IP Library Granted Patent US 9,856,260
Granted Patent B2
US 9,856,260 · App. 15/174,227 · Granted Jan 2, 2018

Compounds useful for inhibiting metastasis from cancer and methods using same

Inventors: Alessandro Fatatis (Penn Valley, PA); Joseph M. Salvino (Chester Springs, PA); Olimpia Meucci (Penn Valley, PA); Whitney L. Gladney (Glenolden, PA)
Assignees: Drexel University; Alliance Discovery, Inc.
C07D487/04A61K31/451A61K31/453A61K31/7088A61K39/3955C07D403/04C07K16/28
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Quick Facts
Patent No.
US 9,856,260
App. No.
15/174,227
Granted
Jan 2, 2018
Kind
B2
Abstract

The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX 3 CR1 or fractalkine antagonist.

Claims (17)

1. A compound of Formula (I):

wherein:

A 1 is CH 2 ;

n is 0, 1, 2, 3, 4 or 5;

A 2 and A 3 are both H, or A 2 and A 3 combine to form a divalent radical selected from the group consisting of methanediyl, ethane-1,2-diyl, or propane-1,3-diyl;

A 4 is CH 2 ;

R 1 and R 2 are both H, and R 3 is

R 4 is nil;

R 7 is H or OH;

wherein:

(a) ring A is selected from the group consisting of phenyl and substituted phenyl, and R 5 is triazolyl, substituted triazolyl, 1,2-benzisoxazolyl or substituted 1,2-benzisoxazolyl; or

(b) ring A is selected from the group consisting of

 and R 5 is phenyl, substituted phenyl, triazolyl, substituted triazolyl, 1,2-benzisoxazolyl, or substituted 1,2-benzisoxazolyl;

a pharmaceutically acceptable salt or solvate thereof, or any combinations thereof.

2. The compound of claim 1 , wherein in (b) R 5 is selected from the group consisting of phenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2-methoxyphenyl, 3-methoxyphenyl, and 4-methoxyphenyl.

3. A pharmaceutical composition comprising the compound of claim 1 and at least one pharmaceutically acceptable carrier.

4. The pharmaceutical composition of claim 3 , which is formulated for an administration route selected from the group consisting of inhalational, oral, rectal, vaginal, parenteral, topical, transdermal, pulmonary, intranasal, buccal, ophthalmic, intrathecal, and any combinations thereof.

Continuity (4)
Continuation 13776220 · Feb 25, 2013
Continuation 13312540 · Dec 6, 2011
Provisional Application 61420640 · Dec 7, 2010
Related Publication 20160264587A1 · Sep 15, 2016