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：AU2016259327A1

公开(公告)日：2016-12-01

申请号：AU2016259327

申请日：2016-11-15

Applicant: VERTEX PHARMA

Inventor： VAN GOOR FREDERICK F ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  ALCACIO TIM EDWARD ,  JOHNSTON STEVEN C ,  KESHAVARZ-SHOKRI ALI ,  LEE ELAINE CHUNGMIN ,  MEDEK ALES ,  SULLIVAN MARK JEFFREY ,  ZAMAN NOREEN TASNEEM ,  ZHANG BEILI ,  ZHANG YUEGANG ,  ZLOKARNIK GREGOR ,  AREKAR SNEHA G ,  KADIYALA IRENA NIKOLAEVNA ,  MUDUNURI PRAVEEN ,  KRAWIEC MARIUSZ

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

Abstract: 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. WRw5 o 0 WRW4 WRw2 Formula I 0 /0 1 0 |0 Formula II R4 R4 R 4 R6 Ry Formula III

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.

公开(公告)号：AU2012377446A1

公开(公告)日：2014-10-23

申请号：AU2012377446

申请日：2012-04-20

Applicant: VERTEX PHARMA

Inventor： LUISI BRIAN ,  AREKAR SNEHA GHANSHYAM ,  COSTACHE ADRIANA ,  DINEHART KIRK RAYMOND ,  JOHNSTON STEVEN C ,  NEUBERT-LANGILLE BOBBIANNA J

IPC: C07D215/56 ,  A61K31/47 ,  A61P25/00

Abstract: The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1- dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith.

公开(公告)号：AU2011242452A1

公开(公告)日：2012-11-08

申请号：AU2011242452

申请日：2011-04-22

Applicant: VERTEX PHARMA

Inventor： VAN GOOR FREDRICK F ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  ALCACIO TIM EDWARD ,  AREKAR SNEHA G ,  JOHNSTON STEVEN C ,  KADIYALA IRINA NIKOLAEVNA ,  KESHAVARZ-SHOKRI ALI ,  KRAWIEC MARIUSZ ,  LEE ELAINE CHUNGMIN ,  MEDEK ALES ,  MUDUNURI PRAVEEN ,  SULLIVAN MARK JEFFREY ,  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 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：AU2011227021A1

公开(公告)日：2012-10-18

申请号：AU2011227021

申请日：2011-03-21

Applicant: VERTEX PHARMA

Inventor： AREKAR SNEHA G ,  JOHNSTON STEVEN C ,  KRAWIEC MARIUSZ ,  MEDEK ALES ,  MUDUNURI PRAVEEN ,  SULLIVAN MARK JEFFREY

IPC: C07D215/56 ,  A61K31/47 ,  A61P11/00

Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

公开(公告)号：MX2011008499A

公开(公告)日：2011-09-06

申请号：MX2011008499

申请日：2010-02-12

Applicant: VERTEX PHARMA

Inventor： SNOONIAN JOHN R ,  VLAHOVA PETINKA ,  EDDLESTON MARK ,  HURREY MICHAEL ,  ALARGOV DIMITAR ,  JOHNSTON STEVEN C ,  ROEPER STEFANIE ,  COWANS BRETT A ,  EBERLIN ALEXANDERS ,  FRAMPTON CHRISTOPHER

IPC: C07D213/82 ,  A61K31/4418

Abstract: Esta invención se refiere a formas sólidas de 2-(2,4-difluorofenil)-6-(1-(2,6-difluorofenil)ureido)nicotinamida y composiciones farmacéuticas de la misma, y métodos y usos con las mismas.

公开(公告)号：AU2010213628A1

公开(公告)日：2011-09-01

申请号：AU2010213628

申请日：2010-02-12

Applicant: VERTEX PHARMA

Inventor： MICHAEL HURREY ,  DIMITAR ALARGOV ,  JOHNSTON STEVEN C ,  STEFANIE ROEPER ,  SNOONIAN JOHN R ,  COWANS BRETT A ,  PETINKA VLAHOVA ,  ALEXANDER EBERLIN ,  MARK EDDLESTON ,  CHRISTOPHER FRAMPTON

IPC: C07D213/82 ,  A61K31/4418

Abstract: This invention relates to solid forms of 2-(2, 4-difluorophenyl)-6-(l- (2,6-difluorophenyl)ureido)nicotinamide and pharmaceutical compositions thereof, and methods and uses therewith.