公开(公告)号：CA3140039A1

公开(公告)日：2020-12-10

申请号：CA3140039

申请日：2020-05-14

Applicant: VERTEX PHARMA

Inventor： BANDARAGE UPUL KEERTHI ,  BLIGH CAVAN MCKEON ,  BOUCHER DIANE ,  BOYD MICHAEL JOHN ,  BRODNEY MICHAEL AARON ,  CLARK MICHAEL PHILIP ,  DAMAGNEZ VERONIQUE ,  FANNING LEV TYLER DEWEY ,  FIMOGNARI ROBERT FRANCIS ,  FLEMING GABRIELLE SIMONE ,  GAGNON KEVIN JAMES ,  GARCIA BARRANTES PEDRO MANUEL ,  GIACOMETTI ROBERT DANIEL ,  GIROUX SIMON ,  GREY JR RONALD LEE ,  GUIDO SAMANTHA ,  HALL AMY BETH ,  HOOD SARAH CAROL ,  HURLEY DENNIS JAMES ,  JOHNSON JR ,  JONES PETER ,  KESAVAN SARATHY ,  LAI MEI-HSIU ,  LIU SIYING ,  LOOKER ADAM ,  MAXWELL BRAD ,  MAXWELL JOHN PATRICK ,  MEDEK ALES ,  NUHANT PHILIPPE MARCEL ,  OVERHOFF KIRK ALAN ,  RODAY SETU ,  ROEPER STEFANIE ,  RONKIN STEVEN M ,  SAWANT RUPA ,  SHI YI ,  SHRESTHA MUNA ,  SPOSATO MARISA ,  STAVROPOULOS KATHY ,  SWETT REBECCA JANE ,  TANG QING ,  TAPLEY TIMOTHY LEWIS ,  THOMSON STEPHEN ,  XU JINWANG ,  ZAKY MARIAM ,  COTTRELL KEVIN MICHAEL

IPC: A61K31/4162 ,  A61K31/429 ,  A61P1/16 ,  A61P11/00 ,  C07D231/56 ,  C07D487/04 ,  C07D498/18 ,  C07D513/04

Abstract: 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：PH12020500066A1

公开(公告)日：2020-09-28

申请号：PH12020500066

申请日：2020-01-08

Applicant: VERTEX PHARMA

Inventor： AHMAD NADIA ,  ANDERSON COREY ,  ARUMUGAM VIJAYALAKSMI ,  ASGIAN IULIANA LUCI ,  CAMP JOANNE LOUISE ,  FANNING LEV TYLER DEWEY ,  HADIDA RUAH SARA SABINA ,  HURLEY DENNIS ,  SCHMIDT YVONNE ,  SHAW DAVID ,  PATEL URVI ,  THOMSON STEPHEN ANDREW ,  MEIRELES LIDIO MARX CARVALHO

IPC: C07C237/42 ,  A61K31/165 ,  A61P29/02 ,  C07D213/81 ,  C07D213/82

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：MA49566A

公开(公告)日：2020-05-20

申请号：MA49566

申请日：2018-07-11

Applicant: VERTEX PHARMA

Inventor： AHMAD NADIA ,  ANDERSON COREY ,  ARUMUGAM VIJAYALAKSMI ,  ASGIAN IULIANA LUCI ,  CAMP JOANNE LOUISE ,  FANNING LEV TYLER DEWEY ,  HADIDA RUAH SARA SABINA ,  HURLEY DENNIS ,  MEIRELES LIDIO MARX CARVALHO ,  PATEL URVI ,  SCHMIDT YVONNE ,  SHAW DAVID ,  THOMSON STEPHEN ANDREW

