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：AU2016211246A1

公开(公告)日：2017-08-10

申请号：AU2016211246

申请日：2016-01-29

Applicant: BIOMED VALLEY DISCOVERIES INC ,  VERTEX PHARMA

Inventor： DECRESCENZO GARY ,  WELSCH DEAN ,  VLAHOVA PETINKA I ,  BOERRIGTER STEPHAN X M ,  ARONOV ALEXANDER ,  KESHAVARZ-SHOKRI ALI ,  SCANGAS ALEXANDER N ,  STAVROPOULOS KATHY ,  LITTLER BENJAMIN ,  KADIYALA IRINA NIKOLAEVNA ,  ALARGOVA ROSSITZA GUEORGUIEVA

IPC: C07D401/04

Abstract: The present invention provides crystalline forms of a compound of formula (I). Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer. It has been discovered that crystalline forms of 4-(5-Chloro-2- isopropylaminopyridin-4-yl)-1 H-pyrrole-2-carboxylic acid [1 -(3-chlorophenyl)-2- hydroxyethyl]amide can be prepared which exhibit improved properties, e.g. surprisingly improved stability and improved solubility characteristics. Thus, the present invention provides crystalline 4-(5-Chloro-2- isopropylaminopyridin-4-yl)-1H-pyrrole-2-carboxylic acid [1 -(3-chlorophenyl)-2- hydroxyethyljamide.

公开(公告)号：AU2008333845B2

公开(公告)日：2013-07-18

申请号：AU2008333845

申请日：2008-12-04

Applicant: VERTEX PHARMA

Inventor： KESHAVARZ-SHOKRI ALI ,  KRAWIEC MARIUSZ ,  ZHANG BEILI

IPC: C07D405/12 ,  A61K31/443 ,  A61P11/00

Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(l-(2,2-difluorobenzo[d][l,3]dioxol-5-yl) cyclopropanecarboxamido)-3- methylPyridin-2-yl)benzoic acid (Form I) of following formula: (I), pharmaceutical compositions thereof, and methods of treatment therewith.

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：NZ585880A

公开(公告)日：2012-08-31

申请号：NZ58588008

申请日：2008-12-04

Applicant: VERTEX PHARMA

Inventor： KESHAVARZ-SHOKRI ALI ,  ZHANG BEILI ,  KRAWIEC MARIUSZ

IPC: C07D405/12 ,  A61K31/443 ,  A61P11/00

Abstract: Disclosed is a crystalline polymorph of 3-(6-(1-(2,2-Difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid, characterized by XRPD as Form I, and a method for its preparation. Form I is 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. The crystalline polymorph is useful for treating 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：CA2986286A1

公开(公告)日：2009-06-11

申请号：CA2986286

申请日：2008-12-04

Applicant: VERTEX PHARMA

Inventor： KESHAVARZ-SHOKRI ALI ,  ZHANG BEILI ,  KRAWIEC MARIUSZ

IPC: A61K31/47 ,  A61K31/443

Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.

公开(公告)号：CA2706920A1

公开(公告)日：2009-06-11

申请号：CA2706920

申请日：2008-12-04

Applicant: VERTEX PHARMA

Inventor： KESHAVARZ-SHOKRI ALI ,  ZHANG BEILI ,  KRAWIEC MARIUSZ

IPC: C07D405/12 ,  A61K31/443 ,  A61P11/00

Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(l-(2,2-difluorobenzo[d][l,3]dioxol-5-yl) cyclopropanecarboxamido)-3- methylPyridin-2-yl)benzoic acid (Form I) of following formula: (I), pharmaceutical compositions thereof, and methods of treatment therewith.

公开(公告)号：AU2008333845A1

公开(公告)日：2009-06-11

申请号：AU2008333845

申请日：2008-12-04

Applicant: VERTEX PHARMA

Inventor： KESHAVARZ-SHOKRI ALI ,  ZHANG BEILI ,  KRAWIEC MARIUSZ

IPC: C07D405/12 ,  A61K31/443 ,  A61P11/00

Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.

公开(公告)号：HUE062892T2

公开(公告)日：2023-12-28

申请号：HUE20206423

申请日：2011-03-25

Applicant: VERTEX PHARMA

Inventor： KESHAVARZ-SHOKRI ALI ,  ZHANG BEILI ,  ALCACIO TIM EDWARD ,  LEE ELAINE CHUNGMIN ,  ZHANG YUEGANG ,  KRAWIEC MARIUSZ

IPC: C07D405/12