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US 2004/0006142 A1Published application
Ocular tension depressor
OwnerRyuji Uenoinventor
Life of this patent
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Abstract
This invention relates to an ocular tension depressor containing a specific benzamide derivative as an active ingredient.
Claims18
An ocular tension depressor containing, as an active ingredient, a compound represented by the general formula (I):
- 7
- wherein
- R1 is hydrogen or lower alkyl,
- R2 is hydrogen, lower alkyl, halo(lower)alkyl, halogen or lower alkoxy,
- R3 is lower alkyl which may be substituted with acyl or acylamino,
- A is O,
- R4 is hydrogen;
- lower alkyl which may be substituted with hydroxy, aryl or acyl;
- or cyclo(lower)alkyl, or
- A is
- 8
- and R9 and R4 may be linked together to form lower alkylene which may be substituted with oxo,
- R5 is hydrogen, halogen, nitro, hydroxy, protected hydroxy, lower alkyl, or lower alkoxy which may be substituted with lower alkylamino,
- R6 is hydrogen, lower alkyl or acyl,
- R7 is hydrogen, halogen, hydroxy or lower alkoxy,
- R8 is hydroxy, aryl, acyl, amino, lower alkoxy which may be substituted with lower alkylamino or acylamino;
- or aryl which may be substituted with at least one substituent selected from the group consisting of lower alkyl, lower alkoxy, halogen, halo(lower)alkyl, hydroxy, amino(lower)alkyl, azido(lower)alkyl, lower alkylamino(lower)alkyl, acylamino(lower)alkyl, hydroxy(lower)alkyl, cyano and acyl, or a pharmacologically acceptable salt thereof.
14 more elements
A method for treating high ocular tension disease and/or glaucoma which comprises administering an effective amount of a compound represented by the general formula (I):
- 10
- wherein
- R1 is hydrogen or lower alkyl,
- R2 is hydrogen, lower alkyl, halo(lower)alkyl, halogen or lower alkoxy,
- R3 is lower alkyl which may be substituted with acyl or acylamino,
- A is O,
- R4 is hydrogen;
- lower alkyl which may be substituted with hydroxy, aryl or acyl;
- or cyclo(lower)alkyl, or
- A is
- 11
- and R9 and R4 may be linked together to form lower alkylene which may be substituted with oxo,
- R5 is hydrogen, halogen, nitro, hydroxy, protected hydroxy, lower alkyl, or lower alkoxy which may be substituted with lower alkylamino,
- R6 is hydrogen, lower alkyl or acyl,
- R7 is hydrogen, halogen, hydroxy or lower alkoxy,
- R8 is hydroxy, aryl, acyl, amino, lower alkoxy which may be substituted with lower alkylamino or acylamino;
- or aryl which may be substituted with at least one substituent selected from the group consisting of lower alkyl, lower alkoxy, halogen, halo(lower)alkyl, hydroxy, amino(lower)alkyl, azido(lower)alkyl, lower alkylamino(lower)alkyl, acylamino(lower)alkyl, hydroxy(lower)alkyl, cyano and acyl, or a pharmaceutically acceptable salt thereof.
14 more elements
Use of a compound to treat high ocular tension disease and/or glaucoma represented by the general formula (I):
- 13
- wherein
- R1 is hydrogen or lower alkyl,
- R2 is hydrogen, lower alkyl, halo(lower)alkyl, halogen or lower alkoxy,
- R3 is lower alkyl which may be substituted with acyl or acylamino,
- A is O,
- R4 is hydrogen;
- lower alkyl which may be substituted with hydroxy, aryl or acyl;
- or cyclo(lower)alkyl, or
- A is
- 14
- and R9 and R4 may be linked together to form lower alkylene which may be substituted with oxo,
- R5 is hydrogen, halogen, nitro, hydroxy, protected hydroxy, lower alkyl, or lower alkoxy which may be substituted with lower alkylamino,
- R6 is hydrogen, lower alkyl or acyl,
- R7 is hydrogen, halogen, hydroxy or lower alkoxy,
- R8 is hydroxy, aryl, acyl, amino, lower alkoxy which may be substituted with lower alkylamino or acylamino;
- or aryl which may be substituted with at least one substituent selected from the group consisting of lower alkyl, lower alkoxy, halogen, halo(lower)alkyl, hydroxy, amino(lower)alkyl, azido(lower)alkyl, lower alkylamino(lower)alkyl, acylamino(lower)alkyl, hydroxy(lower)alkyl, cyano and acyl, or a pharmaceutically acceptable salt thereof.
14 more elements
Dependencies are inferred from the claim text.