US Patent:
20060211755, Sep 21, 2006
Inventors:
Patrick Eacho - Indianapolis IN, US
Ho-Shen Lin - Indianapolis IN, US
Jose Lopez - Fishers IN, US
Marian Mosior - Carmel IN, US
Michael Richett - Indianapolis IN, US
Assignee:
Eli Lilly and Company Patent Division - Indianapolis IN
International Classification:
A61K 31/416
C07D 231/56
Abstract:
The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C-Calkyl; C,—C,haloalkyl, CC,2alkenyl, C-Calkynyl, or C,—C5alkylcycloalkyl, C3-C8cycloalkyl, C, Calkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with one to three substituents independently selected from C,—Ca)kyl, C,—Chaloalkyl, ′C-Calkenyl, C2-Ca)kynyl, phenyl, benzyl, hydroxy, C,—C5 alkoxy, (C}12)000C,—Csalkyl, (CH2)NRR, and C,Calkylcycloalkyl; wherein W and Rare independently selected from hydrogen, C,Calkyl, C-Calkenyl, C-Calkynyl, and C,—C5alkylcycloalkyl; Ris hydrogen; R3, R4, R5, and R6, are independently selected from hydrogen, C,—Calkyl, CC,2haloalkyl, alkenyl, C-Calkynyl, C,—Calkylaryl, C,—Calkylcyclohexyl, C, Calkylcyclopentyl, C,—Calkylheterocyclic, (CH2)000H, (CH2)C0(C,—C,o)alkyl, (CH)COO(C,—C)alkyl, (CH2)COO(C-C)alkylaryl, C,—Calkylamino, halo, (CH)CONH, (CH)CONRaR, phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from Calkyl, C,—Chaloalkyl, C-Calkenyl, CCalkynyl, phenyl, benzyl, hydroxy, C,—C5 alkoxy, (CH2)000C,—Csalkyl, and C,—C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,—Calkyl, C,Chaloalkyl, C-Calkenyl, C-Calkynyl, C,—Calkylaryl, C,—Calkylcyclohexyl, C—Caikylcyclopentyl, C,—Calkylheterocyclic, or aryl; or a pharmaceutically acceptable sallvate thereofi together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase-mediated diseases.