Back to results
US 2008/0176894 A1Published application
Novel aminopyridine-derivatives
AssigneeAltana Pharma AG
InventorThomas Fuchss
Life of this patent
Estimating the term…
Abstract
The compounds of Formula (I) in which R1, R2, R3 and R4 have the meanings as given in the description are novel effective iNOS inhibitors.
Claims21
-15. (canceled)
A method for treating an acute inflammatory disease in a patient comprising administering to said patient a therapeutically effective amount of a compound of formula I
- in which
- R1 is hydrogen or 1-4C-alkyl,
- R2 is hydrogen, halogen, hydroxyl, nitro, amino, 1-7C-alkyl, trifluoromethyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, 1-4C-alkoxy, completely or predominantly fluorine-substituted 1-4C-alkoxy, 1-4C-alkoxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkoxy, 1-4C-alkoxycarbonyl, mono- or di-1-4C-alkylaminocarbonyl, mono- or di-1-4C-alkylaminosulfonyl, 1-4C-alkylcarbonylamino, 1-4C-alkylsulfonylamino, phenyl, R21- and/or R211-substituted phenyl, phenyl-1-4C-alkyl, phenyl-1-4C-alkyl wherein the phenyl moiety is substituted by R22, phenyl-1-4C-alkoxy, pyridyl, pyridyl substituted by R23, pyridyl-1-4C-alkyl, or pyridyl-1-4C-alkyl wherein the pyridyl moiety is substituted by R24, in which
- R21 is cyano, halogen, carboxyl, 1-4C-alkyl, 1-4C-alkoxy, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, 1-4C-alkylcarbonylamino, 1-4C-alkoxycarbonyl, aminosulfonyl, mono- or di-1-4C-alkylaminosulfonyl, amino, mono- or di-1-4C-alkylamino, trifluoromethyl, hydroxyl, phenylsulfonylamino, phenyl-1-4C-alkoxy, or —S(O)2-Het, in which
- Het is bonded to the adjacent sulfonyl group via a ring nitrogen atom, and is a 3- to 7-membered fully saturated heterocyclic ring comprising one nitrogen atom, to which the sulfonyl group is attached, and optionally one further heteroatom selected from the group consisting of N(R210), oxygen and sulfur, in which
- R210 is 1-4C-alkyl,
- R211 is halogen or 1-4C-alkoxy,
- R22 is halogen, 1-4C-alkyl or 1-4C-alkoxy,
- R23 is halogen, 1-4C-alkyl or 1-4C-alkoxy,
- R24 is halogen, 1-4C-alkyl or 1-4C-alkoxy,
- R3 is hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy,
- R4 is 1-4C-alkyl, or 1-4C-alkoxy,
- or a pharmaceutically acceptable salt, N-oxide or salt of an N-oxide thereof.
10 more elements
A method for treating a chronic inflammatory disease of peripheral organs and the central nervous system (CNS) in a patient comprising administering to said patient a therapeutically effective amount of a compound of formula I
- in which
- R1 is hydrogen or 1-4C-alkyl,
- R2 is hydrogen, halogen, hydroxyl, nitro, amino, 1-7C-alkyl, trifluoromethyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, 1-4C-alkoxy, completely or predominantly fluorine-substituted 1-4C-alkoxy, 1-4C-alkoxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkoxy, 1-4C-alkoxycarbonyl, mono- or di-1-4C-alkylaminocarbonyl, mono- or di-1-4C-alkylaminosulfonyl, 1-4C-alkylcarbonylamino, 1-4C-alkylsulfonylamino, phenyl, R21- and/or R211-substituted phenyl, phenyl-1-4C-alkyl, phenyl-1-4C-alkyl wherein the phenyl moiety is substituted by R22, phenyl-1-4C-alkoxy, pyridyl, pyridyl substituted by R23, pyridyl-1-4C-alkyl, or pyridyl-1-4C-alkyl wherein the pyridyl moiety is substituted by R24, in which
- R21 is cyano, halogen, carboxyl, 1-4C-alkyl, 1-4C-alkoxy, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, 1-4C-alkylcarbonylamino, 1-4C-alkoxycarbonyl, aminosulfonyl, mono- or di-1-4C-alkylaminosulfonyl, amino, mono- or di-1-4C-alkylamino, trifluoromethyl, hydroxyl, phenylsulfonylamino, phenyl-1-4C-alkoxy, or —S(O)2-Het, in which
- Het is bonded to the adjacent sulfonyl group via a ring nitrogen atom, and is a 3- to 7-membered fully saturated heterocyclic ring comprising one nitrogen atom, to which the sulfonyl group is attached, and optionally one further heteroatom selected from the group consisting of N(R210), oxygen and sulfur, in which
- R210 is 1-4C-alkyl,
- R211 is halogen or 1-4C-alkoxy,
- R22 is halogen, 1-4C-alkyl or 1-4C-alkoxy,
- R23 is halogen, 1-4C-alkyl or 1-4C-alkoxy,
- R24 is halogen, 1-4C-alkyl or 1-4C-alkoxy,
- R3 is hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy,
- R4 is 1-4C-alkyl, or 1-4C-alkoxy,
- or a pharmaceutically acceptable salt, N-oxide or salt of an N-oxide thereof.
10 more elements
Dependencies are inferred from the claim text.