| US 7,482,366 B2 | ||
| Modulators of LXR | ||
| Christopher D Bayne, San Diego, Calif. (US); Alan T Johnson, Poway, Calif. (US); Shao-Po Lu, San Diego, Calif. (US); Raju Mohan, Encinitas, Calif. (US); Michael C Nyman, San Diego, Calif. (US); Edwin J Schweiger, San Diego, Calif. (US); William C Stevens, Jr., San Diego, Calif. (US); Haixia Wang, San Diego, Calif. (US); and Yinong Xie, San Diego, Calif. (US) | ||
| Assigned to X-Ceptor Therapeutics, Inc., San Diego, Calif. (US) | ||
| Filed on Jul. 24, 2004, as Appl. No. 10/899,458. | ||
| Application 10/899458 is a continuation in part of application No. 10/327813, filed on Dec. 20, 2002. | ||
| Claims priority of provisional application 60/342707, filed on Dec. 21, 2001. | ||
| Prior Publication US 2005/0080111 A1, Apr. 14, 2005 | ||
| Int. Cl. A61K 31/443 (2006.01); A61K 31/4436 (2006.01); C07D 409/04 (2006.01); C07D 405/04 (2006.01) | ||
| U.S. Cl. 514—336 [546/280.4; 546/283.4] | 31 Claims |
1. A compound of formula (I):
 n is 1 to 4;
m is 1 to 4;
ring A is furyl or thienyl, each substituted with n R4 groups;
ring B is phenyl, naphthyl, heterocyclyl, or heteroaryl, each substituted with m R5 groups;
R1 is hydrogen, aralkyl or heteroarylalkyl;
R2 is hydrogen, cyano, —R7—N(R8)2, —R7—N(R8)S(O)2R10 or —R7—N(R8)C(NR8)N(R8)2;
R3 is hydrogen, alkyl, alkenyl, aralkyl, aralkenyl, haloalkyl, haloalkenyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl,
heteroaryl or heteroarylalkyl;
each R4 is independently hydrogen, halo, alkyl or haloalkyl;
each R5 is independently selected from the group consisting of hydrogen, halo, nitro, alkyl, alkenyl, aryl, aralkyl, aralkenyl, haloalkyl,
haloalkenyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, —R7—CN, —R7—N(R8)2, —R7—OR8, —R7—O—R9—C(O)OR8, —R7—C(O)R11, —R7—C(O)OR8, —R7—C(O)N(R8)2, —R7—C(O)N(R8)OR8, —R7—C(O)N(R8)N(R8)2, —R7—C(O)N(R8)—R9—C(O)OR8, —R7—C(S)N(R8)2, —R7—N(R8)C(O)R8, —R7—N(R8)C(O)OR10, —R7—S(O)tR8 (where t is 0 to 2) and —R7—S(O)2N(R8)2;
R6 is —OR7—, —N(R8)—, a direct bond, a straight or branched alkylene chain, a straight or branched alkenylene chain or a straight or branched
alkynylene chain;
each R7 is independently selected from a direct bond, a straight or branched alkylene chain or a straight or branched alkenylene chain;
each R8 is independently selected from hydrogen, alkyl, alkenyl, haloalkyl, haloalkenyl, aryl, aralkyl, aralkenyl, cycloalkyl, cycloalkylalkyl,
heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl;
each R9 is independently selected from a straight or branched alkylene chain or a straight or branched alkenylene chain;
each R10 is independently selected from alkyl, aryl, aralkyl or cycloalkylalkyl; and
R11 is hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heterarylalkyl;
as a mixture of stereoisomers, a racemic mixture thereof of stereoisomers, or as a tautomer;
or as a pharmaceutically acceptable salt or prodrug thereof.
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