公开(公告)号：SG11201602962PA

公开(公告)日：2016-05-30

申请号：SG11201602962P

申请日：2014-10-17

Applicant: VERTEX PHARMA

Inventor： NTI-ADDAE KWAME WIREDU ,  O'NEIL SIMON ADAM ,  ZHANG YUEGANG ,  WALDO MICHAEL ,  MUDUNURI PRAVEEN ,  SONG BIN ,  VAN ALSTEN JOHN GREGG ,  STROHMEIER MARK ,  STAVROPOULOS KATHY ,  KADIYALA IRINA NIKOLAEVNA ,  NAVAMAL METTACHIT

IPC: C07D401/14 ,  A61K31/506 ,  A61P35/00

Abstract: The present invention relates to compositions and co-crystals each comprising a compound of formula I having the structure: wherein each of R 1 and R 2 is H or 2 H and a co-crystal former selected from adipic acid, citric acid, fumaric acid, maleic acid, succinic acid, or benzoic acid. Also within the scope of this invention are methods of making and using the same.

公开(公告)号：AU2011237601B2

公开(公告)日：2015-08-20

申请号：AU2011237601

申请日：2011-04-07

Applicant: VERTEX PHARMA

Inventor： VERWIJS MARINUS JACOBUS ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  KAUSHIK RITU ROHIT ,  KADIYALA IRINA NIKOLAEVNA ,  YOUNG CHRISTOPHER RYAN

IPC: A61K9/20

Abstract: A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2- difluorobenzo [d] [ 1,3 ] dioxol-5 -y1) cyclopropanecarboxamido)-3 -methylpyridin-2-y1)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.

公开(公告)号：AU2015205839A1

公开(公告)日：2015-08-13

申请号：AU2015205839

申请日：2015-07-21

Applicant: VERTEX PHARMA

Inventor： VERWIJS MARINUS JACOBUS ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  KAUSHIK RITU ROHIT ,  KADIYALA IRINA NIKOLAEVNA ,  YOUNG CHRISTOPHER RYAN

IPC: A61K9/20

Abstract: PHARMACEUTICAL COMPOSITIONS OF 3-(6-(1-(2,2 DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3 METHYLPYRIDIN-2-YL)BENZOIC ACID AND ADMINISTRATION THEREOF Abstract A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2 difluorobenzo [d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2 yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.

公开(公告)号：AU2011293658B2

公开(公告)日：2015-03-05

申请号：AU2011293658

申请日：2011-08-22

Applicant: VERTEX PHARMA

Inventor： ALARGOVA ROSSITZA GUEORGUIEVA ,  DUNBAR CRAIG ANTONY ,  KADIYALA IRINA NIKOLAEVNA

IPC: A61K9/20 ,  A61K31/404

Abstract: A pharmaceutical composition comprising Compound 1, (R)-l-(2,2-difluorobenzo[d][l,3]dioxol-5-yl)-N-(l-(2,3-dihydroxypropyl)-6-fluoro-2-(l-hydroxy-2- methylpropan-2-yl)-lH-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.

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：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：CA2808501A1

公开(公告)日：2012-03-01

申请号：CA2808501

申请日：2011-08-22

Applicant: VERTEX PHARMA

Inventor： ALARGOVA ROSSITZA GUEORGUIEVA ,  DUNBAR CRAIG ANTONY ,  KADIYALA IRINA NIKOLAEVNA

IPC: A61K9/20 ,  A61K31/404

Abstract: A pharmaceutical composition comprising Compound 1, (R)-l-(2,2-difluorobenzo[d][l,3]dioxol-5-yl)-N-(l-(2,3-dihydroxypropyl)-6-fluoro-2-(l-hydroxy-2- methylpropan-2-yl)-lH-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.

公开(公告)号：DK2037887T3

公开(公告)日：2011-01-03

申请号：DK07795477

申请日：2007-05-30

Applicant: VERTEX PHARMA

Inventor： KADIYALA IRINA NIKOLAEVNA ,  LIN WU ,  HURTER PATRICIA

IPC: A61K9/16 ,  A61K9/20 ,  A61K31/401

公开(公告)号：PT2037887E

公开(公告)日：2010-12-07

申请号：PT07795477

申请日：2007-05-30

Applicant: VERTEX PHARMA

Inventor： KADIYALA IRINA NIKOLAEVNA ,  LIN WU ,  HURTER PATRICIA

IPC: A61K9/16 ,  A61K9/20 ,  A61K31/401