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：HK1173151A1

公开(公告)日：2013-07-05

申请号：HK13100461

申请日：2013-01-11

Applicant: VERTEX PHARMA

Inventor： ZHANG BEILI ,  KRAWIEC MARIUSZ M ,  LUISI BRIAN B ,  MEDEK ALES A

IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101

公开(公告)号：MX2012004791A

公开(公告)日：2013-02-01

申请号：MX2012004791

申请日：2010-10-21

Applicant: VERTEX PHARMA

Inventor： ZHANG BEILI ,  KRAWIEC MARIUSZ ,  LUISI BRIAN ,  MEDEK ALES

IPC: C07D487/08 ,  A61K31/407 ,  A61P11/00

Abstract: La presente invención se relaciona con formas sustancialmente cristalinas y en estado sólido de formas sólidas de N-(4-(7-azabiciclo[2.2.1]heptan-7-il)-2-trifluorometil)fenil)-4-o xo-5-(trifluorometil)-1,4-dihidroquinolin-3-carboxamida (Forma A-HC1, Forma B B-HC1, o cualquier combinación de estas formas), las composiciones farmacéuticamente aceptables de la misma, y los métodos de tratamiento con la misma.

公开(公告)号：MX2012011655A

公开(公告)日：2012-11-23

申请号：MX2012011655

申请日：2011-04-07

Applicant: VERTEX PHARMA

Inventor： KESHAVARZSHOKRI ALI ,  ZHANG BEILI ,  KRAWIEC MARIUSZ

IPC: A61K9/16 ,  A61K9/20 ,  A61K9/28 ,  C07D213/75 ,  C07D405/12 ,  C07D405/14

Abstract: La presente invención se refiere a una forma sustancialmente sólida del ácido 3-(6-(1-(2,2-difluorobenzo[d] [l, 3] dioxol-5-il) ciclopropanocarboxamido)-3-metilpiridin-2-il) benzoico (Compuesto 1, Forma A del solvato y Compuesto 1, Forma A de la sal de HCL), procesos para la elaboración de tales formas, composiciones farmacéuticas de los mismos, y métodos de tratamiento con ellos.

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：CL2012001007A1

公开(公告)日：2012-09-07

申请号：CL2012001007

申请日：2012-04-20

Applicant: VERTEX PHARMA

Inventor： ZHANG BEILI ,  KRAWIEC MARIUSZ ,  LUISI BRIAN ,  MEDEK ALES

IPC: A61K31/407 ,  A61P11/00 ,  C07D487/08

Abstract: FORMAS CRISTALINAS A-HCl, By B-HCL DE N-(4-(7-A2ABlCICLO [22.1]HEPTAN-7-IL)-2-(TRIFLUOROMETlL)FENIL}4{JXo-5(TRIFLUOROMETlL)-l,4-DIHIDROQUINOLlNA-3-EARBOXAMIDA, MODULADOR DE CFRT; COMPOSICIONES FARMACÉUTICAS; MÉTODO PARA MODULAR CFRT; Y SU USO PARA EL TRATAMIENTO DE LA FIBROSIS QUISTlCA, ASMA, ENTRE OTRAS.

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：CA2778493A1

公开(公告)日：2011-04-28

申请号：CA2778493

申请日：2010-10-21

Applicant: VERTEX PHARMA

Inventor： ZHANG BEILI ,  KRAWIEC MARIUSZ ,  LUISI BRIAN ,  MEDEK ALES

IPC: C07D487/08 ,  A61K31/407 ,  A61P11/00

Abstract: The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith.

公开(公告)号：AU2009308241A1

公开(公告)日：2010-04-29

申请号：AU2009308241

申请日：2009-10-23

Applicant: VERTEX PHARMA

Inventor： ZHANG BEILI ,  KRAWIEC MARIUSZ ,  BOTFIELD MARTYN ,  GROOTENHUIS PETER D J ,  GOOR FREDRICK VAN

IPC: C07D215/56 ,  A61K31/4704 ,  A61P1/00 ,  A61P11/00