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US 2003/0119854 A1Published application
Compounds and methods for modulating CXCR3 function
AssigneeChemoCentryx, Inc.
InventorsThomas J. Schall, Daniel J. Dairaghi, Brian E. McMaster
Life of this patent
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Abstract
Compounds and compositions are provided that bind to the CXCR3 chemokine receptor and which are useful for treating diseases associated with CXCR3 activity, such as multiple sclerosis.
Claims29
A compound having the formula:
- 37
- 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;
- R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl;
- R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl;
- each R3 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 (C2-C8)alkylene and substituted or unsubstituted (C2-C8) heteroalkylene;
- and
- Z is —NR4R5,
- wherein R4 and R5 are independently selected from the group consisting of hydrogen and (C1-C8)alkyl, or optionally are combined with the nitrogen atom to which each is attached to form a 5-, 6- or 7-membered ring.
9 more elements
A composition comprising a pharmaceutically acceptable excipient and a compound having the formula:
- 38
- 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;
- R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl;
- R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl;
- each R3 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 (C2-C8)alkylene and substituted or unsubstituted (C2-C8) heteroalkylene;
- and
- Z is—NR4R5,
- wherein R4 and R5 are independently selected from the group consisting of hydrogen and (C1-C8)alkyl, or optionally are combined with the nitrogen atom to which each is attached to form a 5-, 6- or 7-membered ring.
9 more elements
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:
- 39
- 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;
- R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl;
- R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl;
- each R3 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 (C2-C8)alkylene and substituted or unsubstituted (C2-C8) heteroalkylene;
- and
- Z is —NR4R5,
- wherein R4 and R5 are independently selected from the group consisting of hydrogen and (C1-C8)alkyl, or optionally are combined with the nitrogen atom to which each is attached to form a 5-, 6- or 7-membered ring.
9 more elements
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:
- 40
- 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;
- R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl;
- R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl;
- each R3 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 (C2-C8)alkylene and substituted or unsubstituted (C2-C8) heteroalkylene;
- and
- Z is —NR4R5,
- wherein R4 and R5 are independently selected from the group consisting of hydrogen and (C1-C8)alkyl.
9 more elements
Dependencies are inferred from the claim text.