Methods for inducing apoptosis in cancer cells

Patent metadata

Field	Value
Publication number	US-2018289693-A1
Application number	US-201615767599-A
Country	US
Kind code	A1
Filing date	Oct 12, 2016
Priority date	Oct 12, 2015
Publication date	Oct 11, 2018
Grant date	—

Abstract

Provided are methods for inducing apoptosis of cells using quinolinol compounds. Combinations of quinolinol compounds can be used in the methods. Combinations of one or more quinolinol compound and one or more inhibitors of cell growth arrest, e.g., Nutlin3a, can also be used in the methods. Also provided are compositions comprising of one or more quinolinol compound and one or more pharmaceutically acceptable carrier. The compositions can comprise one or more quinolinol compound, one or more pharmaceutically acceptable carrier, and one or more inhibitors of cell growth arrest, e.g., Nutlin3a.

First claim

1 . A method of inducing apoptosis of cells comprising contacting the cells with a therapeutically effective amount of one or more quinolinol compound having the following structure:

wherein the X 1 , X 2 , and X 3 substituents are independently selected from —H, —Cl, —Br, and —I.

2 . The method of inducing apoptosis of cells of claim 1 , wherein X 1 and X 2 are both —Cl.

3 . The method of inducing apoptosis of cells of claim 1 , wherein X 1 and X 2 are both —Cl and are at the 1 and 2 positions of the ring.

4 . The method of inducing apoptosis of cells of claim 1 , wherein X 1 and X 2 are both —Cl and are at the 2 and 3 positions of the ring.

5 . The method of inducing apoptosis of cells of claim 1 , wherein the quinolinol compound is selected from MMRi6, MMRi61, MMRi62, MMRi63, MMRi64, MMRi65, MMRi68, and combinations thereof.

6 . The method of claim 1 , further comprising contacting the cells with Nutlin3a.

7 . The method of claim 6 , wherein the cells are contacted with one or more quinolinol and Nutlin3a concomitantly or sequentially.

8 . A composition comprising one or more quinolinol compound having the following structure:

wherein the X 1 , X 2 , and X 3 substituents are independently selected from —H, —Cl, —Br, and —I, and a pharmaceutically acceptable carrier.

9 . The composition of claim 8 , wherein the quinolinol compound is selected from MMRi6, MMRi61, MMRi62, MMRi63, MMRi64, MMRi65, MMRi68, and combinations thereof.

10 . The composition of claim 1 , wherein the composition further comprises Nutlin3a.

Assignees

• Health Research Inc

Inventors

• Wang Xinjiang

Classifications

• A61K31/496

  Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K31/4709 Primary

  Non-condensed quinolines and containing further heterocyclic rings · CPC title

• A61K2300/00

  Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00 · CPC title