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US 5,308,857 AGranted
Furylthiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsHisashi Takasugi, Yousuke Katsura, Yoshikazu Inoue, Tetsuo Tomishi
Life of this patent
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Abstract
The invention relates to compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and Q are as described, useful in the treatment of ulcers.
Claims8
A compound of the formula:
- ##STR123## wherein R.sup.1 and R.sup.2 are each hydrogen, furoyl or lower alkyl which may have halogen;
- or
- R.sup.1 and R.sup.2 are linked together to form lower alkylene,
- R.sup.3 is hydrogen or lower alkyl,
- R.sup.4 is amino, carbamoyl, aminocarbamoyl, guanidinocarbamoyl, lower alkylcarbamoyl, sulfamoylaminocarbonyl, lower alkoxycarbonyl, ureido, thioureidosulfamoylamino, lower alkanoylamino, lower alkoxycarbonylamino, lower alkylsulfonylamino, lower alkoxy(lower)alkanoylamino, protected hydroxy(lower)alkanoylamino, lower alkylthio(lower)alkanoylamino, C.sub.6 -C.sub.10 aroylamino optionally substituted by nitro, furoylamino, thenoylamino, nicrotinoylamino, 1-oxonicotinoylamino, morpholinocarbonylamino, lower alkylureido, lower alkylthioureido, lower alkanoylureido, lower alkenylureido, C.sub.6 -C.sub.10 aroylthioureido, furyl(lower)alkylthio(lower)alkanoylamino, furyl(lower)alkylsulfinyl(lower)alkanoylamino, mono or di (lower)-alkylsulfamoylamino, hydroxy(lower)alkylureido, lower alkylisothioureido, thiazolylamino substituted with lower alkyl, triazolylamino substituted with amino, triazolylamino substituted with amino and lower alkyl, benzoisothiazolylamino substituted with oxo, benzothiadiazinylamino substituted with oxo and halogen, pyrimidinyl substituted with oxo and lower alkyl, triazolyl substituted with amino, or a group of the formula:
- ##STR124## wherein n is 0 or 1,
- X is .dbd.CH-- or .dbd.N--,
- R.sup.5 is hydrogen, cyano, nitro, carbamoyl, lower alkoxycarbonyl, sulfamoyl, lower alkylsulfonyl, C.sub.6 -C.sub.10 arenesulfonyl, which is substituted with one or more substituent(s) selected from lower alkyl, lower alkoxy, halogen and amino, or mono or di(lower)alkylsulfamoyl,
- R.sup.6 is hydrogen, lower alkyl, lower alkylthio, lower alkoxy, amino, mono or di(lower)alkylamino, lower alkenylamino, lower alkynylamino, hydroxy(lower)alkylamino, lower alkoxy(lower)alkylamino, or mono or di(lower)alkylamino(lower)alkylamino;
- A is lower alkylene or --CONH--;
- or
- A--R.sup.4 is imidazolyl substituted with lower alkyl or triazolyl substituted with amino, and
- Q is hydrogen or lower alkyl.
10 more elements
A compound of claim 1, wherein
- R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or trihalo(lower)alkyl;
- or
- R.sup.1 and R.sup.2 are linked together to form lower alkylene,
- R.sup.4 is amino, carbamoyl, aminocarbamoyl, guanidinocarbamoyl, lower alkylcarbamoyl, sulfamoylaminocarbonyl, lower alkoxycarbonyl, ureido, thioureido, sulfamoylamino, lower alkanoylamino, lower alkoxycarbonylamino, lower alkylsulfonylamino, lower alkoxy(lower)alkanoylamino, lower alkanoyloxy(lower)alkanoylamino, lower alkylthio(lower)alkanoyloamino, nitrobenzoylamino, furoylamino, thenoylamino, nicotinoylamino, 1-oxonicotinoylamino, morpholinocarbonylamino, 3-lower alkylureido, 3-lower alkylthioureido, 3-lower alkanoylureido, 3-lower alkenylureido, 3-benzoylthioureido, furyl(lower)alkylthio(lower)alkanoylamino, furyl(lower)alkylsulfinyl(lower)alkanoylamino, mono or di(lower)alkylsulfamoylamino, 3-hydroxy(lower)alkylureido, 3-lower alkanoyloxy(lower)alkylureido, 2-lower alkylisothioureido, thiazolylamino substituted with lower alkyl, triazolylamino substuted with amino, triazolylamino substituted with amino and lower alkyl, benzoisothiazolylami8no substituted with oxo, benzothiadiazinylamino substituted with oxo and halogen, pyrimidinyl substituted with oxo and lower alkyl, triazolyl substituted with amino, or a group of the formula:
- ##STR125## wherein n, X and R.sup.6 are as defined in claim 2,
- R.sup.5 is hydrogen, cyano, nitro, carbamoyl, lower alkoxycarbonyl, sulfamoyl, lower alkylsulfonyl, phenylsulfonyl substituted with lower alkyl, phenylsulfonyl substituted with lower alkoxy, phenylsulfonyl substituted with halogen, phenylsulfonyl substituted with amino, mono or di(lower)alkylsulfamoyl,
- A is as defined in claim 2;
- or
- A--R.sup.4 is as defined in claim 2, and
- R.sup.3 and Q are each as defined in claim 2.
7 more elements
Dependencies are inferred from the claim text.