公开(公告)号：US11008305B2

公开(公告)日：2021-05-18

申请号：US16538992

申请日：2019-08-13

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Kevin Michael Cottrell ,  Hongbo Deng ,  John P. Duffy ,  Huai Gao ,  Simon Giroux ,  Jeremy Green ,  Katrina Lee Jackson ,  Joseph M. Kennedy ,  David J. Lauffer ,  Mark Willem Ledeboer ,  Pan Li ,  John Patrick Maxwell ,  Mark A. Morris ,  Albert Charles Pierce ,  Nathan D. Waal ,  Jinwang Xu

IPC: C07D401/14 ,  A61K41/00 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D403/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D495/04 ,  C07D521/00 ,  C07D239/42 ,  C07D417/10 ,  A61K9/20 ,  A61K9/48 ,  A61K31/506 ,  A61K31/5377 ,  A61K47/55 ,  A61K47/54 ,  A61K31/53 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D403/04 ,  C07D413/04

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US20160250212A1

公开(公告)日：2016-09-01

申请号：US15056137

申请日：2016-02-29

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Kevin Michael Cottrell ,  Hongbo Deng ,  John P. Duffy ,  Huai Gao ,  Simon Giroux ,  Jeremy Green ,  Katrina Lee Jackson ,  Joseph M. Kennedy ,  David J. Lauffer ,  Mark Willem Ledeboer ,  Pan Li ,  John Patrick Maxwell ,  Mark A. Morris ,  Albert Charles Pierce ,  Nathan D. Waal ,  Jinwang Xu

IPC: A61K31/506 ,  A61K9/20 ,  A61K31/5377 ,  A61K9/48

CPC classification number: A61K31/506 ,  A61K9/20 ,  A61K9/48 ,  A61K31/53 ,  A61K31/5377 ,  A61K41/0038 ,  A61K47/481 ,  A61K47/545 ,  A61K47/55 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D495/04 ,  C07D521/00

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US09394302B2

公开(公告)日：2016-07-19

申请号：US14666567

申请日：2015-03-24

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Michael P. Clark ,  Upul K. Bandarage ,  Randy S. Bethiel ,  Michael J. Boyd ,  Ioana Davies ,  Hongbo Deng ,  John P. Duffy ,  Luc J. Farmer ,  Huai Gao ,  Wenxin Gu ,  Joseph M. Kennedy ,  Brian Ledford ,  Mark W. Ledeboer ,  Francois Maltais ,  Emanuele Perola ,  Tiansheng Wang

IPC: C07D471/04 ,  A61K31/506 ,  A61K45/06 ,  C07F9/6561

CPC classification number: C07D471/04 ,  A61K31/215 ,  A61K31/351 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  C07F9/6561

Abstract: This invention provides methods of preparing 3-(pyrimidin-2-yl)-1H-pyrrolo[2,3-b]pyridines and 3-(pyrimidin-2-yl)-1H-pyrazolo[3,4-b]pyridines, or pharmaceutically acceptable salts thereof that are useful for inhibiting the replication of influenza viruses in a biological sample or patient, reducing the amount of influenza viruses in a biological sample or patient, and treating influenza in a patient.

Abstract translation: 本发明提供3-（嘧啶-2-基）-1H-吡咯并[2,3-b]吡啶和3-（嘧啶-2-基）-1H-吡唑并[3,4-b]吡啶的制备方法， 或其药学上可接受的盐，其可用于抑制生物样品或患者中流感病毒的复制，减少生物样品或患者中的流感病毒的数量，以及治疗患者的流感。

公开(公告)号：US20150111871A1

公开(公告)日：2015-04-23

申请号：US14515793

申请日：2014-10-16

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Paul S. Charifson ,  Kevin Michael Cottrell ,  Hongbo Deng ,  John P. Duffy ,  Huai Gao ,  Simon Giroux ,  Jeremy Green ,  Katrina Lee Jackson ,  Joseph M. Kennedy ,  David J. Lauffer ,  Mark Willem Ledeboer ,  Pan Li ,  John Patrick Maxwell ,  Mark A. Morris ,  Albert Charles Pierce ,  Nathan D. Waal ,  Jinwang Xu

