US 9,427,442 B2 · Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds

Abstract

Disclosed are compounds of Formula (I): (Formula (I)) wherein: R1 is —CH2CH2CF3; R2 is —CH2CH2CH2F, —CH2CF2CH3, —CH2CH2CF3, —CH2CH(CH3)CF3, —CH2CH2CF2CH3, (Formulae (II), (III), (IV), (V) or (VI): R3 is H or —CH3; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, 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.

Claims7

Dependent claims

A compound of Formula (I):

wherein:
R1 is —CH2CH2CF3;
R2 is —CH2CH2CH2F, —CH2CF2CH3, —CH2CH(CH3)CF3, —CH2CH2CF2CH3,
R3 is H or —CH3;
Ring A is phenyl or pyridinyl;
each Ra is independently F, Cl, —CN, —OH, —CH3, cyclopropyl, —CF3, —OCH3, —OCF3, and/or —O(cyclopropyl);
each Rb is independently F, Cl, —CH3, —CF3, —CN, and/or —OCH3;
y is zero, 1, or 2;
and
z is zero, 1, or 2.

7 more elements

Dependencies are inferred from the claim text.

Facts

Application

14/429,958Filed 20 Sep 2013 · us provisional application

Priority

21 Sep 2012

Published

US 2015/0231152 A120 Aug 2015

Granted

30 Aug 2016

Term ends

Not estimatedThe source records don’t support an estimate.

Classification13 codes

A61K 31/5513
Having two nitrogen atoms, e.g. dilazep: 1,4-Benzodiazepines, e.g. diazepam or clozapine
A61K 31/138
Having aromatic rings , e.g. ketamine, nortriptyline: aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 31/337
Having oxygen as the only ring hetero atom, e.g. fungichromin: having four-membered rings, e.g. taxol
A61K 31/506
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim: not condensed and containing further heterocyclic rings

Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds

Life of this patent

Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds

Life of this patent

Abstract

Claims7