摘要:
A compound of the formula: ##STR1## wherein Z is ethyl or vinyl,R.sub.1 and R.sub.2 are hydrogen, lower alkyl, lower alkenyl or trihalomethyl,R.sub.3 and R.sub.4 are hydrogen, lower alkyl, lower alkenyl, trihalomethyl, cyclopentyl, benzyl or phenyl, andR.sub.5 is lower alkyl, lower alkenyl, trihalomethyl, cyclopentyl, benzyl, or phenyl with the proviso that where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each is hydrogen, R.sub.5 is not methyl attached to the 4-position of the benzene ring, or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof is disclosed as effective in the regulation of the liver microsomal enzyme system.
摘要:
The invention relates to new .alpha.-substituted benzhydrols and pharmaceutically acceptable acid addition salts or quaternary ammonium salts thereof with enzyme promoting or inhibiting effects;
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:
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 new 1,1-diphenylpropan-1-ol 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,R.sub.3 is halogen, trihalomethyl, alkyl having from one to 5 carbon atoms or alkoxy having from one to 5 carbon atoms,R.sub.4 is phenyl optionally substituted by one or more identical or different substituents selected from the group of halogen, trihalomethyl, alkyl, alkoxy, cyano, nitro, amino, alkylamino, dialkylamino, hydroxyl, carboxyl or substituted carboxyl; dialkylaminocarbonyl or alkoxycarbonyl containing from one to 4 carbon atoms in the alkyl and alkoxy moieties, respectively,n is 1, 2, 3, 4, or 5.According to another aspect of the invention there are provided processes for the preparation of the compounds of formula (I).The new compounds induce the polysubstrate monooxigenase enzyme system of liver and are devoid from other pharmacodinamic effects. Pharmaceutical compositions containing compounds of the formula (I) as active ingredient are also within the scope of the invention.
摘要:
The invention relates to new piperidine derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms; andR.sub.2 is hydrogen or alkyl 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 benzhydrylpiperazine derivatives of the formula (I) ##STR1## wherein n is 2 or 3, and acid addition 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. More particularly, they inhibit the microsomal monooxigenase enzyme system of liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
摘要:
.alpha.-ethynyl-benzhydrols, namely 2,5-dimethyl-.alpha.-ethynyl and 4-n-butyl-.alpha.-ethynyl benzhydrol, are made by reacting the starting benzophenone with acetylene in a solvent delivering no protons, in the presence of an alkali metal tertiary alcoholate, preferably potassium-ter.-butylate or potassium-tert.-amylate.
摘要:
New compounds of the general formula (I) ##SPC1##whereinR.sub.1 and R.sub.2 each is 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 substituted or unsubstituted heterocyclic group with or without a further oxygen or nitrogen heteroatom, andR.sub.3 is hydrogen or an acyl group derived from a C.sub.1.sub.-18 carboxylic acid.The compounds are prepared by reducing the corresponding nitro compounds of the general formula (II) ##SPC2##and optionally acylating the obtained product.The compounds of the general formula (I) and their acid addition salts and quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess valuable antipyretic activity and a yohimbine lethality increasing effect characteristic of antidepressants.