Abstract: The invention relates to new hetrazepines of general formula ##STR1## wherein A, Z, n, X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meanings given in the specification.The new compounds are intended for use in treating pathological conditions and diseases in which PAF (platelet activating factor) is implicated.

Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2 ;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position; D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms; or a branched, saturated or straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms; all of which are substituted by fluorine atoms;n is 1, 2, or 3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.7 is hydrogen, halogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group; andR.sub.

Abstract: The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.

Abstract: The invention relates to carbacyclins of general Formula I ##STR1## wherein R.sub.1 is the residue CH.sub.2 OH or ##STR2## with R.sub.2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl residue, a ##STR3## or heterocyclic residue, or R.sub.1 is the residue ##STR4## with R.sub.3 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms or the residue R.sub.2, orR.sub.1 is the residue ##STR5## wherein m is the number 1 or 2, X is an oxygen atom or a CH.sub.2 -group,A is a trans--CH.dbd.CH- or --.tbd.C--group,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,n is the number 1, 2, or 3,D is a straight-chain alkylene group of 1-5 carbon atoms,E is a --C.tbd.C---bond or a --CR.sub.6 =CR.sub.7 --group wherein R.sub.6 and R.sub.7 are different from each other and mean a hydrogen atom or an alkyl group of 1-5 carbon atoms or a hydrogen atom or a halogen atom, preferably chlorine,R.sub.

Abstract: The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1-C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably C1 or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.

Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen or OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2,n is 2, 3, 4, or 5,X is hydrogen or fluorine,A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position, D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms, a branched, saturated or a straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms, all of which can optionally be substituted by fluorine atoms,m is 1, 2, or 3,E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are different from each other and are hydrogen or alkyl or 1-5 carbon atoms, or are hydrogen or halogen,R.sub.

Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CH.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.

Abstract: The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I. ##STR1## wherein A is an anellated and optionally substituted benzene or 5- or 6- membered heterocyclic ring; R.sub.5 and Z are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or .alpha.-pyridyl; Y is ##STR2## and nontoxic, pharmaceutically acceptable acid addition salts thereof.

Abstract: The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II ##STR1## wherein A is an anellated and optionally substituted benzene or 5- or 6-membered heterocyclic ring; R.sub.5 and Z are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or is .alpha.-pyridyl; Y is CO, CS or CH.sub.2 ; and nontoxic, pharmaceutically acceptable acid addition salts thereof.

Abstract: The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II: ##STR1## wherein A is an annealed and optionally substituted benzene or 5- or 6-membered heterocyclic ring; B is an optionally substituted 5-membered heterocyclic ring; R.sub.5 and R.sub.7 are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or .alpha.-pyridyl; and non-toxic, pharmaceutically acceptable acid addition salts thereof.

Abstract: Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group,R.sub.3 and R.sub.4 each independently is hydrogen, alkyl of 1-5 carbon atoms, or fluorine,D is alkylene of 1-2 carbon atoms which can be substituted by alkyl groups of 1-5 carbon atoms,R.sub.5 is hydrogen or alkyl of 1-2 carbon atoms or, when D is alkylene of 1 or 2 carbon atoms, R.sub.5, together with R.sub.6, represents a bond,R.sub.6 and R.sub.7 each independently is hydrogen or alkyl of 1-2 carbon atoms, whereinR.sub.6 (R.sub.7) is halogen when R.sub.7 (R.sub.

Abstract: 17.alpha.-Pregn-4-ene-3-oxo-21-carboxylic acid esters of Formula I ##STR1## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond,--A--B--is ##STR2## --C--D--is ##STR3## and R is an alkyl or alkenyl residue of up to 6 carbon atoms,in addition to antialdosterone activity, exhibit greatly reduced antiandrogenic and progestational side effects.

Abstract: Prostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 wherein R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms substituted, if desired, by halogen, aryl, C.sub.1 -C.sub.4 -alkoxy, or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl, or a heterocyclic residue; or is the residue NHR.sub.4 wherein R.sub.4 means hydrogen, an alkanoyl residue, or an alkanesulfonyl residue of respectively 1-10 carbon atoms,A is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--group,W is a ##STR2## wherein the OH-group can be respectively esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or can be etherified with a tetrahydropyranyl, tetrahydrofuranyl, C.sub.1 -C.sub.4 -alkoxyalkyl, or tri(C.sub.1 -C.sub.4 -alkyl)-silyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,D and E jointly mean a direct bond orD is a straight-chain or branched alkylene group of 1-5 carbon atoms,E is an oxygen atom or a direct bond,R.sub.

