摘要:
A basic ester having the formula ##STR1## wherein Ac is benzoyl substituted by at least two substituents selected from the group which consist of halogen atoms, lower alkyl, lower alkoxy, hydroxy, nitro and sulfamoyl, and A B are hydrogen or lower alkyl or are cycloalkyl together. The compounds are therapeutic for cardic conditions.
摘要:
The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group; orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.The compounds of the general formula (I) can preferably be used for the treatment of cardiovascular diseases.
摘要:
The invention relates to new thiazoloisoquinolines of the general formula (I), or salts thereof, ##SPC1##WhereinA stands for a group of the formula ##EQU1## R.sup.1 stands for hydrogen, hydroxy, alkoxy or aralkoxy, R.sup.2 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.3 stands for hydrogen, alkyl, aryl, nitro, carboxy or a carboxy derivative, andY stands for oxygen, sulfur, or a group of the formula =N--R.sup.4, wherein R.sup.4 stands for hydrogen, alkyl, aryl, acyl, alkylsulfonyl or arylsulfonyl.These new compounds can be used in practice as heart medicines or respiratory analeptics.The new compounds according to the invention can be prepared as follows: an isoquinoline of the general formula (II) or a salt thereof ##SPC2##WhereinR.sup.5 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.6 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.7 stands for hydrogen, alkyl, aryl, carboxy or a carboxy derivative, andX stands for hydrogen, halogen or mercapto,Is reacted with a reactive carbonic acid derivative, provided that at least one of the reactants contains a sulfur atom, and/or an isoquinoline of the general formula (III) ##SPC3##wherein R.sup.5, R.sup.6 and R.sup.7 each have the same meanings as defined above, and Y' stands for oxygen, sulfur or a group of the formula =N--R.sup. 8, wherein R.sup.8 represents hydrogen, alkyl, aryl, acyl, arylsulfonyl or alkylsulfonyl, is oxidized, and/or substituents A', R.sup.5, R.sup.6 and R.sup.7 of the obtained thiazoloisoquinoline of the general formula (IA) ##SPC4##wherein A' stands for a group of the formula ##EQU2## and R.sup.5, R.sup.6, R.sup.7 and Y' each have the same meanings as defined above, are converted into those required in the end-products.
摘要翻译:本发明涉及通式(I)的新的噻唑并喹啉或其盐,其中A代表式-SC-基团,PARALLEL Y R1代表氢,羟基,烷氧基或芳烷氧基,R2代表氢,羟基 ,烷氧基或芳烷氧基,R3代表氢,烷基,芳基,硝基,羧基或羧基衍生物,Y代表氧,硫或式= N-R4的基团,其中R4代表氢,烷基,芳基 ,酰基,烷基磺酰基或芳基磺酰基。
摘要:
The invention relates to new thiazoloisoquinolines of the formula (I), or pharmaceutically acceptable salts thereof, ##STR1## wherein R.sup.1 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.2 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.3 is hydrogen, cyano, alkyl, aryl, nitro, carboxy, carboalkoxy or carboxamido, andY is oxygen, sulfur, or a group of the formula .dbd.N--R.sup.4, wherein R.sup.4 stands for hydrogen, alkyl, aryl, acyl, alkyl-sulfonyl or arysulfonyl.These new compounds can be used in practice as heart medicines or respiratory analeptics.
摘要:
1-Cyano-2-imino-2H,4H-5,6-dihydro-8,9-dimethoxy-1,2-thiazolo(3,2a)isoquinoline or 2-imino-2H,4H-5,6-dihydro-8,9-dimethoxy-1,2-thiazolo(3,2a)isoquinoline or a pharmaceutically acceptable salt thereof. These compounds are effective as heart medicines and respiratory analeptics.
摘要:
A process is described for the preparation of 4-Methyl-5-(2-Chloroalkyl)-thiazole wherein the alkyl ranges from C.sub.2 -C.sub.5, by providing the steps of either a) converting the 3-thiocyanato-5-chloro-2-alkanone into 2-chloro-4-methyl-5-(2-chloroalkyl)-thiazole by gaseous hydrochloric acid in an organic solvent and hydrogenating the compound in the presence of a metal catalyst in an organic solvent, or b) reacting 3-thiocyanato-5-choro-2-alkanone with aqueous mineral acid and treating the thiazole obtained with a halogenating agent, and hydrogenating the 2-chloro-4-methyl-5-(2-chloroalkyl)-thiazole in an organic solvent in presence of a metal catalyst.
摘要:
The invention relates to a process for the preparation of compounds of formula (I) ##STR1## wherein R.sup.1 stands for hydrogen or the group COR.sup.2, whereinR.sup.2 stands for a straight or branched chained alkyl having 1 to 8 carbon atoms optionally substituted with phenyl, naphthyl, tetrahydronaphthyl or m-phenoxy-benzyl, cycloalkyl having 3 to 6 carbon atoms optionally substituted with one or more straight or branched chained alkyl or alkenyl having 1 to 6 carbon atoms, phenyl or naphthyl.The compounds of formula (I) are prepared according to the invention by(a) reacting esters of formula (II) ##STR2## wherein X stands for chlorine or bromine andR.sup.2 has the same meanings as defined above with a phenol alkali metal salt and(b) if desired converting the diphenyl ethers so obtained to a specific compound of formula (I), m-phenoxybenzyl alcohol by the hydrolysis of the ester group.
摘要:
Antitussive compounds of the formula I ##STR1## or physiologically acceptable acid addition salts thereof are disclosed, where A stands for straight or branched chain C.sub.1-5 alkylene or ##STR2## R.sub.1 stands for straight or branched chain C.sub.1-10 alkyl, halogenoalkyl, hydroxyalkyl, C.sub.5-6 cycloalkyl, vinyl, 2-ethoxyethyl, carbonylalkyl or aminoalkyl of the formula ##STR3## wherein R stands for hydrogen or methyl, n is 0 to 3,R.sub.2 stands for hydrogen or straight or branched chain alkyl,R.sub.3 stands for hydrogen or straight or branched chain alkyl or,R.sub.2 and R.sub.3 together with the nitrogen atom may form a 5-6 membered ring, which ring can optionally contain an oxygen or a second nitrogen atom, the latter, optionally substituted by methyl or,R.sub.1 can stand for a phenyl group of the formulaR.sub.4 R.sub.5 C.sub.6 H.sub.3 whereinR.sub.4 and R.sub.5 represent independently hydrogen, chlorine, hydroxy, methoxy, ethoxy, methyl or amino or,R.sub.1 may further stand for hydroxy, in this case the compound of the formula I may exist according to the conditions in the form of tautomers of the formula Ia ##STR4## and R.sub.1 may further stand for benzyl, 2,2-diphenylethyl or theophyllin-7-yl-methyl.
摘要:
A new process is disclosed for the preparation of a compound of the formula (VIII) ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-3 alkoxy, or trifluoromethyl;R.sup.5 is amino or C.sub.1-4 alkoxycarbonylamino; or a salt thereof, which comprises reacting a compound of the formula (II) ##STR2## with gaseous chlorine and a rhodanide of the formula (III)R--SCN (III)wherein R represents a metal ion or ammonium.
摘要:
2-(3-phenoxy-phenyl)-propionic acid or its pharmaceutical treatments, are prepared by hydrolyzing and partially decarboxylating ##STR1## wherein R=C.sub.1 -C.sub.6 alkyl or amino, the latter compounds being themselves new and, where R=C.sub.1 -C.sub.6 alkyl, have antiinflammatory pharmaceutical properties.