IP Library Granted Patent US 7,645,782
Granted Patent B2
US 7,645,782 · App. 10/535,474 · Granted Jan 12, 2010

Thia-epothilone derivatives for the treatment of cancer

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Quick Facts
Patent No.
US 7,645,782
App. No.
10/535,474
Granted
Jan 12, 2010
Kind
B2
Abstract

The present invention relates to new Macrocycles of formula (I) and their use for the treatment of cancer.

Claims (22)

1. A compound of Formula (I)

wherein

A is a group of formula (II):

wherein Q is sulphur or oxygen, z is CH, and R 6 is CH 3 , CH 2 OH or CH 2 NH 2 ,

U is hydrogen,

G-E is selected from the following groups,

wherein R′ is methyl,

R 1 is C 1 -C 4 -alkyl-,

L-V-W is a group of formula CH═CH—CH, CH 2 —CH 2 —CH or CH 2 —CH═C, wherein the double bonds may be cis or trans isomers,

n is 0 or 2,

X is oxygen or NH; and

R 3 and R 4 are each methyl,

or a pharmacologically acceptable salt thereof.

2. A method for treating a patient suffering from or susceptible to breast cancer or epidermoid cancer, comprising administering to the patient a compound of claim 1 .

3. The method of claim 2 wherein the patient is identified as suffering from breast cancer or epidermoid cancer and selected for treatment for breast cancer or epidermoid cancer, and the compound is administered to the identified and selected patient.

4. A compound of claim 1 , wherein X is oxygen or NH.

5. A compound of claim 1 , wherein R 1 is methyl, ethyl or propyl.

6. A compound of claim 1 , wherein R 3 and R 4 are methyl groups.

7. A compound of claim 1 wherein A is

8. A pharmaceutical composition comprising a compound of claim 1 or a pharmacologically acceptable salt-thereof.

9. The pharmaceutical composition of claim 8 , further comprising one or more carriers, adjuvants, diluents or mixtures thereof.

10. A method for treating a patient suffering from or susceptible to ovarian cancer, lung cancer, prostate cancer, cervix carcinoma, cancer of the bladder or leukemia, comprising administering to the patient a compound of claim 1 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 22, 2009
From: R&D-BIOPHARMACEUTICALS GMBH
To: RICHTER, WOLFGANG; GESELLSCHAFT FUER BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF)
Reel/Frame 022992/0561 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2005
From: RICHTER, WOLFGANG; WEBER, LUTZ
To: MORPHOCHEM AKTIENGESELLSCHAFT FUR KOMBINATORISCHE CHEMIE
Reel/Frame 017368/0975 →
CORRECT ASSIGNEE'S ADDRESS Recorded Sep 16, 2004
From: KAROLIN MACHINE TOOL, INC.
To: KMT WATERJET SYSTEMS, INC.
Reel/Frame 015156/0576 →