IPC: A61K31/165 ,  A61P29/02 ,  C07C237/42 ,  C07D213/81 ,  C07D213/82

公开(公告)号：MX2013010476A

公开(公告)日：2013-10-30

申请号：MX2013010476

申请日：2012-03-13

Applicant: VERTEX PHARMA

Inventor： HADIDA-RUAH SARA SABINA ,  MILLER MARK THOMAS ,  ARUMUGAM VIJAYALAKSMI ,  DENINNO MICHAEL PAUL ,  FRIEMAN BRYAN A ,  BINCH HAYLEY MARIE ,  FANNING LEV TYLER DEWEY ,  GROOTENHUIS PETER DIEDERIK JAN ,  HILGRAF NICOLE ,  JOSHI PRAMOD ,  KALLEL EDWARD ADAM ,  PONTILLO JOSEPH ,  SILINA ALINA ,  SHETH URVI JAGDISHBHAI ,  HURLEY DENNIS JAMES

IPC: C07D498/10 ,  A61K31/424 ,  A61P29/00

Abstract: La invención se refiere a compuestos de morfolina-piperidina espirocíclica-amida útiles como inhibidores de canales iónicos. La invención también proporciona composiciones farmacéuticamente aceptables que comprenden los compuestos de la invención y métodos para usar las composiciones en el tratamiento de varios trastornos.

公开(公告)号：AU2011242454A1

公开(公告)日：2012-11-08

申请号：AU2011242454

申请日：2011-04-22

Applicant: VERTEX PHARMA

Inventor： VAN GOOR FREDRICK F ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  ALCACIO TIM EDWARD ,  AREKAR SNEHA G ,  BINCH HAYLEY MARIE ,  BOTFIELD MARTYN CURTIS ,  FANNING LEV TYLER DEWEY ,  GROOTENHUIS PETER DIEDERIK JAN ,  HURLEY DENNIS JAMES ,  JOHNSTON STEVEN C ,  KADIYALA IRINA NIKOLAEVNA ,  KAUSHIK RITU ROHIT ,  KESHAVARZ-SHOKRI ALI ,  KRAWIEC MARIUSZ ,  LEE ELAINE CHUNGMIN ,  LUISI BRIAN ,  MEDEK ALES ,  MUDUNURI PRAVEEN ,  NUMA MEHDI ,  SHETH URVI JAGDISHBHAI ,  SILINA ALINA ,  SULLIVAN MARK JEFFREY ,  VERWIJS MARINUS JACOBUS ,  YANG XIAOQING ,  YOUNG CHRISTOPHER RYAN ,  ZAMAN NOREEN TASNEEM ,  ZHANG BEILI ,  ZHANG YUEGANG ,  ZLOKARNIK GREGOR

IPC: A61K31/4704 ,  A61K31/404 ,  A61K31/443

Abstract: 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.

公开(公告)号：CA2796602A1

公开(公告)日：2011-10-27

申请号：CA2796602

申请日：2011-04-22

Applicant: VERTEX PHARMA

Inventor： VAN GOOR FREDRICK F ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  ALCACIO TIM EDWARD ,  AREKAR SNEHA G ,  BINCH HAYLEY MARIE ,  BOTFIELD MARTYN CURTIS ,  FANNING LEV TYLER DEWEY ,  GROOTENHUIS PETER DIEDERIK JAN ,  HURLEY DENNIS JAMES ,  JOHNSTON STEVEN C ,  KADIYALA IRINA NIKOLAEVNA ,  KAUSHIK RITU ROHIT ,  KESHAVARZ-SHOKRI ALI ,  KRAWIEC MARIUSZ ,  LEE ELAINE CHUNGMIN ,  LUISI BRIAN ,  MEDEK ALES ,  MUDUNURI PRAVEEN ,  NUMA MEHDI ,  SHETH URVI JAGDISHBHAI ,  SILINA ALINA ,  SULLIVAN MARK JEFFREY ,  VERWIJS MARINUS JACOBUS ,  YANG XIAOQING ,  YOUNG CHRISTOPHER RYAN ,  ZAMAN NOREEN TASNEEM ,  ZHANG BEILI ,  ZHANG YUEGANG ,  ZLOKARNIK GREGOR

IPC: A61K31/4704 ,  A61K31/404 ,  A61K31/443

Abstract: 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.

