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公开(公告)号：US10351536B2
公开(公告)日：2019-07-16
申请号：US15038470
申请日：2014-11-20
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.
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公开(公告)号：US12091414B2
公开(公告)日：2024-09-17
申请号：US17427357
申请日：2020-05-08
IPC分类号： C07D487/14
CPC分类号： C07D487/14 , C07B2200/13
摘要： The present application provides a upadacitinib salt compound and a preparation method therefor. The salt involved in the method in the present application has an easy preparation operation, a cheap raw material easy to get, and a good purification effect on upadacitinib, and is beneficial to industrial production.
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公开(公告)号：US20210323971A1
公开(公告)日：2021-10-21
申请号：US17272369
申请日：2019-08-26
IPC分类号： C07D487/14 , C07D207/16 , C07D207/08 , C07D241/20 , C07D487/04
摘要： The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III), wherein, R is a protective group of nitrogen atoms, and R1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.
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公开(公告)号：US11673862B2
公开(公告)日：2023-06-13
申请号：US16256596
申请日：2019-01-24
发明人： Peng Wang , Pixu Li , Qiang Wei , Yuanhua Liu
IPC分类号： C07D207/27 , A61K31/4015 , C07C53/19 , C07C53/50 , C07C67/307 , C07C69/63 , C07C71/00 , C07C209/08 , C07C231/14 , C07C233/05 , C07C237/06
CPC分类号： C07D207/27 , A61K31/4015 , C07C53/19 , C07C53/50 , C07C67/307 , C07C69/63 , C07C71/00 , C07C209/08 , C07C231/14 , C07C233/05 , C07C237/06
摘要： The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.
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公开(公告)号：US20210253567A1
公开(公告)日：2021-08-19
申请号：US17253498
申请日：2019-08-13
发明人： Peng WANG , Pixu LI , Qiang WEI , Dingquan LIU , Hao WU , He CHEN , Wenhui YAO
IPC分类号： C07D455/06
摘要： The present invention relates to amorphous and crystalline forms of valbenazine salt and the methods for their preparation.
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公开(公告)号：US09969701B2
公开(公告)日：2018-05-15
申请号：US15106361
申请日：2014-12-19
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.
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公开(公告)号：US20160297778A1
公开(公告)日：2016-10-13
申请号：US15038470
申请日：2014-11-20
发明人： Minhua CHEN , Yanfeng ZHANG , Chaohui YANG , Xiaoyu ZHANG , Peng WANG , Pixu LI
IPC分类号： C07D249/12
CPC分类号： C07D249/12 , C07B2200/13
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.
摘要翻译： 新型结晶形式的维兰定和其钠盐，其制备方法，包含这些新形式的药物组合物及其用于治疗或延缓与尿酸转运蛋白1（URAT1）蛋白的活性相关的疾病或病症的进展或发作的用途是 披露 这些新颖的形式通过X射线粉末衍射，差示扫描量热法等技术表征。 它们可以容易地制备并且由于其易于处理和优异的药理性质而适合制备固体剂型。
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公开(公告)号：US11161851B2
公开(公告)日：2021-11-02
申请号：US16762122
申请日：2018-11-05
发明人： Peng Wang , Pixu Li , Xiangyong Gu , Yadong Ge , Zhong Wang , Feng Gao , Qiangqiang Du
IPC分类号： C07D471/02 , C07D471/04 , C07D487/04 , C07D213/75 , C07D403/12 , C07F5/02
摘要： The present invention relates to a method for preparing the compound of formula IV, compound of formula XI, and acalabrutinib, a new generation of bruton tyrosine kinase (BTK) inhibitor.
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公开(公告)号：US09751889B2
公开(公告)日：2017-09-05
申请号：US15100247
申请日：2014-11-26
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.
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公开(公告)号：US20170002009A1
公开(公告)日：2017-01-05
申请号：US15100247
申请日：2014-11-26
发明人： Minhua CHEN , Yanfeng ZHANG , Chaohui YANG , Xiaoyu ZHANG , Peng WANG , Pixu LI , Fei LU , Heng GE
IPC分类号： 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.
摘要翻译： 公开了伊布他尼的结晶形式I，其制备方法，包含新形式的药物组合物以及伊布他他啶的I型用于治疗或延迟与布鲁顿酪氨酸激酶（BTK）蛋白的活性相关的疾病或病症的用途。 通过X射线粉末衍射，差示扫描量热法和其他技术对新型形态进行了表征。 它可以容易地制备并且适用于制备固体剂型。
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