公开(公告)号：WO2005030188A3

公开(公告)日：2005-08-04

申请号：PCT/US2004031514

申请日：2004-09-27

Applicant: VERTEX PHARMA ,  GARCIA-GUZMAN BLANCO MIGUEL ,  BERGERON DANIELE ,  GROOTENHUIS PETER D J ,  HURLEY DENNIS JAMES ,  NAKATANI AKIKO ,  MAKINGS LEWIS R ,  DISEPIO DANIEL ,  RAFFAI GABRIEL

Inventor： GARCIA-GUZMAN BLANCO MIGUEL ,  BERGERON DANIELE ,  GROOTENHUIS PETER D J ,  HURLEY DENNIS JAMES ,  NAKATANI AKIKO ,  MAKINGS LEWIS R ,  DISEPIO DANIEL ,  RAFFAI GABRIEL

IPC: A61K31/495 ,  A61K31/496 ,  C07D295/02 ,  C07D295/033 ,  C07D295/073 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D309/14 ,  C07D451/02 ,  C07D451/04 ,  C07D493/08 ,  A61P43/00 ,  C07D295/04

CPC classification number: C07D295/033 ,  A61K31/495 ,  A61K31/496 ,  C07D211/58 ,  C07D295/073 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D309/14 ,  C07D451/02 ,  C07D451/04 ,  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.

Abstract translation: 本发明涉及毒蕈碱受体的调节剂。 本发明还提供了包含这种调节剂的组合物，以及用于治疗毒蕈碱性受体介导的疾病的方法。

公开(公告)号：WO2011072241A9

公开(公告)日：2012-06-14

申请号：PCT/US2010059920

申请日：2010-12-10

Applicant: VERTEX PHARMA ,  SHETH URVI ,  FANNING LEV 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 LEV 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 ,  A61K31/4709 ,  A61P11/00 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08

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-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 invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract translation: 本发明涉及作为ATP结合盒（“ABC”）转运体或其片段的调节剂的4-氧代-1H-喹啉-3-甲酰胺，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：WO2004108133A3

公开(公告)日：2005-03-31

申请号：PCT/US2004017779

申请日：2004-06-04

Applicant: VERTEX PHARMA ,  MAKINGS LEWIS R ,  GROOTENHUIS PETER ,  HURLEY DENNIS JAMES ,  TUNG ROGER D ,  TERMIN ANDREAS P

Inventor： MAKINGS LEWIS R ,  GROOTENHUIS PETER ,  HURLEY DENNIS JAMES ,  TUNG ROGER D ,  TERMIN ANDREAS P

IPC: A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61P1/00 ,  A61P11/00 ,  A61P11/06 ,  A61P13/10 ,  A61P17/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P29/02 ,  A61P43/00 ,  C07D231/56 ,  C07D235/06 ,  C07D235/26 ,  C07D241/44 ,  C07D263/58 ,  C07D277/68 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/02 ,  C07D498/02

CPC classification number: A61K31/497 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/501 ,  A61K31/506 ,  C07D231/56 ,  C07D235/06 ,  C07D235/26 ,  C07D241/44 ,  C07D263/58 ,  C07D277/68 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention relates to compounds useful as modulators of the vanilloid receptor, and 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: 本发明涉及可用作香草素受体调节剂的化合物，并且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：CO2024015820A2

公开(公告)日：2024-11-28

申请号：CO2024015820

申请日：2024-11-21

Applicant: VERTEX PHARMA

Inventor： HADIDA RUAH SARA SABINA ,  MCCARTNEY JASON ,  MILLER MARK THOMAS ,  ZHOU JINGLAN ,  ARUMUGAM VIJAYALAKSMI ,  CHUDYK EWA IWONA ,  HURLEY DENNIS JAMES ,  NEUBERT TIMOTHY DONALD ,  PINDER JOANNE LOUISE ,  DODD JAMES ,  CHAU JACLYN ,  DEMORET ROBERT MARTIN ,  GHIRMAI SENAIT G ,  VALIULIN ROMAN ASKATOVICH ,  KINTZER ALEXANDER FREDERIK ,  SLOCHOWER DAVID ROBERT ,  AERTGEERTS KATHLEEN ,  BECK ELIZABETH MARY ,  MUI JAMES JUN BON ,  WRIGHT MIRANDA ADELE ,  KNEGTEL RONALD MARCELLUS ALPHONSUS ,  SIMPSON IAIN

