公开(公告)号：US20130316945A1

公开(公告)日：2013-11-28

申请号：US13851303

申请日：2013-03-27

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Kevin M. Cottrell ,  Robert B. Perni ,  Janos Pitlik ,  Wayne C. Schairer

IPC: C07K5/10

CPC classification number: C07K5/10 ,  C07K7/06

Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.

公开(公告)号：US09340557B2

公开(公告)日：2016-05-17

申请号：US14205657

申请日：2014-03-12

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： John Patrick Maxwell ,  Paul S. Charifson ,  Qing Tang ,  Steven M. Ronkin ,  Katrina Lee Jackson ,  Albert Charles Pierce ,  David J. Lauffer ,  Pan Li ,  Simon Giroux ,  Jinwang Xu ,  Kevin M. Cottrell ,  Mark A. Morris ,  Nathan D. Waal ,  John J. Court ,  Wenxin Gu ,  Hongbo Deng

IPC: A61K31/498 ,  C07D241/44 ,  C07D513/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  C07D241/40 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D498/08 ,  C07D241/42 ,  C07D413/04 ,  C07D491/052

CPC classification number: A61K31/5377 ,  A61K31/506 ,  A61K31/5386 ,  C07D241/40 ,  C07D241/42 ,  C07D241/44 ,  C07D271/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/08 ,  C07D498/08 ,  C07D513/04

Abstract: The compounds represented by Formula (I) and pharmaceutically acceptable salts thereof are useful as inhibitors of DNA-PK: where each of R1, R2, X, Ring A, Ring B and Ring C is as described herein. Pharmaceutically acceptable compositions comprise said compounds. These compounds and pharmaceutical compositions are used in the treatment of various disease, conditions, or disorders.

Abstract translation: 由式（I）表示的化合物及其药学上可接受的盐可用作DNA-PK的抑制剂：其中R1，R2，X，环A，环B和环C均如本文所述。 药学上可接受的组合物包含所述化合物。 这些化合物和药物组合物用于治疗各种疾病，病症或病症。

公开(公告)号：US20140031277A1

公开(公告)日：2014-01-30

申请号：US13902278

申请日：2013-05-24

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Kevin M. Cottrell ,  John J. Court ,  David D. Deininger ,  Luc J. Farmer ,  Janos Pitlik ,  Robert B. Perni

IPC: C07K5/10 ,  A61K38/07 ,  A61K45/06

CPC classification number: C07K5/10 ,  A61K38/00 ,  A61K38/07 ,  A61K45/06 ,  C07K5/0202 ,  C07K7/02 ,  C07K14/005 ,  C12N2770/24222

Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Abstract translation: 本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐或混合物。 因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。 本发明还涉及包含用于离体使用或用于给予HCV感染患者的这些化合物的组合物和制备该化合物的方法。 本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。 本发明还涉及制备这些化合物的方法。

公开(公告)号：US09359380B2

公开(公告)日：2016-06-07

申请号：US14205508

申请日：2014-03-12

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： John Patrick Maxwell ,  Paul S. Charifson ,  Qing Tang ,  Steven M. Ronkin ,  Katrina Lee Jackson ,  Albert Charles Pierce ,  David J. Lauffer ,  Pan Li ,  Simon Giroux ,  Jinwang Xu ,  Kevin M. Cottrell ,  Mark A. Morris ,  Nathan D. Waal ,  John J. Court ,  Wenxin Gu ,  Hongbo Deng

IPC: C07D513/04 ,  C07D498/00 ,  C07D241/40 ,  C07D405/12 ,  C07D471/04 ,  C07D417/12 ,  C07D413/12 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D498/08 ,  C07D241/42 ,  C07D413/04 ,  C07D241/44 ,  C07D491/052

CPC classification number: A61K31/5377 ,  A61K31/506 ,  A61K31/5386 ,  C07D241/40 ,  C07D241/42 ,  C07D241/44 ,  C07D271/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/08 ,  C07D498/08 ,  C07D513/04

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：US20130157997A1

公开(公告)日：2013-06-20

申请号：US13678854

申请日：2012-11-16

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： James A. Henderson ,  John Maxwell ,  Louis Vaillancourt ,  Mark Morris ,  Ronald Grey, JR. ,  Simon Giroux ,  Laval Chan Chun Kong ,  Sanjoy Kumar Das ,  Bingan Liu ,  Carl Poisson ,  Caroline Cadilhac ,  Monica Bubenik ,  T. Jagadeeswar Reddy ,  Guy Falardeau ,  Constantin Yannopoulos ,  Jian Wang ,  Oswy Z. Pereira ,  Youssef L. Bennani ,  Albert C. Pierce ,  Govinda Rao Bhisetti ,  Kevin M. Cottrell ,  Valerie Marone

