公开(公告)号：US20240150377A1

公开(公告)日：2024-05-09

申请号：US18248071

申请日：2021-10-06

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Jason MCCARTNEY ,  Alexander Russell ABELA ,  Sunny ABRAHAM ,  Corey Don ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Jaclyn CHAU ,  Jeremy CLEMENS ,  Thomas CLEVELAND ,  Timothy Richard COON ,  Timothy A. DWIGHT ,  Lev Tyler Dewey FANNING ,  Bryan A. FRIEMAN ,  Peter GROOTENHUIS ,  Anton V. GULEVICH ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Haripada KHATUYA ,  Paul KRENITSKY ,  Vito MELILLO ,  Mark Thomas MILLER ,  Prasuna PARASELLI ,  Fabrice PIERRE ,  Alina SILINA ,  Joe A. TRAN ,  Johnny UY ,  Lino VALDEZ ,  Troy VICKERS ,  Jinglan ZHOU

IPC分类号： C07D515/08 ,  A61K31/404 ,  A61K31/47 ,  A61K31/529

CPC分类号： C07D515/08 ,  A61K31/404 ,  A61K31/47 ,  A61K31/529

摘要： 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 CFTR mediated diseases, including cystic fibrosis, using such modulators and pharmaceutical compositions, combination pharmaceutical compositions and combination therapies employing those modulators, and processes and intermediates for making such modulators.

公开(公告)号：US20240018161A1

公开(公告)日：2024-01-18

申请号：US18030530

申请日：2021-10-06

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Jason MCCARTNEY ,  Alexander Russell ABELA ,  Sunny ABRAHAM ,  Corey Don ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Jaclyn CHAU ,  Jeremy CLEMENS ,  Thomas CLEVELAND ,  Timothy Richard COON ,  Andrew DINH ,  Timothy A. DWIGHT ,  Lev Tyler Dewey FANNING ,  Bryan A. FRIEMAN ,  Peter GROOTENHUIS ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Paul KRENITSKY ,  Mark Thomas MILLER ,  Fabrice PIERRE ,  Alina SILINA ,  Joe A. TRAN ,  Lino VALDEZ ,  Jinglan ZHOU

IPC分类号： C07D515/04 ,  C07D515/14 ,  A61K45/06

CPC分类号： C07D515/04 ,  A61K45/06 ,  C07D515/14

摘要： 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 CFTR mediated diseases, including 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：US20240336614A1

公开(公告)日：2024-10-10

申请号：US18487690

申请日：2023-10-16

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：US20190016671A1

公开(公告)日：2019-01-17

申请号：US16032799

申请日：2018-07-11

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： 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分类号： C07C235/64 ,  C07D213/81 ,  C07D213/89 ,  C07D239/34 ,  C07D317/46 ,  C07D405/12 ,  C07D213/69 ,  C07D213/82 ,  C07D307/79

摘要： 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：US20230382925A1

公开(公告)日：2023-11-30

申请号：US18030529

申请日：2021-10-06

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Jason MCCARTNEY ,  Alexander Russell ABELA ,  Sunny ABRAHAM ,  Corey Don ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Jaclyn CHAU ,  Jeremy CLEMENS ,  Thomas CLEVELAND ,  Timothy Richard COON ,  Timothy A. DWIGHT ,  Lev Tyler Dewey FANNING ,  Bryan A. FRIEMAN ,  Peter GROOTENHUIS ,  Anton V. GULEVICH ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Haripada KHATUYA ,  Paul KRENITSKY ,  Vito MELILLO ,  Mark Thomas MILLER ,  Prasuna PARASELLI ,  Fabrice PIERRE ,  Alina SILINA ,  Joe A. TRAN ,  Johnny UY ,  Lino VALDEZ ,  Jinglan ZHOU

IPC分类号： C07D515/08 ,  A61K45/06

CPC分类号： C07D515/08 ,  A61K45/06

摘要： 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 CFTR mediated diseases, including 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：US20230286907A1

公开(公告)日：2023-09-14

申请号：US18065208

申请日：2022-12-13

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： 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分类号： 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分类号： 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

摘要： 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.