IPC: A61P9/06 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61P25/02 ,  A61P29/00 ,  C07D215/233 ,  C07D239/91 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D519/00

Abstract: Se proporcionan compuestos, y sales farmacéuticamente aceptables de estos, útiles como inhibidores de canales de sodio. También se proporcionan composiciones farmacéuticas que comprenden los compuestos o sales farmacéuticamente aceptables y métodos de uso de los compuestos, sales farmacéuticamente aceptables y composiciones farmacéuticas en el tratamiento de diversos trastornos, incluido el dolor.

公开(公告)号：CO2022008969A2

公开(公告)日：2022-09-09

申请号：CO2022008969

申请日：2022-06-28

Applicant: VERTEX PHARMA

Inventor： AHMAD NADIA ,  SCHMIDT YVONNE ,  THOMSON STEPHEN ANDREW ,  DURRANT STEVEN JOHN ,  BECK ELIZABETH MARY ,  CARVALHO MEIRELES LIDIO ,  CHUDYK EWA IWONA ,  ETXEBARRIA JARDI GORKA ,  GALAN BHAIRAVI ,  HADIDA RUAH SARA S ,  HURLEY DENNIS JAMES ,  KNEGTEL RONALD MARCELLUS ,  NEUBERT TIMOTHY DONALD ,  PINDER JOANNE LOUISE ,  PONTILLO JOSEPH ,  PULLIN ROBERT ,  SHAW DAVID MATTHEW ,  SKERRATT SARAH ,  STAMOS DEAN ,  VIRANI ANISA NIZARALI ,  WRAY CHRISTOPHER

IPC: C07D405/12 ,  A61K31/443 ,  A61P29/00 ,  C07D405/14

Abstract: Se proporcionan compuestos y sus sales farmacéuticamente aceptables, de utilidad como inhibidores de canales de sodio. También se proporcionan composiciones farmacéuticas que comprenden los compuestos o sales farmacéuticamente aceptables y métodos de uso de los compuestos, sales farmacéuticamente aceptables y composiciones farmacéuticas en el tratamiento de diversos trastornos, incluyendo el dolor.

公开(公告)号：CA3114672A1

公开(公告)日：2020-04-23

申请号：CA3114672

申请日：2019-10-04

Applicant: VERTEX PHARMA

Inventor： BLIGH CAVAN MCKEON ,  BRODNEY MICHAEL AARON ,  ECCLES MARY ELIZABETH ,  GAGNON KEVIN JAMES ,  HOOD SARAH CAROL ,  HUSSEY JOSHUA KENNEDY ,  LOOKER ADAM ,  MAXWELL JOHN PATRICK ,  MEDEK ALES ,  NAVAMAL METTACHIT ,  RODAY SETU ,  ROEPER STEFANIE ,  SAWANT RUPA ,  SHI YI ,  TANG QING ,  WALDO MICHAEL ,  BANDARAGE UPUL KEERTHI ,  BOUCHER DIANE M ,  BOYD MICHAEL JOHN ,  DAMAGNEZ VERONIQUE ,  DEWEY FANNING LEV TYLER ,  FIMOGNARI JR ,  GARCIA BARRANTES PEDRO M ,  GIROUX SIMON ,  GREY JR ,  HALL AMY BETH ,  HURLEY DENNIS JAMES ,  JOHNSON JR ,  JONES PETER ,  KESAVAN SARATHY ,  NUHANT PHILIPPE MARCEL ,  SWETT REBECCA JANE ,  TAPLEY TIMOTHY LEWIS ,  THOMSON STEPHEN A ,  XU JINWANG ,  MAXWELL BRAD D ,  COTTRELL KEVIN MICHAEL

IPC: C07D487/04 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/7056 ,  C07D471/14 ,  C07D487/14 ,  C07D519/00 ,  C07H13/02

Abstract: Novel compounds, compositions, and methods of using and preparing the same, which may be useful for treating alpha-1 antitrypsin deficiency (AATD).

