# US 8,569,356 B2 · Cyclin dependent kinase inhibitors

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- Number: US 8,569,356 B2
- Document ID: US8569356B2
- Status: Granted
- Kind: B2
- Application number: 12/084,184
- Filed: 2006-10-25
- Published: 2010-02-11
- Granted: 2013-10-29
- Earliest claimed: 2005-10-25
- Assignees: University of Florida Research Foundation, Inc.
- Applicants: David A. Ostrov; Brian K. Law; Patrick Corsino
- Inventors: David A. Ostrov; Brian K. Law; Patrick Corsino
- Web page: https://patentgrep.com/patent/US8569356B2

## CPC

- A61K 31/382: having six-membered rings, e.g. thioxanthenes (thiothixene A61K31/496)
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- G16B 15/30: Drug targeting using structural data; Docking or binding prediction
- G16C 20/50: Molecular design, e.g. of drugs
- G16B 15/00: ICT specially adapted for analysing two-dimensional [2D] or three-dimensional [3D] molecular structures, e.g. structural or functional relations or structure alignment
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- G16B: BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
- G16C: COMPUTATIONAL CHEMISTRY; CHEMOINFORMATICS; COMPUTATIONAL MATERIALS SCIENCE

## Abstract

The invention relates to cyclin dependent kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.

## Claims

### Claim 1

A method of treating a subject suffering from breast cancer or prostate cancer, the method comprising administering to subject in need thereof a therapeutically effective amount of a compound capable of stabilizing the interaction of a cyclin-dependent kinase and a cdk inhibitor, or a compound capable of stabilizing an inactive conformation of a cyclin-dependent kinase and/or a complex of a cyclin-dependent kinase and a cyclin, such that the subject is treated wherein the compound is selected from the group consisting of 1-(5-methyl-thiophen-2-yl)-3-phenyl-propenone, 4-t-butyl-2-nitro-aniline, 3-amino-1-sulfanylidene-5,6,7,8-tetrahydroisothiochromene-4-carbonitrile, and 4-p-tolylamino-[1,2]naphthoquinone”.

### Claim 2 (depends on 1)

The method of claim 1, wherein the cdk inhibitor is p27.

### Claim 3 (depends on 2)

The method of claim 2, wherein the compound is selected from

### Claim 4 (depends on 1)

The method of claim 1, wherein the cancer is breast cancer and the compound is 1-(5-methyl-thiophen-2-yl)-3-phenyl-propenone.

### Claim 5

A method for inhibiting breast cancer or prostate cancer cell proliferation, comprising contacting a breast cancer cell or a prostate cancer cell with a compound capable of stabilizing an interaction between a cyclin dependent kinase and p27, such that cancer cell proliferation is inhibited wherein the compound is selected from the group consisting of 1-(5-methyl-thiophen-2-yl)-3-phenyl-propenone, 4-t-butyl-2-nitro-aniline, 3-amino-1-sulfanylidene-5,6,7,8-tetrahydroisothiochromene-4-carbonitrile, and 4-p-tolylamino-[1,2]naphthoquinone”.

### Claim 6 (depends on 5)

The method of claim 5, wherein the cell is a breast cancer cell and the compound is 1-(5-methyl-thiophen-2-yl)-3-phenyl-propenone.

### Claim 7

A method of treating a subject suffering from breast cancer or prostate cancer, the method comprising administering to subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of 1-(5-methyl-thiophen-2-yl)-3-phenyl-propenone, 4-t-butyl-2-nitro-aniline, 3-amino-1-sulfanylidene-5,6,7,8-tetrahydroisothiochromene-4-carbonitrile, and 4-p-tolylamino-[1,2]naphthoquinone, such that the subject is treated.

### Claim 8

A method for inhibiting breast cancer or prostate cancer cell proliferation, comprising contacting a breast cancer cell or a prostate cell with a compound selected from the group consisting of 1-(5-methyl-thiophen-2-yl)-3-phenyl-propenone, 4-t-butyl-2-nitro-aniline, 3-amino-1-sulfanylidene-5,6,7,8-tetrahydroisothiochromene-4-carbonitrile, and 4-p-tolylamino-[1,2]naphthoquinone, such that breast cancer or prostate cancer cell proliferation is inhibited.