公开(公告)号：HRP20211752T1

公开(公告)日：2022-02-18

申请号：HRP20211752

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

公开(公告)号：PL3150198T3

公开(公告)日：2022-01-17

申请号：PL16185289

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

公开(公告)号：CA2795804C

公开(公告)日：2021-10-26

申请号：CA2795804

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

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：AU2015205839B2

公开(公告)日：2016-07-07

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：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：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.