Compounds and compositions for treating obesity

A compound of the formula:

• or an optical isomer, geometric isomer, diastereomer, tautomer, or a pharmaceutically acceptable salt thereof, wherein
• A is —NR2R3 or guanidinyl, the last optionally substituted with C1-6-alkyl, wherein
• R2 and R3 independently of each other are hydrogen, C1-6-alkyl,
• C1-6-alkylene-N(R11)(R12), C1-6-alkylene-CN, C1-6-alkylene-OH,
• C1-6-alkylene-C(O)—N(R11)(R12), (Z1)e-R13, or —CO—R14, wherein
• R11 and R12 independently of each other are hydrogen or C1-6-alkyl;
• Z1 is C1-6-alkylene;
• e is an integer selected from 0 or 1;
• R13 is cycloalkyl, heterocyclyl, aryl, or heteroaryl;
• each of which may be optionally substituted with a substitutent selected from the group consisting of C1-6-alkyl, amino, and —CO—O-Z4-R23, wherein
• Z4 is C1-16-alkylene;
• and
• R23 is aryl;
• and
• R14 is hydrogen, C1-6-alkyl, —N(R15)(R16), C1-6-alkylene-N(R15)(R16),
• C(R17)(R18)—N(R19)(R20), heterocyclyl, (Z2)f-R21, heteroaryl, or C1-6-alkoxy, wherein
• R15 and R16 independently of each other are hydrogen, or C1-6-alkyl;
• R17 and R18 independently of each other are hydrogen,
• C1-6-alkylene-NH2 or (Z3)9—R22), wherein
• Z3 is C1-6-alkylene;
• g is an integer selected from 0 or 1;
• and
• R22 is cycloalkyl, heterocyclyl, aryl or heteroaryl;
• R19 and R20 independently of each other are hydrogen,
• C2-6-alkylene-NH2, C1-6-alkylene-CF3 or cycloalkyl;
• and
• Z2 is C1-6-alkylene;
• f is an integer selected from 0 or 1;
• and
• R21 is cycloalkyl, heterocyclyl, aryl or heteroaryl;
• a is an integer selected from 1, 2, 3, 4, or 5;
• E is cycloalkyl, heterocyclyl, aryl or heteroaryl;
• each of which may be optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy, cyano, nitro, —NR4R5, —CO—R6, C1-6-alkyl, C1-6-alkoxy, trifluoromethyl, trifluoromethoxy, and -L1-Q1, wherein
• R4 and R5 independently of each other are hydrogen, C1-6-alkyl, —CO—R24, or aryl, wherein
• R24 is hydrogen, C1-6-alkyl or C1-6-alkoxy;
• R6 is C1-6-alkyl or C1-6-alkoxy;
• L1 is a direct bond, —CH2—, —O—, —CO—, —CH2—O—, —O—CH2— or —NR25—, wherein
• R25 is hydrogen or C1-6-alkyl;
• and
• Q1 is cycloalkyl, heterocyclyl, aryl or heteroaryl;
• each of which may be optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, —NR26R27, —CO—R28, —S(O)2—R29, C1-6-alkyl, C1-6-alkoxy, C3-7-cycloalkyl and C3-7-cycloalkoxy, wherein
• R26 and R27 independently of each other are hydrogen, C1-6-alkyl, or —CO—R30, wherein
• R30 is hydrogen, C1-6-alkyl or C1-6-alkoxy;
• R28 is C1-6-alkyl or C1-6-alkoxy;
• and
• R29 is C1-6-alkyl, —NH—C1-6-alkyl, or —N(C1-6-alkyl)2;
• or
• Q1 is L3-R31, wherein
• L3 is —CH2—, —O—, —CO—, —CH2—O—, —O—CH2—, —CH2—O—C(O)—, or —C(O)—O—CH2—;
• and
• R31 is aryl or heteroaryl;
• b is an integer selected from 0, 1, or 2;
• G1 is C1-6-alkyl, C1-6-alkoxy, cycloalkyl, C3-7-cycloalkoxy, aryl or heteroaryl;
• each of which may be optionally substituted with halogen, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, —NR7R8, C1-6-alkyl, C1-6-alkoxy, C3-7-cycloalkyl, C3-7-cycloalkoxy, wherein
• R7 and R8 independently of each other are hydrogen, C1-6-alkyl, aryl, heteroaryl,
• —CO—R32 or —SO2—R33, wherein
• R32 is hydrogen, C1-6-alkyl or C1-6-alkoxy;
• and
• R33 is C1-6-alkyl, —NH—C1-6-alkyl, —N(C1-6-alkyl)2;
• G2 is cycloalkyl, heterocyclyl, aryl, or heteroaryl;
• each of which may be optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy, cyano, nitro, difluoromethyl, trifluoromethyl, difluoromethoxy, trifluoromethoxy, —NR9R10, C1-6-alkyl, C1-6-alkoxy, C3-7-cycloalkyl, C3-7-cycloalkoxy or -L2-Q2, wherein
• R9 and R10 are independently hydrogen, C1-6-alkyl, aryl, heteroaryl, —CO—R34 or —SO2—R3, wherein
• R34 is hydrogen, C1-6-alkyl or C1-6-alkoxy;
• and
• R35 is C1-6-alkyl, —NH—C1-6-alkyl, or —N(C1-6-alkyl)2;
• L2 is a direct bond, —CH2—, —O—, —CO—, —CH2—O—, —O—CH2— or —NR36—, wherein
• R36 is hydrogen or C1-6-alkyl;
• and
• Q2 is cycloalkyl, heterocyclyl, aryl or heteroaryl;
• each of which may be optionally substituted with halogen, hydroxy, cyano, nitro, trifluoromethyl, —NR37R38, —CO—R39, —O—R40, C1-6-alkyl, C1-6-hydroxyalkyl, C3-7-cycloalkyl or C3-7-cycloalkoxy, wherein
• R37 and R38 independently of each other are hydrogen, C1-6-alkyl or —CO—R41, wherein
• R41 is hydrogen, C1-6-alkyl or C1-6-alkoxy;
• R39 is hydrogen, C1-6-alkyl or C1-6-alkoxy;
• and
• R40 is C1-6-alkyl or trifluoromethyl;
• c is an integer selected from 0, 1, or 2;
• d is an integer selected from 0, or 1;
• and
• R1 is hydrogen, alkyl, alkenyl, or alkynyl.