IP Library Granted Patent US 8,304,577
Granted Patent B2
US 8,304,577 · App. 12/898,016 · Granted Nov 6, 2012

Modulators of G protein-coupled receptor 88

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Quick Facts
Patent No.
US 8,304,577
App. No.
12/898,016
Granted
Nov 6, 2012
Kind
B2
Abstract

The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

Claims (29)

1. A compound of Formula (I)

or a pharmaceutically acceptable salt thereof, wherein

A is phenyl;

R 1 is C 4 -C 6 alkoxy;

R 2 is selected from hydrogen, C 1 -C 3 alkyl; and halo;

R 3 is hydroxy-C 1 -C 3 alkyl;

R 4 is selected from C 1 -C 3 alkyl and hydroxy-C 1 -C 3 alkyl;

R 4′ is selected from hydrogen and C 1 -C 3 alkyl; or

R 4 and R 4′ , together with the carbon atom to which they are attached, form a C 3 -C 6 cycloalkyl ring; and

R 5 is selected from hydrogen, C 1 -C 3 alkyl, and halo.

2. A compound of formula (II)

or a pharmaceutically acceptable salt thereof, wherein

R 1 is C 4 -C 6 alkoxy;

R 3 is selected from

hydroxy-C 1 -C 3 alkyl; and

(NR a R b )—C 1 alkyl; wherein R a and R b are each independently selected from hydrogen;

C 1 -C 5 alkyl;

C 3 -C 5 cycloalkyl-C 1 alkyl wherein the cycloalkyl is optionally substituted with an amino group;

heterocyclyl-C 1 alkyl;

R 6 —C(O)—; wherein R 6 is selected from

amino-C 1 -C 5 alkyl wherein the alkyl is optionally substituted with a C 1 alkoxy group;

C 3 cycloalkyl-C 2 alkyl wherein the alkyl part is substituted with an amino group;

heterocyclyl; and

heterocyclyl-C 2 alkyl, wherein the alkyl part is substituted with an amino group;

or, R a and R b , together with the nitrogen atom to which they are attached, for a morpholinyl or piperazinyl ring wherein the piperazinyl ring is substituted with C 1 -C 3 alkyl; and

R 4 is selected from C 1 -C 2 alkyl and hydroxy-C 1 alkyl.

3. A compound according to claim 2 selected from

or a pharmaceutically acceptable salt thereof.

4. A composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded May 5, 2026
From: OXFORD FINANCE LLC
To: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS
Reel/Frame 075545/0601 →
SECURITY INTEREST Recorded May 4, 2026
From: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS (NEW JERSEY), INC.; LION ACQUISITION CORPORATION
To: HERCULES CAPITAL, INC., AS AGENT
Reel/Frame 075498/0899 →
SECURITY INTEREST Recorded Mar 17, 2022
From: LEXICON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 059432/0709 →
RELEASE OF SECURITY INTEREST Recorded Sep 14, 2020
From: BIOPHARMA CREDIT PLC
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 053767/0445 →
SECURITY INTEREST Recorded Dec 20, 2017
From: LEXICON PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 044958/0377 →