Aryl-substituted heterocycles, process for their preparation and their use as medicaments
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Accused Products
Abstract
The invention relates to substituted aryl-substituted heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to process for their preparation and to their use as medicaments.
Compounds of the Formula I
in which the radicals have the stated meanings, the N-oxides thereof, and the physiologically tolerated salts thereof, and process for the preparation thereof are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.
106 Citations
12 Claims
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1. A compound of the formula I,
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
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2. A compound of the formula I as claimed in claim 1,
in which the meanings are R1, R2 independently of one another H, (C1-C8)-alkyl, — - (CR13R14)o—
R12, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C3-C8)-alkenyl, (C3-C8)-alkynyl, CO—
(C1-C8)-alkyl, —
CO—
(CH2)o—
R12, CO(C(R15)(R16))qN(R17)(R18), CO(C(R19)(R20))sO(R21);
or R1 and R2 form together with the nitrogen atom to which they are bonded a 4 to 10-membered mono-, bi- or spirocyclic ring which, apart from the nitrogen atom, may include 0 to 4 additional heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the heterocyclic ring system may additionally be substituted by F, Cl, Br, CF3, NO2, CN, (C1-C6)-alkyl, O—
(C1-C8)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, (C0-C8)-alkylene-aryl, oxo, CO(R22), CON(R23)(R24), hydroxy, COO(R25), N(R26)CO(C1-C6)-alkyl or N(R27)(R28);R12 OH, O—
(C1-C6)-alkyl, CN, COO(R29), CON(R30)(R31), N(R32)(R33), 3-12 membered mono-, bi- or spirocyclic ring which may comprise one or more heteroatoms from the group of N, O and S, and the 3-12 membered ring may comprise further substituents such as F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, oxo, O—
(C1-C6)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, S—
(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C8)-cycloalkyl, (C2-C6)-alkynyl, O—
(C0-C8)-alkylene-aryl, (C0-C8)-alkylene-aryl, N(R34)(R35), CO(C1-C6)-alkyl and COO(R36); andR6, R7, R8, R9 independently of one another H, (C1-C8)-alkyl; where the remaining variables for formula I are as defined in claim 1.
- (CR13R14)o—
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3. A compound of the formula I as claimed in claim 1,
in which the meanings are R1, R2 independently of one another H, (C1-C8)-alkyl, — - (CR13R14)o—
R12, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C3-C8)-alkenyl, CO—
(C1-C8)-alkyl, —
CO—
(CH2)o—
R12, CO(C(R15)(R16))qN(R17)(R18), CO(C(R19)(R20))sO(R21);
or R1 and R2 form together with the nitrogen atom to which they are bonded a 4 to 10-membered mono-, bi- or spirocyclic ring which, apart from the nitrogen atom, may include 0 to 2 additional heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the heterocyclic ring system may additionally be substituted by F, Cl, CF3, (C1-C6)-alkyl, O—
(C1-C4)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, (C0-C2)-alkylene-aryl, oxo, CO(R22), CON(R23)(R24), hydroxy, COO(R25), N(R26)CO(C1-C6)-alkyl, N(R27)(R28) or SO2CH3;o 0, 1, 2, 3, 4, 5, 6; q 1, 2, 3; s 0, 1, 2, 3, 4; R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28 independently of one another H, (C1-C6)-alkyl;
orR17 and R18, R23 and R24, R27 and R28 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur;R12 OH, O—
(C1-C6)-alkyl, CN, COO(R29), CON(R30)(R31), 3-12 membered mono-, bi- or spirocyclic ring which may comprise one or more heteroatoms from the group of N, O and S, and the 3-12 membered ring may comprise further substituents such as F, Cl, Br, OH, CF3, CN, oxo, O—
(C1-C6)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C1-C6)-alkyl, O—
