Triphenylethylene compounds and uses thereof

Patent metadata

Field	Value
Publication number	US-9845295-B2
Application number	US-201615358886-A
Country	US
Kind code	B2
Filing date	Nov 22, 2016
Priority date	Nov 24, 2015
Publication date	Dec 19, 2017
Grant date	Dec 19, 2017

Abstract

Triphenylethylene compounds of formula (II)

as dual aromatase inhibitors and selective estrogen receptors modulators are described. Also described are methods for treating patients of breast cancers, and patients of breast cancer comorbid with osteoporosis, using the described triphenylethylence compounds or pharmaceutical formulations thereof.

First claim

What is claimed is:

1. A triphenylethylene compound of the formula (II)

wherein:
R 2 is an amino, hydroxyl, nitro, halo, cyano, or hydrogen;
R 3 is an amino, hydroxyl, nitro, halo, cyano, or hydrogen; and
R 4 is an amino, hydroxyl, nitro, halo, cyano, C1-C6 alkoxy, or hydrogen.

2. The triphenylethylene compound of claim 1 , wherein the compound has the formula (III)

wherein:
R 2 is an amino, hydroxyl, nitro, halo, cyano, or hydrogen; and
R 3 is an amino, hydroxyl, nitro, halo, cyano, or hydrogen.

3. The triphenylethylene compound of claim 1 , wherein the compound has the formula (IV)

4. The triphenylethylene compound of claim 1 , wherein the compound has the formula (V)

5. The triphenylethylene compound of claim 1 , wherein the compound has the formula (VI)

6. The triphenylethylene compound of claim 1 , wherein the compound has the formula (VII)

wherein:
R 2 is an amino, hydroxyl, nitro, halo, cyano, or hydrogen; and
R 3 is an amino, hydroxyl, nitro, halo, cyano, or hydrogen.

7. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and one or more pharmaceutically acceptable carriers, diluents, and excipients.

8. A method for treating a patient of breast cancer comorbid with osteoporosis, the method comprising the step of administering a therapeutically effective amount of a compound of claim 1 , together with one or more pharmaceutically acceptable carriers, diluents, and excipients, to the patient in need of relief from said cancer and osteoporosis.

9. A method for treating a patient of breast cancer comorbid with osteoporosis, the method comprising the step of administering a therapeutically effective amount of a compound of claim 1 , together with a therapeutically effective amount of one or more other compounds used for treating breast cancer with the same or different mode of action and one or more pharmaceutically acceptable carriers, diluents, and excipients, to the patient in need of relief from said cancer and osteoporosis.

Assignees

• Purdue Research Foundation

Inventors

• Cushman Mark S
• Lv Wei
• Zhao li-ming

Classifications

• C07C39/20

  Hydroxy-styrenes · CPC title

• C07C255/36

  the carbon skeleton being further substituted by hydroxy groups · CPC title

• C07D233/64 Primary

  with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine · CPC title

• C07D249/08

  1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles · CPC title

• C07C211/53

  having the nitrogen atom of at least one of the amino groups further bound to a hydrocarbon radical substituted by amino groups · CPC title