公开(公告)号：NZ603043A

公开(公告)日：2015-02-27

申请号：NZ60304311

申请日：2011-04-22

Applicant: VERTEX PHARMA

Inventor： SHETH URVI JAGDISHBHAI ,  BOTFIELD MARTYN CURTIS ,  ALCACIO TIM EDWARD ,  YANG XIAOQING ,  SULLIVAN MARK JEFFREY ,  HURLEY DENNIS JAMES ,  AREKAR SNEHA G ,  KESHAVARZ-SHOKRI ALI ,  ZHANG BEILI ,  ZLOKARNIK GREGOR ,  KRAWIEC MARIUSZ ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  ZHANG YUEGANG ,  BINCH HAYLEY MARIE ,  FANNING LEV TYLER DEWEY ,  JOHNSTON STEVEN C ,  YOUNG CHRISTOPHER RYAN ,  NUMA MEHDI ,  SILINA ALINA ,  GROOTENHUIS PETER DIEDERIK JAN ,  VAN GOOR FREDRICK F ,  ZAMAN NOREEN TASNEEM ,  MUDUNURI PRAVEEN ,  KAUSHIK RITU ROHIT ,  MEDEK ALES ,  KADIYALA IRINA NIKOLAEVNA ,  LEE ELAINE CHUNGMIN ,  LUISI BRIAN ,  VERWIJS MARINUS JACOBUS

IPC: A61K31/443 ,  A61K31/36 ,  A61K31/47 ,  C07D213/75 ,  C07D215/233 ,  C07D215/56 ,  C07D317/46

Abstract: Disclosed is a pharmaceutical composition comprising: Compound 1 SDD Formulation and Compound 3 Form I Tablet Formulation wherein: Compound 1 SDD Formulation is a spray dried dispersion of ivacaftor (VX-770), which comprises from about 45 wt% to about 85 wt% of substantially amorphous ivacaftor by weight of the dispersion, from about 14.45 wt% to about 55.55 wt% of hydroxypropylmethylcellulose acetate succinate (HPMCAS) by weight of the dispersion, and from about 0.45 wt% to about 0.55 wt% sodium lauryl sulfate (SLS) by weight of the dispersion; Compound 3 Form I Tablet Formulation comprises: crystalline form I of lumacaftor (VX-809) (characterized by one or more peaks at 15.2 to 15.6 degrees, 16.1 to 16.5 degrees, and 14.3 to 14.7 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation) in an amount ranging from about 20 wt% to about 80 wt% by weight of the composition; a filler comprising microcrystalline cellulose in an amount ranging from about 20 wt% to about 50 wt% by weight of the composition; a disintegrant comprising sodium croscarmellose sodium in an amount ranging from about 1 wt% to about 5 wt% by weight of the composition; a surfactant comprising sodium lauryl sulfate in an amount ranging from about 2 wt% to about 0.3 wt% by weight of the composition; a diluent comprising mannitol in an amount ranging from about 1 wt% to about 30 wt% by weight of the composition; a lubricant comprising magnesium stearate in an amount ranging from about 0.3 wt% to about 5 wt% by weight of the composition; and at least one of: a binder comprising polyvinylpyrrolidone in an amount ranging from about 0.1 wt% to about 5 wt% by weight of the composition and a glidant comprising colloidal silica in an amount ranging from about 0.05 wt% to about 2 wt% by weight of the composition. Also disclosed is the use of the pharmaceutical composition as defined above in the manufacture of a medicament for treating a CFTR mediated disease in a human, wherein the CFTR mediated disease is selected from cystic fibrosis, COPD, emphysema, dry-eye disease or osteoporosis.

