公开(公告)号：SG10201804026WA

公开(公告)日：2018-06-28

申请号：SG10201804026W

申请日：2014-11-12

Applicant: VERTEX PHARMA

Inventor： NTI-ADDAE KWAME ,  WALDO MICHAEL ,  O'NEIL SIMON ,  VAN ALSTEN JOHN ,  MACIKENAS DAINIUS ,  MUDUNURI PRAVEEN ,  SHI YI ,  LEDEBOER MARK ,  JURKAUSKAS VALDAS ,  MEDEK ALES ,  JONES STEVEN ,  BYRN RANDAL ,  ASMAL MOHAMMED ,  ROBERTSON SARAH ,  TSAI WANJUNG

Abstract: INHIBITORS OF INFLUENZA VIRUSES REPLICATION Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: are Form A of HCl salt of Compound (1)·1/2 Η20, Form F of HCl salt of Compound (1)·3 Η20, Form D of HCl salt of Compound (1), Form A of Compound (1), and Form A of tosylate salt of Compound (1). Such polymorphic forms are employed for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.

公开(公告)号：AU2016259327A1

公开(公告)日：2016-12-01

申请号：AU2016259327

申请日：2016-11-15

Applicant: VERTEX PHARMA

Inventor： VAN GOOR FREDERICK F ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  ALCACIO TIM EDWARD ,  JOHNSTON STEVEN C ,  KESHAVARZ-SHOKRI ALI ,  LEE ELAINE CHUNGMIN ,  MEDEK ALES ,  SULLIVAN MARK JEFFREY ,  ZAMAN NOREEN TASNEEM ,  ZHANG BEILI ,  ZHANG YUEGANG ,  ZLOKARNIK GREGOR ,  AREKAR SNEHA G ,  KADIYALA IRENA 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. WRw5 o 0 WRW4 WRw2 Formula I 0 /0 1 0 |0 Formula II R4 R4 R 4 R6 Ry Formula III

公开(公告)号：PE20161022A1

公开(公告)日：2016-11-12

申请号：PE2016000512

申请日：2014-10-17

Applicant: VERTEX PHARMA

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

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

Abstract: Se refiere a un cocristal que comprende un compuesto de formula I, donde R1 y R2 son hidrogeno o deuterio; y un formador de cocristales tales como acido adipico, acido citrico, acido fumarico, acido maleico, acido succinico o acido benzoico. Son compuestos preferidos: (S)-N-4-metil-2-(8-((1´-metil-[2’-bipirimidin]-4,5-il)amino)propan-6-il)quinolina-2-carboxamida y (S)-N-metil-8-(1-((2’-metil-4’,6’-dideuterio-[4,5’-bipirimidin]-4,5-il)amino)propan-6-il)quinolina-2-carboxamida. Dichos cocristales tienen picos de difraccion de rayos X aproximadamente a 6,46, 7,91, 11,92, 12,26, 12,99, 14,19, 18,68 y 19,07-Theta. Tambien se refiere a una composicion farmaceutica y a un metodo de preparacion. Dichos cocristales inhiben la proteina quinasa dependiente de ADN (DNA-PK) y son utiles en el tratamiento del cancer

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：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：AU2008301907B2

公开(公告)日：2014-02-20

申请号：AU2008301907

申请日：2008-09-15

Applicant: VERTEX PHARMA

Inventor： ZHANG YUEGANG ,  LOOKER ADAM ,  DEMATTEI JOHN ,  ROEPER STEFANIE ,  HARRISON CRISTIAN ,  FENG YUSHI ,  MUDUNURI PRAVEEN

IPC: C07D215/233

Abstract: Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.

公开(公告)号：NZ600865A

公开(公告)日：2014-01-31

申请号：NZ60086508

申请日：2008-09-15

Applicant: VERTEX PHARMA

Inventor： FENG YUSHI ,  LOOKER ADAM ,  ZHANG YUEGANG ,  DEMATTEI JOHN ,  MUDUNURI PRAVEEN ,  ROEPER STEFANIE ,  HARRISON CRISTIAN

IPC: A61K31/47 ,  A61P3/00 ,  A61P3/10 ,  A61P25/28 ,  A61P27/02 ,  A61P35/00 ,  C07D215/233

Abstract: 600865 Disclosed is N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1)• PEG 400 (polyethylene glycol)•KOAc (potassium acetate). Also disclosed are crystalline form and x-ray powder diffraction patterns of Compound 1•PEG 400•KOAc, pharmaceutical combinations comprising Compound 1•PEG 400•KOAc, methods of making Compound 1•PEG 400•KOAc and the use of Compound 1•PEG 400•KOAc in the manufacture of a medicament. The medicament is useful in the treatment of cystic fibrosis, hereditary emphysema, hereditary hemochromatosis, coagulation- fibrinolysis deficiencies, lipid processing deficiencies, lysosomal storage diseases, neurodegenerative diseases, polyglutamine neurological disorders, spongiform encephalopathies, COPD, dry-eye disease, and Sjogren’s disease.

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：AU2011227021A1

公开(公告)日：2012-10-18

申请号：AU2011227021

申请日：2011-03-21

Applicant: VERTEX PHARMA

Inventor： AREKAR SNEHA G ,  JOHNSTON STEVEN C ,  KRAWIEC MARIUSZ ,  MEDEK ALES ,  MUDUNURI PRAVEEN ,  SULLIVAN MARK JEFFREY

IPC: C07D215/56 ,  A61K31/47 ,  A61P11/00

Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.