxyl-6'-((S)-2-méthylpipérazine-1-yl)-3,3'-bipyridyl-6-amine pour au moins l'une de ces caractéristiques : la biodisponibilité, l'hygroscopicité, la solubilité, la stabilité, la pureté, la facilité de préparation, et analogues.
(ZH)
本发明公开了吡啶取代的2-氨基吡啶类蛋白激酶抑制剂的结晶,具体涉及5-((R)-1-(2,6-二氯-3-氟苯基)乙氧基)-4'-甲氧基-6'-((S)-2-甲基哌嗪-1-基)-3,3'-联吡啶-6-胺的柠檬酸盐结晶、其制备方法、结晶组合物和药物组合物,还公开了式Ⅰ化合物柠檬酸盐结晶与蛋白激酶有关疾病的用途,本发明的柠檬酸盐结晶在生物利用度、吸湿性、稳定性、溶解性、纯度、易制备等至少一方面优于5-((R)-1-(2,6-二氯-3-氟苯基)乙氧基)-4'-甲氧基-6'-((S)-2-甲基哌嗪-1-基)-3,3'-联吡啶-6-胺或5-((R)-1-(2,6-二氯-3-氟苯基)乙氧基)-4'-甲氧基-6'-((S)-2-甲基哌嗪-1-基)-3,3'-联吡啶-6-胺的其它盐。
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