| US 7,485,652 B2 | ||
| Indolyl derivatives as liver-X-receptor (LXR) modulators | ||
| Henrietta Dehmlow, Grenzach-Wyhlen (Germany); Bernd Kuhn, Liestal (Switzerland); Narendra Panday, Basel (Switzerland); Hasane Ratni, Habsheim (France); Tanja Schulz-Gasch, Liestal (Switzerland); and Matthew Blake Wright, Basel (Switzerland) | ||
| Assigned to Hoffmann-La Roche Inc., Nutley, N.J. (US) | ||
| Filed on Dec. 11, 2006, as Appl. No. 11/636,925. | ||
| Application 11/636925 is a division of application No. 11/115942, filed on Apr. 27, 2005, granted, now 7,173,048. | ||
| Claims priority of application No. 04101889 (EP), filed on May 03, 2004. | ||
| Prior Publication US 2007/0099916 A1, May 03, 2007 | ||
| Int. Cl. A61K 31/4439 (2006.01); A61K 31/422 (2006.01); A61K 31/404 (2006.01) | ||
| U.S. Cl. 514—340 [514/374; 514/414] | 2 Claims |
1. A method for the treatment of diabetes, comprising the step of administering a therapeutically effective amount of a compound
according to formula (I):
 R1 is hydrogen, alkyl, halogen, formyl, hydroxyalkyl or trifluoromethyl;
R2 is hydrogen, alkyl, alkenyl, alkynyl, cyano or halogen;
R3 is hydrogen or alkyl;
R4 is hydrogen, alkyl, hydroxy or alkoxy;
R5 and R6 are independently selected from hydrogen, alkyl, arylalkyl, heteroarylalkyl, hydroxyalkyl, alkoxycarbonyl, aryl and heteroaryl;
A is aryl or heterocyclyl, wherein aryl and heterocyclyl are optionally substituted with one to three substituents independently
selected from alkyl, halogen, amino, hydroxyalkyl, aryl, aryloxy, alkoxy, arylalkyl, arylalkenyl, alkoxycarbonylamino, aminocarbonyloxy,
carboxy, alkoxycarbonyl, alkoxycarbonylalkyl, aminoalkyl, trifluoromethyl, arylalkylaminocarbonyl, alkoxycarbonylalkylaminocarbonyl,
indolylalkylaminocarbonyl, morpholinylcarbonyl, aminocarbonyl, aminocarbonylalkyl, aminocarbonylalkoxy, alkoxycarbonylalkoxy,
pyridinylalkylaminocarbonyl, alkyloxycarbonylalkylaryl, alkyloxycarbonylalkoxyaryl, carboxyalkylaryl, carboxyalkoxyaryl, aminocarbonylalkylaryl,
aminocarbonylalkoxyaryl, aminocarbonylamino, aminocarbonyloxy, aminocarbonyloxyaryl, carboxyalkyl, carboxyalkoxy, cycloalkylaminocarbonyl,
morpholinylcarbonyloxyaryl, morpholinylcarbonylaryl, arylalkoxyaryl, aminocarbonylaryl, pyrrolidinylcarbonyloxyaryl, pyrrolidinylcarbonylaryl,
piperidinylcarbonylaryl, piperidinylcarbonyloxyaryl, hydroxyalkylaryl, hydroxy(carboxy)alkylaryl, hydroxy(alkoxycarbonyl)alkylaryl,
hydroxy(aminocarbonyl)alkylaryl morpholinyalalkyl, arylalkylaminocarbonyl, alkoxycarbonylalkylaminocarbonyl, trifluoromethylaryl,
alkoxyaryl, alkylaryl, halogenaryl, alkoxycarbonylaryl, carboxyaryl, hydroxyaryl and pyridinyl;
m is zero, 1, 2 or 3;
n is zero or 1;
p is zero, 1, 2 or 3; with the proviso that the sum of m, n and p is 1, 2, 3 or 4;
and, wherein the compound is not 2-(1-benzyl-2,3-dihydro-1H-indol-5-yl)-1,1,1,3,3,3-hexafluoro-propan-2-ol;
and, wherein the bond between the carbon atoms Ca and Cb is a carbon carbon single or double bond and in case the bond between Ca and Cb is a carbon carbon double bond R3 and R4 are absent;
and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, to a patient in need thereof.
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