公开(公告)号：WO2010053471A8

公开(公告)日：2011-09-22

申请号：PCT/US2008012689

申请日：2008-11-12

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

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

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

CPC classification number: C07D405/12 ,  C07D209/08 ,  C07D209/12 ,  C07D209/18 ,  C07D405/14 ,  C07D487/04

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.

Abstract translation: 本发明化合物及其药学上可接受的组合物可用作ATP结合盒（'ABC'）转运蛋白或其片段的调节剂，包括囊性纤维化跨膜电导调节剂（'CFTR'）。 本发明还涉及使用本发明化合物治疗ABC转运蛋白介导的疾病的方法。

公开(公告)号：WO2009064747A3

公开(公告)日：2010-08-19

申请号：PCT/US2008083165

申请日：2008-11-12

Applicant: VERTEX PHARMA ,  STAMOS DEAN ,  MARTINBOROUGH ESTHER ,  NEUBERT TIMOTHY ,  NUMA MEHDI MICHEL DJAMEL ,  WHITNEY TARA ,  ZIMMERMANN NICOLE ,  KAWATKAR AARTI SAMEER

Inventor： STAMOS DEAN ,  MARTINBOROUGH ESTHER ,  NEUBERT TIMOTHY ,  NUMA MEHDI MICHEL DJAMEL ,  WHITNEY TARA ,  ZIMMERMANN NICOLE ,  KAWATKAR AARTI SAMEER

IPC: C07D417/14 ,  A61K31/427 ,  A61P25/04

CPC classification number: C07D417/14

Abstract: The present invention relates to heterocyclic derivatives of formula I useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, like, e.g. pain., (I) or a pharmaceutically acceptable salt thereof, wherein, independently for each occurrence: ring Z is a thiazole or thiadiazole optionally substituted with 0-2 occurrences of R; V is CH2, NH, O, or S; and R, R1, R2, and R3 are hydrogen, C1-C6 aliphatic, aryl, C3-C8 cycloaliphatic, halo, CN, NO2, CF3, OCF3, OH, NH2, NH(C1-C6 aliphatic), N(C1-C6 aliphatic) 2, COOH, COO(C1 -C6 aliphatic), O(C1-C6 aliphatic), CHF2, or CH2F.

Abstract translation: 本发明涉及可用作离子通道抑制剂的式I的杂环衍生物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法，例如， 疼痛，（I）或其药学上可接受的盐，其中独立地为每次出现：环Z是任选被0-2次出现的R取代的噻唑或噻二唑; V是CH 2，NH，O或S; R 1，R 2和R 3是氢，C 1 -C 6脂族基，芳基，C 3 -C 8脂环族基，卤素，CN，NO 2，CF 3，OCF 3，OH，NH 2，NH（C 1 -C 6脂族基） C 6脂族基）2，COOH，COO（C 1 -C 6脂族基），O（C 1 -C 6脂族基），CHF 2或CH 2 F。

公开(公告)号：WO2010002956A2

公开(公告)日：2010-01-07

申请号：PCT/US2009049346

申请日：2009-07-01

Applicant: VERTEX PHARMA ,  ZIMMERMANN NICOLE ,  GROOTENHUIS PETER D J ,  NUMA MEHDI MICHEL DJAMEL ,  STAMOS DEAN ,  ANDERSON COREY DON ,  WHITNEY TARA

Inventor： ZIMMERMANN NICOLE ,  GROOTENHUIS PETER D J ,  NUMA MEHDI MICHEL DJAMEL ,  STAMOS DEAN ,  ANDERSON COREY DON ,  WHITNEY TARA

IPC: C07D471/04 ,  A61K31/436 ,  A61P35/00

CPC classification number: C07D417/14

Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract translation: 本发明涉及可用作离子通道抑制剂的杂环衍生物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。

公开(公告)号：WO2009064752A3

公开(公告)日：2009-08-27

申请号：PCT/US2008083173

申请日：2008-11-12

Applicant: VERTEX PHARMA ,  STAMOS DEAN ,  MARTINBOROUGH ESTHER ,  NEUBERT TIMOTHY ,  NUMA MEHDI MICHEL DJAMEL ,  WHITNEY TARA ,  ZIMMERMANN NICOLE ,  HAMPTON TARA LEANNE

Inventor： STAMOS DEAN ,  MARTINBOROUGH ESTHER ,  NEUBERT TIMOTHY ,  NUMA MEHDI MICHEL DJAMEL ,  WHITNEY TARA ,  ZIMMERMANN NICOLE ,  HAMPTON TARA LEANNE

