Bis(fluoroalkyl)-1,4-benzodiazepinone compounds and prodrugs thereof

Patent metadata

Field	Value
Publication number	US-8999918-B2
Application number	US-201314032333-A
Country	US
Kind code	B2
Filing date	Sep 20, 2013
Priority date	Sep 21, 2012
Publication date	Apr 7, 2015
Grant date	Apr 7, 2015

Abstract

Disclosed are compounds of Formula (I) and/or salts thereof:

wherein R 1 is —CH 2 CH 2 CF 3 ; R 2 is —CH 2 CH 2 CF 3 or —CH 2 CH 2 CH 2 CF 3 ; R 3 is H, —CH 3 , or R x ; R 4 is H or R y ; Ring A is phenyl or pyridinyl; and R x , R y , R a , R b , y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.

First claim

What is claimed is:

1. A compound of Formula (I):

and/or at least one salt thereof, wherein:
R 1 is —CH 2 CH 2 CF 3 ;
R 2 is —CH 2 CH 2 CF 3 or —CH 2 CH 2 CH 2 CF 3 ;
R 3 is H, —CH 3 , or R x ;
R 4 is H or R y ;
R x is: —CH 2 OC(O)CH(CH 3 )NH 2 , —CH 2 OC(O)CH(NH 2 )CH(CH 3 ) 2 ,
—CH 2 OC(O)CH((CH(CH 3 ) 2 )NHC(O)CH(NH 2 )CH(CH 3 ) 2 ,…

Assignees

• Bristol Myers Squibb Co

Inventors

• Gavai Ashvinikumar V
• Delucca George V
• O'Malley Daniel
• Gill Patrice
• Quesnelle Claude A
• Fink Brian E
• Zhao Yufen
• Lee Francis Y

Classifications

• A61P43/00

  Human Necessities · mapped topic

• A61P35/00

  Human Necessities · mapped topic

• A61K31/5513

  Human Necessities · mapped topic

• A61K31/337

  Human Necessities · mapped topic

• A61K45/06

  Human Necessities · mapped topic