IP Library Granted Patent US 9,708,347
Granted Patent B2
US 9,708,347 · App. 14/655,648 · Granted Jul 18, 2017

Heterobicyclo-substituted [1,2,4]triazolo[1,5-C]quinazolin-5-amine compounds with A

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Quick Facts
Patent No.
US 9,708,347
App. No.
14/655,648
Granted
Jul 18, 2017
Kind
B2
Abstract

Disclosed are compounds of Formula G1 (structurally represented): where “RG3” “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Claims (30)

1. A compound, or a pharmaceutically acceptable salt thereof, which is:

wherein:

each R Gda is, independently: (a) H; (b) methyl; or (c) ethyl; and

R Ge is:

2. A compound of claim 1 which is:

2-(2-(2-cyclopropyl-4H-pyrrolo[3,4-d]thiazol-5(6H)-yl)ethyl)-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine;

2-(2-(2-isopropyl-4H-pyrrolo[3,4-d]thiazol-5(6H)-yl)ethyl)-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine;

2-(2-(2-ethyl-4H-pyrrolo[3,4-d]thiazol-5( 6 H)-yl)ethyl)-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine;

7-methoxy-2-(2-(2-methyl-4H-pyrrolo[3,4-d]oxazol-5(6H)-yl)ethyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine;

2-(2-(2-cyclopropyl-4H-pyrrolo[3,4-d]oxazol-5(6H)-yl)ethyl)-7-methoxy -[1,2,4]triazolo[1,5-c]quinazolin-5-amine;

7-methoxy-2-(2-(1-methylpyrrolo[3,4-c]pyrazol-5(1H,4H,6H)-yl)ethyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine;

(R)-7-methoxy-2-(2-(2-methyl-4H-pyrrolo[3,4-d]oxazol-5(6H)-yl)propyl) -[1,2,4]triazolo[1,5-c]quinazolin-5-amine;

(R)-7-methoxy-2-(2-(2-methyl-4H-pyrrolo[3,4-d]oxazol-5(6H)-yl)butyl) -[1,2,4]triazolo[1,5-c]quinazolin-5-amine,

or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition that comprises an inert carrier and the compound of claim 1 , or pharmaceutically acceptable salt thereof.

4. A compound of the Formula:

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 4 which is:

6. The compound of claim 4 in the form of a pharmaceutically acceptable salt.

7. A pharmaceutical composition comprising an inert carrier and the compound of claim 4 or a pharmaceutically acceptable salt thereof.

8. A compound of the Formula:

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 8 , which is:

10. The compound of claim 8 in the form of a pharmaceutically acceptable salt.

11. A pharmaceutical composition comprising an inert carrier and the compound of claim 8 or a pharmaceutically acceptable salt thereof.

12. A compound of the Formula:

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 12 which is:

14. The compound of claim 12 in the form of a pharmaceutically acceptable salt.

15. A pharmaceutical composition comprising an inert carrier and the compound of claim 12 or a pharmaceutically acceptable salt thereof.

Assignments (4)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 30, 2017
From: TEMPEST, PAUL
To: SHANGHAI CHEMPARTNER CO., LTD.
Reel/Frame 041116/0940 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 30, 2017
From: SHANGHAI CHEMPARTNER CO. LTD.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 041117/0051 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 27, 2017
From: ALI, AMJAD; BOYCE, CHRISTOPHER; DENG, QIAOLIN; HENDERSON, TIMOTHY J.; HUANG, XIANHAI; KIM, JAE HUN; KUANG, RONGZE; LIM, YEON HEE; LO, MICHAEL MAN CHU; METZGER, EDWARD; TING, PAULINE; STAMFORD, ANDREW; WU, HEPING; WON, WALTER; XIAO, DONG; YU, YOUNONG; ZHENG, JUNYING; ZORN, NICOLAS; GALLO, GIOCONDA V.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 041521/0128 →