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).

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.