摘要:
The invention relates to compounds of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl,R.sup.3 is dihalophenyl, naphthyl(lower)alkyl, phenyl(lower)alkyl substituted by one or two substituent(s) selected from the group consisting of halogen, lower alkoxy, halo(lower)alkyl and lower alkyl, or thienyl(lower)alkyl,R.sup.4 is carboxy or protected carboxy,Y is carbonyl, thiocarbonyl or sulfonyl andZ is lower alkylene, and pharmaceutically acceptable salts thereof, useful in the treatment of diabetic complications.
摘要:
The invention relates to compounds having aldose reductase-inhibitory activity of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl,R.sup.3 is phenyl(lower)alkyl which may have one or more substituent(s) selected from the group consisting of halogen, lower alkoxy, halo(lower)alkyl and lower alkyl,R.sup.4 is carboxy or protected carboxy,A is sulfur atom,Y is carbonyl, thiocarbonyl or sulfonyl andZ is lower alkylene,and pharmaceutically acceptable salts thereof, useful in treating diabetic complications.
摘要:
A compound of the formula: ##STR1## wherein R.sup.1 --A-- is a group of the formula: ##STR2## in which R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, andX is O or S, andR.sup.2 is hydrogen or lower alkyl, provided that when R.sup.1 is lower alkyl, thenR.sup.1 --A-- is a group of the formula: ##STR3## in which R.sup.1 and X are each as defined above, and pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical composition comprising the same.
摘要:
A compound of the formula: ##STR1## wherein R.sup.1 -A- is a group of the formula: ##STR2## in which R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, andX is O or S, andR.sup.2 is hydrogen or lower alkyl, provided that when R.sup.1 is lower alkyl, thenR.sup.1 -A- is a group of the formula: ##STR3## in which R.sup.1 and X are each as defined above, processes for the preparation thereof and pharmaceutical composition comprising the same.
摘要:
Oxaspiro�2,5! octanes of the formula ##STR1## inhibit angiogenesis and are particularly suitable for the treatment of solid tumors. In preferred embodiments, R.sup.1 is a carbamoyl derivative, R.sup.2 is an alkoxy substituent and R.sup.3 is ##STR2## Pharmaceutical salts of these compounds, such as methyl, amonium and organic amine salts also exhibit desirable properties.
摘要:
A compound of the formula: ##STR1## wherein R' is phenyl, phenyl which is substituted with halogen, lower alkyl, lower alkoxy, halo lower alkyl, lower alkylamino, lower alkylthio, phenoxy, carboxy, lower alkoxycarbonyl, carboxy lower alkyl, lower alkoxycarbonyl, lower alkyl, cyclo lower alkyl; lower alkyl which is substituted with carboxy or lower alkoxyoxycarbonyl; or pyrimidinyl, pyridyl or pyridyl which is substituted with lower alkyl;A is lower alkylene;n is an integer of 0 or 1;R.sup.2 is lower alkyl;R.sup.3 is hydrogen; hydroxy; halogen; halo lower alkyl; lower alkyl; lower alkylamino; lower alkanoyl amino; lower alkanoyl lower alkylamino; lower alkoxy; lower alkoxy which is substituted with phenyl, phthalimido, pyranyl, amino, carboxy, lower alkoxycarbonyl, cyclo lower alkyl or cyclo lower alkyl which is substituted with amino lower alkyl or lower alkoxycarbonylamino lower alkyl; or cyclo lower alkyloxy or cyclo lower alkyloxy which is substituted with carboxy or lower alkoxycarbonyl;R.sup.4 is hydrogen or halogen, andR.sup.5 is hydrogen or halogen, with the provisoR.sup.1 is phenyl substituted with lower alkoxy, lower alkylamino, lower alkylthio, phenoxy, carboxy, lower alkoxycarbonyl, carboxyl lower alkyl or lower alkoxycarbonyl lower alkyl; lower alkyl or lower alkyl substituted with carboxy or lower alkoxycarbonyl; pyrimidinyl; pyridyl or pyridyl substituted with lower alkyl, when R.sup.3 is hydrogen or halogen, or a pharmaceutically acceptable salt thereof. The compounds and compositions containing the same are useful in the treatment of bone diseases.
摘要:
New phospholipid derivatives represented by the formula: ##STR1## wherein R.sup.1 is alkyl, alkoxy, alkylthio, ar(lower)alkoxy or alkanoylamino; R.sup.2 is lower alkyl or ar(lower)alkyl; n is an integer of 0 or 1; A is lower alkylene; R.sup.3 is pyridinio or a group of the formula: ##STR2## in which R.sup.5, R.sup.6 and R.sup.7 are each hydrogen or lower alkyl; and R.sup.4 is hydrogen or lower alkyl; and pharmaceutically acceptable salt thereof, which exhibit anti-hypertensive activity.
摘要:
Compounds of formula (I) where R1 is hydrogen; R2 is nitro, cyano or halo(lower)alkyl; R3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R4 is a group CR6R7R8 wherein R6 and R7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R8 is hydrogen; its prodrug and a salt thereof.
摘要:
New phospholipid derivatives represented by the formula: ##STR1## wherein R.sup.1 is alkyl, alkoxy or alkanoylamino;R.sup.2 is lower alkyl, lower alkanesulfonyl or arenesulfonyl;R.sup.3, R.sup.4 and R.sup.5 are each lower alkyl;n is 0 or 1A is lower alkylene optionally interrupted by a --NHCO-- group; andQ is oxido or lower alkoxy;provided that n is 0 or A is lower alkylene interrupted by a --NHCO-- group, or Q is lower alkoxy, when R.sup.1 is alkoxy and R.sup.2 is lower alkyl; and pharmaceutically acceptable salts thereof, which exhibit antitumor activity.