# US 2014/0194451 A1 · Cdc42 Inhibitor and Uses Thereof

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- Number: US 2014/0194451 A1
- Document ID: US20140194451A1
- Status: Published application
- Kind: A1
- Application number: 14/087,662
- Filed: 2013-11-22
- Published: 2014-07-10
- Earliest claimed: 2012-05-21
- Inventors: Qun Lu; Huchen Zhou; Yanhua Chen; Amy Friesland
- Web page: https://patentgrep.com/patent/US20140194451A1

## CPC

- C07D 239/42: One nitrogen atom (nitro radicals C07D239/30)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 335/12: the carbon skeleton containing six-membered aromatic rings
- C07D 239/69: Benzenesulfonamido-pyrimidines
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit, the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.

## Claims

### Claim 1

A compound of structure A:
structure B:
or a combination thereof, wherein
R1, R2, R3, R4, R5, R6, R7, R8 are each independently selected from the group consisting of fluoro, chloro, bromo, nitro, cyano, amino, methyl, hydroxylmethyl, trifluoromethyl, methoxy, trifluoromethyoxy, and ethyl; and
A, D, E, G, J, M, W, X, Y, Z are each selected from the group consisting of nitrogen, carbon, and substituted carbon, and any of A, D, E, G, J, M, W, X, Y, Z may be missing, such that the ring structure is less than a six-membered ring.

### Claim 2

A compound of structure C:
where R1 and R2 are independently selected from the group consisting of alkyl, cyclic alkyl, aryl, and substituted aryl.

### Claim 3 (depends on 2)

The compound of claim 2 wherein R1 is selected from the group consisting of
and R2 is selected from the group consisting of

### Claim 4 (depends on 2)

The compound of claim 2 wherein the compound is according to formula I:

### Claim 5 (depends on 1)

The compound of claim 1 wherein the compound is prepared as a medicament for at least one of treatment of malignant tumors, prevention and treatment of malignant tumor development and invasion, treatment of diseases of the cardiovascular system treatment of respiratory diseases, and treatment of diseases of nervous system.

### Claim 6 (depends on 2)

The compound of claim 2 wherein the compound is prepared as a medicament for at least one of treatment of malignant tumors, prevention and treatment of malignant tumor development and invasion, treatment of diseases of the cardiovascular system, treatment of respiratory diseases, and treatment of diseases of nervous system.

### Claim 7 (depends on 1)

The compound of claim 1 wherein the compound inhibits a function of Cdc42.

### Claim 8 (depends on 7)

The compound of claim 7 wherein the function of Cdc42 is selected from the group consisting of cell movement, cell adhesion, apoptosis, intracellular transport, cytoskeletal reorganization, cellular endocytosis, regulation of cell cycle, cell transcription, and combinations thereof.

### Claim 9 (depends on 2)

The compound of claim 2 wherein the compound inhibits a function of Cdc42.

### Claim 10 (depends on 9)

The compound of claim 9 wherein the function of Cdc42 is selected from the group consisting of cell movement, cell adhesion, apoptosis, intracellular transport, cytoskeletal reorganization, cellular endocytosis, regulation of cell cycle, cell transcription, and combinations thereof.

### Claim 11 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1 and at least one excipient.

### Claim 12 (depends on 2)

A pharmaceutical composition comprising a compound of claim 2 and at least one excipient.

### Claim 13

A compound of formula I:

### Claim 14 (depends on 13)

The compound of claim 13 wherein the compound is prepared as a medicament for at least one of treatment of malignant tumors, prevention and treatment of malignant tumor development and invasion, treatment of diseases of the cardiovascular system, treatment of respiratory diseases, and treatment of diseases of nervous system.

### Claim 15 (depends on 13)

The compound of claim 13 wherein the compound inhibits a function of Cdc42.

### Claim 16 (depends on 15)

The compound of claim 15 wherein the function of Cdc42 is selected from the group consisting of cell movement, cell adhesion, apoptosis, intracellular transport, cytoskeletal reorganization, cellular endocytosis, regulation of cell cycle, cell transcription, and combinations thereof.