IP Library Granted Patent US 8,889,730
Granted Patent B2
US 8,889,730 · App. 13/831,588 · Granted Nov 18, 2014

Indole and indazole compounds that activate AMPK

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Quick Facts
Patent No.
US 8,889,730
App. No.
13/831,588
Granted
Nov 18, 2014
Kind
B2
Abstract

The present invention relates to indole and indazole compounds of Formula (I) that activate 5′ adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.

Claims (21)

1. A compound of Formula (II)

wherein

X is CH;

L is a bond;

R 1 is —C(O)OR A ;

R A is H;

R 2 is H or F;

R 3 is Cl, F, or CN;

R 4 and R 5 are H;

R 6 and R 7 are independently H, F, or methoxy;

R 9 and R 10 are H; and

R 8 is (C 3 -C 8 )cycloalkyl wherein the (C 3 -C 8 )cycloalkyl is cyclopropyl or cyclobutyl substituted with hydroxy.

2. The compound according to claim 1 that is

6-chloro-5-[2-fluoro-4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid;

6-chloro-5-[3-fluoro-4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid;

or

6-chloro-5-[4-(1-hydroxycyclobutyl)-3-methoxyphenyl]-1H-indole-3-carboxylic acid;

or a pharmaceutically acceptable salt thereof.

3. 6 chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylic acid or a pharmaceutically acceptable salt thereof.

4. A compound of structure

5. A pharmaceutical composition comprising a compound according to claim 1 and at least one pharmaceutically acceptable excipient, diluent, or carrier.

Assignments (3)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 30, 2013
From: BHATTACHARYA, SAMIT; CAMERON, KIMBERLY; DOWLING, MATTHEW; FERNANDO, DILINIE; FILIPSKI, KEVIN; KUNG, DANIEL; LEE, ESTHER; SMITH, AARON; TU, MEIHUA
To: PFIZER INC.
Reel/Frame 031507/0199 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 25, 2013
From: EBNER, DAVID
To: PFIZER INC.
Reel/Frame 030076/0001 →