➤ Get the DrugPatentWatch Daily Briefing

Get Daily Updates on Generic Entry, Litigation, Biosimilars, and more …

Serving leading biopharmaceutical companies globally:

Express Scripts
Colorcon
McKinsey
Baxter
AstraZeneca
Harvard Business School

Last Updated: December 1, 2020

DrugPatentWatch Database Preview

Claims for Patent: 7,528,143

➤ Get the DrugPatentWatch Daily Briefing
» See Plans and Pricing

« Back to Dashboard

Summary for Patent: 7,528,143
Title:Bi-aryl meta-pyrimidine inhibitors of kinases
Abstract: The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases. ##STR00001##
Inventor(s): Noronha; Glenn (Oceanside, CA), Mak; Chi Ching (San Diego, CA), Cao; Jianguo (San Diego, CA), Renick; Joel (San Diego, CA), McPherson; Andrew (San Diego, CA), Zeng; Binqi (San Diego, CA), Pathak; Ved P. (San Diego, CA), Lohse; Daniel L. (San Diego, CA), Hood; John D. (San Diego, CA), Soll; Richard M. (San Diego, CA)
Assignee: TargeGen, Inc. (San Diego, CA)
Application Number:11/588,638
Patent Claims: 1. A compound having the structure (A): ##STR00472## wherein: X is selected from a group consisting of a bond, O, SO.sub.2, and CH.sub.2; Y is selected from a group consisting of a bond or NR.sup.9; or X and Y taken together is a bond; each of R.sup.1 and R.sup.2 is independently selected from a group consisting of H, C.sub.1-C.sub.6 alkyl, cycloalkyl; or R.sup.1 and R.sup.2 taken together is a bond; or R.sup.1 and R.sup.2 taken together form a moiety selected from a group consisting of (CH.sub.2).sub.m, (CH.sub.2).sub.r--S--(CH.sub.2).sub.m, (CH.sub.2).sub.r--SO--(CH.sub.2).sub.m, (CH.sub.2).sub.r--SO.sub.2--(CH.sub.2).sub.m, (CH.sub.2).sub.r--NR.sup.9--(CH.sub.2).sub.m, and (CH.sub.2).sub.r--O--(CH.sub.2).sub.m; each of p, q, r, n, m is independently an integer having the value between 0 and 6, R.sup.9 is selected from a group consisting of H, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 cycloalkyl, C.sub.1-C.sub.6 branched alkyl, C.sub.1-C.sub.6 aminoalkyl, and C.sub.1-C.sub.6 hydroxyalkyl; G.sub.0 is selected from a group consisting of N, O, H, and CH, G is CH or C when bonded to X; R.sup.5 methyl; ##STR00473## wherein each of R.sup.6 and R.sup.7 is independently selected from a group consisting of C.sub.1-C.sub.6 alkenyl, C.sub.1-C.sub.6 alkynyl, C.sub.1-C.sub.6 hydroxyalkyl or aminoalkyl, C.sub.1-C.sub.6 cycloalkyl, C.sub.1-C.sub.6 alkoxy, a halogen, CF.sub.3, OCF.sub.3, SO.sub.2H, SO.sub.2(C.sub.1-C.sub.6 alkyl), SO.sub.2-heterocycle, SO.sub.2-cycloalkyl, SO.sub.2N(C.sub.1-C.sub.6 alkyl)H, SO.sub.2N(C.sub.1-C.sub.6 alkyl)(C.sub.1-C.sub.6 alkyl), SO.sub.2NH(C.sub.1-C.sub.6 cycloalkyl), SO.sub.2NH-heterocycle, (SO.sub.2N(C.sub.1-C.sub.6 branched alkyl)H, NO.sub.2, CN, OH, CONH.sub.2, CO--(C.sub.1-C.sub.6 alkyl), COOH, COO--(C.sub.1-C.sub.6 alkyl), and NHCO--(C.sub.1-C.sub.6 alkyl), and R.sub.8 is independently selected from the group consisting of H, C.sub.1-C.sub.6 alkenyl, C.sub.1-C.sub.6 alkynyl, C.sub.1-C.sub.6 hydroxyalkyl or aminoalkyl, C.sub.1-C.sub.6 cycloalkyl, halogen, CF.sub.3, OCF.sub.3, SO.sub.2H ,SO.sub.2(C.sub.1-C.sub.6 alkyl), SO.sub.2-heterocycle, SO.sub.2-cycloalkyl, SO.sub.2N(C.sub.1-C.sub.6 alkyl)H, SO.sub.2N(C.sub.1-C.sub.6 alkyl)(C.sub.1-C.sub.6 alkyl), SO.sub.2NH(C.sub.1-C.sub.6 cycloalkyl), SO.sub.2NH-heterocycle, (SO.sub.2N(C.sub.1-C.sub.6 branched alkyl)HNO.sub.2, CN, OH, CONH.sub.2, CO--(C.sub.1-C.sub.6 alkyl), COOH, COO--(C.sub.1-C.sub.6 alkyl), and NHCO--(C.sub.1-C.sub.6 alkyl); A is selected from a group consisting of NH, and N--(C.sub.1-C.sub.6 alkyl); G.sub.1 is CH; G.sub.2 is CR.sup.7, with each group R.sup.7 independent of every other group R.sup.7; and R.sup.3 and R.sup.4, taken together form a heterocyclic ring system, or a pharmaceutically acceptable salt thereof.

