Compounds useful as inhibitors of atr kinase

Patent metadata

Field	Value
Publication number	US-2016347754-A1
Application number	US-201615142338-A
Country	US
Kind code	A1
Filing date	Apr 29, 2016
Priority date	Dec 7, 2012
Publication date	Dec 1, 2016
Grant date	—

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.

First claim

1 - 178 . (canceled)

179 . A process for preparing a compound of formula I-G-32:

or a salt thereof,
comprising reacting a compound of formula 6a:

or a salt thereof, under suitable conditions to form an amide bond.

180 . The process of claim 179 , further comprising the step of preparing a compound of formula 6:

or a salt thereof, by reacting a compound of formula 5a:

or a salt thereof, under suitable conditions to form an activated ester.

181 . (canceled)

182 . The process of claim 179 , further comprising the step of preparing a compound of formula 5a:

or a salt thereof, by reacting a compound of formula 4:

or a salt thereof, under suitable deprotection conditions, wherein All is allyl.

183 . The process of claim 182 , further comprising the step of preparing a compound of formula 4a:

or a salt thereof, by reacting a compound of formula 3:

or a salt thereof, under suitable condensation conditions to form a pyrimidine ring.

184 . The process of claim 183 , further comprising the step of preparing the compound of formula 3:

or a salt thereof, by reacting a compound of formula 2:

or a salt thereof, under suitable condensation conditions to form a pyrazole ring.

185 . The process of claim 184 , further comprising the step of preparing a compound of formula 2:

or a salt thereof, by reacting a compound of formula 1:

under suitable anion condensation conditions.

186 - 188 . (canceled)

Assignees

• Vertex Pharma

Inventors

• Ahmad Nadia
• Boyall Dean
• Charrier Jean-Damien
• Davis Christopher John
• Davis Rebecca
• Durrant Steven John
• Etxebarria I Jardi Gorka
• Fraysse Damien
• Jimenez Juan-Miguel
• Kay David
• Knegtel Ronald Marcellus Alphonsus
• MIDDLETON Donald
• O'Donnell Michael Edward
• Panesar Maninder
• Pierard Francoise Yvonne Theodora Marie
• Pinder Joanne
• Shaw David Matthew
• Storck Pierre-Henri
• Studley John R
• Twin Heather

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61P5/00

  Drugs for disorders of the endocrine system · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/02

  specific for leukemia · CPC title

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title