摘要:
A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms of a decahydroquinoline of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and akyl of 1 to 5 carbon atoms, A is selected from the group consisting of --(CH.sub.2).sub.n --, --CH.sub.2 O-- and alkylene substituted with alkyl having a total of 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthyl, optionally substituted indenyl, optionally substituted heteromonocycle of 5 to 6 members and optionally substituted heterobicycle with the proviso that when Z is o-alkoxy-phenyl, A is not --(CH.sub.2).sub.n -- in which n is O, and their non-toxic, pharmaceutically acceptable acid addition salts and their quaternary ammonium salts and intermediates having analgesic, diuretic, hypotensive, anti-arrithmic and anti-cerebral-ischaemic properties.
摘要:
A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## or, if appropriate, its tautomer ##STR4## and ##STR5## or E is --COOR.sub.3 and G is ##STR6## wherein A, Y, R, Ra, R.sub.1 and R.sub.2 are as defined in the specification.
摘要:
A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## wherein A, R, R.sub.1, R.sub.2 and Y are as defined in the specification.
摘要:
A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## wherein, A is a cycloalkyl of 3-6 carbon optionally substituted, R, R.sub.1, R.sub.2 and Y are defined in the specification.
摘要:
Novel indanes in all possible stereoisomer forms of the formula ##STR1## wherein the substrates are as defined in the application and their non-toxic, pharmaceutically acceptable acid addition salts and their hydrates are disclosed as having central analgesic properties as well as antiarrhythmic and diuretic activities.
摘要:
A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms of a decahydroquinoline of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, A is selected from the group consisting of --(CH.sub.2).sub.n --, --CH.sub.2 O-- and alkylene substituted with alkyl having a total of 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthyl, optionally substituted indenyl, optionally substituted heteromonocycle of 5 to 6 members and optionally substituted hetero-bicycle with the proviso that when Z is o-alkoxy-phenyl, A is not --(CH.sub.2).sub.n -- in which n is O, and their non-toxic, pharmaceutically acceptable acid addition salts and their quaternary ammonium salts and intermediates having analgesic, diuretic, hypotensive, anti-arrithmic and anti-cerebral-ischaemic properties.
摘要:
A compound selected from the group consisting of optical isomers and racemates of 4-hydroxy-3-quinoline carboxylates of the formula ##STR1## wherein X is in the 5-, 6-, 7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --SCF.sub.3 and --OCF.sub.3, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl and phenyl substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen, A is either ##STR2## in which R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.5 is selected from the group consisting of aryl of 6 to 14 carbon atoms, heteroaryl of 3 to 14 carbon atoms, alkyl of 1 to 14 carbon atoms, alkyl substituted with --NH.sub.2, --NHAlk or ##STR3## alkenyl of 2 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms substituted with aryl of 6 to 14 carbon atoms, Alk and Alk' are alkyl of 1 to 6 carbon atoms or, when R.sub.1 is hydrogen, A is ##STR4## and R.sub.3a are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aryl and ##STR5## or R.sub.2a and R.sub.3a together form acetonide, R.sub.4a is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.5a is selected from the group consisting of alkyl of 1 to 4 carbon atoms and aryl with the proviso that when X is 8--CF.sub.3, R.sub.1 and R.sub.3 are hydrogen, R.sub.2 is 2-thiazolyl, R.sub.4 is methyl, R.sub.5 is not methyl and their non-toxic, pharmaceutically acceptable salts with acids or bases having analgesic and anti-inflammatory activity.
摘要:
Novel thiophene-acetic acid derivatives of the formulae ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of lower alkyl of 1 to 4 carbon atoms and hydrogen and R.sub.2 is selected from the group consisting of hydrogen, lower alkyl of 1 to 7 carbon atoms and optionally substituted with at least one hydroxy group or an oxygen atoms-containing heterocycle,di-lower alkylamino-lower alkyl, N-heterocyclic alkyl, alkali metals, alkaline earth metals, aluminum and --H,NH (lower alkyl).sub.2 and Ar is selected from the group consisting of phenyl, optionally substituted with at least one member of the group consisting of halogen, trihalogenomethyl, lower alkyl, lower alkoxy and carboxyl, cyclohexyl, thienyl, furyl, tetrahydrofuryl and pyridyl, and in formula II, ArCO is attached to one of the positions .alpha. to the sulfur atom, which compounds have analgesic and anti-inflammatory activity and their preparations.
摘要:
Hypolipemiant compositions comprising an effective amount of at least one 2-alkyl-5-thiazole-carboxylic acid derivative of the formula ##STR1## wherein R is hydrogen, an alkali metal, ammonium, the monovalent residue of an organic base or a substituted or unsubstituted alkyl and where R'.sub.1 is a linear alkyl of 1 to 12 carbon atoms, and a major amount of a pharmaceutical carrier; as well as the method of reducing the amount of sanguine lipids in warm-blooded animals utilizing the above-hypolipemiant compositions.
摘要:
A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula wherein the substituents are defined as in the application having a strong affinity for optical receptors, central analgesic, diuretic, anti-arrythmic, hypotensive and cerebral anti-ischemic activity.