Aryl-substituted heterocycles, process for their preparation and their use as medicaments
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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
94 Citations
17 Claims
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1. A compound of the formula 1,
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)
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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); and
R6, R7, R8, R9 independently of one another H, (C1-C8)-alkyl;
where the further radicals and groups in the compound of the formula I have the meanings stated 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 or 2;
A, B, D, G independently of one another N, 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 five-membered aromatic heterocycle, preferably in which A′
is O, S, NR73,X′
, Y′ and
Z′
are independently of one another CR74 or N, andR73, R74 are independently of one another H, (C1-C8)-alkyl;
X a bond, a group of the formula —
(CR51R52)y—
, in which one or more —
(CR51R52)- groups may be replaced by Y to result in a chemically reasonable radical, C═
C, C≡
C;
R51, R52 independently of one another H, (C1-C4)-alkyl, where R51 and R52 in the y groups may in each case have the same or different meanings;
Y O, S, N(R53), CO;
R53 H, (C1-C8)-alkyl;
E 3-8 membered bivalent carbo- or heterocyclic ring structure having 0-4 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, O-(C1-C4)-alkoxy-(C1-C4)-alkyl, S-(C1-C6)-alkyl, (C1-C6)-alkyl, (C2-C6)-alkenyl, O-(C3-C8)-cycloalkyl, (C2-C6)-alkynyl, (C0-C8)-alkylene-aryl, O-(C0-C8)-alkylene-aryl, S-aryl, N(R54)(R55), SO2—
CH3, N(R58)CO(R59), N(R60)SO2(R61), CO(R62) and be mono- or bicyclic;
R54, R55, R58, R60 independently of one another H, (C1-C8)-alkyl;
R59, R61, R62 independently of one another H, (C1-C8)-alkyl, aryl;
K O, a bond, CH2O, OCH2, S, SO, SO2, N(R80), N(R81)CO, CON(R82), (C(R83)(R84))v, CO, C═
C, C≡
C, SCH2, SO2CH2;
v 1, 2, 3, 4;
R80, R81, R82, R83, R84 independently of one another H, (C1-C8)-alkyl;
R11 H, (C1-C8)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C3-C8)-alkenyl, (C3-C8)-alkynyl, 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, (C1-C4)-alkoxy-(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl, (C0-C8)-alkylene-aryl, oxo, CO(R66), CON(R67)(R68), hydroxy, COO(R69), N(R70)CO(C1-C6)-alkyl, N(R71)(R72) or SO2CH3;
R66, R67, R68, R69, 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.
- (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;
preferably 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)(R11))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 be substituted by F, (C1-C6)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, oxo, CO(R22), hydroxy, N(R27)(R28);
o 0, 1, 2, 3, 4;
preferably 0, 1, 2, 3;
q 1 or 2;
s 0, 1, 2, 3;
preferably 0, 1, 2;
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;
preferably OH, O-(C1-C6)-alkyl, 3-10 membered mono- or bicyclic ring which may comprise 1-2 heteroatoms 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 0 or 2;
preferably 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;
preferably independently of one another H, OH, O-(C1-C6)-alkyl, very particularly preferably H;
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);
particularly preferably H, F, Cl, CF3, CN, (C1-C6)-alkyl, —
(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 heteroaromatic group selected from the group consisting of oxadiazoles, thiadiazoles, thiazoles, oxazoles, triazoles, thiophenes, furans and pyrroles;
Het is very particularly preferably selected from oxadiazoles, thiadiazoles, thiazoles and oxazoles;
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;
preferably a bond, CH2—
CH2, C(R76)(R77), N(R75), CH2Y, CH2Y(R75), CH2—
NCO(R75), CH2—
CON(R75);
C═
C;
particularly preferably a bond, CH2—
CH2, C(R76)(R77), C═
C, (R75)YCH2, CH2—
NCO(R75);
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;
preferably 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, Cl, 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 particularly preferably monocyclic;
e.g. E is benzene, pyridine, pyrimidine, piperidine, pyrrolidine, cyclopentane, cyclohexane, piperazine, homopiperazine, thiazole, thiophene, furan, pyrrole, pyrazole, 1,2,3,6-tetrahydropyridine, 4,5-dihydroisoxazole, oxazole;
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;
preferably 0, a bond, CH2O, OCH2, CON(R82), (C(R83)(R84))v, CO, C≡
C;
v 1, 2, 3;
preferably 1,2;
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;
preferably (C1-C8)-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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5. A compound of the formula I as claimed in any of claims 1 or 2 to 4,
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;
preferably independently of one another H, (C1-C8)-alkyl, —
(CR13R14)n—
, 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 or N(R27)(R28);
very particularly preferably 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-membered 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;
especially preferably independently of one another H, (C1-C8)-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, S, SO2, N(R80), N(R81)CO, CON(R82), (C(R83)(R84))v, CO, C≡
C, SCH2, SO2CH2;
preferably 0, 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 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.
-
-
6. A compound of the formula I as claimed in any of claims 1 to 5,
in which A, B, D, G are independently of one another N or C(R38), and the total number of nitrogen atoms in this ring is 0-2, preferably 0 or 1, and for the case where the total number of nitrogen atoms is 1, particularly preferably A or B are N and very particularly preferably B is N. -
7. A compound of the formula I as claimed in any of claims 1 to 6,
in which n is 1 and m is 1 or 2. -
8. A medicament comprising one or more of the compounds as claimed in any of claims 1 to 7.
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9. A medicament comprising one or more of the compounds as claimed in any of claims 1 to 7 and one or more anorectic active ingredients.
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10. A compound of the formula I as claimed in any of claims 1 to 7 for use as medicament for the prophylaxis or treatment of obesity.
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11. A compound of the formula I as claimed in any of claims 1 to 7 for use as medicament for the prophylaxis or treatment of type 11 diabetes.
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12. A compound of the formula I as claimed in any of claims 1 to 7 in combination with at least one further anorectic active ingredient for use as medicament for the prophylaxis or treatment of obesity.
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13. A compound of the formula I as claimed in any of claims 1 to 7 in combination with at least one further anorectic active ingredient for use as medicament for the prophylaxis or treatment of type 11 diabetes.
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14. A process for producing a medicament comprising one or more of the compounds of the formula I as claimed in any of claims 1 to 7, 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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15. The use of the compounds of the formula I as claimed in any of claims 1 to 7 for producing a medicament for weight reduction in mammals.
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16. The use of the compounds of the formula I as claimed in any of claims 1 to 7 for producing a medicament for the prophylaxis or treatment of obesity.
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17. The use of the compounds of the formula I as claimed in any of claims 1 to 7 for producing a medicament for the prophylaxis or treatment of type II diabetes.
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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 AssigneeAventis Pharma Deutschland GmbH (Sanofi )
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InventorsSchwink, Lothar, Hessler, Gerhard, Stengelin, Siegfried, Gossel, Matthias, Boehme, Thomas, Stahl, Petra
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Granted Patent
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Time in Patent OfficeDays
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Field of Search
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US Class Current514/242
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CPC 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 ...