(C0-C8)-alkylene-aryl, (C0-C8)-alkylene-aryl, N(R34)(R35), CO(C1-C6)-alkyl, COO(R36), S(O)u(R37);u 0, 1, 2; R34, R35 independently of one another H, (C1-C8)-alkyl;
orR34 and R35 optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur, and optionally be substituted by 1-2 oxo groups;R36, R37 H, (C1-C8)-alkyl; R13, R14 independently of one another H, (C1-C8)-alkyl, hydroxy-(C1-C4)-alkyl, OH, (C1-C4)-alkoxy-(C1-C4)-alkyl; R29, R30, R31 independently of one another H, (C1-C8)-alkyl; R3 H, (C1-C6)-alkyl; R4, R5 independently of one another H, (C1-C6)-alkyl, OH, O—
(C1-C6)-alkyl, O—
CO(C1-C6)-alkyl, S—
(C1-C6)-alkyl;R6, R7, R8, R9 H;
orR6 and R7, R8 and R9 independently of one another optionally oxo; n 1; m 1; A, B, D, G C(R38);
orthe groups A and B or D and G are in each case C(R38) and together form an ortho-phenylene unit so that the overall result is a 1,4-bisubstituted naphthalene system; R38 H, F, Cl, Br, CF3, CN, O—
(C1-C6)-alkyl, O—
(C1-C4)-alkoxy-(C1-C4)-alkyl, S—
(C1-C6)-alkyl, (C1-C6)-alkyl, (C0-C8)-alkylene-aryl, O—
(C0-C8)-alkylene-aryl, N(R39)(R40), SO2—
CH3, CON(R41)(R42), N(R43)CO(R44), CO(R47), —
(CR48R49)x—
O(R50);R39, R40, R41, R42, R43 independently of one another H, (C1-C8)-alkyl;
orR39 and R40, R41 and R42 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur;R44, R47 independently of one another H, (C1-C8)-alkyl, aryl; R48, R49 H; R50 H, (C1-C6)-alkyl; x 1, 2; Het is
- (CR13R14)o—
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4. A compound of the formula I as claimed in claim 1 or 3,
in which the meanings are: -
R1, R2 independently of one another H, (C1-C8)-alkyl, —
(CR13R14)o—
R12, (C1-C4)-alkoxy-(C1-C4)-alkyl, CO—
(C1-C8)-alkyl, —
CO—
(CH2)o—
R12, CO(C(R15)(R16))qN(R17)(R18), CO(C(R19)(R20))oO(R21);
or R1 and R2 form together with the nitrogen atom to which they are bonded a 4 to 10-membered mono- or bicyclic ring which, apart from the nitrogen atom, may include 0 to 2 additional heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the heterocyclic ring system may additionally be substituted by F, Cl, CF3, (C1-C6)-alkyl, O—
(C1-C4)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C0-C2)-alkylene-aryl, oxo, CO(R22), hydroxy, N(R27)(R28) or SO2CH3;o 0, 1, 2, 3, 4; q 1 or 2; s 0, 1, 2, 3; R15, R16, R17, R18, R19, R20, R21, R22, R27, R28 independently of one another H, (C1-C6)-alkyl;
orR17 and R18, R27 and R28 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring selected from pyrrolidine, piperidine, N-methylpiperazine and morpholine; R12 OH, O—
(C1-C6)-alkyl, CN, 3-10 membered mono- or bicyclic ring which may comprise 1-3 heteroatoms from the group of N, O and S, and the 3-10 membered ring may comprise further substituents such as F, Cl, Br, OH, CF3, CN, oxo, O—
(C1-C6)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C1-C6)-alkyl, (C0-C2)-alkylene-aryl, N(R34)(R35), CO(C1-C6)-alkyl;u 0 or 2; R34, R35 independently of one another H, (C1-C8)-alkyl;
orR34 and R35 optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur, and optionally be substituted by 1-2 oxo groups;R36, R37 H, (C1-C8)-alkyl; R13, R14 independently of one another H, (C1-C8)-alkyl, hydroxy-(C1-C4)-alkyl, OH, (C1-C4)-alkoxy-(C1-C4)-alkyl; R3 H; R4, R5 independently of one another H, (C1-C6)-alkyl, OH, O—
(C1-C6)-alkyl, O—
CO(C1-C6)-alkyl;R6, R7, R8, R9 H; n 1 m 1; A, B, D, G C(R38); R38 H, F, Cl, Br, CF3, CN, O—
(C1-C6)-alkyl, (C1-C6)-alkyl, SO2—
CH3, CON(R41)(R42), N(R43)CO(R44), CO(R47), —
(CR48R49)x—
O(R50);R41, R42, R43 independently of one another H, (C1-C8)-alkyl;
orR39 and R40, R41 and R42 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur;R47 H, (C1-C8)-alkyl; R48, R49 H; R50 H, (C1-C6)-alkyl; x 1; Het 1,3,4-oxadiazolyl; X a bond, CH2—
CH2, CH2Y, YCH2, (R75)YCH2, CH2—
NCO(R75), CH2CON(R75);
C(R76)(R77), C(R78)(R79)O, N(R75), C═
C, C≡
