PYRIDO[2,3-d]PYRIMIDIN-7-ONES AND RELATED COMPOUNDS AS INHIBITORS OF PROTEIN KINASES

Patent metadata

Field	Value
Publication number	US-2024327403-A1
Application number	US-202418581677-A
Country	US
Kind code	A1
Filing date	Feb 20, 2024
Priority date	May 15, 2017
Publication date	Oct 3, 2024
Grant date	—

Abstract

Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.

First claim

1 - 12 . (canceled)

13 . A compound demonstrating protein kinase inhibitory activity and having a structure of:

wherein R is H, or R is

 at one available ring position, wherein Me is methyl and Et is ethyl;
A and D are independently N or CH;
E is N, CH, or C—R;
B and C are independently N, CH, or C—Cl;
R 1 is H, or R 1 is Cl, F, OCH 3 , C(CH 3 ) 3 , or OH at one available ring position; and
X—Y is C═C.

14 . A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 13 and a pharmaceutically acceptable excipient, adjuvant, carrier, buffer, stabilizer, or mixture thereof.

15 . A method of treating a protein kinase related disease or condition comprising administering the pharmaceutical composition of claim 14 .

16 . A compound demonstrating protein kinase inhibitory activity and having a structure of:

wherein R is H,

 wherein Me is methyl and Et is ethyl;
R 1 is any alkyl or aryl group;
A and D are independently N or CH;
E is N, CH, or C—R;
B and C are independently N, CH, or C—Cl;
R 3 is H, or R 3 is Cl, F, OCH 3 , C(CH 3 ) 3 , or OH at one available ring position; and
X—Y is C═C.

17 . The compound of claim 16 , wherein R 1 is methyl, ethyl, or propyl.

18 . A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 17 and a pharmaceutically acceptable excipient, adjuvant, carrier, buffer, stabilizer, or mixture thereof.

19 . A method of treating a protein kinase related disease or condition comprising administering the pharmaceutical composition of claim 18 .

Assignees

• Univ Houston System
• Tufts College

Inventors

• Cuny Gregory
• Nikhar Sameer
• Degterev Alexei

Classifications

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P19/00

  Drugs for skeletal disorders · CPC title

• C07D471/04 Primary

  Ortho-condensed systems · CPC title