Claims
- 1. A compound of the formula I,
- 2. A compound of formula I as claimed in claim 1 wherein
R7, R8, R9 and R10 are, independently of each other, H, F, Cl, Br, OH, NO2, CN, (C1-C6)-alkyl or O—(C1-C6)-alkyl, where alkyl can be substituted, once or more than once, by F; R1 and R2 are H; R3 is H, F, Cl, Br, NO2, CN, O—R11, O-phenyl, S—R11, COOR11, N(R12)(R13), (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C3-C7)-cycloalkyl or (C3-C7)-cycloalkyl-(C1-C4)-alkylene, where alkyl, cycloalkyl and alkynyl can be substituted, once or more than once, by F, Cl, Br, OR11 or COOR11; R4 is H, F, Cl, NO2, O—R11, N(R12)(R13) or (C1-C6)-alkyl, where alkyl can be substituted, once or more than once, by F; R5 is H, F, Cl, NO2, O—R11, N(R12)(R13) or (C1-C6)-alkyl, where alkyl can be substituted, once or more than once, by F; R6 is H, F, Cl, NO2, O—R11, N(R12)(R13) or (C1-C6)-alkyl, where alkyl can be substituted, once or more than once, by F; R11 is H, (C1-C8)-alkyl, (C1-C8)-alkylene-O—(C1-C8)-alkyl or (C1-C8)-alkyl-OH, where alkyl can be substituted, once or more than once, by F; R12 and R13 are, independently of each other, H or (C1-C8)-alkyl; or R12 and R13 form, together with the nitrogen atom to which they are bonded, a 3-7-membered, saturated heterocyclic ring which can contain up to 3 heteroatoms selected from the group consisting of N, O and S and where the heterocyclic ring can be substituted, up to four times, by F, Cl, Br, OH, Oxo, (C1-C4)-alkyl or N(R14)(R15); R14 and R15 are, independently of each other, H, (C1-C8)-alkyl, (C2-C8)-alkenyl, (C2-C8)-alkynyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C4)-alkylene, COO—(C1-C4)-alkyl, COO—(C2-C4)-alkenyl, phenyl or SO2-phenyl, where the phenyl ring can be substituted, up to two times, by F, Cl, CN, OH, (C1-C6)-alkyl, O—(C1-C6)-alkyl, CF3, OCF3, COOH, COO(C1-C6)-alkyl or CONH2; and physiologically tolerated salts thereof.
- 3. A compound of formula I as claimed in claim 1, wherein
R7, R8, R9 and R10 are, independently of each other, H, F, Cl, Br, CH3 or CF3; R1, R2, R5 are H; R3 is H, F, Cl, NO2, CF3, O—R11, N(R12)(R13) or (C1-C6)-alkyl, where alkyl can be substituted once or more than once by F; R4 is H, F, Cl, NO2, CF3, O—R11, N(R12)(R13) or (C1-C6)-alkyl, where alkyl can be substituted once or more than once by F; R6 is H, F, Cl, NO2, CF3, O—R11, N(R12)(R13) or (C1-C6)-alkyl, where alkyl can be substituted once or more than once by F; R11 is H or (C1-C8)-alkyl, where alkyl can be substituted once or more than once by F, R12 and R13 are H or (C1-C8)-alkyl; or the two radicals R12 and R13 form, together with the nitrogen atom to which they are bonded, a 5-6-membered, saturated heterocyclic ring which can contain a further oxygen atom; and physiologically tolerated salts thereof.
- 4. A compound of the formula I as claimed in claim 1, wherein
R7, R8, R9 and R10 are, independently of each other, H, F, Cl, Br, CH3 or CF3; R1, R2, R4, R5 and R6 are H; R3 is H, F, Cl, NO2, O—R11, N(R12)(R13) or (C1-C6)-alkyl, where alkyl can be substituted once or more than once by F; R11 is H or (C1-C8)-alkyl, where alkyl can be substituted once or more than once by F, R12 and R13 are H or (C1-C8)-alkyl; or the two radicals R12 and R13 form, together with the nitrogen atom to which they are bonded, a 5-6-membered, saturated heterocyclic ring which can contain a further oxygen atom; and the physiologically tolerated salts thereof.
- 5. A trometamol salt of a compound of a formula I as claimed in claim 1.
