公开(公告)号：NZ595151A

公开(公告)日：2013-11-29

申请号：NZ59515110

申请日：2010-03-19

Applicant: VERTEX PHARMA

Inventor： ZLOKARNIK GREGOR ,  YANG XIAOQING ,  GROOTENHUIS PETER D

IPC: C07D215/233 ,  A61K31/47 ,  A61P3/00

Abstract: ABSTRACT - 595151 Disclosed is a compound of formula (I) which are modulators of cystic fibrosis transmembrane conductance regulator ("CFTR"), wherein R is COOH or CH2OH. These compounds are particularly suitable for treating disease selected from cystic fibrosis, smoke induced COPD, pancreatitis, pancreatic insufficiency, hereditary emphysema, COPD, and dry-eye disease.

公开(公告)号：ZA201200722B

公开(公告)日：2013-05-29

申请号：ZA201200722

申请日：2012-01-30

Applicant: VERTEX PHARMA

Inventor： ROWE WILLIAM ,  HURTER PATRICIA ,  YOUNG CHRISTOPHER R ,  DINEHART KIRK ,  VERWIJS MARINUS JACOBUS ,  OVERHOFF KIRK ,  GROOTENHUIS PETER D J ,  BOTFIELD MARTYN ,  GROSSI ALFREDO ,  ZLOKARNIK GREGOR ,  VAN GOOR FREDRICK F

IPC: A61K20060101 ,  A61P20060101

Abstract: The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

公开(公告)号：ZA201106618B

公开(公告)日：2012-11-28

申请号：ZA201106618

申请日：2011-09-09

Applicant: VERTEX PHARMA

Inventor： YANG XIAOQING ,  HADIDA RUAH SARA S ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDERICK F ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101

Abstract: This invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.

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：AU2007227544B2

公开(公告)日：2012-11-01

申请号：AU2007227544

申请日：2007-03-14

Applicant: VERTEX PHARMA

Inventor： CHEN MINZHANG ,  PERNI ROBERT B ,  ZLOKARNIK GREGOR ,  TANOURY GERALD J ,  JUNG YOUNG CHUN ,  FORSLUND RAYMOND E ,  BENNANI YOUSSEF ,  MALTAIS FRANCOIS

IPC: C07C231/20 ,  A61K31/403 ,  A61K31/422 ,  A61K31/498 ,  A61P31/12 ,  C07C237/04 ,  C07D209/52 ,  C07D403/12 ,  C07D403/14 ,  C07D498/10

Abstract: A deuterated α-ketoamido steric specific compound of the formula (I), wherein D denotes a deuterium atom on a steric specific carbon atom.

公开(公告)号：AU2010282986A1

公开(公告)日：2012-02-16

申请号：AU2010282986

申请日：2010-02-18

Applicant: VERTEX PHARMA

Inventor： ROWE WILLIAM ,  HURTER PATRICIA ,  YOUNG CHRISTOPHER R ,  DINEHART KIRK ,  VERWIJS MARINUS JACOBUS ,  OVERHOFF KIRK ,  GROOTENHUIS PETER D J ,  BOTFIELD MARTYN ,  GROSSI ALFREDO ,  ZLOKARNIK GREGOR ,  VAN GOOR FREDRICK F

IPC: A61K9/14 ,  A61K31/47 ,  A61P19/00 ,  A61P19/10 ,  A61P43/00

Abstract: The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis( 1, 1 -dimethylethyl)-5-hydroxyphenyl]- 1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

公开(公告)号：MX2011009868A

公开(公告)日：2012-01-12

申请号：MX2011009868

申请日：2010-03-19

Applicant: VERTEX PHARMA

Inventor： BOTFIELD MARTYN C ,  GROOTENHUIS PETER D J ,  ZLOKARNIK GREGOR ,  YANG XIAOQING ,  RUAH SARA S HADIDA ,  GOOR FREDRICK F VAN

IPC: C07D215/233 ,  A61K31/47 ,  A61P3/00

Abstract: Esta invención se relaciona con un compuesto de la Fórmula I (ver fórmula (I)) o una sal farmacéuticamente aceptable del mismo, en donde R es COOH o CH2OH.

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：BRPI0709567A2

公开(公告)日：2011-07-12

申请号：BRPI0709567

申请日：2007-03-14

Applicant: VERTEX PHARMA

Inventor： PERNI ROBERT B ,  CHEN MINZHANG ,  JUNG YOUNG CHUN ,  FORSLUND RAYMOND E ,  TANOURY GERALD J ,  BENNANI YOUSSEF ,  ZLOKARNIK GREGOR ,  MALTAIS FRANCOIS

IPC: C07C231/20 ,  A61K31/403 ,  A61K31/422 ,  A61K31/498 ,  A61P31/12 ,  C07C237/04 ,  C07D209/52 ,  C07D403/12 ,  C07D403/14 ,  C07D498/10

Abstract: This invention relates to a process for preparing a compound of Formula 1 wherein: the carbon atoms alpha and beta to the carboxy group are stereocenters; R 1 is independently H, optionally substituted aliphatic, optionally substituted cycloaliphatic, optionally substituted arylaliphatic, optionally substituted heteroaliphatic or optionally substituted heteroarylaliphatic; R' 1 is deuterium such that the deuterium enrichment is at least 50%; R' 2 is -NHR 2 or -OE; R 2 is H, optionally substituted aliphatic, optionally substituted cycloaliphatic, optionally substituted arylaliphatic, optionally substituted heteroaliphatic or optionally substituted heteroarylaliphatic; and E is C 1-6 alkyl or benzyl; wherein the process comprises the steps of: a) forming a salt of a compound of Formula 1, and b) crystallizing said salt to give a compound of greater than 55% enantiomeric excess.

公开(公告)号：CA2646229A1

公开(公告)日：2007-09-27

申请号：CA2646229

申请日：2007-03-14

Applicant: VERTEX PHARMA

Inventor： FORSLUND RAYMOND E ,  JUNG YOUNG CHUN ,  TANOURY GERALD J ,  CHEN MINZHANG ,  MALTAIS FRANCOIS ,  BENNANI YOUSSEF ,  ZLOKARNIK GREGOR ,  PERNI ROBERT B

IPC: C07C231/20 ,  A61K31/403 ,  A61K31/422 ,  A61K31/498 ,  A61P31/12 ,  C07C237/04 ,  C07D209/52 ,  C07D403/12 ,  C07D403/14 ,  C07D498/10

Abstract: This invention relates to a process for preparing a compound of Formula 1 wherein: the carbon atoms alpha and beta to the carboxy group are stereocenters; R 1 is independently H, optionally substituted aliphatic, optionally substituted cycloaliphatic, optionally substituted arylaliphatic, optionally substituted heteroaliphatic or optionally substituted heteroarylaliphatic; R' 1 is deuterium such that the deuterium enrichment is at least 50%; R' 2 is -NHR 2 or -OE; R 2 is H, optionally substituted aliphatic, optionally substituted cycloaliphatic, optionally substituted arylaliphatic, optionally substituted heteroaliphatic or optionally substituted heteroarylaliphatic; and E is C 1-6 alkyl or benzyl; wherein the process comprises the steps of: a) forming a salt of a compound of Formula 1, and b) crystallizing said salt to give a compound of greater than 55% enantiomeric excess.