1-aryl-1-hydroxy-2,3-diamino-propyl amines, 1-heteroaryl-1-hydroxy-2,3-diamino-propyl amines and related compounds having analgesic and/or immuno stimulant activity

Patent metadata

Field	Value
Publication number	US-9399628-B2
Application number	US-201313949468-A
Country	US
Kind code	B2
Filing date	Jul 24, 2013
Priority date	Jan 26, 2005
Publication date	Jul 26, 2016
Grant date	Jul 26, 2016

Abstract

Compounds of the formula

where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.

First claim

What is claimed is:

1. A compound having the formula

where:
R 3 is CO—R 7 or CO—O—R 7 ;
R 4 is CO—R 8 ;
R 5 and R 6 are independently selected from H, alkyl of 1 to 6 carbons and alkoxy of 1 to 6 carbons;
R 7 is H, benzyl, alkyl of 1 to 20 carbons substituted with and NH 2 group, with a NHCOOalkyl or with an NH-COalkyl group where the alkyl group has 1 to 6 carbons, or R 7 is aryl, heteroaryl, aryl-alkyl or heteroaryl-alkyl where the alkyl moiety is branched or unbranched and has 1 to 4 carbons, said aryl or heteroaryl groups being optionally substituted with 1 to 3 groups independently selected from the group consisting of halogen, alkyl of 1 to 6 carbons, alkoxy of 1 to 6 carbons and thioxy of 1 to 6 carbons;
R 8 is alkyl of 1 to 6 carbons;

or any other pharmaceutically acceptable salt of said compound.

2. A compound in accordance with claim 1 having the formula

or any other pharmaceutically acceptable salt of said compound.

3. A method of treating pain in a mammal, the method comprising the step of administering to said mammal in need of such treatment a compound in accordance with claim 1 or a pharmaceutically acceptable salt thereof.

4. A method of treating pain in a mammal, the method comprising the step of administering to said mammal in need of such treatment a compound in accordance with claim 2 or a pharmaceutically acceptable salt thereof.

5. The method of claim 3 , wherein said pain is chronic pain.

6. The method of claim 4 , wherein said pain is chronic pain.

7. A pharmaceutical composition comprising a compound in accordance with claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

8. A pharmaceutical composition comprising a compound in accordance with claim 2 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

Assignees

• Allergan Inc

Inventors

• Leblond Bertrand
• Beusoleil Eric
• Taverne Thierry
• Donello John E

Classifications

• A61P37/04

  Immunostimulants · CPC title

• A61P37/02

  Immunomodulators · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title

• A61P29/02

  without antiinflammatory effect · CPC title