2. A compound represented by: a first moiety chemically connected to a second moiety, or a pharmaceutically acceptable salt thereof, wherein the first moiety is selected from the group consisting of: ##STR00474## ##STR00475## ##STR00476## ##STR00477## ##STR00478## ##STR00479## ##STR00480## ##STR00481## ##STR00482## ##STR00483## ##STR00484## ##STR00485## ##STR00486## ##STR00487## ##STR00488## ##STR00489## ##STR00490## ##STR00491## ##STR00492## ##STR00493## ##STR00494## ##STR00495## ##STR00496## and wherein the second moiety is selected from the group consisting of: ##STR00497## ##STR00498## ##STR00499## ##STR00500## ##STR00501## ##STR00502## ##STR00503## ##STR00504##

3. The compound of claim 1, wherein the compound is ##STR00505##

4. The compound of claim 1, wherein the compound is ##STR00506##

5. The compound of claim 1, wherein the compound is ##STR00507##

6. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00508## ##STR00509##

7. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00510##

8. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00511##

9. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00512##

10. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00513##

11. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00514##

12. The compound of claim 1, wherein the compound is ##STR00515##

13. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00516## ##STR00517##

14. A compound represented by: ##STR00518## and a pharmaceutically acceptable salt thereof.

15. The compound of claim 1, wherein the compound is ##STR00519##

16. The compound of claim 1, wherein the compound is ##STR00520##

17. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00521##

18. A compound, wherein the compound is ##STR00522##

19. The compound of claim 1, wherein the compound is ##STR00523##

20. A compound wherein the compound is selected from the group consisting of: ##STR00524## ##STR00525##

21. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00526##

22. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00527##

23. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00528##

24. The compound of claim 1, wherein the compound is ##STR00529##

25. A compound wherein the compound is selected from the group consisting of: ##STR00530## ##STR00531## and a pharmaceutically acceptable salt thereof.

26. The compound of claim 1, wherein the compound is ##STR00532##

27. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00533##

28. The compound of claim 1, wherein the compound is ##STR00534##

29. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00535##

30. The compound of claim 1, wherein the compound is ##STR00536##

31. The compound of claim 1, wherein the compound is ##STR00537##

32. The compound of claim 1, wherein the compound is ##STR00538##

33. The compound of claim 1, wherein the compound is ##STR00539##

34. The compound of claim 1, wherein the compound is ##STR00540##

35. The compound of claim 1, wherein the compound is ##STR00541##

36. The compound of claim 1, wherein the compound is ##STR00542##

37. The compound of claim 1, wherein X is O.

38. The compound of claim 1, wherein G.sub.0 is N.

39. The compound of claim 37, wherein G.sub.0 is N.

40. The compound of claim 39, wherein Y is a bond, and R.sup.1 and R.sup.2 are each H.

41. The compound of claim 40, wherein R.sub.7 is SO.sub.2NH--(C.sub.1-C.sub.6 branched alkyl).

42. The compound of claim 39, wherein G.sub.2 is CH, R.sup.8 is H and R.sup.5 is H.

43. A compound represented by: ##STR00543## or a pharmaceutically acceptable salt thereof.

44. A pharmaceutical composition comprising: ##STR00544## or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

Johnson and Johnson
AstraZeneca
Baxter
Boehringer Ingelheim
Merck
Harvard Business School

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.