C;Y O, S, N(R53); R53 H, (C1-C8)-alkyl; R75, R76, R77, R78, R79 independently of one another H, (C1-C8)-alkyl; E 5-7 membered bivalent carbo- or heterocyclic ring structure having 0-3 heteroatoms from the group of N, O and S, which may optionally have substituents from the group of H, F, Cl, Br, OH, CF3, NO2, CN, OCF3, O—
(C1-C6)-alkyl, S—
(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C6)-alkenyl, O—
(C0-C8)-alkylene-aryl, S-aryl, N(R54)(R55), SO2—
CH3, N(R58)CO(R59), CO(R62) and be mono- or bicyclic;R54, R55, R58 independently of one another H, (C1-C8)-alkyl; R59, R62 independently of one another H, (C1-C8)-alkyl; K O, a bond, CH2O, OCH2, N(R80), N(R81)CO, CON(R82), (C(R83)(R84))v, CO, C≡
C, SCH2;v 1, 2, 3; R80, R81, R83, R84 independently of one another H, (C1-C8)-alkyl; R11 (C1-C8)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, a 3 to 10-membered mono-, bi- or spirocyclic ring which may include 0 to 3 heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the ring system may additionally be substituted by F, Cl, Br, CF3, CN, (C1-C6)-alkyl, O—
(C1-C8)-alkyl, (C0-C2)-alkylene-aryl, oxo, CO(R66), CON(R67)(R68), hydroxy, N(R70)CO(C1-C6)-alkyl, N(R71)(R72) or SO2CH3;R66, R67, R68, R70, R71, R72 independently of one another H, (C1-C8)-alkyl;
orR67 and R68, R71 and R72 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur;
orthe N-oxides thereof and the physiologically tolerated salts thereof.
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5. A compound of the formula I as claimed in claim 1, 2 or 3,
in which radicals R1, R2, R11, R38 and the groups X, E and K have the following meanings: -
R1, R2 independently of one another H, (C1-C8)-alkyl, —
(CR13R14)o—
R12, (C1-C4)-alkoxy-(C1-C4)-alkyl, or R1 and R2 form together with the nitrogen atom to which they are bonded a 4 to 10-membered mono-, bi- or spirocyclic ring which, apart from the nitrogen atom, may include 0 to 2 additional heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the heterocyclic ring system may additionally be substituted by (C1-C6)-alkyl, O—
(C1-C4)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, (C0-C2)-alkylene-aryl, oxo, CO(R22), CON(R23)(R24), hydroxy, N(R27)(R28) or SO2CH3;o 0, 1, 2, 3, 4; R22, R23, R24, R27, R28 independently of one another H, (C1-C6)-alkyl;
orR23 and R24, R27 and R28 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur;R12 OH, O—
(C1-C6)-alkyl, CN 3-12 membered mono-, bi- or spirocyclic ring which may comprise 1 to 3 heteroatoms from the group of N, O and S, and the 3-12 membered ring may comprise further substituents such as F, OH, CF3, CN, oxo, (C1-C6)-alkyl, (C0-C2)-alkylene-aryl, N(R34)(R35), COO(R36), CO(C1-C6)-alkyl;R34, R35 independently of one another H, (C1-C4)-alkyl; R36 H, (C1-C6)-alkyl, (C0-C2)-alkylene-aryl; R13, R14 independently of one another H, (C1-C8)-alkyl, hydroxy-(C1-C4)-alkyl, OH, (C1-C4)-alkoxy-(C1-C4)-alkyl; R38 H, F, Cl, Br, CF3, CN, (C1-C6)-alkyl; X a bond, CH2CH2, C(R76)(R77), N(R75), C═
C, (R75)YCH2, CH2—
NCO(R75), CH2CON(R75);Y O, S, N(R53), CO R75, R76, R77 independently of one another H, (C1-C8)-alkyl; R53 H, (C1-C8)-alkyl; E 5-7 membered bivalent carbo- or heterocyclic ring structure having 0-3 heteroatoms from the group of N, O and S, which may optionally have substituents from the group of H, F, Cl, Br, CF3, OH, CN, OCF3, O—
(C1-C6)-alkyl, (C1-C6)-alkyl, SO2—
CH3, CO(R65);R65 H, (C1-C8)-alkyl; K O, a bond, CH2O, CH2, OCH2, S, SO2, N(R80), N(R81)CO, CON(R82), (C(R83)(R84))v, CO, C≡
C, SCH2, SO2CH2;v 1, 2, 3; R80, R81, R82, R83, R84 independently of one another H, (C1-C8)-alkyl; R11 (C1-C8)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, a 3 to 10-membered mono-, bi- or spirocyclic ring which may include 0 to 4 heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the ring system may additionally be substituted by F, Cl, Br, CF3, CN, (C1-C6)-alkyl, O—
(C1-C8)-alkyl, oxo, CO(R66), hydroxy, N(R70)CO(C1-C6)-alkyl, or SO2CH3;R66, R70 independently of one another H, (C1-C8)-alkyl; the N-oxides thereof and the physiologically tolerated salts thereof.
