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：AU2016213697B2

公开(公告)日：2018-04-05

申请号：AU2016213697

申请日：2016-08-08

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-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：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：PE10222016A1

公开(公告)日：2016-11-12

申请号：PE0005122016

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

CPC classification number: A61K31/506 ,  A61K31/337 ,  A61K31/5025 ,  A61K31/513 ,  A61K31/517 ,  A61K31/555 ,  A61K31/704 ,  A61K31/7048 ,  A61K33/24 ,  A61K38/14 ,  A61K39/39558 ,  A61K45/06 ,  A61N2005/1098 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/13 ,  C07C55/10 ,  C07C55/14 ,  C07C57/145 ,  C07C57/15 ,  C07C59/265 ,  C07C63/08 ,  C07D401/14 ,  C07K16/2863 ,  C07K2317/24

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：MX2016004992A

公开(公告)日：2016-07-19

申请号：MX2016004992

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 ,  ALSTEN JOHN GREGG VAN ,  STROHMEIER MARK ,  STAVROPOULOS KATHY ,  KADIYALA IRINA NIKOLAEVNA ,  NAVAMAL METTACHIT

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

Abstract: La presente invención hace referencia a composiciones y cocristales; cada uno comprende un compuesto de la fórmula I que tiene la estructura en donde cada R1 y R2 es H o 2H y un formador de cocristales seleccionado a partir de ácido adípico, ácido cítrico, ácido fumárico, ácido maleico, ácido succínico o ácido benzoico. Además, el alcance de esta invención también abarca los métodos de preparación y uso.

公开(公告)号：AU2013290444A1

公开(公告)日：2015-01-29

申请号：AU2013290444

申请日：2013-07-15

Applicant: VERTEX PHARMA

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

IPC: A61K9/20 ,  A61K31/404 ,  A61K31/47 ,  A61K45/06 ,  A61P43/00

Abstract: A pharmaceutical composition comprising Compound 1, (

公开(公告)号：CA2878057A1

公开(公告)日：2014-01-23

申请号：CA2878057

申请日：2013-07-15

Applicant: VERTEX PHARMA

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

IPC: A61K9/20 ,  A61K31/404 ,  A61K31/47 ,  A61K45/06 ,  A61P43/00

Abstract: A pharmaceutical composition comprising Compound 1, (R)- 1 -(2,2- difluorobenzo[d] [ 1,3]dioxol-5-yl)-N-( 1 -(2,3-dihydroxypropyl)-6-fluoro-2-( 1 -hydroxy-2- methylpropan-2-yl)- l H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from : a filler, 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：ZA201208225B

公开(公告)日：2013-07-31

申请号：ZA201208225

申请日：2012-11-01

Applicant: VERTEX PHARMA

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

IPC: A61K20060101 ,  C07D20060101

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：MX2012011656A

公开(公告)日：2012-11-23

申请号：MX2012011656

申请日：2011-04-07

Applicant: VERTEX PHARMA

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

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

Abstract: Una composición farmacéutica que comprende el Compuesto 1, ácido (3-(6-(1-(2, 2-difluorobenzo[d] [1, 3] dioxol-5-il)ciclopropancarb oxamido)-3-metilpiridin-2-il)benzoico), y al menos un excipiente seleccionado de: un relleno, un diluyente, un disgregante, un agente tensioactivo, un aglutinante, un deslizante y un lubricante, la composición siendo adecuada para administración oral a una paciente en la necesidad de esto para tratar una enfermedad mediada por CFTR tal como Fibrosis Cística. Métodos para tratar un paciente en a necesidad de esto incluyen la administración de una formulación farmacéutica oral del Compuesto 1 al paciente.

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.