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US 2004/0171638 A1Published application
Chemokine receptor binding heterocyclic compounds
AssigneeAnorMED, Inc.
InventorsGary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
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Abstract
Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.
Claims21
A compound of the formula
- 135
- and the salts and prodrug forms thereof
- wherein
- the dotted lines represent optional unsaturation;
- R1 is a non-interfering substituent selected from halo, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyl, substituted or unsubstituted amino, substituted or unsubstituted thiol, and substituted or unsubstituted acyl;
- k is 0-3;
- each n is independently 0 or 1;
- each R is independently H or alkyl (1-6C);
- W is a 5-6 membered heterocyclic ring comprising one or more heterotoms, optionally fused with a benzene ring, or a benzene ring fused with another 5-6 membered heterocyclic ring, optionally containing a double bond;
- wherein W is optionally substituted with Yj;
- j is 0-3;
- each Y is independently a non-interfering substituent selected from the group consisting of halo, OR;
- SH;
- SO;
- SO2;
- optionally substituted phenyl;
- —(CR2)mOR;
- —(CR2)mCOR;
- —(CR2)mCOOR;
- —(CR2)mN═CH—NR2;
- —(CR2)mCN;
- —(CR2)mNR52;
- —(CR2)mNR(CR2)mNRR4;
- —(CR2)mNR(CR2)mNR(CR2)mNR52;
- —(CR2)mCO(CR2)mNR52;
- —(CR2)mCO(CR2)mNR(CR2)mNRR4;
- —(CR2)mCO(CR2)mNR(CR2)mNR(CR2)mNR52;
- —(CR2)mNRCO(CR2)mNRR4;
- —(CR2)mNRCO(CR2)mNR(CR2)mNR52;
- —(CR2)mNRCO(CR2)mNR(CR2)mNR(CR2)mNR(CR2)mNR52;
- —(CR2)mNROH;
- —(CR2)mCONROH;
- —(CR2)mCR═NOH;
- —(CR2)mguanidino;
- —(CR2)mCONHNHR;
- and
- —(CR2)mamidino;
- wherein R is H or alkyl (1-6C), each m is independently 0-4, and each R4 and each R5 is independently H, alkyl (1-6C), alkenyl (1-6C), alkynyl (1-6C), or acyl (1-6C), each optionally substituted by one or more nonaromatic, nonheterocyclic substituent(s) and a indicates the linker between Ring A and N and b indicates the linker between ring E and the N.
35 more elements
Dependencies are inferred from the claim text.