IP Library Granted Patent US 8,470,841
Granted Patent B2
US 8,470,841 · App. 13/002,933 · Granted Jun 25, 2013

Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof

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Quick Facts
Patent No.
US 8,470,841
App. No.
13/002,933
Granted
Jun 25, 2013
Kind
B2
Abstract

Heterocyclic derivatives, processes for their preparation, medicaments comprising these compounds, and the use thereof. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, W, A, B, D, E, G, L, M, R, T and Y have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example for the treatment of the metabolic syndrome, insulin resistance, obesity and diabetes.

Claims (131)

1. A compound of the formula I

in which the meanings are

A, B, D, E independently of one another C(R5) or N,

where not more than two of the radicals A, B, D, E may have the meaning of N;

G, L, R, T, independently of one another ═C(R6)-, —C(R6)(R7)-, ═N—, —N(R8)- or O, where not more than two of the radicals G, L, R, T may have the meaning of ═N—, —N(R8)- or O;

with the proviso that A, B, D, E and G, L, R, T and the C atoms to which they are bonded do not simultaneously form phenyl;

M ═C—, —C(R9)- or N;

W O, S, CH(R10);

Y (C 2 -C 10 )-alkylene, where one or two CH 2 groups may be replaced by O, S, N(R10a), —CH═CH—, —CH(phenyl)- or CON(R10b);

R1 (C 1 -C 16 )-alkyl, (C 1 -C 2 )-haloalkyl, (C 6 -C 10 )-aryl, (C 3 -C 12 )-heteroaryl, (C 3 -C 12 )-heterocyclyl, (C 3 -C 12 )-cycloalkyl, (C 1 -C 6 )-alkylene-(C 6 -C 10 )-aryl, (C 1 -C 6 )-alkylene-(C 3 -C 12 )-heteroaryl, (C 1 -C 6 )-alkylene-(C 3 -C 12 )-heterocyclyl or (C 1 -C 6 )-alkylene-(C 3 -C 12 )-cycloalkyl,

where aryl, heteroaryl, heterocyclyl or cycloalkyl may be substituted one or more times by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, S—(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 3 -C 8 )-cycloalkyl, O—(C 3 -C 8 )-cycloalkyl, (C 2 -C 6 )-alkynyl, N(R11)(R12), SO 2 —CH 3 , SO 2 —NH 2 , SF 5 , oxo, COOH, COO—(C 1 -C 6 )-alkyl, CON(R13)(R14), N(R15)CO(R16), N(R17)SO 2 (R18), CO(R19), (CR20R21) x -O(R22), O—CO—N(R23)(R24), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R25)(R26);

x 0, 1, 2, 3, 4, 5, 6;

R10a, R10b, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

R2 hydrogen, —CO—N(R3a)-R4, —CO—R4, —CO—O—R4, (C 3 -C 12 )-heteroaryl,

where heteroaryl may be substituted one or more times by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, S—(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 3 -C 8 )-cycloalkyl, O—(C 3 -C 8 )-cycloalkyl, (C 2 -C 6 )-alkynyl, N(R27)(R28), SO 2 —CH 3 , SO 2 —NH 2 , SF 5 , COOH, COO—(C 1 -C 6 )-alkyl, CON(R29)(R30), N(R31)CO(R32), N(R33)SO 2 (R34), CO(R35), (CR36R37) x′ -O(R38), O—CO—N(R39)(R40), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R41)(R42),

x′ 0, 1, 2, 3, 4, 5, 6;

R3, R3a independently of one another hydrogen, (C 1 -C 6 )-alkyl, benzyl;

