公开(公告)号：US10351536B2

公开(公告)日：2019-07-16

申请号：US15038470

申请日：2014-11-20

申请人： CRYSTAL PHARMATECH CO., LTD. ,  SUZHOU PENGXU PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Chaohui Yang ,  Xiaoyu Zhang ,  Peng Wang ,  Pixu Li

IPC分类号： C07D249/12

摘要： Novel crystalline forms of lesinurad and its sodium salt, processes for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transporter 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.

公开(公告)号：US09969701B2

公开(公告)日：2018-05-15

申请号：US15106361

申请日：2014-12-19

申请人： CRYSTAL PHARMATECH, INC. ,  CRYSTAL PHARMATECH CO., LTD. ,  SUZHOU PENGXU PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Chaohui Yang ,  Xiaoyu Zhang ,  Peng Wang ,  Pixu Li

IPC分类号： C07D249/12 ,  C07C59/06 ,  C07D207/16

CPC分类号： C07D249/12 ,  C07B2200/13 ,  C07C59/06 ,  C07D207/16

摘要： Novel salts and cocrystals of lesinurad, processes for their preparation, pharmaceutical compositions comprising these new salt forms and co-crystals, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transport 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.

公开(公告)号：US09957240B2

公开(公告)日：2018-05-01

申请号：US15528153

申请日：2015-12-08

申请人： CRYSTAL PHARMATECH CO., LTD ,  SUZHOU PENGXU PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Chaohui Yang ,  Xiaoyu Zhang ,  Jiaoyang Li ,  Peng Wang ,  Pixu Li

IPC分类号： C07D257/04

CPC分类号： C07D257/04 ,  A61K31/225 ,  A61K31/41 ,  C07B2200/13 ,  C07C233/47 ,  A61K2300/00

摘要： Novel crystalline Forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3′-methyl-T-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.

公开(公告)号：US09751889B2

公开(公告)日：2017-09-05

申请号：US15100247

申请日：2014-11-26

申请人： CRYSTAL PHARMATECH INC. ,  SUZHOU PENGXU PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Chaohui Yang ,  Xiaoyu Zhang ,  Peng Wang ,  Pixu Li ,  Fei Lu ,  Heng Ge

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04

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

摘要： Crystalline Form I of ibrutinib, processes for its preparation, pharmaceutical compositions comprising the new Form, and use of Form I of ibrutinib for treating or delaying diseases or disorders related to activity of Bruton's tyrosine kinase (BTK) proteins are disclosed. The novel Form was characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. It can be readily prepared and is suitable for use in the preparation of solid dosage forms.

公开(公告)号：US10266523B2

公开(公告)日：2019-04-23

申请号：US15579881

申请日：2016-03-30

申请人： CRYSTAL PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Fei Lu ,  Xiaoyu Zhang

IPC分类号： A61K31/5377 ,  C07D413/04 ,  A61P35/00

摘要： The present disclosure relates to novel crystalline forms of N-[6-(cis-2,6-dimethylmorpholine-4-yl)pyridine-3-yl]-2-methyl-4′-(trifluoromethoxy) [1,1′-biphenyl]-3-carboxamide monophosphate, and process of preparation thereof. The crystalline form of the monophosphate of a compound of formula (I) has low hygroscopicity, is convenient to store, has better stability than that of diphosphonate in prior art, can avoid the risk of crystal transformation in the development and production of the drug. The preparation method is simple, has low cost, and has important value for further optimization and development of the drug.

公开(公告)号：US10246437B2

公开(公告)日：2019-04-02

申请号：US15542597

申请日：2016-01-08

申请人： CRYSTAL PHARMATECH CO., LTD

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

IPC分类号： C07D401/12 ,  A61K31/4709 ,  C07C51/41 ,  C07C51/43 ,  C07C57/145

摘要： The present invention relates to novel crystalline forms of Neratinib maleate and the preparation method thereof. The novel crystalline forms of Neratinib maleate in the present invention have high solubility, good stability, good processability, easy post-treatment process and other favorable properties. The preparation method is simple, low cost, and has an important value for future optimization and development of the drug.

公开(公告)号：US20190322646A1

公开(公告)日：2019-10-24

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.

公开(公告)号：US10308641B2

公开(公告)日：2019-06-04

申请号：US15751205

申请日：2016-08-11

申请人： CRYSTAL PHARMATECH CO., LTD.

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

IPC分类号： C07D405/12 ,  A61K31/443 ,  A61K31/47 ,  A61P11/00

摘要： The present disclosure provides crystalline form A of 3-(6-(1-(2, 2-difluorobenzo [d] [1, 3] dioxo-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid and process of preparation thereof. The crystalline form A has low hygroscopicity, good stability, is convenient to store. It has higher solubility than that of prior art and therefore plays an important role in further optimization and development of the drug.

公开(公告)号：US20190092756A1

公开(公告)日：2019-03-28

申请号：US16082830

申请日：2017-03-08

申请人： Crystal Pharmatech Co., Ltd.

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

IPC分类号： C07D403/04 ,  A61P35/04

摘要： Provided are a crystalline form A of 2-[(2R)-2-methyl-2-pyrrolidyl]-1H-benzimidazole-7-carboxamide dihydrochloride and the preparation method and use thereof. The X-ray powder diffraction pattern of crystalline form A shows characteristic peaks at 2theta values of 8.3°±0.2°, 26.7°±0.2°, 16.1°±0.2°. Crystalline form A, compared with the existing crystalline forms, has a surprisingly excellent solubility, mechanical and storage stabilities and particle size distribution, is a more ideal crystalline fotbnn compared with the prior art forms, better satisfies medicinal requirements, and plays an important role in future optimization and development of the drug.

公开(公告)号：US10138239B2

公开(公告)日：2018-11-27

申请号：US15559777

申请日：2016-03-18

申请人： CRYSTAL PHARMATECH CO., LTD.

发明人： Minhua Chen ,  Yanfeng Zhang ,  Liang Zhang ,  Shulin Ji

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D211/32 ,  G01N23/20 ,  G01N25/48

摘要： A preparation method of PCI-32765 crystalline form A, which comprises the following steps: 1) dissolving free base of PCI-32765 in a good solvent; 2) the solution prepared by Step 1) is dropwise added into an anti-solvent, stirred and added seed crystal of PCI-32765 Form A; Or the solution prepared by Step 1) is dropwise added into the suspension containing seed crystal of PCI-32765 Form A; 3) solution obtained by step 2) is continuously stirred and aged until crystal transformation is completed, then the crystal slurry is obtained; 4) crystal slurry in step 3) is filtered, washed, and dried to obtain the powder of PCI-32765 Form A. The preparation method of crystalline Form A provided by the present disclosure is a simple process and can be easily controlled, scaled up stably and conducted reliably. The process has high yield, good impurity removing capacity and is environmentally friendly. In addition, Form A provided by the present disclosure can be stably stored, and the hygroscopicity and solubility of Form A meet the requirements for medicinal use.