IP Library Granted Patent US 10,450,280
Granted Patent B2
US 10,450,280 · App. 15/617,900 · Granted Oct 22, 2019

Tetrazolones as a carboxylic acid bioisosteres

Inventors: Matthew Duncton (San Bruno, CA); Rajinder Singh (Belmont, CA)
Assignee: Rigel Pharmaceuticals, Inc.
C07D257/04A61K31/41A61K31/4155A61K31/4184A61K31/4245A61K31/4709A61K31/4725A61K31/496A61K31/506A61K31/517A61K31/519A61K31/5383A61K31/546A61K31/55A61K31/58C07D401/04C07D401/10C07D401/12C07D401/14C07D403/04C07D403/06C07D403/10C07D403/12C07D403/14C07D413/10C07D471/04C07D487/04C07D498/06C07D501/16C07D501/46C07J43/003C07J9/005
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Quick Facts
Patent No.
US 10,450,280
App. No.
15/617,900
Granted
Oct 22, 2019
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 (14)

1. A method of treating a disease or disorder in a subject in need of treatment, the method comprising:

a) determining that a compound comprising a tetrazolone derivative of a carboxyl group of an active agent has biological activity that is about equal or superior to that of the active agent; and

b) administering to the subject the compound comprising the tetrazolone derivative of a carboxyl group of an active agent,

wherein the active agent is associated with the disease or disorder to be treated.

2. The method of claim 1 , wherein the tetrazolone derivative comprises a tetrazolone or a substituted tetrazolone.

3. The method of claim 1 , wherein the compound is of the formula:

wherein

R 1 is the active agent; and

R 2 is selected from hydrogen, alkyl, and substituted alkyl;

or a salt or stereoisomer thereof.

4. The method of claim 3 , wherein R 2 is hydrogen.

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

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

7. The method of claim 3 , wherein R 2 is alkyl.

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 Aug 14, 2017
From: DUNCTON, MATTHEW; SINGH, RAJINDER
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 043287/0267 →
Continuity (4)
Continuation 15233676 · Aug 10, 2016
Continuation 15005773 · Jan 25, 2016
Provisional Application 62107948 · Jan 26, 2015
Related Publication 20180002297A1 · Jan 4, 2018