公开(公告)号：NZ603477A

公开(公告)日：2014-09-26

申请号：NZ60347711

申请日：2011-05-12

Applicant: VERTEX PHARMA

Inventor： STORCK PIERRE-HENRI ,  KAY DAVID ,  BINCH HAYLEY MARIE ,  FANNING LEV TYLER DEWEY ,  REAPER PHILIP MICHAEL ,  CHARRIER JEAN-DAMIEN ,  YOUNG STEPHEN CLINTON ,  HURLEY DENNIS JAMES ,  KNEGTEL RONALD MARCELLUS ALPHONSUS ,  JOSHI PRAMOD ,  O’DONNELL MICHAEL ,  CLEVELAND THOMAS ,  VIRANI ANISA NIZARALI ,  GROTE MATTHEW PAUL ,  PINDER JOANNE ,  DURRANT STEVEN JOHN

IPC: C07D413/14 ,  A61K31/444 ,  A61K31/497 ,  A61P35/00

Abstract: The disclosure relates to pyrazine and pyridine derivatives of formula (I), wherein the variables are as defined in the specification. These compounds are useful as inhibitors of ATR protein kinase involved in cellular responses to DNA damage, and are suitable for treating various diseases, disorders, and conditions that are mediated by the particular protein kinase, particularly suitable for treating cancer selected from lung cancer, head and neck cancer, pancreatic cancer, gastric cancer, and brain cancer. Processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors are also disclosed.

公开(公告)号：MX2012013081A

公开(公告)日：2013-05-09

申请号：MX2012013081

申请日：2011-05-12

Applicant: VERTEX PHARMA

Inventor： CHARRIER JEAN-DAMIEN ,  KAY DAVID ,  JOSHI PRAMOD ,  YOUNG STEPHEN CLINTON ,  O'DONNELL MICHAEL ,  PINDER JOANNE ,  VIRANI ANISA NIZARALI ,  REAPER PHILIP MICHAEL ,  BINCH HAYLEY MARIE ,  CLEVELAND THOMAS ,  DURRANT STEVEN JOHN ,  KNEGTEL RONALD MARCELLUS ALPHONSUS ,  FANNING LEV TYLER DEWEY ,  HURLEY DENNIS JAMES ,  STORCK PIERRE-HENRI ,  GROTE MATTHEW PAUL

IPC: C07D413/14 ,  A61K31/444 ,  A61K31/497 ,  A61P35/00

Abstract: La presente invención se refiere a compuestos de pirazina y piridina útiles como inhibidores de la proteína cinasa ATR. La invención también se refiere a composiciones farmacéuticamente aceptables que comprenden los compuestos de esta invención; métodos para tratar diversas enfermedades, trastornos y afecciones usando los compuestos de esta invención; procesos para preparar los compuestos de esta invención; intermedios para la preparación de los compuestos de esta invención; y métodos para usar los compuestos en aplicaciones in vitro, tales como el estudio de cinasas en fenómenos biológicos y patológicos; el estudio de vías de transducción de señales intracelulares mediadas por tales cinasas y la evaluación comparativa de nuevos inhibidores de cinasas. Los compuestos de la presente invención tienen la fórmula I donde las variables son tal como se describen en la presente.

公开(公告)号：AU2011253025A1

公开(公告)日：2012-11-29

申请号：AU2011253025

申请日：2011-05-12

Applicant: VERTEX PHARMA

Inventor： CHARRIER JEAN-DAMIEN ,  BINCH HALEY MARIE ,  HURLEY DENNIS JAMES ,  CLEVELAND THOMAS ,  JOSHI PRAMOD ,  FANNING LEV TYLER DEWEY ,  PINDER JOANNE ,  O'DONNELL MICHAEL ,  VIRANI ANISA NIZARALI ,  KNEGTEL RONALD MARCELLUS ALPHONSUS ,  DURRANT STEVEN JOHN ,  YOUNG STEPHEN CLINTON ,  PIERRE-HENRI ,  KAY DAVID ,  REAPER PHILIP MICHAEL ,  GROTE MATTHEW PAUL

IPC: C07D413/14 ,  A61K31/444 ,  A61K31/497 ,  A61P35/00

Abstract: The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I wherein the variables are as defined herein.