公开(公告)号：SG10202101979TA

公开(公告)日：2021-04-29

申请号：SG10202101979T

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

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.

公开(公告)号：AU2016211246B2

公开(公告)日：2020-08-27

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：SI3057953T1

公开(公告)日：2018-12-31

申请号：SI201430963

申请日：2014-10-17

Applicant: VERTEX PHARMA

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

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

公开(公告)号：LT3057953T

公开(公告)日：2018-11-26

申请号：LT14799578

申请日：2014-10-17

Applicant: VERTEX PHARMA

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

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

公开(公告)号：AU2018208694A1

公开(公告)日：2018-08-09

申请号：AU2018208694

申请日：2018-07-26

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)- 1 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：SG11201705924RA

公开(公告)日：2017-08-30

申请号：SG11201705924R

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.

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：CA2975048A1

公开(公告)日：2016-08-04

申请号：CA2975048

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：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：BR112013004443A2

公开(公告)日：2016-06-07

申请号：BR112013004443

申请日：2011-08-22

Applicant: VERTEX PHARMA

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

IPC: A61K9/20 ,  A61K31/404

Abstract: composições farmacêuticas de (r)-1-(2,2-difluorbenzo[d][1,3]dioxol-5-il)-n-(1-(2,3-di-hidróxipropil)-6-flúor-2-(1-hidróxi-2-metilpropan-2-il)-indol-5-il)ciclopropano carboxamida e administração das mesmas. uma composição farmacêutica compreendendo composto 1, (r) -1-(2,2-difluorbenzo[d][1,3]dioxol-5-il) -n-(1-(2,3-di-hidróxipropil) -6-flúor-2-(1-hidróxi-2-metilpropan-2-il) -1h-indol-5-il) ciclopropanocarboxamida, e pelo menos um excipiente selecionado dentre: um material de enchimento, um diluente, um desintegrante, um tensoativo, um deslizante e um lubrificante, a composição sendo adequada para administração oral a um paciente em necessidade da mesma para o tratamento de uma doença mediada por cftr, tal como fibrose cística. métodos para o tratamento de um paciente em necessidade do mesmo incluindo administração da composição farmacêutica de composto 1 são também divulgados.