公开(公告)号：US10323035B2

公开(公告)日：2019-06-18

申请号：US15563344

申请日：2016-04-01

申请人： CRYSTAL PHARMATECH CO., LTD

发明人： Minhua Chen ,  Yanfeng Zhang ,  Qiyue Liu ,  Nan Xia ,  Chaohui Yang ,  Xiaoyu Zhang

IPC分类号： C07D487/04 ,  A61K31/4184 ,  A61K31/519 ,  C07D235/06

摘要： The present disclosure relates to novel co-crystals of a CDK inhibitor and an MEK inhibitor and the preparation methods thereof. Specifically, the present disclosure provides hydrates or anhydrates which are named as Form I, Form II and Form III. The novel co-crystals provided in the present disclosure have good stability, low hygroscopicity and high solubility, and have an important value for further optimization and development of the drug.

公开(公告)号：US10233144B2

公开(公告)日：2019-03-19

申请号：US15559824

申请日：2016-03-18

申请人： CRYSTAL PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Chaohui Yang ,  Shu Yu ,  Xiaoyu Zhang ,  Liang Zhang

IPC分类号： A61K31/41 ,  A61K47/54 ,  A61K47/55 ,  A61K31/216 ,  C07C231/24 ,  C07C233/47 ,  C07C235/74 ,  C07D257/04

摘要： The present disclosure relates to a novel crystalline form of a compound of formula (I), preparation method and use thereof. The novel crystalline form in the present disclosure has good stability, low hygroscopicity, and remarkable purification effect in process. The novel crystalline form of the compound of formula (I) provided by the present disclosure can be used for the preparation of the drug for treating heart failure.

公开(公告)号：US10138250B2

公开(公告)日：2018-11-27

申请号：US15984900

申请日：2018-05-21

申请人： Crystal Pharmatech Co., Ltd.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Xiaoyu Zhang

IPC分类号： C07D487/04 ,  C07D401/14 ,  C07D403/14 ,  A61K31/519 ,  A61P35/00

摘要： The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide (compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.

公开(公告)号：US20180282342A1

公开(公告)日：2018-10-04

申请号：US15984900

申请日：2018-05-21

申请人： Crystal Pharmatech Co., Ltd.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Xiaoyu Zhang

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07B2200/13 ,  C07D401/14 ,  C07D403/14

摘要： The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide(compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.

公开(公告)号：US10562855B2

公开(公告)日：2020-02-18

申请号：US16364114

申请日：2019-03-25

申请人： CRYSTAL PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Xiaojuan Diao ,  Xiaoyu Zhang

IPC分类号： C07D215/48 ,  C07D215/233 ,  A61P35/00

摘要： The present disclosure relates to a novel crystalline form of lenvatinib mesylate and the preparation method thereof. The novel crystalline form of mesylate of the present disclosure can be used for treating invasive and differentiated thyroid cancer. The novel crystalline form of mesylate of the present disclosure has good solubility, stability, and remarkable purification effect in process. The preparation method of this novel crystalline form is simple, low cost, and has an important value for future optimization and development of the drug.

公开(公告)号：US10472369B2

公开(公告)日：2019-11-12

申请号：US16079764

申请日：2017-02-24

申请人： Crystal Pharmatech Co., Ltd.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Po Zou ,  Xiaoyu Zhang

IPC分类号： C07D487/04 ,  A61K31/5377

摘要： The present disclosure relates to novel crystalline form I, form II and form III of 6-(1H-indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]imidazo [1,2-a]pyrazin-8-amine mesylate, and preparation methods and use thereof. Crystalline form I is a dimesylate, and its X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 5.9°±0.2°, 13.5°±0.2° and 21.8°±0.2°. Crystalline form II is a dimesylate, and its X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 15.8°±±0.2°, 17.2°±0.2° and 19.5°±0.2°. Crystalline form III is a monomesylate, and its X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 7.4°±0.2°, 12.9°±0.2° and 19.2°±0.2°. The crystalline forms are more suitable for drug development than prior crystalline forms, and the preparation methods for the crystalline forms are simple and repeatable and have significant value for future drug optimization and development.

公开(公告)号：US10246418B2

公开(公告)日：2019-04-02

申请号：US15575352

申请日：2016-06-08

申请人： CRYSTAL PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Xiaojuan Diao ,  Xiaoyu Zhang

IPC分类号： C07D215/48 ,  A61K31/47 ,  A61P35/00 ,  C07C255/03

摘要： The present disclosure relates to a novel crystalline form of lenvatinib mesylate and the preparation method thereof. The novel crystalline form of mesylate of the present disclosure can be used for treating invasive and differentiated thyroid cancer. The novel crystalline form of mesylate of the present disclosure has good solubility, stability, and remarkable purification effect in process. The preparation method of this novel crystalline form is simple, low cost, and has an important value for future optimization and development of the drug.

公开(公告)号：US09994579B2

公开(公告)日：2018-06-12

申请号：US15535104

申请日：2015-12-11

申请人： Crystal Pharmatech Co., Ltd.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Kai Liu ,  Jiaoyang Li ,  Xiaoyu Zhang

IPC分类号： C07D487/04 ,  C07D403/14 ,  C07D401/14 ,  A61K31/519

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07B2200/13 ,  C07D401/14 ,  C07D403/14

摘要： The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-car boxylic acid dimethylamide(compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.

公开(公告)号：US20170342075A1

公开(公告)日：2017-11-30

申请号：US15535104

申请日：2015-12-11

申请人： Crystal Pharmatech Co., Ltd.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Kai Liu ,  Jiaoyang Li ,  Xiaoyu Zhang

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07B2200/13 ,  C07D401/14 ,  C07D403/14

摘要： The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-car boxylic acid dimethylamide(compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.

公开(公告)号：US10544129B2

公开(公告)日：2020-01-28

申请号：US16344443

申请日：2017-10-25

申请人： Crystal Pharmatech Co., Ltd.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Jinqiu Wang ,  Kai Liu ,  Xiaoyu Zhang

IPC分类号： C07D401/14

摘要： The present disclosure relates to two novel crystalline forms of AP26113 and processes for preparation thereof. The crystalline form CS1 and crystalline form CS2 of the present disclosure have advantages in solubility and stability, are suitable for development, and provide a better choice for preparation of pharmaceutical compositions containing AP26113, which is of great significance for drug development.