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US 2011/0086819 A1Published application
Novel phosphonic acid compounds as inhibitors of serine proteases
AssigneeOrtho-McNeil Pharmaceutical, Inc.
InventorsMichael N. Greco, Harold R. Almond, JR., Michael J. Hawkins, Eugene Powell
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Abstract
The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
Claims12
A compound of Formula (Ia):
- wherein:
- R7 is selected from the group consisting of hydrogen, C1-8 alkyl and C2-8 alkenyl;
- and,
- R8 is selected from the group consisting of piperazine and piperidine,
- optionally substituted with one to four substituents independently selected from the group consisting of:
- C1-4 alkyl, carbonyl (substituted with a substituent selected from the group consisting of C1-4 alkyl, aryl, aryl(C1-4)alkyl and aryl(C2-4)alkenyl) and aryl;
- wherein the aryl substituent and the aryl portions of the carbonyl substituent are optionally substituted with one to two substituents independently selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, di(C1-4 alkyl)amino, halogen, hydroxy and (halo)1-3(C1-4)alkyl;
- and isomers, racemates, enantiomers, diastereomers and salts thereof.
5 more elements
A compound of Formula (Ia):
- wherein
- R7 and R8 are dependently selected from the group consisting of:
- Cpd
- R7
- R8
- 4
- CH3
- 1-[(6-bromo-2-naphthalenyl)carbonyl]-4-piperidinyl
- 6
- CH3
- 1-[1-oxo-3-phenyl-2-propenyl]-4-piperidinyl
- 9
- CH3
- 1-[3-(4-methylphenyl)-1-oxo-2-propenyl]-4-piperidinyl
- 10
- CH3
- 1-[1-oxo-3-[4-(trifluoromethyl)phenyl]-2-propenyl]-4-
- piperidinyl
- 13
- CH3
- 1-[3-[4-(dimethylamino)phenyl]-1-oxo-2-propenyl]-4-
- piperidinyl
- 15
- CH3
- 1-benzoyl-4-piperidinyl
- 18
- CH3
- 1-[1-oxo-3-[4-(trifluoromethyl)phenyl]propyl]-4-piperidinyl
- 20
- CH3
- 1-(2-methyl-1-oxopropyl)-4-piperidinyl
- 24
- CH3
- 1-[(6-hydroxy-2-naphthalenyl)carbonyl]-4-piperidinyl
- 26
- CH3
- 1-acetyl-4-piperidinyl
- And,
- 30
- H
- 1-(2-naphthalenylcarbonyl)-4-piperidinyl
- and isomers, racemates, enantiomers, diastereomers and salts thereof.
39 more elements
Dependencies are inferred from the claim text.