Epothilone derivatives

• US 7,241,755 B2
• Filed: 08/30/2006
• Issued: 07/10/2007
• Est. Priority Date: 07/08/1997
• Status: Expired due to Term

• Current Assignee: R-pharm us operating llc
• Original Assignee: Bristol-Myers Squibb Company
• Inventors: Vite, Gregory D., Johnson, James A., Borzilleri, Robert M., Kim, Soong-Hoon
• Primary Examiner(s): Kifle; Bruck
• Application Number:
  US11/512,623
• Publication Number:
  US 20060287371A1
• Time in Patent Office: 314 Days
• Field of Search: 540/452, 540/462, 540/463, 540/468, 548/202, 548/203, 549/346, 549/355, 514/183, 514/365, 514/366, 514/450
• US Class Current: 514/183
• CPC Class Codes: A61P 19/00 Drugs for skeletal disorders
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: C07D 417/06 linked by a carbon chain containing only aliphatic carbon atoms
• CPC Class Codes: C07D 491/04 Ortho-condensed systems
• CPC Class Codes: C07D 491/044 with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• CPC Class Codes: C07D 493/04 Ortho-condensed systems

Abstract

The present invention relates to compounds of the formula

in which the variables G, W, Q, X, Y, B₁, B₂, Z₁, Z₂, and R₁–R₇ are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Claims

1. A compound of the formula

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:

B₁ is OH and B₂ 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:

R₁, R₂, and R₇ are H; and

R₃, R₄, and R₅ are methyl;

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 5, wherein G is:

7. The compound of claim 6, wherein R₁₁ 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 NR₁₅;

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 8, wherein:

R₁, R₂, and R₇ are H; and

R₃, R₄, and R₅ are methyl;

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 9, wherein G is:

11. The compound of claim 10, wherein R₁₁ 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 R₁₅ 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.