IPC: C07D239/42 ,  C07D471/04 ,  C07D413/10 ,  C07D405/14 ,  A61K41/00 ,  C07D417/10 ,  C07D413/14 ,  C07D495/04 ,  C07D491/048 ,  C07D491/056 ,  C07D401/04 ,  C07D409/14

CPC classification number: A61K31/506 ,  A61K9/20 ,  A61K9/48 ,  A61K31/53 ,  A61K31/5377 ,  A61K41/0038 ,  A61K47/481 ,  A61K47/545 ,  A61K47/55 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D495/04 ,  C07D521/00

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract translation: 本发明涉及可用作DNA-PK抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

公开(公告)号：US08871774B2

公开(公告)日：2014-10-28

申请号：US13918048

申请日：2013-06-14

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Michael P. Clark ,  Upul K. Bandarage ,  Ioana Davies ,  John P. Duffy ,  Huai Gao ,  Jun Feng ,  Jianglin Liang ,  Joseph M. Kennedy ,  Mark W. Ledeboer ,  Brian Ledford ,  Francois Maltais ,  Emanuele Perola

IPC: A01N43/54 ,  C07D239/42 ,  C07D401/04 ,  A61K31/5377 ,  A61K31/506 ,  A61K45/06 ,  C07D471/04

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

Abstract translation: 抑制生物样品或患者中流感病毒复制，减少生物样品或患者中的流感病毒数量和治疗患者流感的方法包括向所述生物样本或患者施用有效量的 由结构式（I）表示的化合物或其药学上可接受的盐，其中结构式（I）的值如本文所述。 化合物由结构式（I）表示或其药学上可接受的盐，其中结构式（I）的值如本文所述。 药物组合物包含有效量的这种化合物或其药学上可接受的盐，以及药学上可接受的载体，佐剂或媒介物。

公开(公告)号：US10391095B2

公开(公告)日：2019-08-27

申请号：US16042206

申请日：2018-07-23

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Kevin Michael Cottrell ,  Hongbo Deng ,  John P. Duffy ,  Huai Gao ,  Simon Giroux ,  Jeremy Green ,  Katrina Lee Jackson ,  Joseph M. Kennedy ,  David J. Lauffer ,  Mark Willem Ledeboer ,  Pan Li ,  John Patrick Maxwell ,  Mark A. Morris ,  Albert Charles Pierce ,  Nathan D. Waal ,  Jinwang Xu

IPC: A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D239/42 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D495/04 ,  C07D521/00 ,  A61K41/00 ,  C07D417/10 ,  A61K9/20 ,  A61K9/48 ,  A61K31/5377 ,  A61K47/55 ,  A61K47/54 ,  A61K31/53

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US09908878B2

公开(公告)日：2018-03-06

申请号：US15177546

申请日：2016-06-09

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Michael P. Clark ,  Upul K. Bandarage ,  Randy S. Bethiel ,  Michael J. Boyd ,  Ioana Davies ,  Hongbo Deng ,  John P. Duffy ,  Luc J. Farmer ,  Huai Gao ,  Wenxin Gu ,  Joseph M. Kennedy ,  Brian Ledford ,  Mark W. Ledeboer ,  Francois Maltais ,  Emanuele Perola ,  Tiansheng Wang

IPC: C07D471/04 ,  A61K31/506 ,  A61K45/06 ,  C07F9/6561 ,  A61K31/215 ,  A61K31/351 ,  A61K31/444 ,  A61K31/497

CPC classification number: C07D471/04 ,  A61K31/215 ,  A61K31/351 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  C07F9/6561

Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

公开(公告)号：US09808459B2

公开(公告)日：2017-11-07

申请号：US15299757

申请日：2016-10-21

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Michael P. Clark ,  Upul K. Bandarage ,  Randy S. Bethiel ,  John J. Court ,  Hongbo Deng ,  Ioana Davies ,  John P. Duffy ,  Luc J. Farmer ,  Huai Gao ,  Wenxin Gu ,  Dylan H. Jacobs ,  Joseph M. Kennedy ,  Mark W. Ledeboer ,  Brian Ledford ,  Francois Maltais ,  Emanuele Perola ,  Tiansheng Wang ,  M. Woods Wannamaker ,  Randal Byrn ,  Yi Zhou ,  Chao Lin ,  Min Jiang ,  Steven Jones ,  Ursula A. Germann ,  Francesco G. Salituro ,  Ann Dak-Yee Kwong

IPC: C07D401/04 ,  A61K31/506

CPC classification number: A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07D239/30 ,  C07D401/04 ,  C07D401/10 ,  C07D471/04

Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

公开(公告)号：US09345708B2

公开(公告)日：2016-05-24

申请号：US14305393

申请日：2014-06-16

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Michael P. Clark ,  Upul K. Bandarage ,  Randy S. Bethiel ,  John J. Court ,  Hongbo Deng ,  Ioana Davies ,  John P. Duffy ,  Luc J. Farmer ,  Huai Gao ,  Wenxin Gu ,  Dylan H. Jacobs ,  Joseph M. Kennedy ,  Mark W. Ledeboer ,  Brian Ledford ,  Francois Maltais ,  Emanuele Perola ,  Tiansheng Wang ,  M. Woods Wannamaker ,  Randal Byrn ,  Yi Zhou ,  Chao Lin ,  Min Jiang ,  Steven Jones ,  Ursula A. Germann ,  Francesco G. Salituro ,  Ann Dak-Yee Kwong

IPC: A61K31/4965 ,  C07D401/00 ,  A61K31/5377 ,  A61K31/506 ,  C07D471/04 ,  C07D401/10 ,  A61K31/55 ,  A61K31/553 ,  C07D239/30 ,  C07D401/04

CPC classification number: A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07D239/30 ,  C07D401/04 ,  C07D401/10 ,  C07D471/04

Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

Abstract translation: 抑制生物样品或患者中流感病毒复制，减少生物样品或患者中的流感病毒数量和治疗患者流感的方法包括向所述生物样本或患者施用有效量的 由结构式（I）表示的化合物或其药学上可接受的盐，其中结构式（IA）的值如本文所述。 化合物由结构式（IA）或其药学上可接受的盐表示，其中结构式（IA）的值如本文所述。 药物组合物包含有效量的这种化合物或其药学上可接受的盐，以及药学上可接受的载体，佐剂或媒介物。

公开(公告)号：US20150191468A1

公开(公告)日：2015-07-09

申请号：US14666567

申请日：2015-03-24

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul S. Charifson ,  Michael P. Clark ,  Upul K. Bandarage ,  Randy S. Bethiel ,  Micheal J. Boyd ,  Ioana Davies ,  Hongbo Deng ,  John P. Duffy ,  Luc J. Farmer ,  Huai Gao ,  Wenxin Gu ,  Joseph M. Kennedy ,  Brian Ledford ,  Mark W. Ledeboer ,  Francois Maltais ,  Emanuele Perola ,  Tiansheng Wang

IPC: C07D471/04 ,  C07F9/6561 ,  A61K45/06 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/215 ,  A61K31/351 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  C07F9/6561

Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

Abstract translation: 抑制生物样品或患者中流感病毒复制，减少生物样品或患者中的流感病毒数量和治疗患者流感的方法包括向所述生物样本或患者施用有效量的 由结构式（I）表示的化合物：或其药学上可接受的盐，其中结构式（I）的值如本文所述。 化合物由结构式（I）表示或其药学上可接受的盐，其中结构式（I）的值如本文所述。 药物组合物包含有效量的这种化合物或其药学上可接受的盐，以及药学上可接受的载体，佐剂或媒介物。