R4 hydrogen, (C 1 -C 16 )-alkyl, (C 1 -C 6 )-alkylen-OH, (C 6 -C 10 )-aryl, (C 3 -C 12 )-heteroaryl, —(C 3 -C 12 )-heterocyclyl, (C 3 -C 12 )-cycloalkyl, (C 1 -C 6 )-alkylene-(C 6 -C 10 )-aryl, (C 1 -C 6 )-alkylene-(C 3 -C 12 )-heteroaryl, (C 1 -C 6 )-alkylene-(C 3 -C 12 )-heterocyclyl or (C 1 -C 6 )-alkylene-(C 3 -C 12 )-cycloalkyl,

where aryl, heteroaryl, heterocyclyl or cycloalkyl may be substituted one or more times by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, S—(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 3 -C 8 )-cycloalkyl, O—(C 3 -C 8 )-cycloalkyl, (C 2 -C 6 )-alkynyl, N(R43)(R44), SO 2 —CH 3 , SO 2 —NH 2 , SF 5 , COOH, COO—(C 1 -C 6 )-alkyl, CON(R45)(R46), N(R47)CO(R48), N(R49)SO 2 (R50), CO(R51), (CR52R53) x″ -O(R54), O—CO—N(R55)(R56), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R57)(R58),

x″ 0, 1, 2, 3, 4, 5, 6;

R27, R28, R29, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41,

R42, R43, R44, R45, R46, R47, R48, R49, R50, R51, R52, R53, R54, R55, R56, R57, R58

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

R5 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, Cl, Br, I, OH, CF 3 , NO 2 , CN, (C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, N(R59)(R60), SO 2 —CH 3 , SO 2 —NH 2 , SF 5 , COOH, COO—(C 1 -C 6 )-alkyl, CON(R61)(R62), N(R63)CO(R64), N(R65)SO 2 (R66), CO(R67), (CR68R69) x″ -O(R70), O—CO—N(R71)(R72), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R73)(R74);

x′″ 0, 1, 2, 3, 4, 5, 6;

R6, R7 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, S—(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, N(R75)(R76), SO 2 —CH 3 , SO 2 —NH 2 , SF 5 , oxo, COOH, COO—(C 1 -C 6 )-alkyl, CON(R77)(R78), N(R79)CO(R80), N(R81)SO 2 (R82), CO(R83), (CR84R85) x″″ -O(R86), O—CO—N(R87)(R88), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R89)(R90);

R8 independently of one another hydrogen, (C 1 -C 6 )-alkyl, CF 3 , CN, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, SO 2 —CH 3 , SO 2 —NH 2 , COO—(C 1 -C 6 )-alkyl, CON(R77)(R78), CO(R83), (CR84R85) x″″ -O(R86);

x″″ 0, 1, 2, 3, 4, 5, 6;

R9, R10 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, OH, CF 3 , (C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, (CR91R92) y -O(R93);

y 0, 1, 2, 3, 4, 5, 6;

R59, R60, R61, R62, R63, R64, R65, R66, R67, R68, R69, R70, R71, R72, R73,

R74, R75, R76, R77, R78, R79, R80, R81, R82, R83, R84, R85, R86, R87, R88, R89, R90, R91, R92, R93

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

and the pharmaceutically acceptable salts thereof.

2. A compound of the formula I as claimed in claim 1 , in which the meanings are

A, B, D, E form with the atoms to which they are bonded a ring system selected from the group:

G, L, R, T and M form a ring system selected from the group:

with the proviso that A, B, D, E and G, L, R, T and the C atoms to which they are bonded do not simultaneously form phenyl;

W O, S, CH(R10);

Y C(R11a)(R11b)C(R11c)(R11d)C(R11e)(R11f)-, O—C(R11a)(R11b)C(R11c)(R11d)-, —S—C(R11a)(R11b)C(R11c)(R11d)-, —CH═CH—C(R11a)(R11b)-;

R1 (C 1 -C 16 )-alkyl, (C 1 -C 2 )-haloalkyl, (C 6 -C 10 )-aryl, (C 3 -C 12 )-heteroaryl, (C 3 -C 12 )-heterocyclyl, (C 3 -C 12 )-cycloalkyl, (C 1 -C 6 )-alkylene-(C 6 -C 10 )-aryl, (C 1 -C 6 )-alkylene-(C 3 -C 12 )-heteroaryl, (C 1 -C 6 )-alkylene-(C 3 -C 12 )-heterocyclyl or (C 1 -C 6 )-alkylene-(C 3 -C 12 )-cycloalkyl,

