Spirobenzofuranone compounds
AssigneeTakeda Chemical Industries, Ltd.
InventorsHirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada
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AssigneeTakeda Chemical Industries, Ltd.
InventorsHirosada Sugihara, Masazumi Watanabe, Mitsuru Kawada, Isuke Imada
Estimating the term…
Novel spiro compounds of the formula: ##STR1## wherein Ring A represents a benzene ring or a naphthalene ring, said rings being unsubstituted or substituted by at least one of lower alkyl, nitro, halogen, amino which may optionally be substituted, hydroxyl which may optionally be substituted, acyl, sulfamoyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may optionally be substituted, ureido which may optionally be substituted, thioureido which may optionally be substituted, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminomethyl which may optionally be substituted, cyano and phenyl, have gastric secretion inhibitive, anti-inflammatory and analgesic activities, and are of value as drugs.
A compound of the formula ##STR18## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1-6 alkyl, nitro, halogen, hydroxyl, C.sub.1-6 alkoxy, mono- or di-C.sub.1-4 alkylamino-C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkyloxy, C.sub.2-6 alkanoyloxy, benzoyloxy, C.sub.2-6 alkanoyl, benzoyl, sulfamoyl, carboxyl, C.sub.2-6 alkoxycarbonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylamino-C.sub.1-4 alkylcarbamoyl, N-C.sub.1-4 alkylpyrrolidinyl-C.sub.1-4 alkylcarbamoyl, ureido, C.sub.1-4 alkylureido, thioureido, C.sub.1-4 alkylthioureido, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, aminomethyl, mono- or di-C.sub.1-4 alkylaminomethyl, cyano, phenyl, amino, mono- or bis-(.beta.-hydroxyethyl)amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.2-4 alkanoylamino, C.sub.1-4 alkanesulfonylamino, 1-pyrrolidinyl, piperidino, a 1-piperazinyl group, or morpholino, said 1-piperazinyl group being unsubstituted or substituted at the nitrogen atom of its 4-position by C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, or
A compound of the formula ##STR19## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1-6 alkyl, nitro, halogen, hydroxyl, C.sub.1-6 alkoxy, mono- or di-C.sub.1-4 alkylamino-C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkyloxy, C.sub.2-6 alkanoyloxy, benzoyloxy, C.sub.2-6 alkanoyl, benzoyl, sulfamoyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.2-4 alkanoylamino, C.sub.1-4 alkanesulfonylamino, 1-pyrrolidinyl, piperidino, a 1-piperazinyl group, or morpholino, said 1-piperazinyl group being unsubstituted or substituted at the nitrogen atom of its 4-position by C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, or
A compound of the formula ##STR20## wherein R.sup.1' is di-C.sub.1-4 alkylamino, or a pharmaceutically acceptable salt thereof.
A compound of the formula ##STR21## wherein R.sup.1" is C.sub.2-6 alkanoyl.
A pharmaceutical composition for managing peptic ulcer which comprises, as an active ingredient, an effective amount of a compound of the formula ##STR22## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1-6 alkyl, nitro, halogen, hydroxyl, C.sub.1-6 alkoxy, mono- or di-C.sub.1-4 alkylamino-C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkyloxy, C.sub.2-6 alkanoyloxy, benzoyloxy, C.sub.2-6 alkanoyl, benzoyl, sulfamoyl, carboxyl, C.sub.2-6 alkoxycarbonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylamino-C.sub.1-4 alkylcarbamoyl, N-C.sub.1-4 alkylpyrrolidinyl-C.sub.1-4 alkylcarbamoyl, ureido, C.sub.1-4 alkylureido, thioureido, C.sub.1-4 alkylthioureido, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, aminomethyl, mono- or di-C.sub.1-4 alkylaminomethyl, cyano, phenyl, amino, mono- or bis-(.beta.-hydroxyethyl)amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.2-4 alkanoylamino, C.sub.1-4 alkanesulfonylamino, 1-pyrrolidinyl, piperidino, a 1-piperazinyl group, or morpholino, said 1-piperazinyl group being unsubstituted or substituted at the nitrogen atom of its 4-position by C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, or
A pharmaceutical composition for managing peptic ulcer which comprises, as an active ingredient, an effective amount of a compound of the formula ##STR23## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently hydrogen, C.sub.1-6 alkyl, nitro, halogen, hydroxyl, C.sub.1-6 alkoxy, mono- or di-C.sub.1-4 alkylamino-C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkyloxy, C.sub.2-6 alkanoyloxy, benzoyloxy, C.sub.2-6 alkanoyl, benzoyl, sulfamoyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.2-4 alkanoylamino, C.sub.1-4 alkanesulfonylamino, 1-pyrrolidinyl, piperidino, a 1-piperazinyl group, or morpholino, said 1-piperazinyl group being unsubstituted or substituted at the nitrogen atom of its 4-position by C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, or
A method of managing peptic ulcer in a patient which comprises administering to said patient a compound of the formula ##STR24## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1-6 alkyl, nitro, halogen, hydroxyl, C.sub.1-6 alkoxy, mono- or di-C.sub.1-4 alkylamino-C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkyloxy, C.sub.2-6 alkanoyloxy, benzoyloxy, C.sub.2-6 alkanoyl, benzoyl, sulfamoyl, carboxyl, C.sub.2-6 alkoxycarbonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylamino-C.sub.1-4 alkylcarbamoyl, N-C.sub.1-4 alkylpyrrolidinyl-C.sub.1-4 alkylcarbamoyl, ureido, C.sub.1-4 alkylureido, thioureido, C.sub.1-4 alkylthioureido, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, aminomethyl, mono- or di-C.sub.1-4 alkylaminomethyl, cyano, phenyl, amino, mono- or bis-(.beta.-hydroxyethyl)amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.2-4 alkanoylamino, C.sub.1-4 alkanesulfonylamino, 1-pyrrolidinyl, piperidino, a 1-piperazinyl group, or morpholino, said 1-piperazinyl group being unsubstituted or substituted at the nitrogen atoms of its 4-position by C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, or
A method of managing peptic ulcer in a patient which comprises administering to said patient a compound of the formula ##STR25## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1-6 alkyl, nitro, halogen, hydroxyl, C.sub.1-6 alkoxy, mono- or di-C.sub.1-4 alkylamino-C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkyloxy, C.sub.2-6 alkanoyloxy, benzoyloxy, C.sub.2-6 alkanoyl, benzoyl, sulfamoyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.2-4 alkanoylamino, C.sub.1-4 alkanesulfonylamino, 1-pyrrolidinyl, piperidino, a 1-piperazinyl group, or morpholino, said 1-piperazinyl group being unsubstituted or substituted at the nitrogen atom of its 4-position by C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, or
A method of managing peptic ulcer in a patient which comprises administering to said patient a compound of the formula ##STR26## wherein R.sup.1' is di-C.sub.1-4 alkylamino, or a pharmaceutically acceptable salt thereof, said compound or salt being administered in an amount effective to manage peptic ulcer in said patient.
A method of managing peptic ulcer in a patient which comprises administering to said patient a compound of the formula ##STR27## wherein R.sup.1" is C.sub.2-6 alkanoyl, said compound being administered in an amount effective to manage peptic ulcer in said patient.
Dependencies are inferred from the claim text.