Phenyloxadiazole derivatives as PGDS inhibitors

Patent metadata

Field	Value
Publication number	US-9937175-B2
Application number	US-201615258892-A
Country	US
Kind code	B2
Filing date	Sep 7, 2016
Priority date	Oct 8, 2009
Publication date	Apr 10, 2018
Grant date	Apr 10, 2018

Abstract

This invention is directed to a compound of formula (I):

wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

First claim

We claim:

1. A pharmaceutical composition comprising 2-pyridin-2-yl-pyrimidine-5-carboxylic acid 3-[5-(1-hydroxy-1-methyl-ethyl)-1,2,4-oxadiazol-3-yl]-benzylamide and a pharmaceutically acceptable carrier.

2. A pharmaceutical composition comprising a pharmaceutically acceptable salt of 2-pyridin-2-yl-pyrimidine-5-carboxylic acid 3-[5-(1-hydroxy-1-methyl-ethyl)-1,2,4-oxadiazol-3-yl]-benzylamide and a pharmaceutically acceptable carrier.

3. A method for treating an allergic or inflammatory disorder in a patient in need thereof, wherein the allergic or inflammatory disorder is selected from the group consisting of allergic rhinitis, asthma, and chronic obstructive pulmonary disease, the method comprising administering to the patient a pharmaceutically effective amount of 2-pyridin-2-yl-pyrimidine-5-carboxylic acid 3-[5-(1-hydroxy-1-methyl-ethyl)-1,2,4-oxadiazol-3-yl]-benzylamide.

4. The method of claim 3 , wherein the allergic or inflammatory disorder is asthma.

5. The method of claim 3 , wherein the allergic or inflammatory disorder is chronic obstructive pulmonary disease.

6. A method for treating an allergic or inflammatory disorder in a patient in need thereof, wherein the allergic or inflammatory disorder is selected from the group consisting of allergic rhinitis, asthma, and chronic obstructive pulmonary disease, the method comprising administering to the patient a pharmaceutically effective amount of a pharmaceutically acceptable salt of 2-pyridin-2-yl-pyrimidine-5-carboxylic acid 3-[5-(1-hydroxy-1-methyl-ethyl)-1,2,4-oxadiazol-3-yl]-benzylamide.

7. The method of claim 6 , wherein the allergic or inflammatory disorder is asthma.

8. The method of claim 6 , wherein the allergic or inflammatory disorder is chronic obstructive pulmonary disease.

Assignees

• Sanofi Sa

Inventors

• Vandeusen Christopher L

Classifications

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P5/00

  Drugs for disorders of the endocrine system · CPC title

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P27/02

  Ophthalmic agents · CPC title