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US 8,013,001 B2Granted
Modulators of LXR
AssigneeExelixis, Inc.
InventorsChristopher D. Bayne, Alan T. Johnson, Shao Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Jr., Haixia Wang, Yinong Xie
Life of this patent
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Abstract
Compounds of the invention, such as compounds of formula (I): where n, m, A, B, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
Claims34
A compound having the following formula (II):
- wherein:
- n is 0 to 4;
- m is 0 to 5;
- R1 is hydrogen, aralkyl or heteroarylalkyl;
- R2 is hydrogen, cyano or —R7—N(R8)2;
- R3 is haloalkyl;
- each R4 is independently halo, alkyl or haloalkyl;
- each R5 is independently selected from the group consisting of 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)OR10, —R7—S(O)tR8 (where t is 0 to 2) and —R7—S(O)2N(R8)2;
- R6 is —OR7—, 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;
- R10 is alkyl, aryl, aralkyl or cycloalkylalkyl;
- and
- R11 is hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heterarylalkyl;
- as a stereoisomer, a mixture of stereoisomers, a racemic mixture of stereoisomers, or as a tautomer;
- or as a pharmaceutically acceptable salt thereof.
14 more elements
Dependencies are inferred from the claim text.