IP Library Granted Patent US 8,415,353
Granted Patent B2
US 8,415,353 · App. 12/920,928 · Granted Apr 9, 2013

Amino-quinoxaline and amino-quinoline compounds for use as adenosine A

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,415,353
App. No.
12/920,928
Granted
Apr 9, 2013
Kind
B2
Abstract

Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(═NOH)NH 2 , —CONHR 1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A 2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.

Claims (20)

1. A compound of the structural Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

Z is independently hydrogen, halogen or haloalkyl;

Q is —CONHR 1 ; or is a heterocyclic radical selected from the group consisting of:

R 1 is aralkyl, aryloxyalkyl, benzocycloalkyl or heteroarylalkyl; and

R 2 is amino, aryl, heteroaryl, arylamino, arylalkyl or heteroarylalkyl.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Q is a heterocyclic radical of the formula:

wherein R 2 is amino, aryl, heteroaryl, arylamino, arylalkyl or heteroarylalkyl.

3. A compound of the structure:

or a pharmaceutically acceptable salt thereof, wherein:

Z is independently hydrogen, halogen or haloalkyl;

Q is independently —CONHR 1 or a heterocyclic radical of the formula:

wherein:

R 1 is aralkyl, benzocycloalkyl or heteroarylalkyl; and

R 2 is aryl, heteroaryl or arylalkyl.

4. The compound of claim 3 , or a pharmaceutically acceptable salt thereof, wherein Q is —CONHR 1 .

5. A pharmaceutical composition comprising at least one compound of claim 3 , or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier, adjuvant or vehicle.

6. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition comprising at least one compound of claim 6 , or a pharmaceutically acceptable salt-thereof and at least one pharmaceutically acceptable carrier, adjuvant or vehicle.

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CHANGE OF NAME Recorded Aug 30, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028884/0151 →