公开(公告)号：EP3476841A1

公开(公告)日：2019-05-01

申请号：EP17814745.0

申请日：2017-06-23

申请人： Chia Tai Tianqing Pharmaceutical Group Co., Ltd. ,  Lianyungang Runzhong Pharmaceutical Co., Ltd. ,  Centaurus BioPharma Co., Ltd.

发明人： ZHU, Yizhong ,  TANG, Jianqiu ,  LIU, Fei ,  ZHANG, Xiquan ,  GU, Hongmei ,  ZHU, Bo ,  WANG, Lulu ,  TANG, Song ,  ZHANG, Yanyang

IPC分类号： C07D403/04 ,  A61K31/506 ,  A61P35/00 ,  A61P35/02

摘要： The present application belongs to the field of medicinal chemistry, and relates to crystals of an aniline pyrimidine compound serving as an EGFR inhibitor. Specifically, the present application relates to crystal A, crystal B and crystal C of N-(2-((2-(dimethyl amino)ethyl)(methyl)amino)-4-methoxy-5-(4-(3-methyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazole-1-base)pyrimidine-2-base amino)phenyl)acrylamide (formula I) hydrochloride, and also relates to the method for preparing the crystal A, the crystal B and the crystal C, a crystal composition comprising the crystal A, the crystal B, and the crystal C, a pharmaceutical composition comprising the crystal A, the crystal B and the crystal C or the crystal composition thereof, and medical uses thereof. The crystal A, the crystal B and the crystal C in the present application has the advantages of high purity, high crystallization degree, good stability and the like.

公开(公告)号：EP3178821A1

公开(公告)日：2017-06-14

申请号：EP15830563.1

申请日：2015-08-05

申请人： Chia Tai Tianqing Pharmaceutical Group Co.,Ltd ,  Centaurus BioPharma Co., Ltd.

发明人： WANG, Lulu ,  ZHANG, Xiquan ,  LIU, Fei ,  ZHU, Yizhong ,  GAO, Chao ,  TANG, Song ,  ZHU, Bo ,  TANG, Jianqiu

IPC分类号： C07D491/048 ,  A61K31/4355 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D491/048 ,  A61K31/4355 ,  C07B2200/13

摘要： Provided are 6-aryl amino pyridone formamide compound crystal and a preparation method therefor. In the present invention, 6-(2-chlorine-4-iodopheny amino)-N-(2-hydroxyl ethyoxyl)-5-methyl-4-oxo-4,5-dihydrofuran[3,2-c]pyridine-7-formamide is dissolved in a polar aprotic solvent, a second solvent is added for recrystallization, and a crystal is obtained. The crystallization method is simple to operate and conducive for industrial production. The produced crystal has high purity, good stability, and is conductive for pharmaceutical production and storage.

摘要翻译： 本发明提供6-芳基氨基吡啶酮甲酰胺化合物结晶及其制备方法。 在本发明中，6-（2-氯-4-氨基iodopheny）-N-（2-羟基ethyoxyl）-5-甲基-4-氧代-4,5-二氢呋喃并[3,2-c]吡啶-7- - 甲酰胺溶于极性非质子溶剂中，加入第二溶剂进行重结晶，得到晶体。 结晶方法操作简单，有利于工业生产。 所生产的晶体纯度高，稳定性好，对药物生产和储存具有导电性。

公开(公告)号：EP3178821B1

公开(公告)日：2020-05-06

申请号：EP15830563.1

申请日：2015-08-05

申请人： Chia Tai Tianqing Pharmaceutical Group Co.,Ltd ,  Centaurus BioPharma Co., Ltd.

发明人： WANG, Lulu ,  ZHANG, Xiquan ,  LIU, Fei ,  ZHU, Yizhong ,  GAO, Chao ,  TANG, Song ,  ZHU, Bo ,  TANG, Jianqiu

IPC分类号： C07D491/048 ,  A61K31/4355 ,  A61P35/00 ,  A61P29/00

公开(公告)号：EP3498690A1

公开(公告)日：2019-06-19

申请号：EP17838795.7

申请日：2017-08-11

申请人： Chia Tai Tianqing Pharmaceutical Group Co., Ltd. ,  Centaurus BioPharma Co., Ltd.

发明人： WANG, Lulu ,  LIU, Fei ,  ZHU, Yizhong ,  ZHANG, Hongying

IPC分类号： C07C335/32 ,  C07D491/048

摘要： Provided is a method for preparing an intermediate of 6-arylaminopyridonecarboxamide compound as an MEK inhibitor, comprising preparing a compound of formula (III) as an intermediate of 6-arylaminopyridonecarboxamide compound using a compound of formula V as a raw material.