POLYCRYSTALLINE FORM OF FREE BASE OR ACID ADDITION SALT OF INHIBITOR EGFR, METHOD OF ITS PRODUCTION AND APPLICATION Russian patent published in 2020 - IPC C07D403/04 A61K31/506 A61P35/00 

Abstract RU 2733412 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to polymorph of N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide (compound of formula I) in form of mesylate salt, selected from a group consisting of crystalline form I–VI of mesylate salt, wherein said crystalline forms are characterized by X-ray powder diffraction patterns such as given in the claim. Invention also relates to a method of producing crystalline forms of I–VI mesylate salt of a compound of formula I and use thereof.

EFFECT: technical result is crystalline forms of I–VI mesylate salt N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide, having improved physical and chemical properties, such as degree of crystallinity, solubility, hygroscopicity and chemical stability, and suitable for preparing a drug for treating a disease mediated by EGFR mutant activity or a deletion-activated mutant in exon 19.

12 cl, 22 tbl, 22 ex, 22 dwg

Similar patents RU2733412C2

Title Year Author Number
POLYMORPHOUS AND AMORPHOUS FORMS OF 8-FLUORO-2-{4-[(METHYLAMINO)METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINE[5,4,3-CD]INDOL-6-ON PHOSPHATE 2005
  • Liu Dzhia
  • Najjar Naresh
  • Guo Ming
  • Vu Zhen-Ping
  • Borer Bennett Shaplin
  • Shrirangam Aparna Nadig
  • Mitchell Mark Brajan
  • Li Ji
  • Chu Dzhan-Dzhon
RU2355691C2
AMINE SOLVATE OF SODIUM GLUCOSE OPENER OF SODIUM GLUCOSE OPENER AND METHOD FOR PRODUCTION THEREOF AND USE THEREOF 2017
  • Zhang Lei
  • Wang Yuan
RU2710230C1
LONG-ACTING DPP-IV INHIBITOR CRYSTAL AND ITS SALTS 2017
  • Sang Guangming
  • Liu Lin
  • Zhang Aiming
  • Qiao Jiabin
  • Guo Xiaopeng
  • Zhang Xiquan
  • Xia Chunguang
RU2753335C2
CRYSTALLINE FORM OF COMPOUND SUPPRESSING PROTEIN KINASE ACTIVITY AND THE USE THEREOF 2017
  • Lyan, Tsunsin
  • Ma, Yunbin
  • Khe, Vej
RU2744264C2
POLYMORPHIC FORMS OF ICOTINIB AND USES THEREOF 2014
  • Hu, Shaojing
  • Long, Wei
  • Wang, Fei
  • Wang, Yinxiang
  • Ding, Lieming
RU2710013C2
QUINAZOLINE INHIBITORS OF ACTIVATING MUTANT FORMS OF EPIDERMAL GROWTH FACTOR RECEPTOR 2014
  • Li David Yunzhi
  • Wang Jiabing
  • Yang Zhenfan
  • Zeng Qingbei
  • Zhang Xiaolin
RU2656597C2
POLYMORPHOUS FORMS OF ICOTINIB MALEATE AND USES THEREOF 2014
  • Hu, Shaojing
  • Long, Wei
  • Wang, Fei
  • Wang, Yinxiang
  • Ding, Lieming
RU2708079C2
DIARYLTHIOHYDANTOIN COMPOUND CRYSTAL 2020
  • Shen Chunli
  • Chen Shenglin
  • Wang Ting
  • Liu Fei
  • Tian Xin
  • Guo Yuying
  • Zhang Lin
  • Wu Jiahu
RU2810214C2
NOVEL POLYMORPHIC FORMS OF ICOTINIB PHOSPHATE AND USES THEREOF 2014
  • Hu, Shaojing
  • Long, Wei
  • Wang, Fei
  • Wang, Yinxiang
  • Ding, Lieming
RU2712169C2
SALT AND POLYMORPH OF A PHENYL-PYRIMIDONE COMPOUND, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF 2018
  • Shen, Jingshan
  • He, Yang
  • Chen, Weiming
  • Li, Jianfeng
  • Tian, Guanghui
  • Gong, Xudong
  • Wang, Zhen
  • Zhang, Rongxia
  • Liu, Yongjian
  • Jiang, Hualiang
RU2761213C2

RU 2 733 412 C2

Authors

Chen Chzhunke

Lyu Fupin

Lyu Lej

Bao Rudi

Dates

2020-10-01Published

2016-12-23Filed