Claims
- 1. An indole derivative of the general formula (I)
- 2. An indole derivative as claimed in claim 1, wherein R is
(i) unsubstituted or substituted 5-, 6-, 7-quinolyl, (ii) unsubstituted or substituted 2-, 3-, 6-, 7- and 8-pyridopyrazinyl, (iii) unsubstituted or substituted 3-, 4-, 5-, 6- and 7-indazolyl, (iv) unsubstituted or substituted 2-, 3-, 4-, 5- and 6-pyridyl, (v) unsubstituted or substituted 3-, 4- and 5-isoxazolyl, (vi) unsubstituted or substituted 3-, 4- and 5-isothiazolyl.
- 3. An indole derivative as claimed in claim 1, wherein R7 is methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, acetyl or propionyl.
- 4. An indole derivative as claimed in claim 1, wherein the compounds of the general formula I is selected from the following group of compounds:
N-{2-[1-(4-chlorobenzyl)-1H-indol-3-yl]-2-oxoacetyl}-N-quinolin-6-ylacetamide (2) methyl {2-[1-(4-chlorobenzyl)-1H-indol-3-yl]-2-oxoacetyl}quinolin-6-ylcarbamate (3) ethyl {2-[1-(4-chlorobenzyl)-1H-indol-3-yl]-2-oxoacetyl}quinolin-6-ylcarbamate (5) propyl {2-[1-(4-chlorobenzyl)-1H-indol-3-yl]-2-oxoacetyl}quinolin-6-ylcarbamate (6) N-{2-[1-(4-chlorobenzyl)-1H-indol-3-yl]-2-oxoacetyl}-N-quinolin-6-ylpropionamide (7) ethyl {2-[l-(4-chlorobenzyl)-1H-indol-3-yl]-2-oxoacetyl}pyridin-4-ylcarbamate (8)
- 5. An indole derivative as claimed in claim 1, wherein R1 is 4-chlorobenzyl, R2-R6 are hydrogen and X, Y are oxygen or sulfur.
- 6. An indole derivative as claimed in claim 1, wherein R3, R4, R5 or R6 is trifluoromethyl.
- 7. An indole derivative of the general formula I,
- 8. An indole derivative as claimed in claim 7, wherein the compound of the general formula I is selected from the following group of compounds:
2-[1-(4-chlorobenzyl)-1H-indol-3-yl]-N-quinolin-6-yl-2-thioxoacetamide (11) 2-[1-(4-chlorobenzyl)-1H-indol-3-yl]-2-oxo-N-pyrido[2,3-b]pyrazin-7-ylacetamide (1) 2-[l-(4-chlorobenzyl)-1H-indol-3-yl]-N-(1H-indazol-5-yl)-2-oxoacetamide (4).
- 9. An indole derivative as claimed in claim 7, wherein R1 is 4-chlorobenzyl, R2-R6 are hydrogen and X, Y are oxygen or sulfur.
- 10. A pharmaceutical composition which comprises at least one of the indole derivatives as claimed in claim 1.
- 11. A pharmaceutical composition as claimed in claim 10 which comprises the indole derivative in a microparticulate or nanoparticulate composition.
- 12. A pharmaceutical composition as claimed in claim 10 which comprises the indole derivative and a pharmaceutically utilizable carrier and/or diluent and auxiliary substance in the form of tablets, sugar-coated tablets, capsules, solutions for infusion or ampoules, suppositories, plasters, powder preparations which can be used inhalatively, suspensions, creams and ointments.
- 13. A method for treating a tumor disease, which comprises administering an indole derivative as claimed in claim 1 to an individual in need of the treatment.
- 14. The method as claimed in claim 13, wherein the tumor disease involves drug resistance against at least one other active compound.
- 15. The method as claimed in claim 13, wherein the tumor disease involves a metastasizing carcinoma.
- 16. A pharmaceutical composition which comprises at least one of the indole derivatives as claimed in claim 7.
- 17. A pharmaceutical composition as claimed in claim 16 which comprises the indole derivative in a microparticulate or nanoparticulate composition.
- 18. A pharmaceutical composition as claimed in claim 16 which comprises the indole derivative and a pharmaceutically utilizable carrier and/or diluent and auxiliary substance in the form of tablets, sugar-coated tablets, capsules, solutions for infusion or ampoules, suppositories, plasters, powder preparations which can be used inhalatively, suspensions, creams and ointments.
- 19. A method for treating a tumor disease, which comprises administering an indole derivative as claimed in claim 7 to an individual in need of the treatment.
- 20. The method as claimed in claim 19, wherein the tumor disease involves drug resistance against at least one other active compound.
- 21. The method as claimed in claim 19, wherein the tumor disease involves a metastasizing carcinoma.
Priority Claims (2)
Number |
Date |
Country |
Kind |
03012868.0 |
Jun 2003 |
EP |
|
04011598.2 |
May 2004 |
EP |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of priority to U.S. Provisional Application Nos. 60/476,277 filed on Jun. 5, 2003, 60/476,794 filed on June 6, 2003 and 60/572,025 filed on May 17, 2004 and European Patent Application Nos. 03012868.0 filed on Jun. 6, 2003 and 04011598.2 filed on May 15, 2004, all of which are incorporated herein by reference in their entirety.
Provisional Applications (3)
|
Number |
Date |
Country |
|
60476277 |
Jun 2003 |
US |
|
60476794 |
Jun 2003 |
US |
|
60572025 |
May 2004 |
US |