| US 7,576,221 B2 | ||
| Substituted imidazole derivatives | ||
| Weibo Wang, Moraga, Calif. (US); Paul A. Barsanti, Pleasant Hill, Calif. (US); Yia Xia, Palo Alto, Calif. (US); Rustum Boyce, Singapore (Singapore); Sabina Pecchi, Oakland, Calif. (US); Nathan Brammeier, Walnut Creek, Calif. (US); Megan C. Phillips, Walnut Creek, Calif. (US); Kris Mendenhall, Concord, Calif. (US); Kelly Wayman, San Rafael, Calif. (US); Liana Marie Lagniton, Berkeley, Calif. (US); Ryan Constantine, Salt Lake City, Utah (US); Hong Yang, Pleasant Hill, Calif. (US); Elizabeth Mieuli, Oakland, Calif. (US); Savithri Ramurthy, Walnut Creek, Calif. (US); Elisa Jazan, Richmond, Calif. (US); Anu Sharma, El Cerrito, Calif. (US); Rama Jain, Fremont, Calif. (US); Sharadha Subramanian, San Ramon, Calif. (US); Paul A. Renhowe, Danville, Calif. (US); Kenneth W. Bair, Oakland, Calif. (US); David Duhl, Oakland, Calif. (US); Annette Walter, Mill Valley, Calif. (US); Tinya Abrams, Richmond, Calif. (US); Kay Huh, San Mateo, Calif. (US); Eric Martin, El Cerrito, Calif. (US); Mark Knapp, Oakland, Calif. (US); and Vincent P. Le, San Francisco, Calif. (US) | ||
| Assigned to Novartis Vaccines and Diagnostics, Inc., Emeryville, Calif. (US) | ||
| Filed on Jun. 20, 2005, as Appl. No. 11/158,574. | ||
| Claims priority of provisional application 60/580927, filed on Jun. 18, 2004. | ||
| Prior Publication US 2006/0009472 A1, Jan. 12, 2006 | ||
| Int. Cl. A61K 31/4174 (2006.01); C07D 233/64 (2006.01) | ||
| U.S. Cl. 548—338.1 [514/400] | 18 Claims |
1. A compound represented by the formula:
 wherein:
X1 is —C(O)—;
A2 is selected from the group consisting of aryl, heteroaryl, heterocyclic, and cycloalkyl, all of which may be optionally substituted
with 1 to 4 substituents selected from the group consisting of alkyl, substituted alkyl, alkoxy, substituted alkoxy, amino,
halo, hydroxy, and nitro;
A is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally
substituted aryl, carboxyl, carboxyl ester, aminoacyl, optionally substituted heteroaryl, optionally substituted heterocyclic,
and optionally substituted cycloalkyl,
wherein the optionally substituted groups are substituted with 1 to 4 substituents selected from the group consisting of alkyl,
substituted alkyl, alkoxy, substituted alkoxy, amino, substituted amino, aryloxy, substituted aryloxy, cyano, aryl, substituted
aryl, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, heterocyclyloxy, substituted heterocyclyloxy,
acyl, carboxyl, carboxyl ester, oxo (except when A is optionally substituted aryl or optionally substituted heteroaryl), halo,
hydroxy, —S(O)2—R9 where R9 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl, and nitro;
R8 is selected from the group consisting of alkyl, alkenyl, alkynyl, —CF3, alkoxy, cyano, halo, and hydroxy;
R4 is -[alkylene]p-NR10R11 wherein p is an integer from 0 to 1,
alkylene is a straight chained alkylene optionally mono- or disubstituted with one of the foregoing substituents selected
from the group consisting of amino, substituted amino, hydroxy, alkyl, substituted alkyl, carboxyl, carboxyl ester, oxo, spirocycloalkyl,
and halo;
R10 and R11 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, —S(O)-alkyl, —S(O)-substituted
alkyl, —S(O)2-alkyl, —S(O)2-substituted alkyl, heterocyclic, substituted heterocyclic, acyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl,
cycloalkyl, and substituted cycloalkyl or when R10 is hydrogen, R11 is hydroxy, alkoxy or substituted alkoxy;
R15 is selected from the group consisting of ethyl, isopropyl, t-butyl, or phenyl;
R16 is hydrogen or methyl;
R17 is hydrogen or methyl;
m1 is an integer equal to 0,1 or 2;
or pharmaceutically acceptable salts, esters or prodrugs thereof.
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