公开(公告)号：US20230365587A1

公开(公告)日：2023-11-16

申请号：US18248065

申请日：2021-10-06

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Jason MCCARTNEY ,  Alexander Russell ABELA ,  Sunny ABRAHAM ,  Corey Don ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Jaclyn CHAU ,  Jeremy CLEMENS ,  Thomas CLEVELAND ,  Timothy A. DWIGHT ,  Bryan A. FRIEMAN ,  Peter GROOTENHUIS ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Paul KRENITSKY ,  Mark Thomas MILLER ,  Fabrice PIERRE ,  Alina SILINA ,  Jinglan ZHOU

IPC: C07D513/04 ,  C07D515/18 ,  C07D515/04

CPC classification number: C07D513/04 ,  C07D515/18 ,  C07D515/04

Abstract: This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having the core structure: pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, combination therapies, and processes and intermediates for making such modulators.

公开(公告)号：US20230286907A1

公开(公告)日：2023-09-14

申请号：US18065208

申请日：2022-12-13

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Nadia M. AHMAD ,  Corey ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Iuliana Luci ASGIAN ,  Joanne Louise CAMP ,  Lev Tyler Dewey FANNING ,  Sara Sabina HADIDA RUAH ,  Dennis HURLEY ,  Yvonne SCHMIDT ,  David SHAW ,  Urvi PATEL ,  Stephen Andrew THOMSON ,  Lidio Marx CARVALHO MEIRELES

IPC: C07C235/64 ,  A61K31/165 ,  C07D307/86 ,  C07C237/42 ,  C07D239/42 ,  C07D213/69 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D239/34 ,  C07D307/79 ,  C07D317/46 ,  C07D405/12

CPC classification number: C07C235/64 ,  A61K31/165 ,  C07D307/86 ,  C07C237/42 ,  C07D239/42 ,  C07D213/69 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D239/34 ,  C07D307/79 ,  C07D317/46 ,  C07D405/12 ,  C07B2200/05 ,  C07C2601/02

Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

公开(公告)号：US20230374038A1

公开(公告)日：2023-11-23

申请号：US18248068

申请日：2021-10-06

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Jason MCCARTNEY ,  Alexander Russell ABELA ,  Sunny ABRAHAM ,  Corey Don ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Jaclyn CHAU ,  Jeremy CLEMENS ,  Thomas CLEVELAND ,  Timothy Richard COON ,  Timothy A. DWIGHT ,  Bryan A. FRIEMAN ,  Peter GROOTENHUIS ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Haripada KHATUYA ,  Paul KRENITSKY ,  Mark Thomas MILLER ,  Prasuna PARASELLI ,  Fabrice PIERRE ,  Alina SILINA ,  Joe A. TRAN ,  Jinglan ZHOU

IPC: C07D515/08 ,  A61K45/06 ,  C07D515/18 ,  A61K31/529 ,  A61K31/5377

CPC classification number: C07D515/08 ,  A61K45/06 ,  C07D515/18 ,  A61K31/529 ,  A61K31/5377

Abstract: This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), having the core structure: pharmaceutical compositions containing at least one such modulator, methods of treatment of mediated diseases, such as cystic fibrosis, using such modulators and pharmaceutical compositions, combination pharmaceutical compositions and therapies comprising such modulators, and processes and intermediates for making such modulators.

公开(公告)号：US20230127655A1

公开(公告)日：2023-04-27

申请号：US17692235

申请日：2022-03-11

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Sara Sabina HADIDA RUAH ,  Peter Diederik Jan GROOTENHUIS ,  Fredrick F. VAN GOOR ,  Jinglan ZHOU ,  Brian Richard BEAR ,  Mark Thomas MILLER ,  Jason McCARTNEY ,  Mehdi Michel Djamel NUMA

IPC: A61K31/47 ,  C07D487/04 ,  G01N33/50 ,  C07D209/08 ,  A61K31/405 ,  A61K31/407 ,  A61K31/4192 ,  A61K31/4045 ,  C07D471/04 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/404 ,  A61K31/5377 ,  C07D233/64 ,  C07D403/12 ,  A61K45/06 ,  C07D405/12 ,  C07D405/14 ,  A61K31/41

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

公开(公告)号：US20230100634A1

公开(公告)日：2023-03-30

申请号：US17217323

申请日：2021-03-30

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Sara Sabina HADIDA RUAH ,  Peter Diederik Jan GROOTENHUIS ,  Fredrick F. VAN GOOR ,  Jinglan ZHOU ,  Brian Richard BEAR ,  Mark Thomas MILLER ,  Jason McCARTNEY ,  Mehdi Michel Djamel NUMA

