Compounds and methods for modulating cxcr3 function

Title: Compounds and methods for modulating cxcr3 function

Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Hetero Ring Is Six-membered And Includes At Least Nitrogen And Oxygen As Ring Hetero Atoms (e.g., Monocyclic 1,2- And 1,3-oxazines, Etc.), Morpholines (i.e., Fully Hydrogenated 1,4- Oxazines), Additional Hetero Ring Attached Directly Or Indirectly To The Morpholine Ring By Nonionic Bonding, Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos, ,

Brief Patent Description - Full Patent Description - Patent Claims

The Patent Description & Claims data below is from USPTO Patent Application 20060063763, Compounds and methods for modulating cxcr3 function.

1. A compound having the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R.sup.1 is a member selected from the group consisting of substituted or unsubstituted (C.sub.5-C.sub.15)alkyl; R.sup.2 is a member selected from the group consisting of substituted or unsubstituted (C.sub.1-C.sub.8)alkyl; each R.sup.3 is an aryl substituent; X is a member selected from the group consisting of CH and N; Y is a member selected from the group consisting of substituted or unsubstituted (C.sub.2-C.sub.8)alkylene and substituted or unsubstituted (C.sub.2-C.sub.8)heteroalkylene; and Z is --NR.sup.4R.sup.5, wherein R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen and (C.sub.1-C.sub.8)alkyl, or optionally are combined with the nitrogen atom to which each is attached to form a 5-, 6- or 7-membered ring.

2. A compound in accordance with claim 1, wherein X is N.

3. A compound in accordance with claim 1, wherein X is N, and Ar is substituted phenyl.

4. A compound in accordance with claim 1, wherein X is N, Ar is substituted phenyl, and R.sup.1 is a (C.sub.8-C.sub.14)acyl group.

5. A compound in accordance with claim 1, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, and R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl.

6. A compound in accordance with claim 1, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl, and Y is (C.sub.2-C.sub.5)alkylene.

7. A compound in accordance with claim 1, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl, Y is (C.sub.2-C.sub.5)alkylene, and Z is dimethylamino.

8. A compound in accordance with claim 1, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl, Y is (C.sub.2-C.sub.5)alkylene, Z is dimethylamino, and n is 0.

9. A compound in accordance with claim 1, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, R.sup.2 is methyl, Y is ethylene, Z is dimethylamino, and n is 0.

10. A compound in accordance with claim 9, wherein said substituted phenyl is selected from the group consisting of 4-fluorophenyl, 4-methoxyphenyl, 4-chlorophenyl, 4-methylphenyl, and 4-bromophenyl.

11. A composition comprising a pharmaceutically acceptable excipient and a compound having the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R.sup.1 is a member selected from the group consisting of substituted or unsubstituted (C.sub.5-C.sub.15)alkyl; R.sup.2 is a member selected from the group consisting of substituted or unsubstituted (C.sub.1-C.sub.8)alkyl; each R.sup.3 is an aryl substituent; X is a member selected from the group consisting of CH and N; Y is a member selected from the group consisting of substituted or unsubstituted (C.sub.2-C.sub.8)alkylene and substituted or unsubstituted (C.sub.2-C.sub.8)heteroalkylene; and Z is --NR.sup.4R.sup.5, wherein R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen and (C.sub.1-C.sub.8)alkyl, or optionally are combined with the nitrogen atom to which each is attached to form a 5-, 6- or 7-membered ring.

12. A composition in accordance with claim 11, wherein X is N.

13. A composition in accordance with claim 11, wherein X is N, and Ar is substituted phenyl.

14. A composition in accordance with claim 11, wherein X is N, Ar is substituted phenyl, and R.sup.1 is a (C.sub.8-C.sub.14)acyl group.

15. A composition in accordance with claim 11, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, and R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl.

16. A composition in accordance with claim 11, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl, and Y is (C.sub.2-C.sub.5)alkylene.

17. A composition in accordance with claim 11, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl, Y is (C.sub.2-C.sub.5)alkylene, and Z is dimethylamino.

18. A composition in accordance with claim 11, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl, Y is (C.sub.2-C.sub.5)alkylene, Z is dimethylamino, and n is 0.

19. A composition in accordance with claim 11, wherein X is N, Ar is substituted phenyl, R.sup.1 is a (C.sub.8-C.sub.14)acyl group, R.sup.2 is methyl, Y is ethylene, Z is dimethylamino, and n is 0.

20. A composition in accordance with claim 19, wherein said substituted phenyl is selected from the group consisting of 4-fluorophenyl, 4-methoxyphenyl, 4-chlorophenyl, 4-methylphenyl, and 4-bromophenyl.

21. A method of modulating CXCR3 function, said method comprising contacting a CXCR3 protein or truncated form thereof with a CXCR3-modulating amount of a compound having the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R.sup.1 is a member selected from the group consisting of substituted or unsubstituted (C.sub.5-C.sub.15)alkyl; R.sup.2 is a member selected from the group consisting of substituted or unsubstituted (C.sub.1-C.sub.8)alkyl; each R.sup.3 is an aryl substituent; X is a member selected from the group consisting of CH and N; Y is a member selected from the group consisting of substituted or unsubstituted (C.sub.2-C.sub.8)alkylene and substituted or unsubstituted (C.sub.2-C.sub.8)heteroalkylene; and Z is --NR.sup.4R.sup.5, wherein R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen and (C.sub.1-C.sub.8)alkyl, or optionally are combined with the nitrogen atom to which each is attached to form a 5-, 6- or 7-membered ring.

22. A method of treating a CXCR3-mediated condition or disease in a subject, said method comprising administering to a subject in need of such treatment an effective amount of a compound having the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R.sup.1 is a member selected from the group consisting of substituted or unsubstituted (C.sub.5-C.sub.15)alkyl; R is a member selected from the group consisting of substituted or unsubstituted (C.sub.1-C.sub.8)alkyl; each R.sup.3 is an aryl substituent; X is a member selected from the group consisting of CH and N; Y is a member selected from the group consisting of substituted or unsubstituted (C.sub.2-C.sub.8)alkylene and substituted or unsubstituted (C.sub.2-C.sub.8)heteroalkylene; and Z is --NR.sup.4R.sup.5, wherein R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen and (C.sub.1-C.sub.8)alkyl.

23. A method in accordance with claim 22, wherein said CXCR3-mediated condition or disease is selected from the group consisting of multiple sclerosis, rheumatoid arthritis, type I diabetes, psoriasis, cancer and HIV infection.

24. A method in accordance with claim 22, wherein said CXCR3-mediated condition or disease is multiple sclerosis.

25. A method in accordance with claim 22, wherein said administration is oral or intravenous.

26. A method in accordance with claim 22, wherein said subject is selected from the group consisting of human, rat, dog, cow, horse, and mouse.

27. A method in accordance with claim 22, wherein said subject is human.

28. A method in accordance with claim 22, wherein n is 0, Ar is substituted phenyl, R.sup.1 is unsubstituted (CS--C.sub.15)acyl, R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl, X is N, Y is unsubstituted (C.sub.2-C.sub.4)alkylene, and Z is selected from the group consisting of methylamino, dimethylamino, ethylamino and diethylamino.

29. A method in accordance with claim 22, wherein said CXCR3-mediated disease or condition is selected from the group consisting of multiple sclerosis, rheumatoid arthritis, type I diabetes, psoriasis, cancer and HIV infection; n is 0, Ar is substituted phenyl, R.sup.1 is unsubstituted (C.sub.5-C.sub.15)acyl, R.sup.2 is unsubstituted (C.sub.1-C.sub.4)alkyl, X is N, Y is unsubstituted (C.sub.2-C.sub.4)alkylene, and Z is selected from the group consisting of methylamino, dimethylamino, ethylamino and diethylamino.

Brief Patent Description - Full Patent Description - Patent Claims

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