IP Library Granted Patent US 7,629,350
Granted Patent B2
US 7,629,350 · App. 10/511,770 · Granted Dec 8, 2009

Compounds

Assignee: SmithKline Beecham Corporation
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Quick Facts
Patent No.
US 7,629,350
App. No.
10/511,770
Granted
Dec 8, 2009
Kind
B2
Abstract

Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Claims (25)

1. The compound which is:

8-(2,4,6-trifluorophenyl)-4-(2,4-difluorophenyl)-2-(2-hydroxy-1-hydroxymethylethylamino)-8H-pyrido[2,3-d]pyrimidin-7-one;

4,8-Bis-(2,4-difluoro-phenyl)-2-(2-hydroxy-1-hydroxymethylethylamino)-8H-pyrido-[2,3-d]-pyrimidin-7-one;

8-(2,4,6-trifluorophenyl)-4-(2-fluorophenyl)-2-(2-hydroxy-1-hydroxymethylethylamino) -8H-pyrido[2,3-d]pyrimidin-7-one;

8-(2,4,6-trifluorophenyl)-4-(4-fluorophenyl)-2-(2-hydroxy-1-hydroxymethylethylamino) -8H-pyrido[2,3-d]pyrimidin-7-one;

4-(2-fluoro-phenyl)-8-(2,4-difluoro-phenyl)-2-((S)-2-hydroxy-1-methyl-ethylamino)-8H-pyrido-[2,3-d]-pyrimidin-7-one;

4-(2,4-Difluoro-phenyl)-8-(4-fluoro-phenyl)-2-((S)-2-hydroxy-1-methyl-ethylamino)-8H-pyrido-[2,3-d]-pyrimidin-7-one;

4,8-Bis-(2,4-difluoro-phenyl)-2-(2-hydroxy-1-methyl-ethylamino)-8H-pyrido-[2,3-d]-pyrimidin-7-one;

8-(2,4-Difluorophenyl)-4-(2-chloro-4-fluorophenyl)-2-(2-hydroxy-1-hydroxymethylethylamino)-8H-pyrido[2,3-d]pyrimidin-7-one; or

8-(2,3-difluorophenyl)-4-(2,4-difluorophenyl)-2-(2-hydroxy-1-hydroxymethyl-ethylamino)-8H-pyrido[2,3-d]pyrimidin-7- one; or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier or diluent.

3. The compound which is:

4-(2,4-difluoro-phenylamino)-6-(2,4,6-trifluorophenylamino)-2-methylsulfanyl-pyrimidine-5-carbaldehyde;

4-(2,4-difluoro-phenyl)-6-(2,4-difluorophenylamino)-2-methylsulfanyl-pyrimidine-5-carbaldehyde;

4-(2-fluorophenyl)-6-(2,4,6-trifluorophenylamino)-2-methylsulfanyl-pyrimidine-5-carbaldehyde;

4-(4-fluorophenyl)-6-(2,4,6-trifluorophenylamino)-2-methylsulfanyl-pyrimidine-5-carbaldehyde;

4-(2-fluorophenyl)-6-(2,4-difluorophenylamino)-2-methylsulfanyl-pyrimidine-5-carbaldehyde;

4-(2-chloro-4-fluorophenyl)-6-(2,4-difluorophenylamino)-2-methylsulfanyl-pyrimidine-5-carbaldehyde; or

4-(2,4-difluorophenyl)-6-(2,3-difluorophenylamino)-2-methylsulfanyl-pyrimidine-5-carbaldehyde.

4. The compound which is:

8-(2,4,6-trifluorophenyl)-4-(2,4-difluorophenyl)-2-(2-hydroxy-1-hydroxymethylethylamino)-8H-pyridio[2,3]pyrimidin-7-one; or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising a compound according to claim 4 and a pharmaceutically acceptable carrier or diluent.

6. The compound which is:

8-(2,4,6-trifluorophenyl)-4-(2,4-difluorophenyl)-2-(2-hydroxy-1-hydroxymethylethylamino)-8H-pyridio[2,3]pyrimidin-7-one.

7. A pharmaceutical composition comprising a compound according to claim 6 and a pharmaceutically acceptable carrier or diluent.

Assignments (2)
CHANGE OF NAME Recorded Jan 6, 2010
From: SMITHKLINE BEECHAM CORPORATION
To: GLAXOSMITHKLINE LLC
Reel/Frame 023731/0748 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 18, 2005
From: BOEHM, JEFFREY C.; WIDDOWSON, KATHERINE L.; CALLAHAN, JAMES F.; WAN, ZEHONG
To: SMITHKLINE BEECHAM CORPORATION
Reel/Frame 016897/0717 →
Continuity (3)
Provisional Application 6037421900 · Apr 19, 2002
Provisional Application 6038855700 · Jun 13, 2002
Related Publication 20060293348A1 · Dec 28, 2006