Aminoalcohol derivatives
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsMinoru Sakurai, Hitoshi Hamashima, Kouji Hattori
Life of this patent
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Abstract
The present invention relates to a compound formula [I]: 1 wherein R1 is hydrogen or halogen, R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, X is bond, —CH2— or —O—, and Y is 2 in which R4 is lower alkoxycarbonyl, 3 in which R5 is carboxy(lower)alkyl, etc., 4 in which R6 is hydroxy, etc., and so on, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
Claims11
A compound of the formula [I]:
- 41
- wherein
- R1 is hydrogen or halogen,
- R2 is hydrogen or an amino protective group,
- R3 is hydrogen or lower alkyl,
- X is bond, —CH2— or —O—, and
- Y is
- 42
- in which R4 is lower alkoxycarbonyl,
- 43
- in which R5 is carboxy(lower)alkyl, (lower alkoxy)carbonyl(lower)alkyl, lower alkanoyl, mono(or di or tri)halo(lower)alkylsulfonyloxy, carboxyphenoxy, (lower alkoxy)carbonylphenoxy, carboxypyridyloxy, (lower alkanoyl)pyridyl, carboxypyrrolidinyl(lower)alkyl, (lower alkoxy)carbonylpyrrolidinyl(lower)alkyl, carboxyphenyl or (lower alkyl)phenyl,
- 44
- in which R6 is —OH, —COOH, —COOC2H5,
- 45
- provided that
- (i) when R6 is —OH, then X is —CH2—,
- (ii) when R6 is —COOH, then R1 is —H, or
- (iii) when R6 is —COOC2H5,
- 46
- then X is —O—,
- 47
- in which
- R7 is —OH, —COOH, —COOC2H5,
- 48
- and
- X is —CH2—,
- 49
- in which R8 is —OH, —COOH, —COOC2H5,
- 50
- provided that when R8 is —OH,
- 51
- then R3 is —CH3,
- 52
- in which R9 is hydroxy, cyclo(lower)alkyl, mono(or di or tri)halo(lower)alkyl, hydroxy(lower)alkoxy, lower alkoxy(lower)alkoxy, carboxy(lower)alkoxy, lower alkoxycarbonyl(lower)alkoxy, phenoxy, nitro, amino, lower alkylamino, [lower alkoxy(lower)-alkyl]amino, [hydroxy(lower)alkyl]amino, [lower alkoxycarbonyl]amino, lower alkanoylamino, [hydroxy(lower)alkanoyl]amino, benzoylamino, (lower alkylsulfonyl)amino, lower alkylthio or phenyl, and
- R10 is carboxy, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, carboxy(lower)alkyl, (lower alkoxycarbonyl)(lower)alkyl, carboxy(lower)-alkenyl, (lower alkoxycarbonyl)(lower)alkenyl or phenyl optionally substituted with carboxy or lower alkoxycarbonyl,
- 53
- in which R11 is halogen or lower alkyl, and
- R12 is carboxy, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, carboxy(lower)alkyl, (lower alkoxycarbonyl)(lower)alkyl, carboxy(lower)-alkenyl or (lower alkoxycarbonyl)(lower)alkenyl,
- 54
- in which
- R13 is —Cl or —CH3,
- R14 is —COOH or —COOC2H5, and
- X is —CH2—,
- 55
- in which
- R15 is —COOH or —COOC2H5, and
- X is —CH2—, or
- 56
- in which
- R16 is lower alkyl or lower alkoxy, and
- R17 is carboxy or lower alkoxycarbonyl,
- or a prodrug thereof or a pharmaceutically acceptable salt thereof.
A compound of calim 1, wherein
- R1 is hydrogen or chloride,
- R2 is hydrogen or benzyl,
- R3 is hydrogen or methyl,
- X is bond, —CH2— or —O—, and
- Y is
- 57
- in which R6 is —OH, —COOH, —COOC2H5,
- 58
- provided that
- (i) when R6 is —OH, then X is —CH2—,
- (ii) when R6 is —COOH, then R1 is —H, or
- (iii) when R6 is —COOC2H5,
- 59
- then X is —O—,
- 60
- in which R7 is —OH, —COOH, —COOC2H5,
- 61
- and X is —CH2—,
- 62
- in which R8 is —OH, —COOH, —COOC2H5,
- 63
- provided that
- when R8 is —OH,
- 64
- then R3 is —CH3,
- 65
- and
- R10 is —COOH, —CHO, —COOCH3, —COOC2H5, —CONH2, —CONHCH3. —CONHC2H5,
- 66
- in which
- R11 is —F, —Cl or —CH3, and
- R12 is —COOH, —CHO, —COOCH3, —COOC2H5, —CONH21—CONHCH3, —CONHC2H5,
- 67
- in which
- R13 is —Cl or —CH3,
- R14 is —COOH or —COOC2H5, and
- X is —CH2—,
- 68
- in which
- R15 is —COOH or —COOC2H5, and
- X is —CH2—, or
- 69
- in which
- R16 is —CH3 or —OCH3, and
- R17 is —COOH, —COOCH3 or —COOC2H5.
Dependencies are inferred from the claim text.