IP Library Granted Patent US 8,633,175
Granted Patent B2
US 8,633,175 · App. 12/376,580 · Granted Jan 21, 2014

Compounds as antagonists or inverse agonists at opioid receptors

Inventors: David John Cowan (Hillsborough, NC); Andrew Lamont Larkin (Wake Forest, NC); Cunyu Zhang (Cary, NC); David Lee Musso (Raleigh, NC); Gary Martin Green (Raleigh, NC); Rodolfo Cadilla (Durham, NC); Paul Kenneth Spearing (Creedmoor, NC); Michael Joseph Bishop (Chapel Hill, NC); Jason Daniel Speake (Cary, NC)
Assignee: GlaxoSmithKline LLC
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Quick Facts
Patent No.
US 8,633,175
App. No.
12/376,580
Granted
Jan 21, 2014
Kind
B2
Abstract

Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.

Claims (10)

1. A compound which is N-{[3,5-difluoro-3′-(1H-1,2,4-triazol-3-yl)-4-biphenylyl]methyl}-2,3-dihydro-1H-inden-2-amine which is

or a salt thereof.

2. A pharmaceutical composition comprising a compound of claim 1 or a salt thereof and at least one excipient.

3. The compound of claim 1 which is a citrate, phosphate or mono- or di-hydrochloride salt.

4. The compound of claim 3 which is a citrate salt of N-{[3,5-difluoro-3′-(1H-1,2,4-triazol-3-yl)-4-biphenylyl]methyl}-2,3-dihydro-1H-inden-2-amine.

5. The compound of claim 3 which is a phosphate salt of N-{[3,5-difluoro-3′-(1H-1,2,4-triazol-3-yl)-4-biphenylyl]methyl}-2,3-dihydro-1H-inden-2-amine.

6. The compound of claim 3 which is a mono-hydrochloride salt of N-{[3,5-difluoro-3′-(1H-1,2,4-triazol-3-yl)-4-biphenylyl]methyl}-2,3-dihydro-1H-inden-2-amine.

7. The compound of claim 3 which is a di-hydrochloride salt of N-{[3,5-difluoro-3′-(1H-1,2,4-triazol-3-yl)-4-biphenylyl]methyl}-2,3-dihydro-1H-inden-2-amine.

8. A method of treatment comprising administering a pharmaceutical composition comprising (i) a compound of claim 1 or a salt thereof and (ii) at least one carrier to a human suffering from the condition of obesity.

9. A method of treatment comprising administering to a human a compound of claim 1 or a salt thereof, wherein said treatment is obesity.

Assignments (1)
CHANGE OF NAME Recorded Mar 28, 2011
From: SMITHKLINE BEECHAM CORPORATION
To: GLAXOSMITHKLINE LLC
Reel/Frame 026028/0509 →
Continuity (2)
Provisional Application 60821845 · Aug 9, 2006
Related Publication 20110124559A1 · May 26, 2011