| US 7,553,854 B2 | ||
| 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling | ||
| James C Sutton, Pleasanton, Calif. (US); Marion Wiesmann, Brisbane, Calif. (US); Weibo Wang, Moraga, Calif. (US); Mika Lindvall, Oakland, Calif. (US); Jiong Lan, Moraga, Calif. (US); Savithri Ramurthy, Walnut Creek, Calif. (US); Anu Sharma, El Cerrito, Calif. (US); Elizabeth J. Mieuli, Stanford, Calif. (US); Liana M. Klivansky, Oakland, Calif. (US); William Lenahan, San Leandro, Calif. (US); Susan Kaufman, Lafayette, Calif. (US); Hong Yang, Foster City, Calif. (US); Simon C. Ng, Walnut Creek, Calif. (US); Keith Pfister, San Ramon, Calif. (US); Allan S. Wagman, Belmont, Calif. (US); Victoria Sung, San Francisco, Calif. (US); and Martin Sendzik, San Mateo, Calif. (US) | ||
| Assigned to Novartis Vaccines and Diagnostics, Inc., Emeryville, Calif. (US) | ||
| Filed on Apr. 18, 2007, as Appl. No. 11/737,069. | ||
| Claims priority of provisional application 60/793517, filed on Apr. 19, 2006. | ||
| Claims priority of provisional application 60/893857, filed on Mar. 08, 2007. | ||
| Prior Publication US 2008/0045528 A1, Feb. 21, 2008 | ||
| Int. Cl. C07D 215/00 (2006.01); A61K 31/44 (2006.01) | ||
| U.S. Cl. 514—312 [514/338; 546/153; 546/270.1; 546/271.7] | 78 Claims |
1. A compound, stereoisomer, tautomer, oxide, or ester, of Formula (I) or a pharmaceutically acceptable salt thereof
 wherein X is O, S, or S(O);
R1 and R2 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, acyl, cycloalkyl, substituted
cycloalkyl, cycloalkenyl, substituted cycloalkenyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl,
and substituted heteroaryl; or
R1 and R2 are taken together to form a group selected from heterocyclyl, substituted heterocyclyl, heteroaryl, or substituted heteroaryl;
R3 is selected from the group consisting of halo, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl,
carbonitrile, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heteroaryl,
substituted heteroaryl, heterocyclyl, substituted heterocyclyl, amino, substituted amino, acyl, acylamino, alkoxy, substituted
alkoxy, carboxyl, carboxyl ester, substituted sulfonyl, aminosulfonyl, and aminocarbonyl;
each R6 is independently alkyl, substituted alkyl, alkoxy, substituted alkoxy, amino, substituted amino, or halo;
n is 0, 1, or 2; and
when X is O, R4 is hydrogen, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, or substituted alkynyl, and R5 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aminocarbonyl, halo, heteroaryl,
substituted heteroaryl, cycloalkyl, or substituted cycloalkyl, or R4 and R5 are taken together to form a group selected from heterocyclyl, substituted heterocyclyl, cycloalkyl, substituted cycloalkyl,
aryl, substituted aryl, heteroaryl, and substituted heteroaryl; and
when X is S or S(O), R4 is hydrogen, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, or substituted alkynyl, and R5 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aminocarbonyl, halo, heteroaryl,
substituted heteroaryl, cycloalkyl, or substituted cycloalkyl.
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