| US 7,501,541 B2 | ||
| Malonamides as orexin antagonists | ||
| Luca Gobbi, Oberwil BL (Switzerland); Henner Knust, Rheinfelden (Germany); Parichehr Malherbe, Muttenz (Switzerland); Matthias Nettekoven, Grenzach-Wyhlen (Germany); Emmanuel Pinard, Linsdorf (France); Olivier Roche, Folgensbourg (France); and Mark Rogers-Evans, Oberwil BL (Switzerland) | ||
| Assigned to Hoffmann-La Roche Inc., Nutley, N.J. (US) | ||
| Filed on Mar. 07, 2008, as Appl. No. 12/44,002. | ||
| Claims priority of application No. 07104232 (EP), filed on Mar. 15, 2007. | ||
| Prior Publication US 2008/0249180 A1, Oct. 09, 2008 | ||
| Int. Cl. C07C 233/05 (2006.01); A61K 31/65 (2006.01) | ||
| U.S. Cl. 564—156 [514/352; 514/354; 514/357; 514/451; 514/616; 546/309; 546/314; 546/328; 546/329; 549/424] | 23 Claims |
1. A compound of formula I
 wherein
Ar1 and Ar2 are each independently unsubstituted or substituted aryl or heteroaryl;
R1 and R2 are each independently hydrogen, lower alkyl, lower alkyl substituted by halogen, —(CH2)o—O-lower alkyl, —(CH2)o—N-(lower alkyl)2, (CH2)p-cycloalkyl, (CH2)p-heterocycloalkyl, (CH2)p-aryl, or (CH2)p-heteroaryl, wherein cycloalkyl, heterocycloalkyl, aryl, and heteroaryl are optionally substituted by R, or
R1 and R2 together with the N-atom to which they are attached form a heterocyclic ring, optionally containing further ring-heteroatoms
selected from N, O and S, which ring is optionally substituted by R;
R is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen;
R3 is hydrogen or lower alkyl;
n is 0, 1, 2, 3 or 4;
o is 1, 2 or 3; and
p is 0, 1 or 2; or a pharmaceutically suitable acid addition salt, optically pure enantiomer, racemate or diastereomeric mixture thereof.
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