摘要:
Novel, therapeutically active 21-aminosteroids of formula (I) ##STR1## with pregnane skeleton, are disclosed wherein two of X, Y and Z are a nitrogen atom each and the third one is a methine group; R.sup.1 and R.sup.2 are independently from each other, a primary amino group bearing as substituent a branched-chain C.sub.4-8 alkyl -alkenyl or -alkynyl group, or a C.sub.4-10 cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by at least one C.sub.1-3 alkyl group; or R.sup.1 and R.sup.2 are each a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as additional heteroatom; or one of R.sup.1 and R.sup.2 is an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by at least one C.sub.1-4 alkyl group; and n is 1 or 2, as well as their acid addition salts and pharmaceutical compositions containing these compounds.
摘要:
The invention relates to novel eburnamenine derivatives of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 as well as R.sup.3 and R.sup.4, independently from each other, stand for hydrogen, C.sub.2-6 alkyl group, C.sub.2-6 alkenyl group; or a C.sub.3-10 alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means .alpha.-/.alpha.-, .alpha.-/.beta.- or .beta.-/.alpha.- steric position, as well as their acid addition salts and solvates. The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for preparing the compounds of formula (I). The compounds of formula (I) possess antioxidant effect and therefore, they are useful for inhibiting the peroxidation of lipids occurring in mammals (including human).
摘要:
The invention relates to new 4-hydroxy-benzhydrols of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms, with the proviso that if R.sub.1 is hydrogen, R.sub.2 is other than hydrogen or a 3-trifluoromethyl group, or if R.sub.1 is a 2-methyl group, R.sub.2 is other than a 5-methyl group.According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. In particular, they are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them as active ingredients are also within the scope of the invention.
摘要:
The invention relates to the preparation of new diethylaminoalkoxybenzhydrol derivatives of the formula (I) ##STR1## wherein R.sub.1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms,R.sub.2 is halogen, trihalomethyl, or alkoxy having from one to 4 carbon atoms, andn is 1, 2, 3 or 4,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention, there are provided new compounds of the formula (I), and acid addition and quaternary salts thereof. The compounds can be used for the treatment of acute ethanolic intoxication and depression syndromes. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
摘要:
The invention relates to the preparation of 3-trifluoromethyl- and 2,5-dimethyl-4'-hydroxy-.alpha.-ethyl-benzhydrol. Both compounds have so far been described only as metabolites of corresponding benzhydrol derivatives containing no hydroxyl group. Neither their physico-chemical characteristics nor their manufacturing processes have been disclosed in the known publications.3-Trifluoromethyl- and 2,5-dimethyl-4'-hydroxy-.alpha.-ethyl-benzhydrol are suitable for the treatment of acute ethanolic intoxication. Accordingly, another aspect of the invention is a pharmaceutical composition containing one of these compounds as active ingredient.
摘要:
The invention relates to new aminopropanol derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkoxy having from one to 3 carbon atoms or alkyl having from one to 3 carbon atoms,R.sub.2 is alkyl having from one to 3 carbon atoms, andR.sub.3 is cycloalkyl having from 3 to 6 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen they are attached to form an up to 8 membered ring optionally containing oxygen or a further nitrogen as an additional hetero atom, and optionally substituted with alkyl having from one to 4 carbon atoms or benzyl,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them are also within the scope of the invention.
摘要:
The invention relates to new dialkylaminoalkoxybenzylalcohol derivatives of the formula (I) ##STR1## wherein R.sub.1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms;R.sub.2 is halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms;R.sub.3 and R.sub.4 independently stand for an alkyl group having from 3 to 5 carbon atoms; andn is 2, 3, 4 or 5,and acid addition and quanernary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds provided by the invention are pharmaceutically active, in particular, they are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them as active ingredient are another aspect of the invention.
摘要:
The invention relates to new resorcin derivatives of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, trihalomethyl, alkyl having from one to 3 carbon atoms or alkoxy having from one to 3 carbon atoms.According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. In particular, they are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
摘要:
The invention relates to an apparatus for supplying high-power electric loads operated in a pulse-like manner, particularly to X-ray equipment.The apparatus makes use of the mechanical energy of rotation of a flywheel rotated through a time period which is substantially longer than the pulse duration of the load by a driving power being substantially smaller than the pulse power of the load to generate a supply voltage for the load in expense of this mechanical energy. The driving period of the flywheel and the associated moderate driving power provide an energy balance with the short pulses with high power consumption. The apparatus comprises a generator unit with at least one electric rotary machine which has a rotor that rotates together with the flywheel. The excitation of the rotary machine is provided by a field power supply being controlled by a control unit. The control unit controls the excitation of the generator unit to provide predetermined output voltage and current levels for the load.The apparatus according to the invention can provide a specified operation control for the load.According to an aspect of the invention a method has been provided for carrying out fluorography which can see to an increased sensed light intensity. According to this method fluoroscopy is carried out by pulsed X-ray irradiation with small average intensity and high pulse intensity, in which the repetition frequency of the pulse is high enough to provide for a continuous light sensation. Such pulsed irradiation provides for an image on the fluoroscopic screen in which the sensed light intensity is increased by the ratio of the peak and average radiation intensities compared to the light intensity of a conventional continuous irradiation with the average intensity.