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公开(公告)号:SG10201902206QA
公开(公告)日:2019-04-29
申请号:SG10201902206Q
申请日:2015-05-28
Applicant: VERTEX PHARMA
Inventor: AHMAD NADIA , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , KNEGTEL RONALD , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , STORCK PIERRE-HENRI , STUDLEY JOHN
Abstract: RADIOLABELLED DERIVATIVES OF A 2-AMINO-6-FLUORO-N-[5-FLUORO-PYRIDIN- 3-YL]-PYRAZOLO[1,5-A]PYRIMIDIN-3-CARBOXAMIDE COMPOUND USEFUL AS ATR KINASE INHIBITOR, THE PREPARATION OF SAID COMPOUND AND DIFFERENT SOLID FORMS THEREOF The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of 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 solid forms of the compounds of this invention. The compounds of this invention have formula (I-l) or (I-A) ; wherein the variables are as defined herein. Figure: None
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公开(公告)号:HUE037371T2
公开(公告)日:2018-08-28
申请号:HUE13811716
申请日:2013-12-06
Applicant: VERTEX PHARMA
Inventor: AHMAD NADIA , BOYALL DEAN , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , DAVIS REBECCA , DURRANT STEVEN , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , JIMENEZ JUAN-MIGUEL , KAY DAVID , KNEGTEL RONALD , MIDDLETON DONALD , ODONNELL MICHAEL , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , SHAW DAVID , STORCK PIERRE-HENRI , STUDLEY JOHN , TWIN HEATHER
IPC: A61P35/00
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公开(公告)号:AU2018204431A1
公开(公告)日:2018-07-05
申请号:AU2018204431
申请日:2018-06-20
Applicant: VERTEX PHARMA
Inventor: AHMAD NADIA , BOYALL DEAN , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , DAVIS REBECCA , DURRANT STEVEN , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , JIMENEZ JUAN-MIGUEL , KAY DAVID , KNEGTEL RONALD , MIDDLETON DONALD , ODONNELL MICHAEL , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , SHAW DAVID , STORCK PIERRE-HENRI , STUDLEY JOHN , TWIN HEATHER
IPC: C07D487/04 , A61K31/495 , A61P35/00
Abstract: The present invention relates to 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 of 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: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: N N R3 %I H N I-A or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
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公开(公告)号:AU2013355124B2
公开(公告)日:2018-03-22
申请号:AU2013355124
申请日:2013-12-06
Applicant: VERTEX PHARMA
Inventor: AHMAD NADIA , BOYALL DEAN , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , DAVIS REBECCA , DURRANT STEVEN , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , JIMENEZ JUAN-MIGUEL , KAY DAVID , KNEGTEL RONALD , MIDDLETON DONALD , ODONNELL MICHAEL , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , SHAW DAVID , STORCK PIERRE-HENRI , STUDLEY JOHN , TWIN HEATHER
IPC: C07D487/04 , A61K31/495 , A61P35/00
Abstract: The present invention relates to 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 of 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
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公开(公告)号:NZ630457A
公开(公告)日:2017-05-26
申请号:NZ63045713
申请日:2013-12-06
Applicant: VERTEX PHARMA
Inventor: AHMAD NADIA , BOYALL DEAN , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , DAVIS REBECCA , DURRANT STEVEN , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , JIMENEZ JUAN-MIGUEL , KAY DAVID , KNEGTEL RONALD , MIDDLETON DONALD , ODONNELL MICHAEL , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , SHAW DAVID , STORCK PIERRE-HENRI , STUDLEY JOHN , TWIN HEATHER
IPC: C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/519 , A61P35/00 , C07D211/62 , C07D213/75 , C07D295/182 , C07D305/08
Abstract: Disclosed are 2-amino-6-fluoro-N-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives and analogues such as 2-amino-6-fluoro-N-(5-fluoro-4-(4-(4-(oxetan-3-yl)piperazine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide (I-G-32). Also disclosed is a pharmaceutical composition comprising the compound I-G-32 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, for use in the treatment of cancer. Also disclosed is the synthetic intermediate tert-butyl N-(3-fluoro-5-aminopyridin-4-yl)-piperidine-4-carboxylate and its use in the preparation of (I-G-32).
