公开(公告)号：WO2006023852A3

公开(公告)日：2006-08-31

申请号：PCT/US2005029780

申请日：2005-08-19

Applicant: VERTEX PHARMA ,  MAKINGS LEWIS R ,  GARCIA-GUZMAN BLANCO MIGUEL ,  HURLEY DENNIS J ,  DRUTU IOANA ,  RAFFAI GABRIEL ,  BERGERON DANIELE M ,  NAKATANI AKIKO ,  TERMIN ANDREAS P ,  SILINA ALINA

Inventor： MAKINGS LEWIS R ,  GARCIA-GUZMAN BLANCO MIGUEL ,  HURLEY DENNIS J ,  DRUTU IOANA ,  RAFFAI GABRIEL ,  BERGERON DANIELE M ,  NAKATANI AKIKO ,  TERMIN ANDREAS P ,  SILINA ALINA

IPC: A61K31/435 ,  A61K31/438 ,  A61P25/00 ,  A61P43/00 ,  C07D471/00

CPC classification number: C07D401/06 ,  A61K31/435 ,  A61K31/438 ,  A61K31/4747 ,  A61K31/55 ,  C07D221/20 ,  C07D223/32 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D451/02 ,  C07D451/04 ,  C07D471/10 ,  C07D491/10

Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.

公开(公告)号：WO2016057572A1

公开(公告)日：2016-04-14

申请号：PCT/US2015/054316

申请日：2015-10-06

Applicant: MILLER, Mark Thomas ,  ANDERSON, Corey ,  ARUMUGAM, Vijayalaksmi ,  BEAR, Brian Richard ,  BINCH, Hayley Marie ,  CLEMENS, Jeremy J. ,  CLEVELAND, Thomas ,  CONROY, Erica ,  COON, Timothy Richard ,  FRIEMAN, Bryan A. ,  GROOTENHUIS, Peter Diederik Jan ,  GROSS, Raymond Stanley ,  HADIDA-RUAH, Sara Sabina ,  HARIPADA, Khatuya ,  JOSHI, Pramod Virupax ,  KRENITSKY, Paul John ,  LIN, Chun-Chieh ,  MARELIUS, Gulin Erdgogan ,  MELILLO, Vito ,  MCCARTNEY, Jason ,  NICHOLLS, Georgia McGaughey ,  PIERRE, Fabrice Jean Denis ,  SILINA, Alina ,  TERMIN, Andreas P. ,  UY, Johnny ,  ZHOU, Jinglan

Inventor： MILLER, Mark Thomas ,  ANDERSON, Corey ,  ARUMUGAM, Vijayalaksmi ,  BEAR, Brian Richard ,  BINCH, Hayley Marie ,  CLEMENS, Jeremy J. ,  CLEVELAND, Thomas ,  CONROY, Erica ,  COON, Timothy Richard ,  FRIEMAN, Bryan A. ,  GROOTENHUIS, Peter Diederik Jan ,  GROSS, Raymond Stanley ,  HADIDA-RUAH, Sara Sabina ,  HARIPADA, Khatuya ,  JOSHI, Pramod Virupax ,  KRENITSKY, Paul John ,  LIN, Chun-Chieh ,  MARELIUS, Gulin Erdgogan ,  MELILLO, Vito ,  MCCARTNEY, Jason ,  NICHOLLS, Georgia McGaughey ,  PIERRE, Fabrice Jean Denis ,  SILINA, Alina ,  TERMIN, Andreas P. ,  UY, Johnny ,  ZHOU, Jinglan

IPC: A01N41/06 ,  A61K31/18

CPC classification number: A61K31/506 ,  A61J1/035 ,  A61K31/404 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4525 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  C07D209/18 ,  C07D209/42 ,  C07D209/49 ,  C07D213/64 ,  C07D213/73 ,  C07D213/82 ,  C07D213/84 ,  C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D235/24 ,  C07D239/34 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/14 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention features a compound of formula (I): (I) or a pharmaceutically acceptable salt thereof, where R 1 , R 2 , R 3 , W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

