# US 10,369,145 B2 · Coumarin derivatives and methods of use in treating hyperproliferative diseases

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- Number: US 10,369,145 B2
- Document ID: US10369145B2
- Status: Granted
- Kind: B2
- Application number: 14/775,050
- Filed: 2014-03-14
- Published: 2016-02-11
- Granted: 2019-08-06
- Earliest claimed: 2013-03-15
- Assignees: Discoverybiomed, Inc.
- Applicants: Discoverybiomed, Inc.
- Inventors: Erik Schwiebert; John Streiff; John Dixon; Hongwu Gao; Joseph P. Ritchie; Eric C. Seales; Deborah Mai
- Web page: https://patentgrep.com/patent/US10369145B2

## CPC

- A61K 31/4709: Non-condensed quinolines and containing further heterocyclic rings
- A61K 31/422: not condensed and containing further heterocyclic rings
- A61K 31/427: not condensed and containing further heterocyclic rings
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/12: of the kidneys
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 405/04: directly linked by a ring-member-to-ring-member bond
- C07D 413/04: directly linked by a ring-member-to-ring-member bond
- C07D 417/04: directly linked by a ring-member-to-ring-member bond
- C07D 417/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D 491/052: the oxygen-containing ring being six-membered
- C07D 493/04: Ortho-condensed systems
- C07D 498/04: Ortho-condensed systems
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Coumarin derivative compounds and methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The methods include administering to a subject a compound as described herein. Also provided are methods for inhibiting the interaction between two or more heat shock protein chaperones in a cell.

## Claims

### Claim 1

A method for treating polycystic kidney disease in a subject, comprising:
administering to a subject an effective amount of a compound of the following formula:
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
R1 is hydrogen, halogen, substituted or unsubstituted amino, or substituted or unsubstituted C1-6 alkyl;
R2 is halogen, nitro, trifluoromethyl, substituted or unsubstituted amino, or substituted or unsubstituted C1-6 alkyl; and
R5, R6, R7, R8, and R9 are each independently selected from hydrogen, halogen, substituted or unsubstituted alkoxy, trifluoromethyl, or substituted or unsubstituted C1-6 alkyl.

### Claim 2 (depends on 1)

The method of claim 1, wherein
R2 is C1-6 alkyl, halogen, or trifluoromethyl; and
R5, R6, R7, R8, and R9 are each independently selected from hydrogen and methoxy.

### Claim 3 (depends on 1)

The method of claim 1, wherein R5 is substituted or unsubstituted alkoxy.

### Claim 4 (depends on 1)

The method of claim 1, wherein the compound is

### Claim 5

A method for treating polycystic kidney disease in a subject, comprising:
administering to a subject an effective amount of a compound selected from the group consisting of:
or a pharmaceutically acceptable salt or prodrug thereof.