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Claims for Patent: 7,125,899

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Claims for Patent: 7,125,899

Title:Epothilone derivatives
Abstract:The present invention relates to epothilone derivatives, having the following formula: ##STR00001## in which the variables G, W, Q, X, Y, B.sub.1, B.sub.2, Z.sub.1, Z.sub.2, and R.sub.1 R.sub.7 are defined herein, methods for preparation of the derivatives and intermediates thereof.
Inventor(s): Vite; Gregory D. (Titusville, NJ), Kim; Soong-Hoon (Lawrenceville, NJ), Borzilleri; Robert M. (Lawrenceville, NJ), Johnson; James A. (Lawrenceville, NJ)
Assignee: Bristol-Myers Squibb Company (Princeton, NJ)
Application Number:10/405,886
Patent Claims: 1. A compound having the formula V: ##STR00051## wherein, Q is ##STR00052## R.sub.8 is methyl; G is 1-methyl-2-(2-methyl-4-thiazolyl)ethenyl; W is NH; X is O; Y is O; Z.sub.1 and Z.sub.2 are CH.sub.2; B.sub.1 and B.sub.2 are OH; R.sub.1, R.sub.2, and R.sub.7 are hydrogen; and R.sub.3, R.sub.4, R.sub.5 and R.sub.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: ##STR00053##

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.
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