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6. A medicament comprising one or more of the compounds as claimed in claim 1.
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7. A medicament comprising one or more of the compounds as claimed in claim 1 and one or more anorectic active ingredients.
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8. A process for producing a medicament comprising one or more of the compounds of the formula I as claimed in claim 1, which comprises mixing the active ingredient with a pharmaceutically suitable carrier, and converting this mixture into a form suitable for administration.
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9. A compound of the formula I as claimed in claim 4, in which the meanings are:
-
R1, R2independently of one another H, (C1-C8)-alkyl, —
(CR13R14)0—
R12, (C1-C4)-alkyl, CO—
(C1-C8)-alkyl, —
CO—
(CH2)0—
R12, CO(C(R15)(R16))qN(R17)(R18), or R1 and R2 form together with the nitrogen atom to which they are bonded a 4 to 10-membered mono- or bicyclic ring which, apart from the nitrogen atom, may include 0 to 2 additional heteroatoms selected from the group of oxygen and nitrogen, where the heterocyclic ring system may additionally he substituted by F, (C1-C6)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, oxo, CO(R22), hydroxy, N(R27)(R28);o 0, 1, 2, 3; q 1 or 2; s 0, 1, 2; R15, R16, R17, R18, R19, R20, R21, R22, R27, R28 independently of one another H, (C1-C6)-alkyl;
orR17 and R18, R27and R28 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring selected from pyrrolidine, piperidine, N-methylpiperazine and morpholine; R12 OH, O—
(C1-C6)-alkyl, 3-10 membered mono- or bicyclic ring which may comprise 1-2 hetero atoms from the group of N, O and S, and the 3-10 membered ring may comprise further substituents such as F, OH, oxo, (C1-C6)-alkyl, CO(C1-C6)-alkyl;u 2; R34, R35 independently of one another H, (C1-C5)-alkyl;
orR34 and R35 optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur, and optionally be substituted by 1-2 oxo groups;R36, R37 H, (C1-C8)-alkyl; R13, R14 independently of one another H, (C1-C8)-alkyl, hydroxy-(C1-C4)-alkyl, OH, (C1-C4)-alkoxy-(C1-C4)-alkyl; R3 H; R4, R5 independently of one another H, OH, O—
(C1-C6)-alkyl;R6, R7, R8, R9 H; n 1 m 1; A,B,D,G C(R38); R38 H, F, Cl, CF3, CN, (C1-C6)-alkyl, —
(CR48R49)x—
O(R50);R41, R42, R43 independently of one another 1-I, (C1-C8)-alkyl;
orR39 and R40, R41 and R42 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur;R47 H, (C1-C8)-alkyl; R48, R49 H;
R50 H, (C1-C6)-alkyl;x 1; Het 1,3,4-oxadiazolyl; X a bond, CH2—
CH2, C(R76)(R77), N(R75), CH2Y, CH2Y(R75), CH2—
NCO(R75), CH2—
CON(R75);
C═
C;Y O, S, N(R53); R53 H, (C1-C8)-alkyl; R75, R76, R77, R78, R79 independently of one another H, (C1-C8)-alkyl; E 5-7 membered bivalent carbo- or heterocyclic ring structure having 0-2 heteroatoms from the group of N, O and S, which may optionally have substituents from the group of H, F, CI, Br, OH, CF3, NO2, OCF3, O—
(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C6)-alkenyl, N(R54)(R55), SO2—
CH3, CO(R62), and which is monocyclic;R54, R55, R58 independently of one another H, (C1-C8)-alkyl; R59, R62 independently of one another H, (C1-C8)-alkyl; K O, a bond, CH2O1 OCH2, CON(R82), (C(R83)(R84))v, CO, C≡
C;v 1, 2; R80, R81, R83, R84 independently of one another H, (C1-C8)-alkyl; R11 preferably (C1C8)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, a 3 to 10-membered mono- or bicyclic ring which may include 0 to 2 heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the ring system may additionally be substituted by F, Cl, Br, CF3, CN, (C1-C6)-alkyl, O—
(C1-C8)-alkyl, oxo, CO(R66), CON(R67)(R68), N(R70)CO(C1-C6)-alkyl, or SO2CH3;R66, R67, R68, R70, R71, R72 independently of one another H, (C1 -C8)-alkyl;
orR67 and R68, R71 and R72 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur;
orthe N-oxides thereof and the physiologically tolerated salts thereof.