where aryl, heteroaryl, heterocyclyl or cycloalkyl may be substituted one or more times by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, S—(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 3 -C 8 )-cycloalkyl, O—(C 3 -C 8 )-cycloalkyl, (C 2 -C 6 )-alkynyl, N(R11)(R12), SO 2 —CH 3 , SO 2 —NH 2 , SF 5 , oxo, COOH, COO—(C 1 -C 6 )-alkyl, CON(R13)(R14), N(R15)CO(R16), N(R17)SO 2 (R18), CO(R19), (CR20R21) x -O(R22), O—CO—N(R23)(R24), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R25)(R26);

x 0, 1, 2, 3, 4, 5, 6;

R10a, R10b, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

R11a, R11b, R11c, R11d, R11e, R11f

independently of one another hydrogen, (C 1 -C 3 )-alkyl, phenyl;

R2 CO—N(R3a)-R4, —CO—R4, —CO—O—R4,

R3, R3a independently of one another hydrogen, (C 1 -C 6 )-alkyl, benzyl;

R4 hydrogen, (C 1 -C 12 )-alkyl, (C 1 -C 6 )-alkylene-OH, phenyl (C 3 -C 12 )-heteroaryl, (C 3 -C 12 )-heterocyclyl, (C 3 -C 12 )-cycloalkyl, (C 1 -C 6 )-alkylene-(C 6 -C 10 )-aryl, (C 1 -C 6 )-alkylene-(C 3 -C 12 )-heteroaryl, (C 1 -C 6 )-alkylene-(C 3 -C 12 )-heterocyclyl or (C 1 -C 6 )-alkylene-(C 3 -C 12 )-cycloalkyl,

where aryl, heteroaryl, heterocyclyl or cycloalkyl may be substituted one or more times by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, S—(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 3 -C 8 )-cycloalkyl, O—(C 3 -C 8 )-cycloalkyl, (C 2 -C 6 )-alkynyl, N(R43)(R44), SO 2 —CH 3 , SO 2 —NH 2 , COOH, COO—(C 1 -C 6 )-alkyl, CON(R45)(R46), N(R47)CO(R48), N(R49)SO 2 (R50), CO(R51), (CR52R53) x″ -O(R54), O—CO—N(R55)(R56), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R57)(R58);

x″ 0, 1, 2, 3;

R43, R44, R45, R46, R47, R48, R49, R50, R51, R52, R53, R54, R55, R56, R57, R58

independently of one another, hydrogen, (C 1 -C 6 )-alkyl;

R5 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, Cl, Br, I, OH, CF 3 , NO 2 , CN, (C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, N(R59)(R60), SO 2 —CH 3 , SO 2 —NH 2 , SF 5 , COOH, COO—(C 1 -C 6 )-alkyl, CON(R61)(R62), N(R63)CO(R64), N(R65)SO 2 (R66), CO(R67), (CR68R69) x″ -O(R70), O—CO—N(R71)(R72), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R73)(R74);

x′″ 0, 1, 2, 3, 4, 5, 6;

R6, R7 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, S—(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, N(R75)(R76), SO 2 —CH 3 , SO 2 —NH 2 , SF 5 , oxo, COOH, COO—(C 1 -C 6 )-alkyl, CON(R77)(R78), N(R79)CO(R80), N(R81)SO 2 (R82), CO(R83), (CR84R85) x″″ -O(R86), O—CO—N(R87)(R88), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl, O—CO—(C 1 -C 6 )-alkylene-CO—OH, O—CO—(C 1 -C 6 )-alkylene-CO—N(R89)(R90);

x″″0, 1, 2, 3, 4, 5, 6;

R10 hydrogen, (C 1 -C 6 )-alkyl, F, OH, CF 3 ;

R59, R60, R61, R62, R63, R64, R65, R66, R67, R68, R69, R70, R75, R76, R77, R78, R79, R80, R81, R82, R83, R84, R85, R86, R87, R88, R89, R90

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

and the pharmaceutically acceptable salts thereof.