IPC: A61K31/47 ,  C07D471/04 ,  C07D209/08 ,  C07D405/12 ,  C07D405/14 ,  C07D233/64 ,  C07D403/12 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D487/04 ,  G01N33/50 ,  A61K31/405 ,  A61K31/404

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

公开(公告)号：US20190016671A1

公开(公告)日：2019-01-17

申请号：US16032799

申请日：2018-07-11

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Nadia AHMAD ,  Corey ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Iuliana Luci ASGIAN ,  Joanne Louise CAMP ,  Lev Tyler Dewey FANNING ,  Sara Sabina HADIDA RUAH ,  Dennis HURLEY ,  Yvonne SCHMIDT ,  David SHAW ,  Urvi Jagdishbhai SHETH ,  Stephen Andrew THOMSON

IPC: C07C235/64 ,  C07D213/81 ,  C07D213/89 ,  C07D239/34 ,  C07D317/46 ,  C07D405/12 ,  C07D213/69 ,  C07D213/82 ,  C07D307/79

Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

公开(公告)号：US20170145011A1

公开(公告)日：2017-05-25

申请号：US15369029

申请日：2016-12-05

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Sara Sabina HADIDA RUAH ,  Edward Adam KALLEL ,  Mark Thomas MILLER ,  Vijayalaksmi ARUMUGAM ,  Jason McCARTNEY ,  Corey ANDERSON ,  Peter Diederik Jan GROOTENHUIS ,  Licong JIANG

IPC: C07D471/20 ,  A61K31/499

CPC classification number: C07D471/20 ,  A61K31/499 ,  A61K31/506 ,  C07D519/00

Abstract: The invention relates to pyrrolopyrazine-spirocyclic piperidine amide compounds useful as inhibitors of ion channels. 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.

公开(公告)号：US20230416275A1

公开(公告)日：2023-12-28

申请号：US18030537

申请日：2021-10-06

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Jason MCCARTNEY ,  Alexander Russell ABELA ,  Sunny ABRAHAM ,  Corey Don ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Jaclyn CHAU ,  Jeremy CLEMENS ,  Thomas CLEVELAND ,  Timothy A. DWIGHT ,  Bryan A. FRIEMAN ,  Peter GROOTENHUIS ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Mark Thomas MILLER ,  Alina SILINA ,  Jinglan ZHOU

IPC: C07D515/18 ,  C07D515/22 ,  C07D515/08 ,  A61K45/06

CPC classification number: C07D515/18 ,  C07D515/22 ,  C07D515/08 ,  A61K45/06 ,  C07B2200/09

Abstract: This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having core structure (I), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, combination pharmaceutical compositions and combination therapies, and processes and intermediates for making such modulators.

公开(公告)号：US20230373939A1

公开(公告)日：2023-11-23

申请号：US18030519

申请日：2021-10-06

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Jason MCCARTNEY ,  Sunny ABRAHAM ,  Corey Don ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Jaclyn CHAU ,  Thomas CLEVELAND ,  Timothy A. DWIGHT ,  Bryan A. FRIEMAN ,  Peter GROOTENHUIS ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Mark Thomas MILLER ,  Alina SILINA ,  Jinglan ZHOU

IPC: C07D279/06 ,  C07D241/22 ,  C07D251/24 ,  C07D239/69 ,  C07D403/04 ,  C07D213/76 ,  C07D401/14 ,  C07D401/12 ,  A61K45/06

CPC classification number: C07D279/06 ,  C07D241/22 ,  C07D251/24 ,  C07D239/69 ,  C07D403/04 ,  C07D213/76 ,  C07D401/14 ,  C07D401/12 ,  A61K45/06 ,  C07B2200/05

Abstract: This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having the structure: (I), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, combination therapies, and processes and intermediates for making such modulators.

公开(公告)号：US20230312616A1

公开(公告)日：2023-10-05

申请号：US17861567

申请日：2022-07-11

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Alexander Russell ABELA ,  Jeremy J. CLEMENS ,  Peter Diederik Jan GROOTENHUIS ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Haripada KHATUYA ,  Jason McCARTNEY ,  Mark Thomas MILLER ,  Fabrice Jean Denis PIERRE ,  Joe Anh TRAN ,  Jinglan ZHOU

IPC: C07F7/08 ,  C07F7/30

CPC classification number: C07F7/0816 ,  C07F7/30 ,  C07F7/083 ,  C07F7/0814

Abstract: This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, and processes for making such modulators.