公开(公告)号：CA2852991A1

公开(公告)日：2013-05-16

申请号：CA2852991

申请日：2012-11-08

Applicant: VERTEX PHARMA

Inventor： LOOKER ADAM R ,  LITTLER BENJAMIN JOSEPH ,  CHOUDHURY ANUSUYA ,  HARRISON CRISTIAN L ,  VELURI RAVIKANTH ,  RYAN MICHAEL P ,  JIANG LICONG ,  LUSS-LUSIS EDUARD

IPC: C07D405/12 ,  A61K31/405 ,  A61K31/553 ,  A61P1/00 ,  A61P3/00 ,  A61P11/00 ,  A61P25/00 ,  A61P27/00 ,  A61P35/00 ,  C07D405/14 ,  C07D498/04

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR"). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

公开(公告)号：ZA201106619B

公开(公告)日：2012-11-28

申请号：ZA201106619

申请日：2011-09-09

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 FREDERICK F ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

IPC: C07D20060101

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 2; in the presence of a coupling agent.

公开(公告)号：SG174410A1

公开(公告)日：2011-11-28

申请号：SG2011066578

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 FREDERICK F ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

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：AU2010226400A1

公开(公告)日：2011-10-06

申请号：AU2010226400

申请日：2010-03-19

Applicant: VERTEX PHARMA

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

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：CA3071058A1

公开(公告)日：2010-09-23

申请号：CA3071058

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 FREDERICK F ,  BOTFIELD MARTYN C ,  ZLOKARNIK GREGOR

IPC: C07D307/83 ,  C07C68/06 ,  C07D215/56

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 2; in the presence of a coupling agent.

公开(公告)号：CA2756031A1

公开(公告)日：2010-09-23

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：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：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：HRP20170458T1

公开(公告)日：2017-05-19

申请号：HRP20170458

申请日：2017-03-21

Applicant: VERTEX PHARMA

Inventor： LOOKER ADAM R ,  LITTLER BENJAMIN JOSEPH ,  CHOUDHURY ANUSUYA ,  HARRISON CRISTIAN ,  VELURI RAVIKANTH ,  RYAN MICHAEL P ,  JIANG LICONG ,  LUSS-LUSIS EDUARD

IPC: C07D405/12 ,  A61K31/405 ,  A61K31/553 ,  A61P1/00 ,  A61P3/00 ,  A61P11/00 ,  A61P25/00 ,  A61P27/00 ,  A61P35/00 ,  C07D405/14 ,  C07D498/04

公开(公告)号：NZ624440A

公开(公告)日：2016-09-30

申请号：NZ62444012

申请日：2012-11-08

Applicant: VERTEX PHARMA

Inventor： LITTLER BENJAMIN JOSEPH ,  LOOKER ADAM R ,  CHOUDHURY ANUSUYA ,  HARRISON CRISTIAN L ,  VELURI RAVIKANTH ,  RYAN MICHAEL P ,  JIANG LICONG ,  LUSS-LUSIS EDUARD

IPC: C07D405/12 ,  A61K31/405 ,  A61K31/553 ,  A61P1/00 ,  A61P3/00 ,  A61P11/00 ,  A61P25/00 ,  A61P27/00 ,  A61P35/00 ,  C07D209/12 ,  C07D209/24 ,  C07D405/14 ,  C07D498/04

Abstract: Disclosed are indole compounds of formula (II), wherein the substituents are as defined in the specification. The disclosed compounds are useful as modulators of ATP-Binding Cassette (”ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (”CFTR”). An example of a compound of formula (II) is: (R)-2-(5-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-1-(2,3-dihydroxypropyl)-6-fluoro-1H-indol-2-yl)-2- methylpropanoic acid