IP Library Granted Patent US 10,538,526
Granted Patent B2
US 10,538,526 · App. 16/132,411 · Granted Jan 21, 2020

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
C07D487/04A61K31/197A61K31/519A61K45/06C07D405/12
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Quick Facts
Patent No.
US 10,538,526
App. No.
16/132,411
Granted
Jan 21, 2020
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 the alkyl or cycloalkyl may optionally be substituted with halo, alkoxy or heterocycloalkyl; and

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 Clinked or N-linked 3 to 10 membered non-aromatic, monocyclic ring, wherein the 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 (7)
Division 15682346 · Aug 21, 2017
Division 15172126 · Jun 2, 2016
Continuation 14618829 · Feb 10, 2015
Continuation 13889921 · May 8, 2013
Division 12997721
Provisional Application 61075538 · Jun 25, 2008
Related Publication 20190031668A1 · Jan 31, 2019