IP Library Granted Patent US 9,120,778
Granted Patent B2
US 9,120,778 · App. 14/681,981 · Granted Sep 1, 2015

Uracil derivatives as AXL and c-MET kinase inhibitors

Inventors: Reddeppa Reddy Dandu (Downingtown, PA); Robert L. Hudkins (Chester Springs, PA); Kurt A. Josef (Radnor, PA); Catherine P. Prouty (Doylestown, PA); Rabindranath Tripathy (Churchville, PA)
Assignee: Ignyta, Inc.
C07D401/12A61K31/4725A61K31/506C07D239/54C07D403/12
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Quick Facts
Patent No.
US 9,120,778
App. No.
14/681,981
Granted
Sep 1, 2015
Kind
B2
Abstract

The present application provides compounds of Formula I or salt forms thereof, wherein R a , R b , R c , R d , D, W, R 1a , R 1b , R 1c , Y, R 3 , X, E and G are as defined herein, compositions, methods of treatment and uses thereof.

Claims (13)

1. A compound which is 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide having the structure

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound which is 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide having the structure

or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

3. The pharmaceutical composition according to claim 2 , wherein the composition comprises from about 0.1 mg to about 1,000 mg of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

4. The pharmaceutical composition according to claim 3 , wherein the composition comprises from about 1 mg to about 1,000 mg of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

5. The pharmaceutical composition according to claim 4 , wherein the composition comprises from about 1 mg to about 500 mg of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

6. The pharmaceutical composition according to claim 5 , wherein the composition comprises from about 1 mg to about 100 mg of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

7. The pharmaceutical composition according to claim 2 , wherein the composition comprises from about 1% to about 95% (w/w) of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

8. The pharmaceutical composition according to claim 7 , wherein the composition comprises from about 10% to about 80% (w/w) of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

9. The pharmaceutical composition according to claim 8 , wherein the composition comprises from about 20% to about 70% (w/w) of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

10. The pharmaceutical composition according to claim 9 , wherein the composition comprises from about 30% to about 60% (w/w) of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

11. The pharmaceutical composition according to claim 10 , wherein the composition comprises from about 40% to about 50% (w/w) of 3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid [4-(6,7-dimethoxyquinolin-4-yloxy)-3-fluorophenyl]-amide, or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2015
From: DANDU, REDDEPPA REDDY; HUDKINS, ROBERT L.; JOSEF, KURT A.; PROUTY, CATHERINE P.; TRIPATHY, RABINDRANATH
To: CEPHALON, INC.
Reel/Frame 035691/0979 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2015
From: CEPHALON, INC.
To: IGNYTA, INC.
Reel/Frame 035692/0026 →
Continuity (4)
Continuation 14276138 · May 13, 2014
Continuation PCTUS2012065019 · Nov 14, 2012
Provisional Application 61559312 · Nov 14, 2011
Related Publication 20150210670A1 · Jul 30, 2015