摘要:
Pharmaceutical preparations having an antiphlogistic action are described. The preparations contain, as active ingredient, a benzazole derivative corresponding to the general tautomeric formulae I ##STR1## wherein X represents a sulphur or oxygen atom and R.sup.1 represents a hydrogen atom and R.sup.2 a hydroxymethyl, formyl, lower carbalkoxy or lower acyl group or R.sup.1 and R.sup.2 together represent the group ##STR2## wherein R.sup.3 and R.sup.4 denote, independently of one another, a hydrogen atom or a C.sub.1 -C.sub.6 -alkyl group, or they contain a physiologically acceptable salt thereof. These pharmaceutical preparations are suitable in particular for the treatment of inflammatory conditions and for inhibiting the lipoxygenase and/or cyclooxygenase route of arachidonic acid metabolism.
摘要:
Thiomethylpyridine derivatives having bronchosecretolytic and mucolytic activity according to the formula: ##STR1## wherein R is a group attached in the 2-, 3- or 4-position of the pyridine ring which corresponds to the following general formula:Q--S--CH.sub.2 -- (II)wherein Q is a substituted or unsubstituted aryl group or a 5- or 6-membered heterocyclic group which may optionally contain one or more substituents and/or which may be condensed with an optionally substituted phenyl group or with an optionally substituted heterocycle; R' is a lower alkyl group, a halogen atom or an aminoalkyl group; and n is 0 or an integer of from 1 to 4; and the therapeutically-acceptable acid addition salts thereof.The new compounds are distinguished by surprising activity compared with known compounds, such as "Ambroxol".
摘要:
Thiomethylpyridine derivatives having bronchosecretolytic and mucolytic activity according to the formula: ##STR1## wherein R is a group attached in the 2-, 3- or 4-position of the pyridine ring which corresponds to the following general formula:Q--S--CH.sub.2 -- (II) wherein Q is a substituted or unsubstituted aryl group or a 5- or 6-membered heterocyclic group which may optionally contain one or more substituents and/or which may be condensed with an optionally substituted phenyl group or with an optionally substituted heterocycle;R' is a lower alkyl group, a halogen atom or an aminoalkyl group; andn is 0 or an integer of from 1 to 4;and the therapeutically-acceptable acid addition salts thereof.The new compounds are distinguished by surprising activity compared with known compounds, such as "Ambroxol".
摘要:
Benzothiazole derivatives corresponding to the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent, independently of one another, a hydrogen atom, a halogen atom, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group, R.sup.5 represents a hydrogen atom or a linear C.sub.1 -C.sub.3 -alkyl group, R.sup.6 represents a hydrogen atom, and R.sup.7 represents a formyl group, a carbalkoxy group of the formula ##STR2## wherein R.sup.8 denotes a linear or branch chained C.sub.1 -C.sub.4 -alkyl group, or it represents an acyl group of the formula ##STR3## wherein R.sup.9 denotes a linear C.sub.1 -C.sub.3 -alkyl group, or R.sup.6 and R.sup.7 together represent the group ##STR4## wherein R.sup.10 and R.sup.11 represent, independently of one another, a hydrogen atom or a linear C.sub.1 -C.sub.6 -alkyl group or R.sup.6 and R.sup.7 represent the group ##STR5## wherein R.sup.12 and R.sup.13 represent, independently of one another, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group or R.sup.6 and R.sup.7 represent the group ##STR6## wherein R.sup.14 denotes a linear C.sub.1 -C.sub.3 -alkyl group, as well as the physiologically acceptable salts thereof, a process for the preparation of these compounds, and a pharmaceutical preparation containing them, are described.
摘要:
New dihydropryidazinone derivatives corresponding to the following formula ##STR1## and a process for their preparation and pharmaceutical preparations containing these compounds are described. These compounds are effective positively inotropic substances with an improved therapeutic profile.
摘要:
The invention relates to pyrimidine-thioalkyl pyridine derivatives corresponding to the following general formula ##STR1## in which R.sub.1 to R.sub.4, independently of one another, represent hydrogen, lower alkyl, halogen, amino or hydroxy groups, R.sub.5 represents a free electron pair or a lower alkyl group, a halogen atom, m has the value 0 or 1, the pyrimidine-thioalkyl group being bonded in the 2-, 3- or 4-position of the pyridine ring, and to therapeutically compatible acid addition salts thereof. The invention also relates to a process for producing the new pyrimidine-thioalkyl pyridine derivatives and to medicaments containing these compounds.
摘要:
The invention relates to new 1,4-piperazine compounds corresponding to the following general formula ##STR1## which show improved antimycotic activity in relation to the known compounds miconazol and ketoconazol.
摘要:
New compounds which act on the cardiac circulation and correspond to the general formula ##STR1## and may be used for the treatment of cardiac diseases, in certain forms of hypertension and in diseases of arterial occlusion are described.Methods of preparation for these compounds and medicaments containing these compounds are also described.
摘要:
New benzimidazoles corresponding to the general formula I ##STR1## are described, in which the pyridazinone ring is attached in the 5- or 6- position of the benzimidazole ring and R.sup.1 denotes a hydrogen atom or a straight chained or branched C.sub.1 to C.sub.4 alkyl group, R.sup.2 denotes a hydrogen atom, a straight chained or branched C.sub.1 to C.sub.4 alkyl group, a C.sub.1 to C.sub.4 alkoxy group, a hydroxy group, a halogen atom, an amino group or a nitro group, A denotes a hydrogen atom, a group of the formula ##STR2## wherein R.sup.3 denotes a hydrogen atom, an optionally substituted C.sub.1 to C.sub.4 alkyl group or a C.sub.1 to C.sub.4 alkoxy group and B denotes a cyano group, a benzoyl group or a phenylsulphonyl group, or A denotes a group of the formula ##STR3## in which m has the value of 2 or 3 and n represents an integer from 1 to 6, and the physiologically acceptable salts thereof as well as processes for their preparation and pharmaceutical preparations containing these compounds. These compounds are new, effective, positive inotropic substances which do not act by the mechanism of phosphodiesterase inhibition.
摘要:
New guanidine carboxylic acid esters corresponding to the general formula I ##STR1## and a process for the preparation of these compounds are described. The compounds according to the invention are H.sub.2 -agonists optionally having an additional H.sub.1 -antagonistic component. They are distinguished by their improved oral activity. The use of the above-mentioned guanidine carboxylic acid esters and of pharmaceutical preparations containing these esters is also described.