公开(公告)号：US10273233B2

公开(公告)日：2019-04-30

申请号：US15807984

申请日：2017-11-09

申请人： Vertex Pharmaceuticals Incorporated

发明人： Luc J. Farmer ,  Michael John Boyd ,  Dean Shannon ,  Michael Waldo ,  Kwame W. Nti-Addae ,  Yuegang Zhang

IPC分类号： C07D471/04 ,  A61K31/506 ,  A61K31/4965 ,  A61K45/06

摘要： Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: include Hydrate 2 of Compound (1), Hydrate 3 of Compound (1), Form A of Compound (1), Form B of Compound (1), Form C of Compound (1), Form D of Compound (1), and amorphous Compound (1). Such polymorphic forms are useful for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.

公开(公告)号：US20160214980A1

公开(公告)日：2016-07-28

申请号：US15024698

申请日：2014-09-25

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Michael John Boyd ,  Alex Aronov ,  Hardwin O'Dowd ,  Jeremy Green

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to a compound useful as a selective inhibitor of PI3Kγ. 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.

摘要翻译： 本发明涉及可用作PI3Kγ选择性抑制剂的化合物。 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：US10301304B2

公开(公告)日：2019-05-28

申请号：US15024698

申请日：2014-09-25

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Michael John Boyd ,  Alex Aronov ,  Hardwin O'Dowd ,  Jeremy Green

IPC分类号： C07D471/04

摘要： The present invention relates to a compound useful as a selective inhibitor of PI3Kγ. 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：US11884672B2

公开(公告)日：2024-01-30

申请号：US15931256

申请日：2020-05-13

申请人： Vertex Pharmaceuticals Incorporated

发明人： Upul Keerthi Bandarage ,  Cavan McKeon Bligh ,  Diane Boucher ,  Michael John Boyd ,  Michael Aaron Brodney ,  Michael Philip Clark ,  Veronique Damagnez ,  Lev Tyler Dewey Fanning ,  Robert Francis Fimognari ,  Gabrielle Simone Fleming ,  Kevin James Gagnon ,  Pedro Manuel Garcia Barrantes ,  Robert Daniel Giacometti ,  Simon Giroux ,  Ronald Lee Grey, Jr. ,  Samantha Guido ,  Amy Beth Hall ,  Sarah Carol Hood ,  Dennis James Hurley ,  Mac Arthur Johnson, Jr. ,  Peter Jones ,  Sarathy Kesavan ,  Mei-Hsiu Lai ,  Siying Liu ,  Adam Looker ,  Brad Maxwell ,  John Patrick Maxwell ,  Ales Medek ,  Philippe Marcel Nuhant ,  Kirk Alan Overhoff ,  Setu Roday ,  Stefanie Roeper ,  Steven M. Ronkin ,  Rupa Sawant ,  Yi Shi ,  Muna Shrestha ,  Marisa Sposato ,  Kathy Stavropoulos ,  Rebecca Jane Swett ,  Timothy Lewis Tapley ,  Qing Tang ,  Stephen Thomson ,  Jinwang Xu ,  Mariam Zaky ,  Kevin Michael Cottrell

IPC分类号： C07D487/04 ,  A61K9/16 ,  A61K31/4162 ,  C07D491/18 ,  C07D513/04 ,  C07D519/00 ,  C07F9/6561 ,  C07H15/26

CPC分类号： C07D487/04 ,  A61K9/1635 ,  A61K9/1652 ,  A61K31/4162 ,  C07D491/18 ,  C07D513/04 ,  C07D519/00 ,  C07F9/6561 ,  C07H15/26 ,  C07B2200/13

摘要： The disclosure provides compounds useful for treating alpha-1 antitrypsin deficiency (AATD), according to formula (I):




tautomers thereof, pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable salts of the tautomers, deuterated derivatives of the compounds, deuterated derivatives of the tautomers, and deuterated derivatives of the salts, solid forms of those compounds and processes for making those compounds.

公开(公告)号：US11623924B2

公开(公告)日：2023-04-11

申请号：US16593118

申请日：2019-10-04

申请人： Vertex Pharmaceuticals Incorporated

发明人： Upul Keerthi Bandarage ,  Cavan McKeon Bligh ,  Michael John Boyd ,  Diane M. Boucher ,  Michael Aaron Brodney ,  Veronique Damagnez ,  Lev Tyler Dewey Fanning ,  Mary Elizabeth Eccles ,  Robert Francis Fimognari, Jr. ,  Kevin James Gagnon ,  Pedro M. Garcia Barrantes ,  Simon Giroux ,  Ronald Lee Grey, Jr. ,  Amy Beth Hall ,  Sarah Carol Hood ,  Dennis James Hurley ,  Joshua Kennedy Hussey ,  Mac Arthur Johnson, Jr. ,  Peter Jones ,  Sarathy Kesavan ,  Adam Looker ,  Brad D. Maxwell ,  John Patrick Maxwell ,  Ales Medek ,  Mettachit Navamal ,  Philippe Marcel Nuhant ,  Setu Roday ,  Stefanie Roeper ,  Rupa Sawant ,  Yi Shi ,  Rebecca Jane Swett ,  Qing Tang ,  Timothy Lewis Tapley ,  Stephen A. Thomson ,  Michael Waldo ,  Jinwang Xu ,  Kevin Michael Cottrell

IPC分类号： C07D403/04 ,  C07D519/00

摘要： Novel compounds, compositions, and methods of using and preparing the same, which may be useful for treating alpha-1 antitrypsin deficiency (AATD).

公开(公告)号：US10533004B2

公开(公告)日：2020-01-14

申请号：US15807877

申请日：2017-11-09

申请人： Vertex Pharmaceuticals Incorporated

发明人： Luc J. Farmer ,  Michael John Boyd ,  David B. Miller, Jr. ,  Valerie Ann Cwynar

IPC分类号： C07D471/04

摘要： A method of preparing a compound of Formula (I) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (1): or a pharmaceutically acceptable salt thereof with Compound (2): in the presence of water, an organic solvent, a base, and a transition metal catalyst to generate a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20180065963A1

公开(公告)日：2018-03-08

申请号：US15807984

申请日：2017-11-09

申请人： Vertex Pharmaceuticals Incorporated

发明人： Luc J. Farmer ,  Michael John Boyd ,  Dean Shannon ,  Michael Waldo ,  Kwame W. Nti-Addae ,  Yuegang Zhang

IPC分类号： C07D471/04 ,  A61K31/4965 ,  A61K45/06 ,  A61K31/506

CPC分类号： C07D471/04 ,  A61K31/4965 ,  A61K31/506 ,  A61K45/06 ,  C07B2200/13

摘要： Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: include Hydrate 2 of Compound (1), Hydrate 3 of Compound (1), Form A of Compound (1), Form B of Compound (1), Form C of Compound (1), Form D of Compound (1), and amorphous Compound (1). Such polymorphic forms are useful for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.

公开(公告)号：US20180065962A1

公开(公告)日：2018-03-08

申请号：US15807877

申请日：2017-11-09

申请人： Vertex Pharmaceuticals Incorporated

发明人： Luc J. Farmer ,  Michael John Boyd ,  David B. Miller, JR. ,  Valerie Ann Cwynar

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07D239/42

摘要： A method of preparing a compound of Formula (I) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (1): or a pharmaceutically acceptable salt thereof with Compound (2): in the presence of water, an organic solvent, a base, and a transition metal catalyst to generate a compound of Formula (I) or a pharmaceutically acceptable salt thereof.