3. A compound of the formula I as claimed in claim 1 or 2 , in which the meanings are

A, B, D, E form with the atoms to which they are bonded a ring system selected from the group:

G, L, R, T and M form a ring system selected from the group:

with the proviso that A, B, D, E and G, L, R, T and the C atoms to which they are bonded do not simultaneously form phenyl;

W O, CHOH, CH 2 ;

Y C(R11a)(R11b)C(R11c)(R11d)C(R11e)(R11f)-, O—C(R11a)(R11b)C(R11c)(R11d)-, —S—C(R11a)(R11b)C(R11c)(R11d)-, —CH═CH—C(R11a)(R11b)-;

R1 (C 1 -C 8 )-alkyl, CF 3 , phenyl, (C 3 -C 8 )-heteroaryl, (C 3 -C 8 )-heterocyclyl, (C 3 -C 8 )-cycloalkyl, —CH 2 -phenyl, —CH 2 —(C 3 -C 8 )-heteroaryl, —CH 2 —(C 3 -C 8 )-heterocyclyl or —CH 2 —(C 3 -C 8 )-cycloalkyl,

where aryl, heteroaryl, heterocyclyl or cycloalkyl may be substituted one or more times by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, S—(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, N(R11)(R12), SO 2 —CH 3 , SO 2 —NH 2 , oxo, COOH, COO—(C 1 -C 6 )-alkyl, CON(R13)(R14), N(R15)CO(R16), N(R17)SO 2 (R18), CO(R19), (CR20R21) x -O(R22), O—CO—N(R23)(R24), O—CO—(C 1 -C 6 )-alkylene-CO—O—(C 1 -C 6 )-alkyl;

x 0, 1, 2, 3;

R11a, R11b, R11, R11d, R11e, R11f

independently of one another hydrogen, methyl, isopropyl, phenyl;

R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

R2 —CO—R4, —CO—O—R4;

R3 hydrogen, (C 1 -C 6 )-alkyl;

R4 hydrogen, methyl, benzyl, cyclopropyl, CH 2 OH, NH 2 ;

R5 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, Cl, Br, I, OH, CF 3 , N(R59)(R60), COO—(C 1 -C 6 )-alkyl, CON(R61)(R62), N(R63)CO(R64), CO(R67), (CR68R69) x′″ -O(R70);

x′″ 0, 1, 2, 3, 4, 5, 6;

R6, R7 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, Cl, Br, I, OH, CF 3 , O—(C 1 -C 6 )-alkyl, O—(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, N(R75) (R76), COO—(C 1 -C 6 )-alkyl, CON(R77)(R78), CO(R83), (CR84R85) x″″ -O(R86);

x″″ 0, 1, 2, 3, 4, 5, 6;

R59, R60, R61, R62, R63, R64, R67, R68, R69, R70, R75, R76, R77, R78, R83, R84, R85, R86

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

and the pharmaceutically acceptable salts thereof.

4. A compound of the formula I as claimed in claim 1 , 2 or 3 , in which the meanings are

A, B, D, E form with the atoms to which they are bonded a ring system selected from the group:

G, L, R, T and M form a ring system selected from the group:

with the proviso that A, B, D, E and G, L, R, T and the C atoms to which they are bonded do not simultaneously form phenyl;

W O, CHOH, CH 2 ;

Y C(R11a)(R11b)C(R11c)(R11d)C(R11e)(R11f)-, O—C(R11a)(R11b)C(R11c)(R11d)-, —S—C(R11a)(R11b)C(R11c)(R11d)-, —CH═CH—C(R11a)(R11b)-;

R1 (C 3 -C 8 )-alkyl, CF 3 , phenyl, pyridyl, isoxazolyl, pyrrolidinyl, cyclopentyl, tetrahydrofuranyl, —CH 2 -phenyl, —CH 2 -isoxazolyl, —CH 2 -pyrrolidinyl, —CH 2-cyclobutyl, —CH 2 -cyclopropyl or —CH 2 -cyclopentyl;

where each of the rings may be substituted once or twice by F, Cl, Br, I, OH, CF 3 , O—(C 1 -C 6 )-alkyl (C 1 -C 6 )-alkyl, (C 2 -C 4 )-haloalkyl, O—(C 2 -C 4 )-haloalkyl, N(R11)(R12), CO(R19), (CR20R21) x -O(R22), O—CO—N(R23)(R24);

x 0, 1, 2, 3;

