.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 7,241,755

« Back to Dashboard

Details for Patent: 7,241,755

Title:Epothilone derivatives
Abstract: The present invention relates to compounds of the 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 as defined herein, methods for the 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)
Filing Date:Aug 30, 2006
Application Number:11/512,623
Claims:1. A compound of the formula ##STR00052## wherein: ##STR00053## G is selected from the group consisting of alkyl; substituted alkyl; substituted aryl; a 4 to 7 membered monocyclic, 7 to 11 membered bicyclic, or 10 to 15 membered tricyclic saturated or unsaturated ring system having between 1 and 3 heteroatoms selected from nitrogen, oxygen, and sulfur; ##STR00054## W is O or NR.sub.15; X is O or H, H; Y is selected from the group consisting of O; H, OR.sub.16; OR.sub.17, OR.sub.17; NOR.sub.18; H, NHOR.sub.19; H, NR.sub.20R.sub.21; H, H; and CHR.sub.22; wherein OR.sub.17, OR.sub.17 can be a cyclic ketal; Z.sub.1 and Z.sub.2 are independently CH.sub.2; B.sub.1 and B.sub.2 are independently selected from the group consisting of OR.sub.24, OCOR.sub.25, and O--C(.dbd.O)--NR.sub.26R.sub.27, and when B.sub.1 is OH and Y is OH, H they can form a six-membered ring ketal or acetal; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.13, R.sub.14, R.sub.18, R.sub.19, R.sub.20, R.sub.21, R.sub.22, R.sub.26, and selected from the group consisting of H, alkyl, substituted alkyl, and aryl, and when R.sub.1 and R.sub.2 are alky, they can be joined to form a cycloalkyl; and when R.sub.3 and R.sub.4 are alkyl they can be joined to form a cycloalkyl; R.sub.6 is methyl; R.sub.16, R.sub.17, R.sub.24, and R.sub.25 are selected from the group consisting of H, alkyl, and substituted alkyl; R.sub.11, R.sub.12, R.sub.32, and R.sub.33 are selected from the group consisting of H; alkyl; substituted alkyl; aryl; substituted aryl; cycloalkyl containing 1 to 3 rings and 3 to 7 carbons per ring which may be further fused with an unsaturated C.sub.3 C.sub.7 carbocyclic ring; and a 4 to 7 membered monocyclic, 7 to 11 membered bicyclic, or 10 to 15 membered tricyclic saturated or unsaturated ring system having between 1 and 3 heteroatoms selected from nitrogen, oxygen, and sulfur; R.sub.8 is hydrogen or methyl; R.sub.15 is selected from the group consisting of H; alkyl; substituted alkyl; aryl; substituted aryl; cycloalkyl containing 1 to 3 rings and 3 to 7 carbons per ring which may be further fused with an unsaturated C.sub.3 C.sub.7 carbocyclic ring; a 4 to 7 membered monocyclic, 7 to 11 membered bicyclic, or 10 to 15 membered tricyclic saturated or unsaturated ring system having between 1 and 3 heteroatoms selected from nitrogen, oxygen, and sulfur; R.sub.32C.dbd.O, R.sub.33SO2, hydroxy, O-alkyl or O-substituted alkyl; or a pharmaceutically acceptable salt thereof; with the proviso that compounds wherein W and X are both O; and R.sub.1, R.sub.2 and R.sub.7 are H; and R.sub.3 and R.sub.4 are methyl; and G is 1-methyl-2-(substituted)-4-thiazolyl-ethenyl; are excluded.

2. The compound of claim 1, wherein: X is O and Y is O; or a pharmaceutically acceptable salt thereof.

3. The compound of claim 2, wherein: B.sub.1 is OH and B.sub.2 is OH; or a pharmaceutically acceptable salt thereof.

4. The compound of claim 3, wherein W is O; or a pharmaceutically acceptable salt thereof.

5. The compound of claim 4, wherein: R.sub.1, R.sub.2, and R.sub.7 are H; and R.sub.3, R.sub.4, and R.sub.5 are methyl; or a pharmaceutically acceptable salt thereof.

6. The compound of claim 5, wherein G is: ##STR00055## or a pharmaceutically acceptable salt thereof.

7. The compound of claim 6, wherein R.sub.11 is a 4 to 7 membered monocyclic saturated or unsaturated ring system having from 1 and 3 heteroatoms selected from nitrogen, oxygen, and sulfur; or a pharmaceutically acceptable salt thereof.

8. The compound of claim 3, wherein W is NR.sub.15; or a pharmaceutically acceptable salt thereof.

9. The compound of claim 8, wherein: R.sub.1, R.sub.2, and R.sub.7 are H; and R.sub.3, R.sub.4, and R.sub.5 are methyl; or a pharmaceutically acceptable salt thereof.

10. The compound of claim 9, wherein G is: ##STR00056## or a pharmaceutically acceptable salt thereof.

11. The compound of claim 10, wherein R.sub.11 is a 4 to 7 membered monocyclic saturated or unsaturated ring system having from 1 and 3 heteroatoms selected from nitrogen, oxygen, and sulfur; or a pharmaceutically acceptable salt thereof.

12. The compound of claim 11, wherein R.sub.15 is H; or a pharmaceutically acceptable salt thereof.

13. A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable vehicle or diluent.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc