公开(公告)号：PL2821400T3

公开(公告)日：2018-04-30

申请号：PL14182117

申请日：2010-03-19

Applicant: VERTEX PHARMA

Inventor： DEMATTEI JOHN ,  LOOKER ADAM R ,  NEUBERT-LANGILLE BOBBIANA ,  TRUDEAU MARTIN ,  ROPER STEFANIE ,  RYAN MICHAEL ,  YAP DAHRIKA MILFRED LAO ,  KRUEGER BRIAN R ,  GROOTENHUIS PETER D J ,  VAN GROOR FREDERICK F ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

IPC: C07D215/233

公开(公告)号：AU2016244296B2

公开(公告)日：2018-04-19

申请号：AU2016244296

申请日：2016-10-13

Applicant: VERTEX PHARMA

Inventor： DEMATTEI JOHN ,  LOOKER ADAM R ,  NEUBERT-LANGILLE BOBBIANNA J ,  TRUDEAU MARTIN ,  ROEPER STEFANIE ,  RYAN MICHAEL P ,  GUERETTE DAHRIKA MILFRED LAO YAP ,  KRUEGER BRIAN R ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK F ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

IPC: C07D215/233

Abstract: The invention provides a process for the preparation of a compound of Formula 1, N H (Rx-X H R2 Formula 1 comprising coupling a carboxylic acid of Formula 2 (Rx-X OH Formula 2 with an aniline of Formula 3 Formula 3 in the presence of a coupling agent.

公开(公告)号：LT2821400T

公开(公告)日：2018-02-12

申请号：LT14182117

申请日：2010-03-19

Applicant: VERTEX PHARMA

Inventor： DEMATTEI JOHN ,  LOOKER ADAM R ,  NEUBERT LANGILLE BOBBIANA ,  TRUDEAU MARTIN ,  ROPER STEFANIE ,  RYAN MICHAEL ,  YAP DAHRIKA MILFRED LAO ,  KRUEGER BRIAN R ,  GROOTENHUIS PETER D J ,  VAN GROOR FREDERICK F ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

IPC: C07D215/233

公开(公告)号：CA2756031C

公开(公告)日：2018-01-02

申请号：CA2756031

申请日：2010-03-19

Applicant: VERTEX PHARMA

Inventor： DEMATTEI JOHN ,  LOOKER ADAM R ,  NEUBERT-LANGILLE BOBBIANNA ,  TRUDEAU MARTIN ,  ROEPER STEFANIE ,  RYAN MICHAEL P ,  YAP DAHRIKA MILFRED LAO ,  KRUEGER BRIAN R ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK F ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

IPC: C07D215/233

Abstract: The invention provides a process for the preparation of a compound of Formula 1; comprising coupling a carboxylic acid of Formula 2; with an aniline of Formula 3; in the presence of a coupling agent.

公开(公告)号：NZ624460A

公开(公告)日：2015-12-24

申请号：NZ62446010

申请日：2010-03-19

Applicant: VERTEX PHARMA

Inventor： KRUEGER BRIAN R ,  ROEPER STEFANIE ,  ZLOKARNIK GREGOR ,  NEUBERT-LANGILLE BOBBIANNA ,  TRUDEAU MARTIN ,  YAP DAHRIKA MILFRED LAO ,  LOOKER ADAM R ,  GROOTENHUIS PETER D J ,  DEMATTEI JOHN ,  RYAN MICHAEL P ,  BOTFIELD MARTYN C ,  VAN GOOR FREDRICK F

IPC: C07C201/08 ,  C07B63/04 ,  C07C205/43 ,  C07C209/36 ,  C07C211/45

Abstract: The disclosure provides a process for the preparation of a compound of Formula 8; comprising nitrating a compound of Formula 7; The compound of Formula 5 may further be prepared by reduction of 8. where R2 and R4 are each tert-butyl, and PG is a protecting group such as propoxy formyl, methanesulfonyl, 4-nitrobenzoyl, ethoxy formyl, butoxy formyl, t-butoxy formyl, i-propoxy formyl or methoxy formyl.

公开(公告)号：PT2408750E

公开(公告)日：2015-10-15

申请号：PT10710749

申请日：2010-03-19

Applicant: VERTEX PHARMA

Inventor： GROOTENHUIS PETER D J ,  DEMATTEI JOHN ,  LOOKER ADAM R ,  NEUBERT-LANGILLE BOBBIANNA ,  TRUDEAU MARTIN ,  ROEPER STEFANIE ,  RYAN MICHAEL P ,  YAP DAHRIKA MILFRED LAO ,  KRUEGER BRIAN R ,  GOOR FREDERICK F VAN ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

