摘要:
Indoles of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, --CF.sub.3, alkyl of 1 to 8 carbon atoms and alkoxy of 1 to 8 carbon atoms, R.sub.2 is in the 2,3 or 4 position and is selected from the group consisting of halogen, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 8 carbon atoms, A is selected from the group consisting of branched alkylene of 3 to 5 carbon atoms and --(CH.sub.2).sub.n -- and n is a number of 2 to 5 and R.sub.3 and R.sub.4 are alkyl of 1 to 8 carbon atoms or taken together with the nitrogen atom form a heterocyclic ring selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, piperazinyl and N-alkyl piperazinyl with 1 to 4 alkyl carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and their preparation.
摘要:
Novel 3-(4-quinolylamino)-2-thiophene-carboxylates of the formula ##STR1## wherein X is in the 6, 7 or 8-position and is selected from the group consisting of hydrogen, halogen, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms, n is 2, 3, 4 or 5, Y is in the 2, 3 or 4-position and is selected from the group consisting of hydrogen, halogen, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and process and intermediates for their preparation.
摘要:
Novel 3-quinoline-carboxamides of the formula ##SPC1##Wherein R is selected from the group consisting of halogen, --CF.sub.3, --OCF.sub.3 and --SCF.sub.3 in the 7- or 8-position, R.sub.1 is selected from the group consisting of hydrogen and acyl of an aliphatic carboxylic acid of 2 to 4 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of thiazloyl, pyridinyl and oxazolyl and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and their preparation and novel intermediates.
摘要:
A method of inducing immunostimulating activity in warm-blooded animals comprising administering to warm-blooded animals an immunostimulating amount of at least one maleo-pimaric acid compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 together with the nitrogen to which they are attached form an optionally substituted saturated heterocycle optionally containing at least one other heteroatom, Y is selected from the group consisting of hydrogen, amino, alkyl of 1 to 5 carbon atoms optionally substituted with at least one hydroxy, dialkylamino with alkyl of 1 to 5 carbon atoms, alkoxy carbonyl of 2 to 5 carbon atoms, acyl of an organic carboxylic acid of 1 to 5 carbon atoms and ##STR2## X is an alkylene of 1 to 5 carbon atoms and R.sub.1 and R.sub.2 have the above definition.
摘要:
A novel method of treating inflammation of the colon and rectum of warm-blooded animals comprising administering to the colon and rectum of warm-blooded animals an anti-inflammatorily effective amount of 9.alpha.,11.beta.-dichloro-16.alpha.-methyl-21-oxycarbonyldicyclohexylmethoxy-.DELTA..sup.1,4 -pregnadiene-3,20-dione.
摘要:
Novel compounds 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 O--, CF.sub.3 S-- and CF.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 hydrogen or an optionally unsaturated ring able to contain one or more heteroatoms of the group consisting of --S--, --O-- and --N-- optionally substituted with one or more members of the group consisting of (a) halogens, (b) alkyl of 1 to 4 carbon atoms optionally substituted with NH.sub.2, --NHAlK or --N---(AlK).sub.2 and AlK is alkyl of 1 to 3 carbon atoms, (c) phenyl, (d) alkoxy of 1 to 4 carbon atoms, (e) --OH, (f) --CF.sub.3 and (g) --NO.sub.2 or R.sub.1 ' together with the nitrogen atom to which they are attached form an optionally unsaturated ring, the said ring then being connected to the nitrogen atom by a double bond, R.sub.3 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and halogen, R.sub.5 is a halogen with the proviso that R.sub.3, R.sub.4 and R.sub.5 can not all be fluorine and R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and an acyl of an organic carboxylic acid of 2 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts and their salts with non-toxic, pharmaceutically acceptable bases having a remarkable analgesic activity, a very weak anti-inflammatory activity and a good tolerance by the gastrointestinal system and their preparation and their intermediates.
摘要:
Novel carboxylic acids of the formula ##STR1## wherein Z is an aliphatic hydrocarbon chain selected from the group consisting of --(CH.sub.2).sub.n -- and --CH.dbd.CH--(CH.sub.2).sub.n-2 -- where the double bond may be at any point in the chain, n is an integer from 5 to 10 and X, X.sub.1, X.sub.2 and X.sub.3 are individually selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, alkylthio of 1 to 5 carbon atoms, CF.sub.3 --, CF.sub.3 O-- and CF.sub.3 S-- and their non-toxic, pharmaceutically acceptable organic and inorganic salts and esters having analgesic and anti-inflammatory activity and their preparation.
摘要:
Derivatives of 2-(4-quinolinylamino)-5-fluorobenzoic acid compounds of the formula ##STR1## wherein X is selected from the group consisting of chlorine and --CF.sub.3 in the 7- or 8-position and R is selected from the group consisting of hydrogen, an esterifying group, alkali metals, alkaline earth metals, ammonium and non-toxic, pharmaceutically acceptable organic amines and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable analgesic properties and their preparation.
摘要:
Novel .DELTA..sup.4 -androstenes of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, Y is selected from the group consisting of hydrogen, fluorine and methyl, R.sub.2 is selected from the group consisting of saturated and unsaturated alkyl of 1 to 12 carbon atoms, --CF.sub.3, aryl of 6 to 12 carbon atoms and aralkyl of 7 to 12 carbon atoms and the dotted lines in the A and B rings indicate the optional presence of one or two double bonds in the 1(2) and 6(7)-positions with the proviso that when R.sub.1 is methyl, R.sub.2 is saturated or unsaturated alkyl and the B ring is saturated, Y is methyl having anti-inflammatory activity and novel intermediates.
摘要:
Novel indoles of the formula ##STR1## wherein R is in the 2-, 3- or 4-position and is selected from the group consisting of hydrogen, halogen, --CF.sub.3, --SCF.sub.3, --OCF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity.