Tetrazolones as a carboxylic acid bioisosteres

Patent metadata

Field	Value
Publication number	US-10450280-B2
Application number	US-201715617900-A
Country	US
Kind code	B2
Filing date	Jun 8, 2017
Priority date	Jan 26, 2015
Publication date	Oct 22, 2019
Grant date	Oct 22, 2019

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.

First claim

What is claimed is:

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.

Assignees

• Rigel Pharmaceuticals Inc

Inventors

• Duncton Matthew
• Singh Rajinder

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/04

  Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title