IPC: C07D417/14 ,  A61K31/427 ,  A61K31/4427

CPC classification number: C07D417/14

Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract translation: 本发明涉及可用作离子通道抑制剂的杂环衍生物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。

公开(公告)号：WO2010054138A3

公开(公告)日：2010-11-11

申请号：PCT/US2009063475

申请日：2009-11-06

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

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 ,  A61P3/00 ,  A61P25/00 ,  C07D209/08 ,  C07D209/12 ,  C07D209/18

CPC classification number: C07D209/12 ,  C07D209/08 ,  C07D209/18 ,  C07D405/12 ,  C07D405/14 ,  C07D487/04 ,  Y02P20/582

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.

Abstract translation: 本发明化合物及其药学上可接受的组合物可用作ATP结合盒（“ABC”）转运蛋白或其片段（包括囊性纤维化跨膜电导调节剂（“CFTR”））的调节剂。 本发明还涉及使用本发明化合物治疗ABC转运蛋白介导的疾病的方法。

公开(公告)号：WO2010048526A3

公开(公告)日：2010-09-16

申请号：PCT/US2009061882

申请日：2009-10-23

Applicant: VERTEX PHARMA ,  BINCH HAYLEY ,  FANNING LEV T D ,  HURLEY DENNIS ,  SHETH URVI ,  SILINA ALINA ,  YANG XIAOQING ,  BOTFIELD MARTYN ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK ,  NUMA MEHDI MICHEL DJAMEL

Inventor： BINCH HAYLEY ,  FANNING LEV T D ,  HURLEY DENNIS ,  SHETH URVI ,  SILINA ALINA ,  YANG XIAOQING ,  BOTFIELD MARTYN ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK ,  NUMA MEHDI MICHEL DJAMEL

IPC: C07D451/02 ,  A61K31/439 ,  A61P11/00

CPC classification number: A61K31/4709 ,  A61K45/06 ,  C07D215/56 ,  C07D221/22 ,  C07D451/02 ,  C07D471/06 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07F7/1856 ,  G01N33/5041 ,  G01N33/6872 ,  G01N2800/382

Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. (l); or pharmaceutically acceptable salts thereof, wherein: ring A is selected from:

Abstract translation: 本发明涉及囊性纤维化跨膜传导调节剂（“CFTR”）的调节剂，其组合物及其方法。 本发明还涉及使用CFTR的调节剂治疗疾病的方法。 （升）; 或其药学上可接受的盐，其中：环A选自：

公开(公告)号：CA2742821C

公开(公告)日：2018-10-23

申请号：CA2742821

申请日：2008-11-12

Applicant: VERTEX PHARMA

Inventor： RUAH SARA S HADIDA ,  GROOTENHUIS PETER D ,  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 modula-tors 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：NZ719598A

公开(公告)日：2017-03-31

申请号：NZ71959808

申请日：2008-11-12

Applicant: VERTEX PHARMA

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

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

Abstract: Disclosed herein is a use of an indol-cyclopropanecarboxamide derivative represented by structural formula shown herein in the manufacture of a medicament for treating a condition, disease, or disorder in a patient implicated by ABC transporter activity. Said compound is a modulator of ATP-Binding Cassette (’ABC’) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) and is also suitable for treating a condition, disease, or disorder selected from cystic fibrosis, hereditary emphysema, hereditary hemochromatosis, coagulation-fibrinolysis deficiencies, lipid processing deficiencies, lysosomal storage diseases, neurodegenerative diseases, polyglutamine neurological disorders, spongiform encephalopathies, chronic obstructive pulmonary disease (COPD), dry-eye disease, and Sjögren’s disease.

公开(公告)号：AU2009308232B2

公开(公告)日：2016-02-04

申请号：AU2009308232

申请日：2009-10-23

Applicant: VERTEX PHARMA

Inventor： BINCH HAYLEY ,  FANNING LEV T D ,  BOTFIELD MARTYN ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK ,  NUMA MEHDI MICHEL DJAMEL

IPC: C07D487/08 ,  A61K31/4709 ,  A61P11/00 ,  A61P43/00

Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR (Formula I) or pharmaceutically acceptable salts thereof, wherein: ring A is selected from: (a), (b), (c), (d), wherein: R

公开(公告)号：DK2365972T3

公开(公告)日：2015-01-19

申请号：DK08876364

申请日：2008-11-12

Applicant: VERTEX PHARMA

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

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