公开(公告)号：US10059688B2

公开(公告)日：2018-08-28

申请号：US15694620

申请日：2017-09-01

Applicant: BETTA PHARMACEUTICALS CO., LTD.

Inventor： Shaojing Hu ,  Xiangyong Liu ,  Jinlong Bai ,  Wei Long

IPC: A61K31/33 ,  C07D401/12 ,  C07D239/48 ,  C07D405/12 ,  C07D403/12 ,  C07D401/14 ,  C07D413/12 ,  A61K31/495 ,  A61K31/395

CPC classification number: C07D401/12 ,  A61K31/33 ,  A61K31/395 ,  A61K31/495 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

Abstract: Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.

公开(公告)号：US20220259235A1

公开(公告)日：2022-08-18

申请号：US17629976

申请日：2020-07-23

Applicant: BETTA PHARMACEUTICALS CO., LTD

Inventor： Xiangyong Liu ,  Changyong Qiu ,  Qichao Shen ,  Mengqiang Liu ,  Haitong Sheng ,  Xiaodong Song ,  Guolong Du ,  Jiabing Wang ,  Lieming Ding

IPC: C07F9/6558 ,  A61P35/00 ,  C07F9/6561

Abstract: The present invention relates to compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

公开(公告)号：US20160145237A1

公开(公告)日：2016-05-26

申请号：US14903369

申请日：2014-07-11

Applicant: BETTA PHARMACEUTICALS CO., LTD

Inventor： Shaojing Hu ,  Xiangyong Liu ,  Jinlong Bai ,  Wei Long

IPC: C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D239/48

CPC classification number: C07D401/12 ,  A61K31/33 ,  A61K31/395 ,  A61K31/495 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

Abstract: Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.

Abstract translation: 公开了调节突变型选择性表皮生长因子受体（EGFR）和ALK激酶活性的杂环嘧啶化合物。 更具体地，本发明提供了抑制，调节和/或调节激酶受体的嘧啶，特别是在选择性调节各种EGFR突变体活性和ALK激酶活性方面。 公开了包含嘧啶衍生物的药物组合物和与蛋白激酶酶活性相关的疾病的治疗方法，特别是EGFR或ALK激酶活性，包括给予嘧啶衍生物的非小细胞肺癌。

公开(公告)号：US09783524B2

公开(公告)日：2017-10-10

申请号：US14903369

申请日：2014-07-11

Applicant: BETTA PHARMACEUTICALS CO., LTD.

Inventor： Shaojing Hu ,  Xiangyong Liu ,  Jinlong Bai ,  Wei Long

IPC: C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D239/48 ,  C07D403/12 ,  C07D413/12

CPC classification number: C07D401/12 ,  A61K31/33 ,  A61K31/395 ,  A61K31/495 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

Abstract: Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.

公开(公告)号：US12275737B2

公开(公告)日：2025-04-15

申请号：US17594104

申请日：2020-04-01

Applicant: Meryx, Inc. ,  The University of North Carolina at Chapel Hill ,  Betta Pharmaceuticals Co., Ltd

Inventor： Xiaodong Wang ,  Weihe Zhang ,  Xiangyong Liu ,  Changlong Han ,  Zongquan Li

IPC: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02

Abstract: The invention relates to new crystal forms of compound (trans)-4-((2-cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl) cyclohexanol trihydrochloride, its hydrate, or solvate, as shown in Formula I. The invention also relates to methods for preparation of the described compound, crystal form, and related intermediate compounds, as well as pharmaceutical compositions containing the compounds. Further described is, the use of the compounds or crystal forms in the production of a medicament for the treatment of a disease, symptom, or condition, or the use in treatment of a disease, symptom or condition.

公开(公告)号：US20250051301A1

公开(公告)日：2025-02-13

申请号：US18847130

申请日：2023-03-14

Applicant: Betta Pharmaceuticals Co., Ltd

Inventor： Yabin Li ,  Xiaofeng Xu ,  Xizhen Song ,  Jingwei Ding ,  Yunlai Zhang ,  Jie Chen ,  Xiangyong Liu ,  Lieming Ding ,  Jiabing Wang

IPC: C07D401/04 ,  A61K31/53

Abstract: Disclosed are a compound represented by formula (I) as a mutant isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) inhibitor, a preparation method therefor, and a pharmaceutical composition thereof. Also disclosed is a use of the described compound or the pharmaceutical composition thereof in the treatment of mutant IDH1 and IDH2-mediated diseases.

公开(公告)号：US11365196B2

公开(公告)日：2022-06-21

申请号：US16488899

申请日：2018-02-27

Applicant: Betta Pharmaceuticals Co., Ltd.

Inventor： Xiaofeng Xu ,  Jiabing Wang ,  Lieming Ding ,  Xiangyong Liu

IPC: C07D471/14 ,  A61K31/519 ,  A61P35/00 ,  C07D519/00

Abstract: An azatricyclic compound (as represented by Formula I) which acts as an inhibitor of fibroblast growth factor receptors (FGFR), as well as a pharmaceutical composition thereof, a preparation method, and a use therefor in the treatment of FGFR-mediated diseases are provided. The azatricyclic compound exerts an effect by means of participating in the regulation of a plurality of processes such as cell proliferation, apoptosis, migration, neovascularization, and the like.

公开(公告)号：US20180009782A1

公开(公告)日：2018-01-11

申请号：US15694620

申请日：2017-09-01

Applicant: BETTA PHARMACEUTICALS CO., LTD.

Inventor： Shaojing HU ,  Xiangyong Liu ,  Jinlong Bai ,  Wei Long

IPC: C07D401/12 ,  C07D403/12 ,  C07D239/48 ,  C07D401/14 ,  C07D413/12 ,  C07D405/12

CPC classification number: C07D401/12 ,  A61K31/33 ,  A61K31/395 ,  A61K31/495 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

Abstract: Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.