IP Library Granted Patent US 9,701,647
Granted Patent B2
US 9,701,647 · App. 15/233,676 · Granted Jul 11, 2017

Tetrazolones as a carboxylic acid bioisosteres

Inventors: Matthew Duncton (San Bruno, CA); Rajinder Singh (Belmont, CA)
Assignee: Rigel Pharmaceuticals, Inc.
C07D257/04A61K31/41A61K31/4184A61K31/4245A61K31/4709A61K31/496A61K31/506A61K31/519A61K31/546A61K31/55A61K31/58C07D401/04C07D401/10C07D401/12C07D401/14C07D403/06C07D403/12C07D403/14C07D413/10C07D471/04C07D487/04C07D501/16C07J43/003
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Quick Facts
Patent No.
US 9,701,647
App. No.
15/233,676
Granted
Jul 11, 2017
Kind
B2
Abstract

The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

Claims (8)

1. A method of treating a disease or disorder in a subject in need of treatment, the method comprising administering to the subject a compound comprising a tetrazolone derivative of a carboxyl group of an active agent wherein said compound is of formula:

wherein

R1 is the active agent; and

R2 is selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, and substituted heteroaryl; or a salt or stereoisomer thereof.

2. The method of claim 1 , wherein R 2 is hydrogen or alkyl.

3. A The method of claim 1 , wherein the active agent is a therapeutically effective active agent.

4. The method of claim 1 , wherein the tetrazolone derivative is produced from the carboxyl group of the active agent.

5. The method of claim 1 , wherein the compound is selected from:

Assignments (2)
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2016
From: DUNCTON, MATTHEW; SINGH, RAJINDER
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 039936/0793 →
Continuity (3)
Continuation 15005773 · Jan 25, 2016
Provisional Application 62107948 · Jan 26, 2015
Related Publication 20170129862A1 · May 11, 2017