Epothilone derivatives
View Patent ↗The present invention relates to epothilone derivatives, having the following formula: in which the variables G, W, Q, X, Y, B 1 , B 2 , Z 1 , Z 2 , and R 1–R 7 are defined herein, methods for preparation of the derivatives and intermediates thereof.
1. A compound having the formula V:
wherein,
Q is
R 8 is methyl;
G is 1-methyl-2-(2-methyl-4-thiazolyl)ethenyl;
W is NH;
X is O;
Y is O;
Z 1 and Z 2 are CH 2 ;
B 1 and B 2 are OH;
R 1 , R 2 , and R 7 are hydrogen; and
R 3 , R 4 , R 5 and R 6 are methyl; and/or a pharmaceutically-acceptable hydrate, solvate, and/or geometric, optical, and/or stereoisomer thereof.
2. A method of treating cancer in a patient comprising administering to the patient a therapeutically-effective amount of the compound according to claim 1 , and/or one or more hydrates, solvates, and/or isomers thereof, wherein the cancer is selected from one or more of cancer of the bladder, breast, colon, kidney, liver, lung, ovary, pancreas, stomach, cervix, thyroid, and/or prostate.
3. A method of treating breast cancer in a patient comprising administering to the patient a therapeutically-effective amount of the compound according to claim 1 , and/or one or more hydrates, solvates, and/or isomers thereof.
4. A method of treating lung cancer in a patient comprising administering to the patient a therapeutically-effective amount of the compound according to claim 1 , and/or one or more hydrates, solvates, and/or isomers thereof.
5. A pharmaceutical composition comprising the compound according to claim 1 , and/or one or more hydrates, solvates, and/or isomers thereof, and one or more pharmaceutically-acceptable diluents, vehicles and/or additives.
6. A method of treating cancer in a patient comprising administering to the patient a therapeutically-effective amount of the pharmaceutical composition according to claim 5 , wherein the cancer is selected from one or more of cancer of the bladder, breast, colon, kidney, liver, lung, ovary, pancreas, stomach, cervix, thyroid, and/or prostate.
7. A compound having the formula:
8. A solvate of the compound of claim 7 .
9. A hydrate of the compound of claim 7 .
10. A compound which is a geometric, optical or stereoisomer of the compound of claim 7 , or a mixture comprising the compound of claim 7 and one or more geometric, optical and/or stereoisomers of the compound of claim 7 .
11. A pharmaceutical composition comprising a solvate according to claim 8 and a pharmaceutically-acceptable diluent, vehicle, and/or additive.
12. A pharmaceutical composition comprising a hydrate according to claim 9 and a pharmaceutically-acceptable diluent, vehicle, and/or additive.
13. A pharmaceutical composition comprising a compound or mixture of compounds according to claim 10 and a pharmaceutically-acceptable diluent, vehicle, and/or additive.
14. A method of treating cancer in a patient comprising administering to the patient a therapeutically-effective amount of a pharmaceutical composition according to claim 11 , wherein the cancer is selected from one or more of cancer of the bladder, breast, colon, kidney, liver, lung, ovary, pancreas, stomach, cervix, thyroid, and/or prostate.
15. A method of treating cancer in a patient comprising administering to the patient a therapeutically-effective amount of a pharmaceutical composition according to claim 12 , wherein the cancer is selected from one or more of cancer of the bladder, breast, colon, kidney, liver, lung, ovary, pancreas, stomach, cervix, thyroid, and/or prostate.
16. A method of treating cancer in a patient comprising administering to the patient a therapeutically-effective amount of a pharmaceutical composition according to claim 13 , wherein the cancer is selected from one or more of cancer of the bladder, breast, colon, kidney, liver, lung, ovary, pancreas, stomach, cervix, thyroid, and/or prostate.
17. The method of claim 16 comprising the treatment of breast cancer.
18. The method of claim 2 comprising the treatment of prostate cancer.
19. The method of claim 2 comprising the treatment of kidney cancer.
20. The method of claim 2 comprising the treatment of pancreatic cancer.