IP Library Granted Patent US 9,399,628
Granted Patent B2
US 9,399,628 · App. 13/949,468 · Granted Jul 26, 2016

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

Inventors: Bertrand Leblond (Paris, FR); Eric Beusoleil (Paris, FR); Thierry Taverne (St. Martin Boulogne sur Mer, FR); John E. Donello (Dana Point, CA)
Assignee: Allergan, Inc.
C07D265/30A61K31/40A61K31/4025A61K31/4409A61K31/4439A61K31/4545A61K31/4709A61K31/496A61K31/5375A61K31/5377A61K31/541C07D213/64C07D295/12C07D319/18
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Quick Facts
Patent No.
US 9,399,628
App. No.
13/949,468
Granted
Jul 26, 2016
Kind
B2
Abstract

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

Claims (16)

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.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 19, 2015
From: BEAUSOLEIL, ERIC; LEBLOND, BERTRAND; TAVERNE, THIERRY; DONELLO, JOHN E.
To: ALLERGAN, INC.
Reel/Frame 035208/0188 →
Continuity (4)
Division 13196132 · Aug 2, 2011
Continuation 11814601
Provisional Application 60647271 · Jan 26, 2005
Related Publication 20130310383A1 · Nov 21, 2013