Substituted chroman derivatives, medicaments and use in therapy
Novel substituted chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.
1. A method for the treatment of cancer or a tumour mass, which comprises administering to a subject in need thereof a therapeutically effective amount of a compound of formula (I-b):
wherein:
R 1 is C 1-6 alkyl;
the drawing “---” and R 2 together represent a double bond or
the drawing “---” represents a single bond and R 2 is hydrogen or hydroxy,
R 3 , R 4 and R 5 are independently hydrogen, hydroxy, halo, NR 10 R 11 , C 1-6 alkoxy, C 1-6 fluoroalkyl or C 1-6 alkyl;
R 6 is hydrogen;
R 7 is hydroxy or C 1-6 alkoxy;
R 8 and R 9 are independently hydrogen, hydroxy, halo, NR 10 R 11 , C 1-6 alkoxy, C 1-6 fluoroalkyl or C 1-6 alkyl; and
R 10 and R 11 are independently hydrogen, C 1-6 alkyl or trialkyl silyl.
2. The method of claim 1 , wherein the compound of formula (I-b) is selected from compound Nos. 1 to 9 as set forth below:
3. The method of claim 1 , wherein the cancer or tumour mass is of epithelial origin, of mesenchymal origin or of neural origin.
4. The method of claim 3 , wherein the cancer or tumour mass of epithelial origin is prostate, ovarian, cervical, breast, gall-bladder, pancreatic, colorectal, renal or non-small lung cancer.
5. The method of claim 3 , wherein the cancer or tumour mass of mesenchymal origin is melanoma, mesothelioma or sarcoma cancer.
6. The method of claim 3 , wherein the cancer or tumour mass of neural origin is glioma.
7. The method of claim 1 , wherein the compound is simultaneously administered with an anti-cancer agent.
8. The method of claim 1 , wherein the compound is sequentially administered with an anti-cancer agent.
9. The method of claim 7 , wherein the anti-cancer agent is cisplatin, dehydroequol or paclitaxel.
10. The method of claim 8 , wherein the anti-cancer agent is cisplatin, dehydroequol or paclitaxel.
11. The method of claim 7 , wherein the compound of formula (I-b) is:
said anti-cancer agent is dehydroequol, and said subject is afflicted with ovarian or pancreatic cancer.
12. The method of claim 8 , wherein the compound of formula (I-b) is:
said anti-cancer agent is dehydroequol, and said subject is afflicted with ovarian or pancreatic cancer.
13. The method of claim 1 , wherein the compound acts as a chemosensitising agent.