IP Library Granted Patent US 10,208,043
Granted Patent B2
US 10,208,043 · App. 13/972,649 · Granted Feb 19, 2019

Methods for inhibiting fascin

Inventors: Xin-Yun Huang (New York, NY); Christy Young Shue (Englewood Cliffs, NJ)
Assignees: Cornell University; Novita Pharmaceuticals, Inc.
C07D487/04A61K31/428A61K31/433A61K31/522C07D249/12C07D277/82C07D285/08C07D405/12
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Quick Facts
Patent No.
US 10,208,043
App. No.
13/972,649
Granted
Feb 19, 2019
Kind
B2
Abstract

Provided are compositions and methods for treating a condition or disorder mediated by fascin activity in a subject in need thereof which method comprises administering to the subject a therapeutically effective amount of at least one compound of any one of Formula I-a to I-n, II, II-a, II-b or III or a pharmaceutically acceptable salt thereof.

Claims (17)

1. A method of inhibiting fascin expression or fascin activity, comprising administering an effective amount of a fascin inhibitor to a cell with fascin expression to thereby inhibit fascin expression or fascin activity in the cell, wherein the fascin inhibitor is a compound having the following structure:

or a tautomer thereof, and/or a pharmaceutically acceptable salt thereof,

wherein

L 1 is selected from the group consisting —(C(R 8 ) 2 ) j —, —(C(R 8 ) 2 ) q —C(O)—(C(R 8 ) 2 ) r —, —(C(R 8 ) 2 ) q —C(O)N(R 8 )—(C(R 8 ) 2 ) r —, —(C(R 8 ) 2 ) q —N(R 8 )C(O)—(C(R 8 ) 2 ) r —, —(C(R 8 ) 2 ) q —N(R 8 )S(O) 2 —(C(R 8 ) 2 ) r —, —(CH 2 ) q —S(O) 2 N(R 8 )—(CH 2 ) r —, —S—, —O— and —NR 8 —;

each R 6 is independently selected from the group consisting of halo and lower alkyl optionally substituted with 1-3 halo; or two adjacent R 6 on a phenyl ring form a 5- or 6-membered cycloalkyl or heterocycloalkyl fused with the phenyl ring;

R 8 is hydrogen or lower alkyl;

j is 1, 2 or 3;

q is 0 or 1;

r is 0 or 1; and

u is 1, 2 or 3.

2. The method of claim 1 , wherein L 1 is CH 2 .

3. The method of claim 1 , wherein the fascin inhibitor is a compound having the following structure:

or a tautomer thereof, and/or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein R 6 is halo.

5. The method of claim 4 , wherein u is 2.

6. The method of claim 2 , wherein the cell with fascin expression is in an animal.

7. The method of claim 6 , wherein the animal is a human.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2014
From: HUANG, XIN-YUN
To: CORNELL UNIVERSITY
Reel/Frame 032295/0136 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2014
From: SHUE, CHRISTY YOUNG
To: NOVITA PHARMACEUTICALS, INC.
Reel/Frame 032295/0169 →
Continuity (3)
Provisional Application 61692177 · Aug 22, 2012
Provisional Application 61778015 · Mar 12, 2013
Related Publication 20140080843A1 · Mar 20, 2014