Abstract translation: 本发明的特征在于式（I）化合物：（I）或其药学上可接受的盐，其中R1，R2，R3，W，X，Y，Z，n，o，p和q如本文所定义， 治疗CFTR介导的疾病，如囊性纤维化。 本发明还特征在于药物组合物，治疗方法及其试剂盒。

公开(公告)号：WO2011133953A1

公开(公告)日：2011-10-27

申请号：PCT/US2011/033689

申请日：2011-04-22

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  VAN GOOR, Fredrick, F. ,  ALARGOVA, Rossitza, Gueorguieva ,  ALCACIO, Tim, Edward ,  AREKAR, Sneha, G. ,  BINCH, Hayley, Marie ,  BOTFIELD, Martyn, Curtis ,  FANNING, Lev, Tyler Dewey ,  GROOTENHUIS, Peter, Diederik Jan ,  HURLEY, Dennis, James ,  JOHNSTON, Steven, C. ,  KADIYALA, Irina, Nikolaevna ,  KAUSHIK, Ritu, Rohit ,  KESHAVARZ-SHOKRI, Ali ,  KRAWIEC, Mariusz ,  LEE, Elaine, Chungmin ,  LUISI, Brian ,  MEDEK, Ales ,  MUDUNURI, Praveen ,  NUMA, Mehdi ,  SHETH, Urvi Jagdishbhai ,  SILINA, Alina ,  SULLIVAN, Mark Jeffrey ,  VERWIJS, Marinus Jacobus ,  YANG, Xiaoqing ,  YOUNG, Christopher Ryan ,  ZAMAN, Noreen Tasneem ,  ZHANG, Beili ,  ZHANG, Yuegang ,  ZLOKARNIK, Gregor

Inventor： VAN GOOR, Fredrick, F. ,  ALARGOVA, Rossitza, Gueorguieva ,  ALCACIO, Tim, Edward ,  AREKAR, Sneha, G. ,  BINCH, Hayley, Marie ,  BOTFIELD, Martyn, Curtis ,  FANNING, Lev, Tyler Dewey ,  GROOTENHUIS, Peter, Diederik Jan ,  HURLEY, Dennis, James ,  JOHNSTON, Steven, C. ,  KADIYALA, Irina, Nikolaevna ,  KAUSHIK, Ritu, Rohit ,  KESHAVARZ-SHOKRI, Ali ,  KRAWIEC, Mariusz ,  LEE, Elaine, Chungmin ,  LUISI, Brian ,  MEDEK, Ales ,  MUDUNURI, Praveen ,  NUMA, Mehdi ,  SHETH, Urvi Jagdishbhai ,  SILINA, Alina ,  SULLIVAN, Mark Jeffrey ,  VERWIJS, Marinus Jacobus ,  YANG, Xiaoqing ,  YOUNG, Christopher Ryan ,  ZAMAN, Noreen Tasneem ,  ZHANG, Beili ,  ZHANG, Yuegang ,  ZLOKARNIK, Gregor

IPC: A61K31/4704 ,  A61K31/404 ,  A61K31/443

CPC classification number: A61K31/4709 ,  A61K31/404 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/47 ,  A61K31/4704 ,  G01N33/6872 ,  G01N2333/4703 ,  A61K2300/00

Abstract: The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.

Abstract translation: 本发明涉及包含式I和II化合物，任选与式III化合物和/或式IV化合物组合的药物组合物。 本发明还涉及固体形式及其药物制剂，以及使用这些组合物治疗CFTR介导的疾病，特别是囊性纤维化的方法。

