Abstract
Compounds represented by structural formula I 1
including its N-oxides wherein 2
R1 is H or (C1-C6)alkyl;
R2 is H, (C1-C6)alkyl, (C3-C9)cycloalkyl or (C3-C7)cycloalkyl(C1-C6)alkyl; 3
Z is OR10, —N(R9)(R10) or —NH2;
j is 0, 1 or 2;
k is 1 or 2;
l is 0, 1 or 2;
m is 0, 1 or 2;
R4 is 1-3 substituents independently selected from the group consisting of H, —OH, halogen, haloalkyl, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, —CN, —O(C1-C6)alkyl, —O(C3-C7)cycloalkyl, —O(C1-C6)alkyl(C3-C7)cycloalkyl, —S(C1-C6)alkyl, —S(C3-C7)cycloalkyl, —S(C1-C6)alkyl(C3-C7)cycloalkyl, —NH2, —NR9R10, —NO2, —CONH2, —CONR9R10 and NR2COR10;
R5 is 1-3 substituents independently selected from the group consisting of H, halogen, —OH, haloalkyl, haloalkoxy, —CN, —NO2, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, —O(C1-C6)alkyl, —O(C3-C7)cycloalkyl, —O(C1-C6)alkyl(C3-C7)cycloalkyl, —CONH2 and —CONR9R10;
R6 is —SO2(C1-C6)alkyl, —SO2(C3-C7)cycloalkyl, —SO2(C1-C6)alkyl(CC7)cycloalkyl, —SO2(C1-C6)haloalkyl, —SO2(hydroxy(C2-C6)alkyl), —SO2(amino(C2-C6)alkyl), —SO2(alkoxy(C2-C6)alkyl), —SO2(alkylamino(C2-C6)alkyl), —SO2(dialkylamino(C2-C6)alkyl), —SO2(aryl), —SO2(heteroaryl), —SO2(aryl(C2-C6-alkyl), SO2N H2, —SO2N R9R10, —C(O)C1-C6alkyl, —C(O)C3-C7cycloalkyl, —C(O)aryl, —C(O)heteroaryl, —C(O)NR9R10, —C(O)NH2, —C(S)NR9R10, —C(S)NH2, aryl, heteroaryl, —(CH2)nC(O)NH2, —(CH2)nC(O)NR9R10, —C(═NCN)alkylthio, —C(═NCN)NR9R10, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, aryl(C1-C6)alkyl, heteroaryl(C1-C6)alkyl or —C(O)OR9, N=1 to 6;
R7=H or alkyl;
R8 is H, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, aryl, heteroaryl, —SO2(C1-C6)alkyl, —SO2(C3-C7)cycloalkyl, —SO2(C1-C6) alkyl(C3-C7)cycloalkyl, —SO2(C1-C6)haloalkyl or —SO2(aryl);
R9 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, aryl(C1-C6)alkyl, aryl or heteroaryl; and,
R10 is hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, aryl(C1-C6)alkyl, aryl or heteroaryl; or a pharmaceutically acceptable addition salt and/or hydrate thereof, or prodrug thereof,
or R9 and R10 taken together can form a 4-7 membered ring containing 1 or 2 heteroatoms; or where applicable, a geometric or optical isomer or a racemic mixture thereof, are claimed, as well as additional novel compounds; also claimed are pharmaceutical compositions and methods of using the aforesaid compounds in the treatment of obesity, eating disorders such as hyperphagia and diabetes.