IP Library › Granted Patent US 10,040,770
Granted Patent B2
US 10,040,770 · App. 15/616,039 · Granted Aug 7, 2018

Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith

Inventors: Mercedes Delgado (San Diego, CA); Jan Elsner (Solana Beach, CA); Paul Erdman (San Diego, CA); Robert Hilgraf (San Diego, CA); Laurie Ann LeBrun (San Diego, CA); Meg McCarrick (San Diego, CA); Mark A. Nagy (Encinitas, CA); Stephen Norris (San Diego, CA); David A. Paisner (Portland, OR); Yoshitaka Satoh (Poway, CA); Marianne Sloss (San Diego, CA); Jayashree Tikhe (San Diego, CA); Won Hyung Yoon (San Diego, CA)
Assignee: Signal Pharmaceuticals, LLC
C07D239/48A61K31/505C07D401/04C07D401/12C07D403/12C07D405/12C07D409/12
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Quick Facts
Patent No.
US 10,040,770
App. No.
15/616,039
Granted
Aug 7, 2018
Kind
B2
Abstract

Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R 1 , R 2 , R 3 , and R 4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.

Claims (27)

1. A compound of formula (I):

or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof,

wherein:

R 1 is substituted or unsubstituted branched C 3-8 alkyl; and

R 2 is substituted or unsubstituted cyclohexyl,

wherein the compound at a concentration of 10 μM inhibits JNK1 by at least about 50%.

2. The compound of claim 1 , wherein R 1 is an unsubstituted branched C 3-8 alkyl.

3. The compound of claim 1 , wherein R 2 is a substituted cyclohexyl.

4. A compound of formula (TB):

or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof,

wherein:

R 3 is substituted or unsubstituted branched C 3-8 alkyl; and

R 4 is substituted or unsubstituted cyclohexyl.

5. The compound of claim 4 , wherein R 4 is a substituted cyclohexyl.

6. A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, and a pharmaceutically acceptable carrier, excipient or vehicle.

7. The compound of claim 1 , wherein the compound is 4-((1R,3S)-3-hydroxycyclohexylamino)-2-(isopropylamino)pyrimidine-5-carboxamide.

8. The compound of claim 1 , wherein the compound is 4-((1R,3S)-3-hydroxy-3-methylcyclohexylamino)-2-(isopropylamino)pyrimidine-5-carboxamide.

9. The compound of claim 1 , wherein the compound is 4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-2-(isopropylamino)pyrimidine-5-carboxamide.

10. The compound of claim 1 , wherein the compound is 4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-2-(tert-pentylamino)pyrimidine-5-carboxamide.

11. The compound of claim 1 , wherein the compound is 2-(tert-Butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide.

12. The compound of claim 1 , wherein the compound is 4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-2-(3-methylpentan-3-ylamino)pyrimidine-5-carboxamide.

13. The compound of claim 1 , wherein the compound is 4-((1R,3S)-3-hydroxycyclohexylamino)-2-(tert-pentylamino)pyrimidine-5-carboxamide.

14. The compound of claim 1 , wherein the compound is 2-(2,3-dimethylbutan-2-ylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)pyrimidine-5-carboxamide.

15. The compound of claim 1 , wherein the compound is 2-(sec-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)pyrimidine-5-carboxamide.

16. The compound of claim 1 , wherein the compound is 2-((R)-3,3-dimethylbutan-2-ylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)pyrimidine-5-carboxamide.

17. The compound of claim 4 , wherein the compound at a concentration of 10 μM inhibits JNK1 by at least about 50%.

18. A pharmaceutical composition comprising an effective amount of a compound of claim 4 , or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, and a pharmaceutically acceptable carrier, excipient or vehicle.

Continuity (5)
Continuation 14814633 · Jul 31, 2015
Continuation 13451574 · Apr 20, 2012
Provisional Application 61555339 · Nov 3, 2011
Provisional Application 61478076 · Apr 22, 2011
Related Publication 20170267647A1 · Sep 21, 2017