公开(公告)号：WO2011133956A1

公开(公告)日：2011-10-27

申请号：PCT/US2011/033693

申请日：2011-04-22

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  VAN GOOR, Fredrick, F. ,  ALARGOVA, Rossitza, Gueorguieva ,  ALCACIO, Tim, Edward ,  BINCH, Hayley, Marie ,  BOTFIELD, Martyn, Curtis ,  FANNING, Lev Tyler, Dewey ,  GROOTENHUIS, Peter Diederik, Jan ,  HURLEY, Dennis, James ,  KADIYALA, Irina, Nikolaevna ,  KAUSHIK, Ritu, Rohit ,  KESHAVARZ-SHOKRI, Ali ,  KRAWIEC, Mariusz ,  LEE, Elaine, Chungmin ,  LUISI, Brian ,  MEDEK, Ales ,  NUMA, Mehdi ,  SHETH, Urvi, Jagdishbhai ,  SILINA, Alina ,  VERWIJS, Marinus, Jacobus ,  YANG, Xiaoqing ,  YOUNG, Christopher Ryan ,  ZAMAN, Noreen, Tasneem ,  ZHANG, Beili ,  ZHANG, Yuegang ,  ZLOKARNIK, Gregor

Inventor： VAN GOOR, Fredrick, F. ,  ALARGOVA, Rossitza, Gueorguieva ,  ALCACIO, Tim, Edward ,  BINCH, Hayley, Marie ,  BOTFIELD, Martyn, Curtis ,  FANNING, Lev Tyler, Dewey ,  GROOTENHUIS, Peter Diederik, Jan ,  HURLEY, Dennis, James ,  KADIYALA, Irina, Nikolaevna ,  KAUSHIK, Ritu, Rohit ,  KESHAVARZ-SHOKRI, Ali ,  KRAWIEC, Mariusz ,  LEE, Elaine, Chungmin ,  LUISI, Brian ,  MEDEK, Ales ,  NUMA, Mehdi ,  SHETH, Urvi, Jagdishbhai ,  SILINA, Alina ,  VERWIJS, Marinus, Jacobus ,  YANG, Xiaoqing ,  YOUNG, Christopher Ryan ,  ZAMAN, Noreen, Tasneem ,  ZHANG, Beili ,  ZHANG, Yuegang ,  ZLOKARNIK, Gregor

IPC: A61K31/4704 ,  A61K31/404 ,  A61K31/443

CPC classification number: A61K31/4709 ,  A61K31/404 ,  A61K31/443 ,  A61K31/4704 ,  A61K45/06 ,  C07D405/12 ,  C12Q1/34 ,  G01N2500/04 ,  G01N2500/20 ,  A61K2300/00

Abstract: The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.(Formula I), (Formula II), (Formula III).

Abstract translation: 本发明涉及药物组合物，其包含与式II化合物和/或式III化合物中的一种或两种结合的式I化合物。 本发明还涉及固体形式及其药物制剂，以及使用这些组合物治疗CFTR介导的疾病，特别是囊性纤维化的方法（式I），（式II），（式III）。

公开(公告)号：WO2007076070A2

公开(公告)日：2007-07-05

申请号：PCT/US2006049141

申请日：2006-12-22

Applicant: VERTEX PHARMA ,  MAKINGS LEWIS R ,  GARCIA-GUZMAN BLANCO MIGUEL ,  HURLEY DENNIS J ,  DRUTU IOANA ,  RAFFAI GABRIEL ,  BERGERON DANIELE M ,  NAKATANI AKIKO ,  TERMIN ANDREAS P ,  SILINA ALINA

Inventor： MAKINGS LEWIS R ,  GARCIA-GUZMAN BLANCO MIGUEL ,  HURLEY DENNIS J ,  DRUTU IOANA ,  RAFFAI GABRIEL ,  BERGERON DANIELE M ,  NAKATANI AKIKO ,  TERMIN ANDREAS P ,  SILINA ALINA

CPC classification number: A61K31/4545 ,  A61K31/438 ,  A61K31/46 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  C07D221/20 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D417/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/10

Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.

