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 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 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 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 fodder additives comprising a compound inducing the microsomal enzyme system of the liver, preferably a compound of the formula (I) ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are identical or different and stand for hydrogen, halogen, trihalomethyl, or alkyl or alkoxy each containing from 1 to 6 carbon atoms;R.sub.4 is phenyl, dialkylaminocarbonyl or alkoxycarbonyl having from 1 to 6 carbon atoms in the alkyl and alkoxy moieties, respectively;R.sub.5 is hydrogen or methyl, or together with R.sub.4 and the adjacent nitrogen atom forms a hetero-ring having up to 8 members;n is 1, 2, 3, 4 or 5;m is 0 or 1;a is 0 or 1,with the proviso that if a=0, R.sub.1 is trihalomethyl and R.sub.2 and R.sub.3 both are hydrogen, preferably in amount of 0.5 to 99% by weight, in an admixture with conventional carriers and/or additives and optionally at least one further active ingredient conventionally used in the animal husbandry.The enzyme inducing compounds used according to the invention accelerate the elimination of various xenobiotics metabolizing in the liver.
摘要:
The invention relates to a novel diffusion-osmotic controlled drug-release pharmaceutical composition containing a one-layer tablet core including a polymeric film-coat, a therapeutically active agent and a hydrophilic polymer; if desired, a two-layer tablet core including active agent and hydrophilic polymer in the first layer thereof and a hydrophilic polymer in the second layer thereof; at least one bore on the part of film-coat in contact with the core or core layer containing the active agent; and, if desired, containing one or more bore(s) in the part thereof in contact with the second layer containing the hydrophilic polymer, which comprises an ammonium methacrylate copolymer as coating material and hydroxypropyl-methylcellulose as hydrophilic polymer. The composition according to the invention is useful for preparing controlled drug-release tablets containing as active agents e.g. .beta.-adrenergic inhibitors (e.g. propranolol) calcium-antagonists (e.g. nifedipine), angiotensin convertase enzyme (ACE) inhibitors (e.g. captopril); prazosin; or nitroglycerol, all used in heart and circulation diseases; vasodilatory active agents (e.g. pentoxyfylline), nonsteroidal antiinflammatory agents (e.g. naproxene), analgetic drugs (e.g. morphine) and drugs acting on the central nervous system (e.g. amitriptyline, buspiron). The invention furthermore relates to a process for the preparation of the above compositions.
摘要:
The invention relates to oral solid pharmaceutical composition containing as active ingredient gemfibrozil and conventional pharmaceutical auxiliary agents comprising as surfactant bis-(2-ethyl-hexyl)-sodium-sulfosuccinate in an amount of 0.05-0.5% by weight relative to gemfibrozil content of the composition. The pharmaceutical compositions according to the present invention contain a relatively small amount of a surfactant, provide uniform dissolution of the active ingredient among the different batches and the standard deviation of the dissolution rate is low.