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：CA2948104A1

公开(公告)日：2010-05-14

申请号：CA2948104

申请日：2009-11-06

Applicant: VERTEX PHARMA

Inventor： RUAH SARA S HADIDA ,  GROOTENHUIS PETER D J ,  MILLER MARK T ,  MCCARTNEY JASON ,  VAN GOOR FREDRICK ,  NUMA MEHDI MICHEL DJAMEL ,  ZHOU JINGLAN ,  BEAR BRIAN

IPC: C07D405/12 ,  A61K31/404

Abstract: Compounds and pharmaceutically acceptable compositions thereof are disclosed, which may be used as modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR").

公开(公告)号：CA2742821A1

公开(公告)日：2010-05-14

申请号：CA2742821

申请日：2008-11-12

Applicant: VERTEX PHARMA

Inventor： RUAH SARA HADIDA S ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK ,  MILLER MARK T ,  MCCARTNEY JASON ,  ZHOU JINGLAN ,  BEAR BRIAN ,  NUMA MEHDI MICHEL DJAMEL

IPC: C07D405/12 ,  A61K31/404 ,  A61P3/00 ,  A61P25/00

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：CA2741178A1

公开(公告)日：2010-04-29

申请号：CA2741178

申请日：2009-10-23

Applicant: VERTEX PHARMA

Inventor： ZHANG BEILI ,  KRAWIEC MARIUSZ ,  BOTFIELD MARTYN ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK

IPC: C07D215/56 ,  A61K31/4704 ,  A61P1/00 ,  A61P11/00

Abstract: The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith.

公开(公告)号：NZ546365A

公开(公告)日：2010-01-29

申请号：NZ54636504

申请日：2004-10-08

Applicant: VERTEX PHARMA

Inventor： HADIDA RUAH SARA S ,  MILLER MARK T ,  HAMILTON MATTHEW ,  GROOTENHUIS PETER D J ,  SINGH ASHVANI K

IPC: C07D307/87 ,  A61K31/00 ,  A61K31/335 ,  A61K31/38 ,  A61K31/40 ,  A61K31/41 ,  A61K31/435 ,  A61K31/495 ,  A61K45/06 ,  C07C233/11 ,  C07C233/22 ,  C07C233/60 ,  C07C233/65 ,  C07C233/73 ,  C07C235/34 ,  C07C235/46 ,  C07C235/48 ,  C07C307/00 ,  C07C311/16 ,  C07C311/17 ,  C07C323/60 ,  C07D209/42 ,  C07D213/82 ,  C07D215/54 ,  C07D215/56 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D237/28 ,  C07D261/20 ,  C07D307/68 ,  C07D307/85 ,  C07D333/32 ,  C07D333/70 ,  C07D407/12

Abstract: Disclosed is a compound of formula II wherein A is C(O) or SO2, RC and RD taken together form a 3-6 membered cycloalkyl ring; RB is (C1-C4)alkoxy, Z is a substituent of formula I and wherein the rest of the substituents are disclosed within the specification. Also disclosed is the modulating ARP- Binding Cassette (ABC) transporter activity of the compound of formula II.

公开(公告)号：ZA200803887B

公开(公告)日：2009-12-30

申请号：ZA200803887

申请日：2006-11-08

Applicant: VERTEX PHARMA

Inventor： HADIDA RUAH SARA ,  HAMILTON MATTHEW ,  MILLER MARK ,  GROOTENHUIS PETER D J ,  BEAR BRIAN ,  MCCARTHY JASON ,  ZHOU JINGLAN

IPC: A61K20100101 ,  A61P20100101 ,  C07D20100101

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：AU2008322616A1

公开(公告)日：2009-05-22

申请号：AU2008322616

申请日：2008-11-14

Applicant: VERTEX PHARMA

Inventor： RUAH SARA HADIDA ,  BEAR BRIAN ,  GROOTENHUIS PETER D J ,  ZHOU JINGLAN ,  MILLER MARK

IPC: C07D217/22 ,  A61K31/472 ,  A61K31/4725 ,  A61P11/00 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14

公开(公告)号：CA2699382A1

公开(公告)日：2009-03-19

申请号：CA2699382

申请日：2008-09-15

Applicant: VERTEX PHARMA

Inventor： BINCH HAYLEY ,  GROOTENHUIS PETER D J ,  HADIDA RUAH SARA S ,  ZHOU JINGLAN ,  HAZLEWOOD ANNA ,  FANNING LEV T D

IPC: C07D471/04 ,  A61K31/4375 ,  A61P3/00

Abstract: The present invention relates to modulators of ATP-B inding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

公开(公告)号：AU2006331614A1

公开(公告)日：2007-07-05

申请号：AU2006331614

申请日：2006-12-21

Applicant: VERTEX PHARMA

Inventor： ARUMUGAM VIJAYALAKSMI ,  BINCH HAYLEY ,  RUAH SARA HADIDA ,  GUTIERREZ COREY ,  ZHOU JINGLAN ,  GROOTENHUIS PETER D J ,  HAZLEWOOD ANNA

IPC: C07F9/60 ,  A61K31/47 ,  A61K31/661 ,  A61P29/00 ,  A61P31/00 ,  C07D215/56

Abstract: The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.