摘要:
The invention relates to a new crystal modification of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine (cimetidine), a histamine H-2 receptor antagonist having the Formula (I) ##STR1## as well as to a process for preparing same. In the description, this new modification is named N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine Z (cimetidine Z).
摘要:
The invention relates to the new monohydrate of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine (cimetidine), a histamine-H.sub.2 receptor antagonist which is called N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine H (cimetidine H) as well as to a process for the preparation of same, which comprises pouring a hot, homogeneous aqueous solution of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine, optionally containing also methylamine, onto ice and separating the N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine monohydrate.
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:
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:
The invention relates to new propionamidine derivatives of formula (I) ##STR1## wherein X is halogen,and to a process for their preparation. According to the invention compounds of the formula (I) are prepared by reacting a 3-halopropionitrile of the formula (III) ##STR2## wherein X is as defined above,with sulfamide of the formula (II) ##STR3## in the presence of a hydrogen halide. Compounds of the formula (I) are useful intermediates in the preparation of famotidine.
摘要:
The invention relates to a new process for the preparation of N-sulfamyl-3-(2-guanidinothiazol-4-yl-methylthio)-propionitrile (famotidine) of the formula (I) ##STR1## by S-alkylation of 2-guanidino-thiazol-4-yl-methanethiol obtained from S-(2-guanidino-thiazol-4-yl-methyl)-isothiourea dihydrochloride of the formula (III) ##STR2## by in situ treatment with a base, which comprises carrying out S-alkylation with a N-sulfamyl-3-halopropionamidine of the formula (II) ##STR3## wherein X stands for halogen.
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 invention relates to fused heterocyclic compounds with ring junction nitrogen atom of the formula: ##STR1## wherein Q stands for 2-indolizinyl, 2-imidazo[1,2-a]pyridinyl, 2-imidazo[1,2-a]pyrimidinyl, 6-(2,3-dihydroimidazo[2,1-b]thiazol)-yl or 6-imidazo[2,1-b]thiazolyl group; and n is an integer from 2 to 4, as well as therapeutically useful salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions. The compounds of formula (I) exhibit mainly antipsychotic effects so the invention relates also to a method of treatment of schizophrenia, organic mental disorders, affective disorders, anxiety and personality disorders.
摘要:
The present invention relates to novel compounds of the general formula (I) ##STR1## wherein R means hydrogen or C.sub.1-4 alkyl group; andY stands for cyano, trifluoromethyl, aryloxy or aryl(C.sub.1-4 alkyl)oxy group.The compounds according to the invention show a gastric acid secretion-inhibiting effect and therefore, they are useful for the treatment of gastric and duodenal ulcers. In addition, they exert a cytoprotective action against gastric laesions induced, e.g. by indomethacin or acid-containing alcohol.
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.