- 6. A pharmaceutical composition comprising one or more compounds as claimed in claim 1 and a pharmaceutically acceptable excipient.
- 7. The pharmaceutical composition of claim 6, further comprising one or more blood sugar-lowering active agents.
- 8. The pharmaceutical composition of claim 6, further comprising an HMGCoA reductase inhibitor.
- 9. A method for treating type 2 diabetes comprising administering to a subject in need thereof, one or more compounds as claimed in claim 1.
- 10. The method of claim 9, further comprising administering one or agents selected from the group consisting of insulin and insulin derivatives, hypoglycemic compounds, an HMGCoA reductase inhibitor, a cholesterol absorption inhibitor, a PPAR gamma agonist, a PPAR alpha agonist, a mixed PPAR alpha/gamma agonist, a fibrate, an MTP inhibitor, a bile acid absorption inhibitor, a CETP inhibitor, a polymeric bile acid adsorber, an LDL receptor inducer, an ACAT inhibitor, an antioxidant, a lipoprotein lipase inhibitor, an ATP citrate lyase inhibitor, a squalene synthetase inhibitor, a lipoprotein(a) antagonist, a lipase inhibitor, a sulfonylurea, a biguanide, a meglitinide, a thiazolidinedione, an α-glucosidase inhibitor, a CART agonist, a NPY agonist, a MC4 agonist, a orexin agonist, a H3 agonist, a TNF agonist, a GLP-1 derivative, a CRF agonist, a CRF BP antagonist, a urocortin agonist, a β3 agonist, a MSH (melanocyt-stimulating hormone) agonist, a CCK agonist, a serotonin-reuptake inhibitor, a mixed serotonin and noradrenergic compound, a 5HT agonist, a bombesin agonist, a galanin antagonist, a growth hormone, a growth hormone-releasing compound, a TRH agonists, a decoupling protein 2- or 3-modulators, a leptin agonist, a DA agonists (bromocriptine, doprexin), a lipase/amylase inhibitor, a PPAR modulator, a RXR modulator a TR-β-agonist, an amphetamine and compounds which act on an ATP-dependent potassium channel of a beta cell.
- 11. The method of claim 9, wherein said subject is a human.
- 12. A method for lowering blood sugar comprising administering to a subject in need thereof, one or compounds as claimed in claim 1.
- 13. The method of claim 12 further comprising administering one or more blood sugar-lowering active agents.
- 14. The method of claim 12, wherein said subject is a human.
- 15. A method for inhibiting glycogen phosphorylase comprising administering to a subject in need thereof, an effective amount of one or more compounds as claimed in claim 1.
- 16. The method of claim 15, wherein said subject is a human.
- 17. A process for producing a pharmaceutical comprising mixing one or more compounds as claimed in claim 1 with a pharmaceutically suitable excipient and bringing this mixture into a form which is suitable for administration.
- 18. A process for the preparation of a compound of formula I as claimed in claim 1 wherein a urea of formula 2 or an aniline derivative of formula 3 is reacted with a compound of formula 4 or its aroyl iso-cyanates, reactive acid derivatives, acid chlorides or anhydrides;
- 19. The process of claim 18, wherein an aroyl isocyanate of the formula 4a is reacted with an acid of the formula 3a
- 20. A process for the preparation of physiologically tolerated salts of compounds of the formula I as claimed in claim 1, wherein acids of compounds of the formula I are reacted with a corresponding base.
- 21. The process of claim 20, wherein said base is α,α,α-tris(hydroxymethyl)-methylamine.
- 22. A process for the preparation of the compounds of formula I as claimed in claim 1 wherein said process comprises the following reaction scheme:
- 23. A process for the preparation of the compounds of formula I as claimed in claim 1 wherein said process comprises the following reaction scheme:
- 24. A method of reducing body weight comprising administering to a subject in need thereof, one or compounds as claimed in claim 1.
Priority Claims (1)
Number |
Date |
Country |
Kind |
10215907.6 |
Apr 2002 |
DE |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority under 35 U.S.C. § 119 to DE 10215907.6 filed Apr. 11, 2002. This application also claims priority under 35 U.S.C. § 120 to U.S. Provisional No. 60/402,779, filed Aug. 12, 2002. Both of these documents are incorporated herein by reference in their entirety.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60402779 |
Aug 2002 |
US |