公开(公告)号：WO2010093889A3

公开(公告)日：2010-10-28

申请号：PCT/US2010024053

申请日：2010-02-12

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

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

IPC: C07D213/82 ,  A61K31/4418

CPC classification number: C07D213/82

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.

Abstract translation: 本发明涉及2-（2,4-二氟苯基）-6-（1-（2,6-二氟苯基）脲基）烟酰胺及其药物组合物的固体形式及其方法和用途。

公开(公告)号：CA2792207A1

公开(公告)日：2011-09-22

申请号：CA2792207

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：NZ603042A

公开(公告)日：2015-02-27

申请号：NZ60304211

申请日：2011-04-22

Applicant: VERTEX PHARMA

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

IPC: A61K31/404 ,  A61K31/36 ,  A61K31/47 ,  C07D209/12 ,  C07D215/233 ,  C07D215/56 ,  C07D317/46

Abstract: Disclosed is a pharmaceutical composition comprising: Compound 1 SDD Formulation and VX-661 in Amorphous Form, 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. 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：CA2869847A1

公开(公告)日：2013-10-24

申请号：CA2869847

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：CA2752544A1

公开(公告)日：2010-08-19

申请号：CA2752544

申请日：2010-02-12

Applicant: VERTEX PHARMA

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

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.

公开(公告)号：CA2796642A1

公开(公告)日：2011-10-27

申请号：CA2796642

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：AU2010213628A2

公开(公告)日：2011-09-29

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.

公开(公告)号：AU2018226453B2

公开(公告)日：2019-07-11

申请号：AU2018226453

申请日：2018-09-06

Applicant: VERTEX PHARMA

Inventor： ALARGOVA ROSSITZA GUEORGUIEVA ,  ALCACIO TIM EDWARD ,  JOHNSTON STEVEN C ,  VAN GOOR FREDRICK F ,  KESHAVARZ-SHOKRI ALI ,  LEE ELAINE CHUNGMIN ,  MEDEK ALES ,  SULLIVAN MARK JEFFREY ,  ZAMAN NOREEN TASNEEM ,  ZHANG BEILI ,  ZHANG YUEGANG ,  ZLOKARNIK GREGOR ,  AREKAR SNEHA G ,  KADIYALA IRINA 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. o o WR W4 N r O H WRw2 Formula I T \ N Formula II R 0 RN, R8 Ry Formula III

公开(公告)号：AU2018226453A1

公开(公告)日：2018-09-27

申请号：AU2018226453

申请日：2018-09-06

Applicant: VERTEX PHARMA

Inventor： ALARGOVA ROSSITZA GUEORGUIEVA ,  ALCACIO TIM EDWARD ,  JOHNSTON STEVEN C ,  VAN GOOR FREDRICK F ,  KESHAVARZ-SHOKRI ALI ,  LEE ELAINE CHUNGMIN ,  MEDEK ALES ,  SULLIVAN MARK JEFFREY ,  ZAMAN NOREEN TASNEEM ,  ZHANG BEILI ,  ZHANG YUEGANG ,  ZLOKARNIK GREGOR ,  AREKAR SNEHA G ,  KADIYALA IRINA 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. o o WR W4 N r O H WRw2 Formula I T \ N Formula II R 0 RN, R8 Ry Formula III

公开(公告)号：NZ602557A

公开(公告)日：2014-09-26

申请号：NZ60255711

申请日：2011-03-21

Applicant: VERTEX PHARMA

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

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

Abstract: The present disclosure relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1, Ivacaftor), pharmaceutical compositions thereof and methods therewith. The compounds are useful in the treatment of CFTR-mediated diseases such as cystic fibrosis.