R11a, R11b, R11, R11d, R11e, R11f

independently of one another hydrogen, methyl, isopropyl, phenyl;

R11, R12, R19, R20, R21, R22, R23, R24

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

R2 —CO—R4, —CO—O—R4;

R3 hydrogen, (C 1 -C 6 )-alkyl;

R4 hydrogen, methyl, benzyl, cyclopropyl, CH 2 OH, NH 2 ;

R5 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, Cl, Br, I, OH, CF 3 , O—(C 1 -C 6 )-alkyl, N(R59)(R60), COO—(C 1 -C 6 )-alkyl, CO(R67);

R6, R7 independently of one another hydrogen, (C 1 -C 6 )-alkyl, F, Cl, Br, I, OH, CF 3 , O—(C 1 -C 6 )-alkyl, N(R75)(R76), COO—(C 1 -C 6 )-alkyl, CO(R83);

R59, R60, R67, R75, R76, R83

independently of one another hydrogen, (C 1 -C 6 )-alkyl;

and the pharmaceutically acceptable salts thereof.

5. A compound of the formula I as claimed in claims 1 to 4 , in which

Y is —CH 2 —CH 2 —CH(CH 3 )—, —O—CH 2 —CH(CH 3 )— or —CH═CH—CH(CH 3 )—.

6. A compound of the formula I as claimed in claim 1 , 2 or 3 , in which

W is O.

7. A compound of the formula Ic

in which the symbols R1, Y, R2, R3 have the meanings mentioned in claims 1 to 4 , and the pharmaceutically acceptable salts thereof.

8. A compound of the formula Id

in which the symbols R1, Y, R2, R3 have the meanings mentioned in claims 1 to 4 , and the pharmaceutically acceptable salts thereof.

9. A compound of the formula Ia

in which the symbols R1, Y, R2, R3 have the meanings mentioned in claims 1 to 4 , and the pharmaceutically acceptable salts thereof.

10. A compound of the formula Ib

in which the symbols R1, Y, R2, R3 have the meanings mentioned in claims 1 to 4 , and the pharmaceutically acceptable salts thereof.

11. A compound of the formula I as claimed in claims 1 to 10 , in which

R2 is CO—CH 3 ;

R3 is hydrogen;

and the pharmaceutically acceptable salts thereof.

12. A pharmaceutical composition comprising the compound of claim 1 .

13. The pharmaceutical composition according to claim 12 , further comprising one or more active ingredients.

14. The pharmaceutical composition according to claim 13 , wherein said one or more active ingredients comprises one or more antidiabetics.

15. The pharmaceutical composition according to claim 13 , wherein said one or more active ingredients comprises one or more lipid modulators.

16. The pharmaceutical composition according to claim 13 , wherein said one or more active ingredients comprises one or more antiobesity agents.

17. A method of treating diabetes mellitus in a patient in need thereof comprising administering to said patient a therapeutically effective amount of the pharmaceutical composition of claim 12 .

18. A method of treating obesity in a patient in need thereof comprising administering to said patient a therapeutically effective amount of the pharmaceutical composition of claim 12 .

19. A process for the manufacture of a medicament comprising one or more of the compounds as claimed in one or more of claims 1 to 11 , which comprises mixing the active ingredient with a pharmaceutically suitable carrier and converting this mixture into a form suitable for administration.

Assignments (2)
CHANGE OF NAME Recorded Jun 20, 2012
From: SANOFI-AVENTIS
To: SANOFI
Reel/Frame 028413/0927 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 14, 2011
From: ZOLLER, GERHARD; SCHMOLL, DIETER; MUELLER, MARCO; HASCHKE, GUIDO; FOCKEN, INGO
To: SANOFI-AVENTIS
Reel/Frame 026128/0857 →