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公开(公告)号:SG10201606373XA
公开(公告)日:2016-09-29
申请号:SG10201606373X
申请日:2013-12-06
Applicant: VERTEX PHARMA
Inventor: AHMAD NADIA , BOYALL DEAN , CHARRIER JEAN-DAMIEN , DAVIS CHRIS , DAVIS REBECCA , DURRANT STEVEN , ETXEBARRIA I JARDI GORKA , FRAYSSE DAMIEN , JIMENEZ JUAN-MIGUEL , KAY DAVID , KNEGTEL RONALD , MIDDLETON DONALD , ODONNELL MICHAEL , PANESAR MANINDER , PIERARD FRANCOISE , PINDER JOANNE , SHAW DAVID , STORCK PIERRE-HENRI , STUDLEY JOHN , TWIN HEATHER
Abstract: The present invention relates to 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 of 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:or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula I-A:or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
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公开(公告)号:IN943KON2014A
公开(公告)日:2015-08-21
申请号:IN943KON2014
申请日:2014-04-30
Applicant: VERTEX PHARMA
Inventor: CHARRIER JEAN-DAMIEN , STORCK PIERRE-HENRI , STUDLEY JOHN , PIERARD FRANCOISE YVONNE THEODORA MARIE , DURRANT STEVEN JOHN , LITTLER BENJAMIN JOSEPH , ANGELL PAUL , HUGHES ROBERT MICHAEL , SIESEL DAVID ANDREW , URBINA ARMANDO , ZWICKER CARL , LOCONTE NICHOLAS , BARDER TIMOTHY
IPC: C07D413/14 , A61K31/497 , A61P35/00
Abstract: The present invention relates to 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 of 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; solid forms 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-1: wherein the variables are as defined herein. Additionally, the compounds of this invention have formula II: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein.
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58.
公开(公告)号:MX2014003796A
公开(公告)日:2015-01-16
申请号:MX2014003796
申请日:2012-09-28
Applicant: VERTEX PHARMA
Inventor: STORCK PIERRE-HENRI , DURRANT STEVEN JOHN , CHARRIER JEAN-DAMIEN , STUDLEY JOHN , PIERARD FRANCOISE YVONNE THEODORA MARIE , LITTLER BENJAMIN JOSEPH , HUGHES ROBERT MICHAEL , SIESEL DAVID ANDREW , ANGELL PAUL , URBINA ARMANDO , ZWICKER CARL , LOCONTE NICHOLAS , BARDER TIMOTHY
IPC: C07D413/14 , A61K31/497 , A61P35/00
Abstract: La presente invención se refiere a compuestos útiles como inhibidores de la proteína cinasa ATR. La invención se refiere, además, a composiciones farmacéuticamente aceptables que comprenden los compuestos de esta invención; métodos para tratar diversas enfermedades, trastornos y condiciones con el uso de los compuestos de esta invención, procesos para preparar los compuestos de esta invención, intermedios para preparar los compuestos de esta invención, formas sólidas de los compuestos de esta invención, y métodos de uso de los compuestos en aplicaciones in vitro tales como el estudio de cinasas en fenómenos biológicos y patológicos, el estudio de las vías de transducción de señales intracelulares mediadas por esas cinasas, y la evaluación comparativa de nuevos inhibidores de cinasas. Los compuestos de esta invención tienen la fórmula I-1: (ver formula) en donde las variables son tal como se definan en la presente descripción. Además, los compuestos de esta invención tienen la formula II: (ver formula II) O una sal farmacéuticamente aceptable de estos, en donde las variables son como se definen en la presente descripción.
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公开(公告)号:MX2013011450A
公开(公告)日:2014-02-03
申请号:MX2013011450
申请日:2012-04-05
Applicant: VERTEX PHARMA
Inventor: CHARRIER JEANDAMIEN , MACCORMICK SOMHAIRLE , STORCK PIERRE-HENRI , PINDER JOANNE , O'DONNELL MICHAEL EDWARD , KNEGTEL RONALD MARCELLUS ALPHONSUS , YOUNG STEPHEN CLINTON YOUNG , KAY DAVID , REAPER PHILIP MICHAEL , DURRANT STEVEN JOHN , TWIN HEATHER CLARE , DAVIS CHRISTOPHER JOHN
IPC: C07D413/14 , A61K31/497 , A61P35/00
Abstract: La presente invención se refiere a compuestos útiles como inhibidores de la proteína cinasa ATR. La invención se refiere, además, a composiciones farmacéuticamente aceptable que comprende los compuestos de esta invención; método para tratar diversas enfermedades, trastornos y condiciones con el uso de los compuestos de esta invención; procesos para preparar los compuestos de esta invención; intermediarios para preparar los compuestos de esta invención; métodos para usar los compuestos en aplicaciones in vitro, tal como el estudio de cinasas en fenómenos biológicos; el estudio de rutas de transducción de señales intracelulares mediadas por las cinasas; y la evaluación comparativa de nuevos inhibidores de cinasa.
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公开(公告)号:SG185524A1
公开(公告)日:2012-12-28
申请号:SG2012083176
申请日:2011-05-12
Applicant: VERTEX PHARMA
Inventor: CHARRIER JEAN-DAMIEN , BINCH HAYLEY 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 , STORCK PIERRE-HENRI , KAY DAVID , REAPER PHILIP MICHAEL , GROTE MATTHEW PAUL
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.
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