公开(公告)号：HK1088314A1

公开(公告)日：2006-11-03

申请号：HK06108587

申请日：2006-08-02

Applicant: VERTEX PHARMA

Inventor： GONZALES JESUS E III ,  WILSON DEAN MITCHELL ,  TERMIN ANDREAS PETER ,  GROOTENHUIS PETER DIEDERIK JAN ,  ZHANG YULIAN ,  PETZOLDT BENJAMIN JOHN ,  FANNING LEV TYLER DEWEY ,  NEUBERT TIMOTHY DONALD ,  TUNG ROGER D ,  MARTINBOROUGH ESTHER ,  ZIMMERMANN NICOLE

IPC: A61K20060101 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  C07D20060101 ,  C07D239/91 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium 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：NO20054546A

公开(公告)日：2005-11-25

申请号：NO20054546

申请日：2005-10-03

Applicant: VERTEX PHARMA

Inventor： GONZALES III JESUS E ,  WILSON DEAN MIRCHELL ,  TERMIN ANDREAS PETER ,  GROOTENHUIS PETER DIEDERIK JAN ,  ZHANG YULIAN ,  PETZOLDT BENJAMIN JOHN ,  FANNING LEV TYLER DEWEY ,  NEUBERT TIMOTHY DONALD ,  TUNG ROGER D ,  MARTINBOROUGH ESTHER ,  ZIMMERMANN NICOLE

IPC: C07D239/94 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  C07D20060101 ,  C07D239/91 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D239/94 ,  C07D239/91 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

公开(公告)号：PE10592004A1

公开(公告)日：2005-02-07

申请号：PE0002362004

申请日：2004-03-03

Applicant: VERTEX PHARMA

Inventor： WILSON DEAN MITCHELL ,  TERMIN ANDREAS PETER ,  GROOTENHUIS PETER DIEDERIK JAN ,  PETZOLDT BENJAMIN JOHN ,  NEUBERT TIMOTHY DONALD ,  GONZALES III JESUS E ,  ZIMMERMANN NICOLE ,  MARTINBOROUGH ESTHER ,  TUNG ROGER D ,  FANNING LEV TYLER DEWEY ,  ZHANG YULIAN

IPC: A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  C07D20060101 ,  C07D239/91 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D239/94 ,  C07D239/91 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: SE REFIERE A QUINAZOLINAS DE FORMULA I DONDE R1 Y R2 JUNTO A ATOMO DE N AL CUAL ESTAN ENLAZADOS FORMAN UN MONOCICLICO O BICICLICO SATURADO CON 3 A 12 MIEMBROS; EL ANILLO A ES UN ARILO MONOCICLICO CON 5 A 7 MIEMBROS O UN ANILLO BICICLICO DE 8 A 10 MIEMBROS QUE CONTIENE 0 A 3 HETEROATOMOS SELECCIONADOS DE N, O, S; x ES 0 A 4; R3, R4 Y R5 SON Q-RX DONDE Q ES UN ENLACE O UNA CADENA ALQUILIDENO CARACTERIZADO PORQUE HASTA DOS UNIDADES DE METILENO NO ADYACENTE DE Q SON REEMPLAZADAS POR -NR-, -S-, -O-, -CS, -CO2-, ENTRE OTROS; CADA R ES H, GRUPO ALIFATICO C1-C6, DONDE CADA OCURRENCIA DE R' ES H, GRUPO ALIFATICO C1-C6, ANILLO MONOCICLO SATURADO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS 2-(2-METOXI-FENIL)-7-TRIFLUOROMETIL-3H-QUINAZOLIN-4-ONA ENTRE OTROS. LOS COMPUESTOS DE FORMULA I ACTUAN COMOMODULADORES DE CANALES IONICOS SODICOS Y CALCICOS Y SON UTILES PARA EL TRATAMIENTO DE DOLOR, ARTRITIS, MIGRANA, TRASTORNOS NEURODEGENARATIVOS