IPC: C07D403/14 ,  C07D495/04 ,  C07D417/14 ,  C07D413/14 ,  C07D409/14 ,  C07D405/14

CPC classification number: C07K5/06052 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B′, X, Y, R1, R1′, R2, R2′, R3, R3′, R5, R5′, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Abstract translation: 由式I表示的化合物或其药学上可接受的盐和溶剂化物，其中A，B，B'，X，Y，R1，R1'，R2，R2'，R3，R3'，R5，R5'，R6， n或p如本文所定义，可用于治疗黄病毒科病毒感染。

公开(公告)号：US20130090364A1

公开(公告)日：2013-04-11

申请号：US13625160

申请日：2012-09-24

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Laval Chan Chun Kong ,  Simon Giroux ,  Jagadeeswar T. Reddy ,  Youssef L. Bennani ,  Sanjoy Kumar Das ,  John Maxwell ,  Constantin Yannopoulos ,  Bingcan Liu ,  Jingwang Xu ,  Kevin M. Cottrell ,  Mark A. Morris

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R1, R2, R2′, R3, R3′, R4, R4′, R5, R5′m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

公开(公告)号：US12005127B2

公开(公告)日：2024-06-11

申请号：US16962442

申请日：2019-01-16

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： John Patrick Maxwell ,  Katrina Lee Jackson ,  Qing Tang ,  Mark A. Morris ,  Steven M. Ronkin ,  Jinwang Xu ,  Kevin M. Cottrell ,  Paul S. Charifson

IPC: C07D239/74 ,  A61K48/00 ,  C07D239/88 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D491/048

CPC classification number: A61K48/0066 ,  A61K48/0075 ,  C07D239/74 ,  C07D239/88 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D491/048

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 diseases, conditions, or disorders.

公开(公告)号：US20140243257A1

公开(公告)日：2014-08-28

申请号：US14272699

申请日：2014-05-08

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： James A. Henderson ,  John Maxwell ,  Louis Vaillancourt ,  Mark Morris ,  Ronald Grey, JR. ,  Simon Giroux ,  Laval Chan Chun Kong ,  Sanjoy Kumar Das ,  Bingcan Liu ,  Carl Poisson ,  Caroline Cadilhac ,  Monica Bubenik ,  T. Jagadeeswar Reddy ,  Guy Falardeau ,  Constantin Yannopoulos ,  Jian Wang ,  Oswy Z. Pereira ,  Youssef L. Bennani ,  Albert C. Pierce ,  Govinda Rao Bhisetti ,  Kevin M. Cottrell ,  Valerie Marone

IPC: C07K5/062 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

CPC classification number: C07K5/06052 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B′, X, Y, R1, R1′, R2, R2′, R3, R3′, R5, R5′, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Abstract translation: 其中A，B，B'，X，Y，R1，R1'，R2，R2'，R3，R3'，R5，R5'，R6，m， n或p如本文所定义，可用于治疗黄病毒科病毒感染。

公开(公告)号：US08765731B2

公开(公告)日：2014-07-01

申请号：US13678854

申请日：2012-11-16

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： James A. Henderson ,  John Maxwell ,  Louis Vaillancourt ,  Mark Morris ,  Ronald Grey, Jr. ,  Simon Giroux ,  Laval Chan Chun Kong ,  Sanjoy Kumar Das ,  Bingan Liu ,  Carl Poisson ,  Caroline Cadilhac ,  Monica Bubenik ,  T. Jagadeeswar Reddy ,  Guy Falardeau ,  Constantin Yannopoulos ,  Jian Wang ,  Oswy Z. Pereira ,  Youssef L. Bennani ,  Albert C. Pierce ,  Govinda Rao Bhisetti ,  Kevin M. Cottrell ,  Valerie Marone

IPC: A61K31/4184 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/4439 ,  C07D495/04 ,  C07D417/14 ,  C07D413/14 ,  C07D409/14 ,  C07D405/14

CPC classification number: C07K5/06052 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B′, X, Y, R1, R1′, R2, R2′, R3, R3′, R5, R5′, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Abstract translation: 其中A，B，B'，X，Y，R1，R1'，R2，R2'，R3，R3'，R5，R5'，R6，m， n或p如本文所定义，可用于治疗黄病毒科病毒感染。

公开(公告)号：US20130102629A1

公开(公告)日：2013-04-25

申请号：US13625137

申请日：2012-09-24

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： John Maxwell ,  Youssef L. Bennani ,  Sanjoy Kumar Das ,  Laval Chan Chun Kong ,  Jagadeeswar T. Reddy ,  Bingcan Liu ,  Caroline Cadilhac ,  Simon Giroux ,  James Henderson ,  Oswy Z. Pereira ,  Kevin M. Cottrell ,  Mark A. Morris

IPC: C07D495/04 ,  C07D471/04 ,  C07D417/14 ,  C07D413/14 ,  C07D403/14

CPC classification number: C07D495/04 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds represented by formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R1, R2, R2′, R3, R3′, R4, R4′, R5, R5′, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Abstract translation: 由式（I）表示的化合物或其药学上可接受的盐，其中A，B，B'，X，Y，R1，R2，R2'，R3，R3'，R4，R4'，R5，R5'，m， 或p如本文所定义，可用于治疗黄病毒科病毒感染。