公开(公告)号：WO2006058294A3

公开(公告)日：2006-06-01

申请号：PCT/US2005/042931

申请日：2005-11-29

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  HURLEY, Dennis, J. ,  BERGERON, Daniele, M. ,  DRUTU, Ioana ,  GARCIA-GUZMAN BLANCO, Miguel ,  MAKINGS, Lewis, R. ,  NAKATANI, Akiko ,  RAFFAI, Gabriel ,  SILINA, Alina

Inventor： HURLEY, Dennis, J. ,  BERGERON, Daniele, M. ,  DRUTU, Ioana ,  GARCIA-GUZMAN BLANCO, Miguel ,  MAKINGS, Lewis, R. ,  NAKATANI, Akiko ,  RAFFAI, Gabriel ,  SILINA, Alina

IPC: A61K31/4439 ,  A61K31/454 ,  A61P25/18

Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.

公开(公告)号：WO2006058294A2

公开(公告)日：2006-06-01

申请号：PCT/US2005042931

申请日：2005-11-29

Applicant: VERTEX PHARMA ,  HURLEY DENNIS J ,  BERGERON DANIELE M ,  DRUTU IOANA ,  GARCIA-GUZMAN BLANCO MIGUEL ,  MAKINGS LEWIS R ,  NAKATANI AKIKO ,  RAFFAI GABRIEL ,  SILINA ALINA

Inventor： HURLEY DENNIS J ,  BERGERON DANIELE M ,  DRUTU IOANA ,  GARCIA-GUZMAN BLANCO MIGUEL ,  MAKINGS LEWIS R ,  NAKATANI AKIKO ,  RAFFAI GABRIEL ,  SILINA ALINA

CPC classification number: C07D211/10 ,  A61K31/4439 ,  C07D211/18 ,  C07D211/32 ,  C07D211/34 ,  C07D211/38 ,  C07D211/42 ,  C07D211/52 ,  C07D211/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/10 ,  C07D417/10 ,  C07D417/12 ,  C07D451/02 ,  C07D493/08

Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.

公开(公告)号：WO2011072241A1

公开(公告)日：2011-06-16

申请号：PCT/US2010/059920

申请日：2010-12-10

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  SHETH, Urvi ,  FANNING, Tev, T.d. ,  NUMA, Mehdi ,  BINCH, Hayley ,  HURLEY, Dennis, James ,  ZHOU, Jinglan ,  HADIDA RUAH, Sara, S. ,  HAZLEWOOD, Anna, R. ,  SILINA, Alina ,  VAIRAGOUNDAR, Rajendran ,  VAN GOOR, Fredrick, F. ,  GROOTENHUIS, Peter, Diederik Jan ,  BOTFIELD, Martyn, C.

Inventor： SHETH, Urvi ,  FANNING, Tev, T.d. ,  NUMA, Mehdi ,  BINCH, Hayley ,  HURLEY, Dennis, James ,  ZHOU, Jinglan ,  HADIDA RUAH, Sara, S. ,  HAZLEWOOD, Anna, R. ,  SILINA, Alina ,  VAIRAGOUNDAR, Rajendran ,  VAN GOOR, Fredrick, F. ,  GROOTENHUIS, Peter, Diederik Jan ,  BOTFIELD, Martyn, C.

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

CPC classification number: C07C215/76 ,  C07D209/08 ,  C07D209/14 ,  C07D209/18 ,  C07D209/42 ,  C07D209/94 ,  C07D213/20 ,  C07D213/73 ,  C07D215/227 ,  C07D215/38 ,  C07D215/56 ,  C07D217/06 ,  C07D223/16 ,  C07D265/36 ,  C07D279/16 ,  C07D311/58 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10

Abstract: The present invention relates to 4 -oxo- lH-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 Invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract translation: 本发明涉及4-氧代-1H-喹啉-3-甲酰胺作为ATP结合盒（“ABC”）转运体或其片段的调节剂，包括囊性纤维化跨膜电导调节剂，其组合物及其方法。 本发明还涉及使用这种调节剂治疗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：WO2010048526A2

公开(公告)日：2010-04-29

申请号：PCT/US2009/061882

申请日：2009-10-23

Applicant: VERTEX PHARMACEUTICALS, INCORPORATED ,  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: A61K31/439 ,  C07D453/04 ,  C12Q1/02

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.

Abstract translation: 本发明涉及囊性纤维化跨膜电导调节剂（“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。