公开(公告)号：NZ603043A

公开(公告)日：2015-02-27

申请号：NZ60304311

申请日：2011-04-22

Applicant: VERTEX PHARMA

Inventor： SHETH URVI JAGDISHBHAI ,  BOTFIELD MARTYN CURTIS ,  ALCACIO TIM EDWARD ,  YANG XIAOQING ,  SULLIVAN MARK JEFFREY ,  HURLEY DENNIS JAMES ,  AREKAR SNEHA G ,  KESHAVARZ-SHOKRI ALI ,  ZHANG BEILI ,  ZLOKARNIK GREGOR ,  KRAWIEC MARIUSZ ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  ZHANG YUEGANG ,  BINCH HAYLEY MARIE ,  FANNING LEV TYLER DEWEY ,  JOHNSTON STEVEN C ,  YOUNG CHRISTOPHER RYAN ,  NUMA MEHDI ,  SILINA ALINA ,  GROOTENHUIS PETER DIEDERIK JAN ,  VAN GOOR FREDRICK F ,  ZAMAN NOREEN TASNEEM ,  MUDUNURI PRAVEEN ,  KAUSHIK RITU ROHIT ,  MEDEK ALES ,  KADIYALA IRINA NIKOLAEVNA ,  LEE ELAINE CHUNGMIN ,  LUISI BRIAN ,  VERWIJS MARINUS JACOBUS

IPC: A61K31/443 ,  A61K31/36 ,  A61K31/47 ,  C07D213/75 ,  C07D215/233 ,  C07D215/56 ,  C07D317/46

Abstract: Disclosed is a pharmaceutical composition comprising: Compound 1 SDD Formulation and Compound 3 Form I Tablet Formulation wherein: Compound 1 SDD Formulation is a spray dried dispersion of ivacaftor (VX-770), which comprises from about 45 wt% to about 85 wt% of substantially amorphous ivacaftor by weight of the dispersion, from about 14.45 wt% to about 55.55 wt% of hydroxypropylmethylcellulose acetate succinate (HPMCAS) by weight of the dispersion, and from about 0.45 wt% to about 0.55 wt% sodium lauryl sulfate (SLS) by weight of the dispersion; Compound 3 Form I Tablet Formulation comprises: crystalline form I of lumacaftor (VX-809) (characterized by one or more peaks at 15.2 to 15.6 degrees, 16.1 to 16.5 degrees, and 14.3 to 14.7 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation) in an amount ranging from about 20 wt% to about 80 wt% by weight of the composition; a filler comprising microcrystalline cellulose in an amount ranging from about 20 wt% to about 50 wt% by weight of the composition; a disintegrant comprising sodium croscarmellose sodium in an amount ranging from about 1 wt% to about 5 wt% by weight of the composition; a surfactant comprising sodium lauryl sulfate in an amount ranging from about 2 wt% to about 0.3 wt% by weight of the composition; a diluent comprising mannitol in an amount ranging from about 1 wt% to about 30 wt% by weight of the composition; a lubricant comprising magnesium stearate in an amount ranging from about 0.3 wt% to about 5 wt% by weight of the composition; and at least one of: a binder comprising polyvinylpyrrolidone in an amount ranging from about 0.1 wt% to about 5 wt% by weight of the composition and a glidant comprising colloidal silica in an amount ranging from about 0.05 wt% to about 2 wt% by weight of the composition. Also disclosed is the use of the pharmaceutical composition as defined above in the manufacture of a medicament for treating a CFTR mediated disease in a human, wherein the CFTR mediated disease is selected from cystic fibrosis, COPD, emphysema, dry-eye disease or osteoporosis.