Abstract: Compounds of Formula I ##STR1## wherein X is oxygen or CH.sub.2 ;A is CH.sub.2 --CH.sub.2, trans-CH.dbd.CH or C.tbd.C;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## and the OH groups may be in the .alpha.- or the .beta.-position; D is straight chain or branched, saturated or unsaturated hydrocarbon aliphatic of from 1 to 10 carbon atoms, which may be substituted by fluorine;E is C.tbd.C or CR.sub.3 .dbd.CR.sub.4, R.sub.3 and R.sub.4 being different and being hydrogen or alkyl of 1 to 5 carbon atoms;R.sub.1 is free or functionally modified hydroxy; andR.sub.2 is alkyl, cycloalkyl, optionally substituted aryl or heterocyclic,have valuable pharmacological properties, e.g., hypotensive and bronchodilatory characteristics. They can furthermore be used for prophylaxis and therapy of coronary infarct and as a treatment for stroke. They are produced by means of reduction of the corresponding 1-carbonic acid derivatives.

Abstract: Prostacyclin, although having a useful dilating effect on blood vessels, is not sufficiently stable to ensure successful use as a hypotensive agent.A 7-oxo prostacyclin derivative of the general formula ##STR1## in which R.sub.1 represents the radical OR.sub.3 whereinR.sub.3 represents hydrogen, a straight-chain or branched optionally substituted, (C.sub.1 -C.sub.10)alkyl, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted heterocyclic,orR.sub.1 represents the radical NHR.sub.4 whereinR.sub.4 represents hydrogen, or a group derived from an unsaturated or saturated, unsubstituted or substituted, (C.sub.1 -C.sub.15)organic carboxylic or sulphonic acid,A represents --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH-- or trans--CH.dbd.CH--,W represents ##STR2## either having a free or functionally modified hydroxy group which may be in the .alpha.- or .beta.

Abstract: Novel 6.beta.,7.beta.-methylene-17.alpha.-pregn-4-ene-21,17-carbolactones of Formula I ##STR1## wherein R and R' each is hydrogen or jointly form a methylene group.These exhibit a good antimineralocorticoid effect with low side effects.

Abstract: 7.alpha.-Alkoxycarbonyl-15.beta.,16.beta.-methylene-4-androstene compounds of Formula I ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is alkyl of 1-4 carbon atoms,X is ##STR2## and Y is carbonyl, andthe bond between the C-1 and C-2 carbon atoms is a single or double bond, orwhen the bond between the C-1 and C-2 carbon atoms is a single bond,X can also be ##STR3## when Y is ##STR4## possess valuable pharmacological properties, e.g., as aldosterone antagonists, i.e. they reverse the effect of deoxycorticosterone on the excretion of sodium and potassium.

Abstract: Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group.

Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.

Abstract: Prostacyclin derivatives of the formula ##STR1## wherein R.sub.1 is OR.sub.3 wherein R.sub.3 is hydrogen or alkyl of 1-10 carbon atoms, or R.sub.1 is NHR.sub.4 wherein R.sub.4 is alkanoyl or alkanesulfonyl,B is alkylene of 1-5 carbon atoms,A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--,W is hydroxymethylene or ##STR2## wherein the OH-group is optionally substituted by alkanoyl of 1-4 carbon atoms and the free or substituted OH-group can be in the .alpha.- or .beta.- position,R.sub.2 is alkyl of 1-6 carbon atoms optionally substituted by phenyl, or R.sub.2 is phenyl,R.sub.5 is hydroxy optionally substituted by alkanoyl of 1-4 carbon atoms,R.sub.6 is hydrogen, fluorine, or alkyl of 1-4 carbon atomsor when R.sub.3 is hydrogen, a salt thereof with a physiologically compatible base,have pharmacological activity e.g., blood pressure-lowering and bronchodilatory effects.