# US 8,772,244 B2 · Tubulin inhibitors

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- Number: US 8,772,244 B2
- Document ID: US8772244B2
- Status: Granted
- Kind: B2
- Application number: 13/509,060
- Filed: 2010-11-12
- Published: 2012-10-04
- Granted: 2014-07-08
- Earliest claimed: 2009-11-12
- Assignees: R&D-Biopharmaceuticals GmbH
- Applicants: Wolfgang Richter
- Inventors: Wolfgang Richter
- Web page: https://patentgrep.com/patent/US8772244B2

## CPC

- C07D 277/28: Radicals substituted by nitrogen atoms
- A61P 35/00: Antineoplastic agents
- C07K 5/06139: {with the first amino acid being heterocyclic}
- C07D 211/18: with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)

## Abstract

The present invention relates to novel tubulin binding molecules of formula (I) and their use for the treatment of cancer and other diseases.

## Claims

### Claim 1

Compound of formula (I):
wherein
R is H or an alkyl, alkenyl, alkynyl, CO-alkyl or heteroalkyl group, all of which may optionally be substituted;
R′ is H or an alkyl, alkenyl, alkynyl, CO-alkyl or heteroalkyl group, all of which may optionally be substituted;
R″ is a group of formula —CH2OH or
n is 0, 1, 2, 3, 4 or 5;
Y is independently optionally substituted alkyl, heteroalkyl, halogen, CN, NO2 or OH;
or a pharmacologically acceptable salt, solvate, hydrate or a pharmacologically acceptable formulation thereof.

### Claim 2 (depends on 1)

Compound according to claim 1 wherein R is H or C1-C6 alkyl.

### Claim 3 (depends on 1)

Compound according to claim 1, wherein R′ is —CO-alkyl, alkyl or heteroalkyl.

### Claim 4 (depends on 1)

Compound according to claim 1, wherein R″ is

### Claim 5 (depends on 1)

Compound according to claim 1, wherein R″ is CH2OH.

### Claim 6 (depends on 1)

Compound according to claim 1, wherein n is 0.

### Claim 7 (depends on 1)

Compound according to claim 1 wherein R is C1-C6 alkyl, R′ is —CO-alkyl or heteroalkyl, n is 0 and R″ is —CH2OH or

### Claim 8 (depends on 1)

Compound according to claim 1 wherein R is methyl, R′ is acetyl, n is 0 and R″ is

### Claim 9 (depends on 1)

Pharmaceutical composition containing a compound according to claim 1 and optionally one or more carriers or adjuvants.

### Claim 10 (depends on 1)

A method for treating cancer comprising administering a compound of claim 1 to a subject in need thereof, thereby treating the subject's cancer.

### Claim 11 (depends on 9)

A method for treating cancer comprising administering a pharmaceutical composition of claim 9 to a subject in need thereof, thereby treating the subject's cancer.