Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic ester 21-carbonic esters of the formula I: are described, in which A is CHOH and CHCl, CH2, C═O or 9(11) double bond; Y is H, F or Cl; Z is H, F or methyl; R(1) is aryl or hetaryl; R(2) is alkyl and R(3) is H or methyl. They are obtained, inter alia, by reacting a compound of the formula II: in which R(5) is OH, with an activated carboxylic acid of the formula III:  R(6)-CO—(O)n[(C1-C4)-alkyl]m-R(1)  III. They have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses.

Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds

Abstract: An apparatus advantageously influences the wing root airflow along the wing root of an aircraft having a high lift system including leading edge slats provided on the main wings. The apparatus includes a respective vortex generator arranged on the inboard end of each leading edge slat in the area of the wing root, and further includes a respective transition fairing arranged on a separation edge that is let into the leading edge of the wing root and that borders along the inboard edge of the respective slat. The vortex generator is a rigid member fixed to the leading edge slat and may be in the shape of a horn, a disk, or a winglet. The transition fairing may be a rigid member fixed to the wing root along the separation edge, or may be a flexible elastic member that can be inflated to have a variable outer contour. The present system avoids the need of additional independently movable auxiliary flaps, and thus achieves a reduced weight, complexity, and maintenance requirement.

Abstract: 17-Deoxycorticoid-21-carboxylic esters of the formula I ##STR1## are described, in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl and R(2) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(4) is OH, with an activated carboxylic acid of the formula III,R(5)-CO--X-R(1) III.The compounds I possess very strong local and topical antiinflammatory activity and exhibit a very good ratio of local to systemic antiinflammatory effect, which ratio is often clearly superior to that of structurally related corticoid 21-esters which do not carry any aryl or hetaryl group in the 21-ester residue or to that of analogous 17-deoxycorticoids having an unesterified, that is a free, 21-hydroxyl group.

Abstract: The invention relates to a process which comprises a compound of the formula II ##STR1##

Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R, 7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxyme thyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive steps.

Abstract: Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I ##STR1## are described in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl; n and m are zero or 1; R(2) is alkyl or --(CH.sub.2).sub.2 --OCH.sub.3 ; R(3) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(5) is OH, with an activated carboxylic acid of the formula III,R(6)--CO--(O).sub.n --(X)--R(1) III.The compounds I have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects, which ratio is often markedly superior to that of analogous corticoid 17-alkyl carbonate 21-esters which do not carry any aryl or heteraryl group in the 21-ester radical.

Abstract: The invention relates to a process for the preparation of cephem prodrug esters of the formula: ##STR1## in which R.sup.1 is C.sub.1 -C.sub.5 -alkanoyloxy-C.sub.1 -C.sub.3 -alkyl or C.sub.1 -C.sub.5 -alkoxycarbonyloxy-C.sub.1 -C.sub.3 -alkyl and X is an inorganic or organic anion, and in which the hydroxyimino group is present in the syn-form.

Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(metho xymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.

Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(metho xymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.

Abstract: The present invention relates to a process for the preparation of 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid (I) from 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid esters (II) or their salts by ester cleavage.The process comprises treating the compound II with formic acid, trifluoroacetic acid, methanesulfonic acid or trifluoromethanesulfonic acid or a mixture of two of these acids in each case.

Abstract: The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.

Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, ##STR1## which can optionally also be in the form of an acid addition salt of physiologically acceptable inorganic or organic acids, where R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen, a hydroxyl or a methoxy group, R.sup.3 is hydrogen or a hydroxyl group, R.sup.4 is hydrogen or a hydroxyl group, R.sup.5 hydrogen, a hydroxyl or a methoxycarbonyl group, R.sup.6 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH and R.sup.

Abstract: The present invention relates to a novel mono-functional and bis-functional anthraquinone-(oxy-2,3-oxido-propanes) and to a process for their preparation. The compounds according to the invention are useful as intermediates in the preparation of drugs possessing a .beta.-receptor blocker action and as crosslinking agents in the preparation of polymers, and moreover exhibit cytostatic activity.

Abstract: What is disclosed are steroid-21-halogeno-17-(alkyl carbonates), useful as medicaments for the treatment of inflammatory dermatoses, and a method for making them.

Abstract: What is disclosed is corticoid 17-(alkyl carbonates) of the formula ##STR1## as defined in the specification, which compounds can be used in veterinary therapy and human therapy, in the form of suspensions, ointments, creams, sprays and the like, for the treatment of inflammatory dermatoses of very diverse cause.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1 and R.sup.1' are identical or different and represent hydrogen, an alkyl radical or alkoxy radical having 1-4 carbon atoms, the allyl group, a halogen atom or the nitro group, R.sup.2 represents an acrylic acid radical or an acrylic acid nitrile radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, an alkyl radical having 1-5 carbon atoms, an aryl radical or aryl-lower alkyl radical either unsubstituted or substituted by lower alkyl or alkoxy, R.sup.6 represents hydrogen or an alkyl radical having 1-8 carbon atoms, R.sup.7 represents hydrogen, a lower alkyl radical or an aryl-lower alkyl radical, R.sup.3 and R.sup.4 represent together with the nitrogen atom a heterocyclic ring with 5-7 members being optionally substituted by C.sub.1 -C.sub.4 alkyl, in which ring one carbon atom may be replaced by one oxygen atom, sulfur atom or one further nitrogen atom, the latter may be substituted, or wherein R.sup.3 represents hydrogen and R.sup.

Abstract: Cyclic 2',3'-ethers of 3-hydroxy-14,15.beta.-oxido-14.beta.-bufa-4,20,22-trienolide, 3.beta.-(.alpha.-L-rhamnopyranoside) and process for preparing them. The compounds have a strongly positive inotropic activity and may be used in the therapy of cardiac insufficiency.

Abstract: Digoxigenine-3-[2', 3'-didesoxy-glycosides] of the formula ##SPC1##In which R.sup.1 is the digoxigenine radical and R.sup.2 is hydrogen, methyl or --CH.sub.2 OH, which are prepared by a reaction of a digoxigenine-12-monoacylate with an acylated 1,2-glycal, a catalytic hydrogenation of the 12-acylates obtained and a subsequent hydrolysis. The products have a cardiotonic, diuretic and especially venotonic activity.

Abstract: 12-Dehydro digoxin mono-4'" and 3'"-alkyl ethers and a process for their manufacture.The compounds have a cardiotonic and diuretic activity.