公开(公告)号：US20200377535A1

公开(公告)日：2020-12-03

申请号：US16998426

申请日：2020-08-20

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Corey Anderson ,  Sara Sabina Hadida Ruah ,  Julian Marian Charles Golec ,  Beili Zhang ,  Benjamin Joseph Littler ,  Ali Keshavarz-Shokri ,  Tim Edward Alcacio ,  Daniel T. Belmont

IPC分类号： C07F9/58 ,  C07F9/59 ,  C07F9/576 ,  A61K31/675 ,  A61K45/06

摘要： The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.

公开(公告)号：US20200283405A1

公开(公告)日：2020-09-10

申请号：US16702891

申请日：2019-12-04

申请人： Vertex Pharmaceuticals Incorporated

发明人： Timothy Alcacio ,  Minson Baek ,  Peter Grootenhuis ,  Sara Sabina Hadida Ruah ,  Robert M. Hughes ,  Ali Keshavarz-Shokri ,  Rachel McAuley-Aoki ,  Jason McCartney ,  Mark Thomas Miller ,  Fredrick Van Goor ,  Beili Zhang ,  Corey Anderson ,  Thomas Cleveland ,  Bryan A. Frieman ,  Haripada Khatuya ,  Pramod Virupax Joshi ,  Paul John Krenitsky ,  Vito Melillo ,  Fabrice Jean Denis Pierre ,  Andreas P. Termin ,  Johnny Uy ,  Jinglan Zhou ,  Alexander Russell Abela ,  Brett Bradley Busch ,  Prasuna Paraselli

IPC分类号： C07D401/14 ,  C07D471/14 ,  C07D498/14 ,  C07B59/00

摘要： Compounds of Formula I: pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

公开(公告)号：US20190276483A1

公开(公告)日：2019-09-12

申请号：US16283904

申请日：2019-02-25

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Corey Anderson ,  Sara Sabina Hadida Ruah ,  Julian Marian Charles Golec ,  Beili Zhang ,  Benjamin Joseph Littler ,  Ali Keshavarz-Shokri ,  Tim Edward Alcacio ,  Daniel T. Belmont

IPC分类号： C07F9/58 ,  C07F9/59 ,  A61K31/675 ,  A61K45/06 ,  C07F9/576

摘要： The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.

公开(公告)号：US20190119253A1

公开(公告)日：2019-04-25

申请号：US16165849

申请日：2018-10-19

申请人： Vertex Pharmaceuticals Incorporated

发明人： Varsha Dhamankar ,  Kirk Raymond Dinehart ,  Eleni Dokou ,  Lori Ann Ferris ,  Nishanth Gopinathan ,  Katie McCarty ,  Catherine Metzler ,  Beili Zhang

IPC分类号： C07D401/14 ,  A61K9/20 ,  A61P11/00

摘要： Crystalline Forms of Compound I: and pharmaceutically acceptable salts thereofare disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

公开(公告)号：US20190038615A1

公开(公告)日：2019-02-07

申请号：US15898683

申请日：2018-02-19

申请人： Vertex Pharmaceuticals Incorporated

发明人： Fredrick F. Van Goor ,  Rossitza Gueorguieva Alargova ,  Tim Edward Alcacio ,  Sneha G. Arekar ,  Steven C. Johnston ,  Irina Nicolaevna Kadiyala ,  Ali Keshavarz-Shokri ,  Mariusz Krawiec ,  Elaine Chungmin Lee ,  Ales Medek ,  Praveen Mudunuri ,  Mark Jeffrey Sullivan ,  Noreen Tasneem Zaman ,  Beili Zhang ,  Yuegang Zhang ,  Gregor Zlokarnik

IPC分类号： A61K31/47 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4704 ,  A61K31/404 ,  G01N33/50

摘要： The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.

公开(公告)号：US20160376295A1

公开(公告)日：2016-12-29

申请号：US15260778

申请日：2016-09-09

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Corey Anderson ,  Sara Sabina Hadida-Ruah ,  Julian Marian Charles Golec ,  Beili Zhang ,  Benjamin Joseph Littler ,  Ali Keshavarz-Shokri ,  Tim Edward Alcacio ,  Daniel T. Belmont

IPC分类号： C07F9/58 ,  A61K45/06 ,  A61K31/675

CPC分类号： C07F9/58 ,  A61K31/675 ,  A61K45/06 ,  C07F9/576 ,  C07F9/59

摘要： The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.

