IP Library › Granted Patent US 10,799,504
Granted Patent B2
US 10,799,504 · App. 13/740,182 · Granted Oct 13, 2020

Heterocyclic compounds and uses as anticancer agents

Inventors: Xiao Xu (San Diego, CA); Xiaobo Wang (San Diego, CA); Long Mao (San Diego, CA); Li Zhao (San Diego, CA); Biao Xi (San Diego, CA)
Assignee: ACEA THERAPEUTICS, INC.
A61K31/519A61K31/506A61K31/52A61K45/06C07D239/42C07D239/46C07D239/47C07D239/48C07D401/12C07D401/14C07D403/12C07D473/16C07D473/24C07D473/32C07D473/34C07D473/40C07D487/02C07D487/04
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Quick Facts
Patent No.
US 10,799,504
App. No.
13/740,182
Granted
Oct 13, 2020
Kind
B2
Abstract

The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.

Claims (34)

1. A compound of Formula Ic:

wherein

X is; CF 2 or CH 2 ;

R 3 and R 4 are independently hydrogen or C 1 -C 6 alkyl;

R 5 is hydrogen;

R 6 is hydrogen;

R 7 is hydrogen or C 1 -C 6 alkyl;

is

R 20 is selected from C 1 -C 6 alkoxy and C 1 -C 6 haloalkoxy;

R 21 is hydrogen;

R 22 is selected from hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, and hydroxy;

R 23 is selected from hydrogen, halogen, C 1 -C 6 alkyl, and hydroxy; and

Q is CH, CR 23 , or N;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is Formula IIa

where X 1 is C 1 -C 6 alkoxy.

3. The compound of claim 1 , wherein the compound is Formula III:

wherein

X is; CF 2 or CH 2 ;

R 3 and R 4 are each hydrogen;

R 5 is hydrogen;

R 6 is hydrogen;

R 7 is hydrogen or C 1 -C 6 alkyl;

R 20 is selected from C 1 -C 6 alkoxy and C 1 -C 6 haloalkoxy;

R 21 is hydrogen;

R 22 is selected from hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, and hydroxy;

R 23 is selected from hydrogen, halogen, C 1 -C 6 alkyl, and hydroxy; and

Q is CH, CR 23 , or N;

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 3 , wherein R 20 is C 1 -C 6 alkoxy.

5. A pharmaceutical composition comprising a compound of claim 1 admixed with at least one pharmaceutically acceptable carrier or excipient.

6. A combination for treating cancer in a subject, which combination comprises an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and an effective amount of a second prophylactic or therapeutic agent for treating and/or preventing cancer in a subject.

7. A method for treating cancer in a subject, which method comprises administering to a subject in need thereof an effective amount of the combination of claim 6 .

8. The compound of claim 1 , wherein the compound is

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2018
From: ACEA BIOSCIENCES, INC.
To: ACEA THERAPEUTICS, INC.
Reel/Frame 047492/0140 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2014
From: XU, XIAO; WANG, XIAOBO; MAO, LONG; ZHAO, LI; XI, BIAO
To: ACEA BIOSCIENCES, INC.
Reel/Frame 033557/0559 →
Continuity (2)
Provisional Application 61586718 · Jan 13, 2012
Related Publication 20130190320A1 · Jul 25, 2013