摘要:
6-Substituted-1,2-benzisothiazolin-3-ones carrying an aminoalkyl group in the 2-position and being optionally substituted in the 4- and/or 5-position are antithrombotic agents. The compounds, of which 2-(2-diethylaminoethyl)-4,5-dimethyl-1,2-benzisothiazolin-3-one is a representative embodiment, can be prepared by cyclization of an appropriately substituted bis-[2-(aminoalkylcarbamyl)phenyl]disulfide, or by other disclosed methods.
摘要:
6-Substituted-1,2-benzisothiazolin-3-ones carrying an aminoalkyl group in the 2-position and being optionally substituted in the 4- and/or 5-position are antithrombotic agents. The compounds, of which 2-(2-diethylaminoethyl)-4,5-dimethyl-1,2-benzisothiazolin-3-one is a representative embodiment, can be prepared by cyclization of an appropriately substituted bis-[2-(aminoalkylcarbamyl)phenyl]disulfide, or by other disclosed methods.
摘要:
The invention provides novel antithrombotics diphenyl-disulphide-2,2'-bis-carboxylic acid amides of the general formula ##STR1## in which R.sup.1 represents a hydrogen or halogen atom or an optionally substituted alkyl, alkoxy or aralkoxy group,R.sup.2 represents a hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group, or together with R.sup.1, and adjacent carbon atoms of the benzenoid nucleus, forms an optionally substituted aliphatic or carbocyclic aromatic ring,R.sup.3 represents an optionally substituted alkyl group,A represents a single bond or an optionally substituted alkylene chain andM and n each represents 0 or a number from 1 to 5, m and n together having a value of 2-5, and acid addition salts thereof.Also included in the invention are compositions containing said antithrombotic compounds and methods for using said compounds or compositions for combating thrombo-embolic illness. In addition, the invention includes methods for the preparation of the antithrombotic compounds.
摘要:
An ether derivative of a dihydroxybenzene of the formula ##STR1## in which R.sup.1 is 1 to 3 identical or different substituents selected from hydrogen, halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto and carbalkoxy, with in each case 1 to 4 carbon atoms in the alkyl and alkoxy groups, andR.sup.2 and R.sup.3 are different and each is an alkyl or alkenyl chain in which 1 or 2 CH.sub.2 chain members are optionally replaced by O, S, CO or a phenylene group, and/or in which the chain is optionally substituted by 1 to 3 identical or different substituents selected from hydroxyl, halogen, trifluoromethyl, phenyl, carboxyl, alkyl, alkoxy, alkylmercapto, carbalkoxy, and acyl, the phenyl radical in turn optionally being substituted by halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto or carbaloxy, and the abovementioned alkyl, alkoxy and acyl groups in each case containing 1 to 4 carbon atoms, and in which at least one of the radicals R.sup.2 or R.sup.3 is substituted and/or in at least one of the radicals R.sup.2 or R.sup.3 1 or 2 chain members are replaced by 1 or 2 identical or different radicals selected from O, S, CO and phenylene, is effective in combating cardiac infarcations, angina pectoric, thromboembolic illnesses, in venous and arterial regions and arteriosclerosis.
摘要:
Benzomorphanes of the formula: ##SPC1##WhereinR is cyclopropylmethyl or cyclobutylmethyl;R.sup.1 and R.sup.2 are the same or different and each is lower alkyl;R.sup.3 is hydrogen; a straight, branched or cyclic, saturated, partially unsaturated or unsaturated aliphatic hydrocarbon unsubstituted or substituted by 1 or more substituents selected from the group consisting of lower alkoxy, lower alkoxycarbonyl, lower alkylmercapto, aryloxy, arylmercapto, arylamino, and an acid amide; an unsubstituted or substituted aromatic moiety; an unsubstituted or substituted 5-, 6- or 7-membered heterocyclic ring; lower alkylamino; di(lower alkyl)amino; arylamino; lower alkyl-arylamino; lower alkoxy; urethane; an acid amide; lower alkoxycarbonylamino; or lower alkoxycarbonyl-lower alkylamino; andA is a bivalent, straight- or branched-chain, saturated, partially unsaturated or unsaturated hydrocarbon of 2 to 10 carbon atoms, unsubstituted or substituted by phenyl or by phenyl substituted by at least 1 substituent selected from the group consisting of lower alkyl, lower alkoxy, nitro, amino and halogen,And pharmaceutically acceptable nontoxic salts thereof, are useful as analgesics.