公开(公告)号：US20160251353A1

公开(公告)日：2016-09-01

申请号：US15150459

申请日：2016-05-10

申请人： Vertex Pharmaceuticals Incorporated

发明人： Kwame W. Nti-Addae ,  Michael Waldo ,  Simon Adam O'Neil ,  John Gregg Van Alsten ,  Dainius Macikenas ,  Praveen Mudunuri ,  Yi Shi ,  Mark Willem Ledeboer ,  Valdas Jurkauskas ,  Ales Medek ,  Steven Jones ,  Randal Byrn ,  Mohammed Asmal ,  Sarah Marie Robertson ,  Wanjung Tsai

IPC分类号： C07D471/04 ,  A61K45/06 ,  A61K31/4965 ,  A61K31/16 ,  A61K31/351 ,  A61K31/506 ,  C07C309/30

CPC分类号： C07D471/04 ,  A61K31/16 ,  A61K31/351 ,  A61K31/4965 ,  A61K31/506 ,  A61K45/06 ,  C07C309/30 ,  C07D403/04

摘要： Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: are Form A of HCl salt of Compound (1).½H2O, Form F of HCl salt of Compound (1).3H2O, Form D of HCl salt of Compound (1), Form A of Compound (1), and Form A of tosylate salt of Compound (1). Such polymorphic forms are employed for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.

摘要翻译： 化合物（1）的多晶型或其药学上可接受的盐，其中化合物（1）由以下结构式表示：化合物（1）的HCl盐的形式A。化合物（1）的HCl盐的形式F ）.3H 2 O，化合物（1）的HCl盐的形式D，化合物（1）的形式A和化合物（1）的甲苯磺酸盐的形式A. 这种多晶型用于治疗流感，抑制流感病毒的复制，或减少生物样品或受试者中流感病毒的数量。

公开(公告)号：US20200016181A1

公开(公告)日：2020-01-16

申请号：US16336195

申请日：2017-09-27

申请人： Vertex Pharmaceuticals Incorporated

发明人： Diane M. Boucher ,  Shawn M. Hillier ,  Wanjung Tsai ,  Brian Hare ,  William Markland ,  David A. Newsome ,  Marina S. Penney

IPC分类号： A61K31/704 ,  A61K9/127 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04 ,  A61P35/00

摘要： Described herein are methods of treating a proliferative disease in a subject by administering a DNA-damaging agent and between about 8 and about 48 hours later administering to the subject a DNA-PK inhibitor. Exemplary DNA-PK inhibitors are represented by Formula (B-I): and by pharmaceutically acceptable salts thereof, wherein R1, Q, Ring A, and Ring B are as defined herein.

公开(公告)号：US20220088043A1

公开(公告)日：2022-03-24

申请号：US17444033

申请日：2021-07-29

申请人： Vertex Pharmaceuticals Incorporated

发明人： Diane Boucher ,  Shawn M. Hillier ,  Wanjung Tsai ,  Brian Hare ,  William Markland ,  David A. Newsome ,  Marina S. Penney

IPC分类号： A61K31/704 ,  A61P35/00 ,  A61K9/127 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04

摘要： Described herein are methods of treating a proliferative disease in a subject by administering a DNA-damaging agent and between about 8 and about 48 hours later administering to the subject a DNA-PK inhibitor. Exemplary DNA-PK inhibitors are represented by Formula (B-I): and by pharmaceutically acceptable salts thereof, wherein R1, Q, Ring A, and Ring B are as defined herein.

公开(公告)号：US11980633B2

公开(公告)日：2024-05-14

申请号：US17444033

申请日：2021-07-29

申请人： Vertex Pharmaceuticals Incorporated

发明人： Diane Boucher ,  Shawn M. Hillier ,  Wanjung Tsai ,  Brian Hare ,  William Markland ,  David A. Newsome ,  Marina S. Penney

IPC分类号： A61K31/704 ,  A61K9/127 ,  A61P35/00 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04

CPC分类号： A61K31/704 ,  A61K9/1271 ,  A61P35/00 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04

摘要： Described herein are methods of treating a proliferative disease in a subject by administering a DNA-damaging agent and between about 8 and about 48 hours later administering to the subject a DNA-PK inhibitor. Exemplary DNA-PK inhibitors are represented by Formula (B-I): and by pharmaceutically acceptable salts thereof, wherein R1, Q, Ring A, and Ring B are as defined herein.

公开(公告)号：US11110108B2

公开(公告)日：2021-09-07

申请号：US16336195

申请日：2017-09-27

申请人： Vertex Pharmaceuticals Incorporated

发明人： Diane M. Boucher ,  Shawn M. Hillier ,  Wanjung Tsai ,  Brian Hare ,  William Markland ,  David A. Newsome ,  Marina S. Penney

IPC分类号： A61K31/704 ,  A61P35/00 ,  A61K9/127 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04

摘要： Described herein are methods of treating a proliferative disease in a subject by administering a DNA-damaging agent and between about 8 and about 48 hours later administering to the subject a DNA-PK inhibitor. Exemplary DNA-PK inhibitors are represented by Formula (B-I): and by pharmaceutically acceptable salts thereof, wherein R1, Q, Ring A, and Ring B are as defined herein.

公开(公告)号：US09771361B2

公开(公告)日：2017-09-26

申请号：US15150459

申请日：2016-05-10

申请人： Vertex Pharmaceuticals Incorporated

发明人： Kwame W. Nti-Addae ,  Michael Waldo ,  Simon Adam O'Neil ,  John Gregg Van Alsten ,  Dainius Macikenas ,  Praveen Mudunuri ,  Yi Shi ,  Mark Willem Ledeboer ,  Valdas Jurkauskas ,  Ales Medek ,  Steven Jones ,  Randal Byrn ,  Mohammed Asmal ,  Sarah Marie Robertson ,  Wanjung Tsai

IPC分类号： C07D471/04 ,  C07D403/04 ,  A61K31/506 ,  A61K31/16 ,  A61K31/351 ,  A61K31/4965 ,  A61K45/06 ,  C07C309/30

CPC分类号： C07D471/04 ,  A61K31/16 ,  A61K31/351 ,  A61K31/4965 ,  A61K31/506 ,  A61K45/06 ,  C07C309/30 ,  C07D403/04

摘要： Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: are Form A of HCl salt of Compound (1).½H2O, Form F of HCl salt of Compound (1).3H2O, Form D of HCl salt of Compound (1), Form A of Compound (1), and Form A of tosylate salt of Compound (1). Such polymorphic forms are employed for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.