摘要:
The invention relates to new 2-pyridine-thiol derivatives of the formula (I), ##STR1## wherein R is hydrogen or alkyl having from 1 to 4 carbon atoms,Z is phenyl optionally substituted by one or more halogen atoms and/or alkyl groups having from 1 to 4 carbon atoms,R.sup.1 and R.sup.2 each independently represents hydrogen, alkyl having from 1 to 4 carbon atoms, alkylphenyl having from 1 to 4 carbon atoms in the alkyl moiety or an ##STR2## group, in which R has the same meaning as defined above, and the substituent ##STR3## is attached to the pyridine ring in the position 3 or 4, with the proviso that if R.sup.1 and R.sup.2 are both methyl and Z is 4-chlorophenyl, R is other than hydrogen, and acid addition salts thereof.The invention further relates to processes for the preparation of the above compounds and to pharmaceutical compositions containing them as active ingredient.The compounds are pharmaceutically active, in particular show cytoprotective activity.
摘要:
The compound N-{2-[(3-benzoyl-1-pyridyl)-thio]-ethyl}-N'-cyano-S-methyl-isothiourea and pharmaceutically acceptable acid addition salts thereof are disclosed as well as pharmaceutical compositions containing same and a method of treatment employing same. The compound or its acid addition salts are effective in treating gastric oedema and thus are useful in ulcer therapy.
摘要:
New intermediate compounds of the formula (I) are disclosed ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.4 alkyl;Z is phenyl optionally substituted by one or more halogen atoms and/or alkyl groups having 1 to 4 carbon atoms; andD is hydroxy, mesyloxy, p-tosyloxy, or halogen; or pharmaceutically acceptable acid addition salt thereof. The compounds of the Formula (I) are intermediates in the preparation of new compounds having anti-ulcer activity.
摘要:
The present invention relates to a method of treating a gastric ulcer by administering a 2-thia-zolone of the formula (I), ##STR1## wherein X stands for --CN, --CONH.sub.2, --CO.sub.2 H or --CO.sub.2 R group, wherein R is a C.sub.1-5 alkyl group; andn is 0, 1 or 2, with the proviso, that when X stands for CO.sub.2 H, CO.sub.2 R, n is other than 0.
摘要:
The present invention relates to compounds of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or nitro group;R.sub.2 means a C.sub.1-7 alkyl group optionally substituted by: a hydroxyl or oxo group; or an ester group containing 1 to 4 carbon atoms in the alkoxy moiety; or a C.sub.1-4 alkoxy, cyano, amino, C.sub.1-4 alkylamino, or dialkylamino group; or an acyl group containing 1 to 7 carbon atoms in the alkyl moiety; orR.sub.2 means an aryl-C.sub.1-7 alkyl group optionally bearing the substituents defined above for R.sub.2 in the alkyl chain and optionally substituted by halogen, nitro, C.sub.1-4 alkyl or alkoxy group in the benzene ring; orR.sub.2 represents an allyl, phenylallyl or phenylsulfonyl group, both latter groups optionally being substituted by halogen or a C.sub.1-4 alkyl group in the benzene ring; orR.sub.2 stands for a carbamoyl group substituted by one or two C.sub.1-4 alkyl group(s) or phenyl group on the nitrogen atom.The compounds according to the invention show a cytoprotective and acid secretion-inhibiting action and are effective against gastric and duodenal ulcers.
摘要:
New thiazolidine compounds of the formula (I) having anti-ulcer activity are disclosed: ##STR1## wherein Ar is a 2-furyl or a phenyl, naphthyl or pyridyl group optionally substituted by one or more C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, halo-C.sub.1-4 -alkoxy, dihalomethyl, trihalomethyl, hydroxyl or nitro groups or by a group of the formula (II), ##STR2## wherein Y is nitrogen or CH;Z is cyano or carbamoyl if Y is nitrogen, and represents a nitro group if Y is CH.Also disclosed are several processes for preparing the new compounds as well as pharmaceutical compositions and method of treatment employing same.
摘要:
The present invention relates to novel 2-thiazolidinone derivatives of the general formula (I), ##STR1## wherein A stands for hydrogen, halogen or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or nitro group; andn is 0 or 1.The compounds according to the invention show a cytoprotective and gastric acid secretion-inhibiting effect and thus, may be used in the therapy of gastric and duodenal ulcers.
摘要:
Novel acrylic acid salts of formula ##STR1## wherein R represents a hydrogen or a halogen atom, a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group,M represents a cation derived from bismuth, zinc or a pharmaceutically acceptable organic base,X represents an inorganic anion,n is an integer of from 0 to 2,m is an integer of from 1 to 3,p is 0 or 1, andr is an integer of from 0 to 6having cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.
摘要:
The invention relates to new 1,2,3,4,6,7,12,12b-octahydroindolo[2,3,-a]quinolizin-1-yl-alkanecarboxylic acid amides of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently for a hydrogen or halogen atom, or a hydroxyl, nitro or C.sub.1-4 alkoxy group;R.sub.3 and R.sub.4 stand independently for a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.5 and R.sub.6 stand independently for a hydrogen atom, C.sub.1-8 alkyl group, C.sub.3-8 alkenyl or cycloalkyl group, aryl or aralkyl group, heteroaryl or heteroaralkyl group containing oxygen, nitrogen or sulphur atom, all these groups being optionally substituted; orR.sub.5 and R.sub.6 together form an optionally substituted C.sub.2-8 .alpha.,.omega.-alkylene group, wherein one carbon atom may optionally be replaced by an oxygen or nitrogen atom; andG means a C.sub.1-4 straight chained alkylene group, as well as to their therapeutically suitable acid addition salts and pharmaceutical compositions containing these compounds. The compounds of the formula (I) have valuable therapeutic properties, namely vasodilatory, spasmolytic, antiarrhythmic and gastrocytoprotective effects. The gastrocytoprotective effect is particularly important.
摘要:
Ulcer production in animals is prevented during prolonged antiphlogistic treatment with ulcerogenic quantities of indomethacin by using it in a composition of 1 part of indomethacin to 7.5 to 25 parts, preferably 10 parts by weight of a salicylate. Indomethacin is the most potent ulcerating compound among approved non-steroid antiinflammatory agents.