IP Library › Granted Patent US 8,436,024
Granted Patent B2
US 8,436,024 · App. 12/895,995 · Granted May 7, 2013

2-pyridone compounds

Inventors: Andiappan Murugan (Bangalore, IN); Lena Kristina Bergstrom (Lund, SE); Anna Kristoffersson (Lund, SE); Martin Lindsjö (Lund, SE); Peter Olof Sjö (Lund, SE); Mark David Ashton (Manchester, GB); Jon Meigh (Manchester, GB)
Assignee: Astrazeneca AB
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Quick Facts
Patent No.
US 8,436,024
App. No.
12/895,995
Granted
May 7, 2013
Kind
B2
Abstract

The invention provides compounds of formula wherein R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , L, X and Y are as defined in the specification; together with processes and intermediates for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.

Claims (6)

1. The compound 3-(5-(1-(4-cyanophenyl)-1H-pyrazol-5-yl)-6-methyl-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamido)-N,N,N-trimethylpropan-1-aminium Y;

wherein Y represents a pharmaceutically acceptable anion.

2. The compound as defined in claim 1 which is 3-(5-(1-(4-cyanophenyl)-1H-pyrazol-5-yl)-6-methyl-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamido)-N,N,N-trimethylpropan-1-aminium benzenesulfonate.

3. A pharmaceutical composition comprising a compound as claimed in claim 1 in association with a pharmaceutically acceptable adjuvant, diluent or carrier.

4. The compound as defined in claim 2 which is 3-(5-(1-(4-cyanophenyl)-1H-pyrazol-5-yl)-6-methyl-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamido)-N,N,N-trimethylpropan-1-aminium benzenesulfonate Form A, characterized in that said Form A has an X-ray powder diffraction pattern with specific peaks at 4.3, 11.5 and 23.1°2θ when measured using CuKα1 radiation.

5. The compound as defined in claim 2 which is 3-(5-(1-(4-cyanophenyl)-1H-pyrazol-5-yl)-6-methyl-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamido)-N,N,N-trimethylpropan-1-aminium benzenesulfonate Form B, characterized in that said Form B has an X-ray powder diffraction pattern with specific peaks at 5.8, 7.5 and 17.2°2θ when measured using CuKα1 radiation.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2012
From: MEIGH, JON; ASHTON, MARK DAVID
To: SIGMA-ALDRICH COMPANY LTD
Reel/Frame 029463/0298 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2012
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 029463/0397 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2012
From: SIGMA-ALDRICH COMPANY LTD
To: ASTRAZENECA UK LIMITED
Reel/Frame 029463/0481 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2012
From: BERGSTROM, LENA KRISTINA; KRISTOFFERSSON, ANNA; LINDSJO, MARTIN; SJO, PETER OLOF
To: ASTRAZENECA AB
Reel/Frame 029463/0622 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2012
From: MURUGAN, ANDIAPPAN
To: ASTRAZENECA INDIA PRIVATE LIMITED
Reel/Frame 029463/0668 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2012
From: ASTRAZENECA INDIA PRIVATE LIMITED
To: ASTRAZENECA AB
Reel/Frame 029463/0713 →
Continuity (2)
Provisional Application 61248081 · Oct 2, 2009
Related Publication 20110082155A1 · Apr 7, 2011