IP Library Granted Patent US 9,765,080
Granted Patent B2
US 9,765,080 · App. 15/172,126 · Granted Sep 19, 2017

Triazolo[4,5-D] pyramidine derivatives and their use as purine receptor antagonists

Inventors: Samantha Jane Bamford (Winnersh, GB); Roger John Gillespie (Winnersh, GB); Richard Simon Todd (Winnersh, GB)
Assignee: Vernalis (R&D) Limited
C07D487/04C07D405/12
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Quick Facts
Patent No.
US 9,765,080
App. No.
15/172,126
Granted
Sep 19, 2017
Kind
B2
Abstract

Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.

Claims (18)

1. A compound of formula

or a tautomer, stereoisomer, or pharmaceutically acceptable salt thereof, wherein

R is —(CR a R b )—O—R 2;

R a is H or alkyl;

R b is H or alkyl; or R a and R b together with the atom to which they are attached form a 3 to 8 membered saturated or partially saturated hydrocarbon ring or form a 4 to 8 membered saturated or partially saturated heterocylic ring comprising a ring member selected from O, N(R 3 ) and S;

R 2 is H, alkyl, cycloalkyl or heterocycloalkyl, wherein said alkyl or cycloalkyl may optionally be substituted with halo, alkoxy or heterocycloalkyl;

R 3 is H or alkyl;

wherein

heteroaryl is a 5 or 6 membered aromatic ring, comprising one or two ring members selected from N, N(R 4 ), S and O;

alkyl (or the alkyl group of the alkoxy group) is a linear or branched saturated hydrocarbon containing up to 10 carbon atoms;

heterocycloalkyl is a C-linked or N-linked 3 to 10 membered non-aromatic, monocyclic ring, wherein said heterocycloalkyl ring comprises 1, 2 or 3 ring members independently selected from N, N(R 4 ), S(O) q and O;

R 4 is H or alkyl; and

q is 0, 1 or 2.

2. The compound of claim 1 , wherein

R a and R b are independently H; and

R 2 is tetrahydrofuranyl.

3. The compound of claim 1 , wherein R a and R b are independently H.

4. The compound of claim 1 , wherein R is

Assignments (2)
CHANGE OF NAME Recorded Jan 24, 2022
From: VERNALIS DEVELOPMENT LIMITED
To: LIGAND UK DEVELOPMENT LIMITED
Reel/Frame 058738/0271 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 24, 2022
From: VERNALIS (R&D) LIMITED
To: VERNALIS DEVELOPMENT LIMITED
Reel/Frame 058822/0570 →
Priority Claims (1)
GB 0906579.8 · Apr 16, 2009 · national
Continuity (5)
Continuation 14618829 · Feb 10, 2015
Continuation 13889921 · May 8, 2013
Division 12997721
Provisional Application 61075538 · Jun 25, 2008
Related Publication 20170088552A1 · Mar 30, 2017