摘要:
The invention is directed to a new substituted derivative of .alpha.-ethylnyl-benzophenone, namely, the 3-iodo-.alpha.-ethynyl-benzhydrol which has high antifungal activity.
摘要:
The invention is a new process for the preparation of .alpha.-ethynyl-benzohydrols and of ring-substituted derivatives thereof by reacting the starting benzophenone or a ring-substituted derivative thereof with acetylene in a solvent delivering no protons, in the presence of an alkali metal tertiary alcoholate, preferably potassium-tert.-butylate or potassium-tert.-amylate. Also new substituted derivatives of .alpha.-ethynyl-benzhydrol are prepared by the invention.
摘要:
The invention relates to new aminoethoxybenzylalcohol 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;R.sub.3 and R.sub.4 stand for methyl or together with the adjacent nitrogen form an up to 8-membered ring optionally containing oxygen,and acid addition or quaternary ammonium salts thereof.The compounds of formula (I) are pharmacologically active, thus show enzyme-inducing effect. The pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
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:
New compounds of the general formula (I), ##STR1## wherein R.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl, are prepared by reacting a compound of the general formula ##STR2## wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.
摘要:
New compounds of the formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straightchained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom form a substituted or unsubstituted heterocyclic group which can contain a further oxygen or nitrogen hetero atom,But when R.sub.1 is methyl, R.sub.2 is a group other than methyl, are prepared by reacting a compound of the formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2. (iii)the new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.
摘要:
The invention relates to novel, therapeutically active 4-methylene-2-oxo-8-azaspiro[4,5]decane derivatives of the compound, ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen, C.sub.1-12 alkyl, C.sub.3-6 cycloalkyl, carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 arylC.sub.1-4 alkyl group, the latter two being optionally substituted on their aromatic moiety by one or more, same or different halogen(s) or one or more C.sub.1-4 alkyl group(s) or by one or more C.sub.1-4 alkoxy group(s);R.sup.3 and R.sup.4, which are the same or different, represent hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl group or hydroxyl group optionally esterified by a C.sub.1-4 alkanoic acid; andis 1 or 2,their isomers, solvates, hydrates, acid addition and quaternary ammonium salts.
摘要:
The invention relates to new pyridine derivatives 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,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 compounds of the formula (I) are pharmacologically active. In particular, they inhibit the microsomal monooxigenase enzyme system of the liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
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.