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10. A compound of the formula I as claimed in claim 5, in which radicals R1, R2, R11, R38 and the groups X, E and K have the following meanings:
-
R1, R2 independently of one another H, (C1-C8)-alkyl, or R1 and R2 form together with the nitrogen atom to which they are bonded a 5 to 6-menibered monocyclic ring which, apart from the nitrogen atom, may include 0 to 1 additional heteroatoms selected from the group of oxygen, nitrogen and sulfur, where the heterocyclic ring system may additionally be substituted by (C1-C6)-alkyl; o 0, 1, 2, 3, 4; R22, R23, R24, R27, R28 independently of one another H, (C1-C6)-alkyl;
orR23 and R24, R27 and R28 independently of one another optionally together with the nitrogen atom to which they are bonded a 5-6 membered ring which, apart from the nitrogen atom, may also include 0-1 further heteroatoms from the group of NH, N—
(C1-C6)-alkyl, oxygen and sulfur;R12 OH, O—
(C1-C6)-alkyl, CN 3-12 membered mono-, bi- or spirocyclic ring which may comprise 1 to 3 heteroatoms from the group of N, O and S, and the 3-12 membered ring may comprise further substituents such as F, OH, CF3, CN, oxo, (C1-C6)-alkyl, (C0-C2)-alkylene-aryl, N(R34)(R35), COO(R36), CO(C1-C6)-alkyl;R34, R35 independently of one another H, (C1-C4)-alkyl; R36 H, (C1-C6)-alkyl, (C0-C2)-alkylene-aryl; R13, R14 independently of one another H, (C1-C8)-alkyl, hydroxy-(C1-C4)-alkyl, OH, (C1 -C4-alkoxy-(C1-C4)-alkyl; R38 H, F, Cl, Br, CF3, CN, (C1-C6)-alkyl; X a bond, CH2CH2, C(R76)(R77), N(R75), C═
C, (R75)YCH2, CH2—
NCO(R75), CH2CON(R75);Y O, S, N(R53), CO R75, R76, R77 independently of one another H, (C1-C8)-alkyl; R53 H, (C1-C8)-alkyl; E 5-7 membered bivalent carbo- or heterocyclic ring structure having 0-3 heteroatoms from the group of N, O and S, which may optionally have substituents from the group of H, F, Cl, Br, CF3, OH, CN, OCF3, O—
(C1-C6)-alkyl, (C1-C6)-alkyl, SO2—
CH3, CO(R65);R65 H, (C1-C8)-alkyl; K O, a bond, CH2O, CH2, OCH2, N(R80), C≡
C;v 1, 2, 3; R80, R81, R82, R83, R84 independently of one another H, (C1-C8)-alkyl; R11 (C1-C8)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, a 3 to 10-membered mono-, bi- or spirocyclic ring which may include 0 to 4 heteroatoins selected from the group of oxygen, nitrogen and sulfur, where the ring system may additionally be substituted by F, Cl, Br, CF3, CN, (C1-C6)-alkyl, O—
(C1-C6)-alkyl, oxo, CO(R66), hydroxy, N(R70)CO(C1-C6)-alkyl, or SO2CH3;R66, R70 independently of one another H, (C1-C8)-alkyl; the N-oxides thereof and the physiologically tolerated salts thereof.
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11. A method of treating obesity comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula I as claimed in claim 1 or a pharmaceutically acceptable salt thereof.
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12. A method of treating type II diabetes comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula I as claimed in claim 1 or a pharmaceutically acceptable salt thereof.
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2. A compound of the formula I as claimed in claim 1,
Specification
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Current AssigneeSanofi-Aventis Deutschland GmbH (Sanofi )
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Original AssigneeSanofi-Aventis Deutschland GmbH (Sanofi )
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InventorsSchwink, Lothar, Hessler, Gerhard, Stengelin, Siegfried, Gossel, Matthias, Boehme, Thomas, Stahl, Petra
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Primary Examiner(s)Anderson; Rebecca
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Assistant Examiner(s)Barker; Michael P.
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Application NumberUS11/042,563Publication NumberTime in Patent Office1,085 DaysField of Search514/364, 548/143, 548/145US Class Current514/364CPC Class CodesA61K 2300/00 Mixtures or combinations of...A61K 31/4439 containing a five-membered ...A61K 31/497 containing further heterocy...A61K 31/501 not condensed and containin...A61K 45/06 Mixtures of active ingredie...A61P 3/00 Drugs for disorders of the ...