摘要翻译： 其中R2，R3，R5，R7和X如本文所定义。 本发明还提供包含本发明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（包括疼痛）的方法。 式I的化合物具有有利的溶解度和物理化学性质。

公开(公告)号：US20160067239A9

公开(公告)日：2016-03-10

申请号：US14603779

申请日：2015-01-23

申请人： Vertex Pharmaceuticals Incorporated

发明人： Fredrick F. Van Goor ,  Rossitza Gueorguieva Alargova ,  Tim Edward Alcacio ,  Sneha G. Arekar ,  Steven C. Johnston ,  Irina Nikolaevna Kadiyala ,  Ali Keshavarz-Shokri ,  Mariusz Krawiec ,  Elaine Chungmin Lee ,  Ales Medek ,  Praveen Mudunuri ,  Mark Jeffrey Sullivan ,  Noreen Tasneem Zaman ,  Beili Zhang ,  Yuegang Zhang ,  Gregor Zlokarnik

IPC分类号： A61K31/47 ,  A61K31/404 ,  G01N33/50 ,  A61K31/443

CPC分类号： A61K31/47 ,  A61K31/404 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4704 ,  G01N33/5032 ,  G01N2500/04 ,  A61K2300/00

摘要： The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.

公开(公告)号：US20160052916A1

公开(公告)日：2016-02-25

申请号：US14841163

申请日：2015-08-31

申请人： Vertex Pharmaceuticals Incorporated

发明人： Ali Keshavarz-Shokri ,  Beili Zhang ,  Mariusz Krawiec

IPC分类号： C07D405/12

CPC分类号： C07D405/12 ,  A61K31/4709 ,  C07B2200/13

摘要： The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.

摘要翻译： 本发明涉及3-（6-（1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）环丙烷甲酰氨基）-3-甲基吡啶-2-基的结晶和游离固体形式 - 基）苯甲酸（I型），其药物组合物及其处理方法。

公开(公告)号：US20160022665A2

公开(公告)日：2016-01-28

申请号：US14630778

申请日：2015-02-25

申请人： Vertex Pharmaceuticals Incorporated

发明人： Fredrick F. Van Goor ,  Rossitza Gueorguieva Alargova ,  Tim Edward Alcacio ,  Sneha G. Arekar ,  Hayley Marie Binch ,  Martyn Curtis Botfield ,  Lev Tyler Dewey Fanning ,  Peter Diederik Jan Grootenhuis ,  Dennis James Hurley ,  Steven C. Johnston ,  Irina Nikolaevna Kadiyala ,  Ritu Rohit Kaushik ,  Ali Keshavarz-Shokri ,  Mariusz Krawiec ,  Elaine Chungmin Lee ,  Brian Luisi ,  Ales Medek ,  Praveen Mudunuri ,  Mehdi Numa ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Mark Jeffrey Sullivan ,  Marinus Jacobus Verwijs ,  Xiaoqing Yang ,  Christopher Ryan Young ,  Noreen Tasneem Zaman ,  Beili Zhang ,  Yuegang Zhang ,  Gregor Zlokarnik

IPC分类号： A61K31/4709 ,  G01N33/68 ,  A61K31/404 ,  A61K31/47 ,  A61K31/443

CPC分类号： A61K31/4709 ,  A61K31/404 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/47 ,  A61K31/4704 ,  G01N33/6872 ,  G01N2333/4703 ,  A61K2300/00

摘要： The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.

摘要翻译： 本发明涉及包含式I和II化合物，任选与式III化合物和/或式IV化合物组合的药物组合物。 本发明还涉及固体形式及其药物制剂，以及使用这些组合物治疗CFTR介导的疾病，特别是囊性纤维化的方法。

公开(公告)号：US09163042B2

公开(公告)日：2015-10-20

申请号：US14568391

申请日：2014-12-12

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Corey Anderson ,  Sara Sabina Hadida-Ruah ,  Julian Marian Charles Golec ,  Beili Zhang ,  Benjamin Joseph Littler ,  Ali Keshavarz-Shokri ,  Tim Edward Alacio ,  Daniel T. Belmont

IPC分类号： C07D213/75 ,  A61K31/44 ,  C07F9/59

CPC分类号： C07F9/58 ,  A61K31/675 ,  A61K45/06 ,  C07F9/576 ,  C07F9/59

摘要： The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.

摘要翻译： 本发明涉及式I的前药化合物：其中R2，R3，R5，R7和X如本文所定义。 本发明还提供包含本发明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（包括疼痛）的方法。 式I的化合物具有有利的溶解度和物理化学性质。