IPC: C07D215/233

公开(公告)号：NZ600707A

公开(公告)日：2014-09-26

申请号：NZ60070710

申请日：2010-12-10

Applicant: VERTEX PHARMA

Inventor： VAN GOOR FREDRICK F ,  SILINA ALINA ,  SHETH URVI ,  VAIRAGOUNDAR RAJENDRAN ,  HAZLEWOOD ANNA R ,  NUMA MEHDI ,  HADIDA RUAH SARA S ,  BINCH HAYLEY ,  HURLEY DENNIS JAMES ,  FANNING LEV T D ,  BOTFIELD MARTYN C ,  TENHUIS PETER DIEDERIK JAN ,  ZHOU JINGLAN

IPC: C07D215/56 ,  A61K31/47 ,  A61K31/4709 ,  A61P11/00 ,  A61P11/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08 ,  G01N33/50

Abstract: The present disclosure relates to 4-oxo-1H-quinoline-3-carboxamides as modulators of ATP-Binding Cassette (”ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present disclosure also relates to methods of treating ABC transporter mediated diseases using such modulators. 6,7-difluoro-N-(2-fluoro-5-hydroxy-4-tert-butyl-phenyl)-4-oxo-1H-quinoHne-3-carboxarnide; N-[4-(3,3-dimethylpyrrolidin-1-yl)-2-(trifluoromethyl)phenyl]-6-methyl-4-oxo-1H-quinoline-3-carboxamide; 8-cyano-N-(5-hydroxy-2,4-ditert-butyl-phenyl)-4-oxo-1H-quinaline-3-carboxamide; and (2S,3S)-methyl 3-methyl-1-(4-(4-oxo-1,4-dihydroquinoline-3-carboxamide)-3-(trifluoromethyl)phenyl)pyrrolidine-2-carboxylate. conditions which may be treated by the compounds of the disclosure include: cystic fibrosis, chronic bronchitis, recurrent bronchitis, acute bronchitis, male infertility caused by congenital bilateral absence of the vas deferens (CBAVD), female infertility caused by congenital absence of the uterus and vagina (CAUV), idiopathic chronic pancreatitis (ICP), idiopathic recurrent pancreatitis, idiopathic acute pancreatitis, chronic rhinosinusitis, primary sclerosing cholangitis, diabetes, dry eye, constipation, allergic bronchopulmonary aspergillosis (ABPA), bone diseases, and asthma

公开(公告)号：MX2012006764A

公开(公告)日：2012-11-23

申请号：MX2012006764

申请日：2010-12-10

Applicant: VERTEX PHARMA

Inventor： BOTFIELD MARTYN C ,  SILINA ALINA ,  BINCH HAYLEY ,  ZHOU JINGLAN ,  FANNING LEV T D ,  SHETH URVI ,  RUAH SARA S HADIDA ,  GOOR FREDRICK F VAN ,  HURLEY DENNIS JAMES ,  NUMA MEHDI ,  VAIRAGOUNDAR RAJENDRA ,  HAZLEWOOD ANNA R ,  GROOTENHUIS PETER DIEDERIK JAN

IPC: C07D215/56 ,  A61K31/4709 ,  A61P11/00 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08

Abstract: La presente invención se relaciona con 4-oxo-1H-quinolin-3-carboxa midas como moduladores de transportadores del Casete de Unión con ATP ("ABC") o fragmentos de los mismos, entre los que se incluyen el Regulador de Conductancia Transmembrana de Fibrosis Quística, las composiciones de los mismos, y los métodos con los mismos. La presente invención también se relaciona con los métodos para tratar enfermedades provocadas por el transportador del ABC utilizando estos moduladores.

公开(公告)号：ZA201101097B

公开(公告)日：2012-05-30

申请号：ZA201101097

申请日：2011-02-10

Applicant: VERTEX PHARMA

Inventor： ROWE WILLIAM ,  HURTER PATRICIA ,  YOUNG CHRISTOPHER ,  DINEHART KIRK ,  VERWIJS MARINUS JACOBUS ,  OVERHOFF KIRK ,  GROOTENHUIS PETER D J ,  BOTFIELD MARTYN C ,  GROSSI ALFREDO

IPC: A61K20060101

Abstract: The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

公开(公告)号：MX2011009867A

公开(公告)日：2012-01-12

申请号：MX2011009867

申请日：2010-03-19

Applicant: VERTEX PHARMA

Inventor： TRUDEAU MARTIN ,  BOTFIELD MARTYN C ,  GROOTENHUIS PETER D J ,  DEMATTEI JOHN ,  ZLOKARNIK GREGOR ,  LOOKER ADAM R ,  ROEPER STEFANIE ,  NEUBERT-LANGILLE BOBBIANNA ,  RYAN MICHAEL P ,  YAP DAHRIKA MILFRED LAO ,  KRUEGER BRIAN R ,  GOOR FREDERICK F VAN

IPC: C07D215/233

Abstract: La invención proporciona un proceso para la preparación de un compuesto de la Fórmula I (ver fórmula (1), que comprende acoplar un ácido carboxílico de la Fórmula 2 (ver fórmula (2)); con una anilina de la Fórmula 3 (ver fórmula (3)); en presencia de un agente de acoplamiento.