Abstract: The utility of known and novel staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is formyl, an aliphatic hydrocarbon radical having up to 29 carbon atoms that is unsubstituted or substituted by aryl, or is an aryl radical,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, benzoyl, lower alkanoyl or .alpha.-aminoacyl having a free or protected amino group, andR.sub.3 is hydrogen, hydroxy, lower alkoxy or oxo,or whereinR.sub.1 is methoxycarbonylmethyl,R.sub.2 is benzoyl, andR.sub.3 is hydrogen,for avoiding or removing multi-drug resistance to anti-tumour agents, such as vinblastine or adriamycin, is described.

Abstract: N-(tetrahydropyran-4-yloxy-alkanoyl)-staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, hydroxy, lower alkoxy or oxo,R.sub.2 is hydrogen or C.sub.1-4 alkyl andR.sub.3 is hydrogen or C.sub.1-4 alkyl,processes and novel intermediates for the preparation thereof and processes for the preparation of the intermediates are described. The compounds of formula I inhibit the enzyme protein kinase C with a high degree of selectivity and can be used especially as tumour-inhibiting active ingredients.

Abstract: A tetrahydropyran-4-yloxy-alkanoic acid of formula III ##STR1## wherein R.sub.2 is hydrogen or C.sub.1-4 alkyl and R.sub.3 is hydrogen or C.sub.1-4 alkyl.

Abstract: Staurosporin derivatives of the formula I are described, ##STR1## in which R.sub.1 is hydrogen, hydroxyl, lower alkoxy or oxo and R.sub.2 is a radical of the formula II ##STR2## in which the configuration of the sugar moiety is derived from D-glucose, D-galactose or D-mannose, and R.sub.3 -R.sub.7 are as defined below.These compounds have a pronounced and selective inhibitory action on the enzyme proteinkinase C and have, inter alia, an antitumor action.

Abstract: Described are phosphatidyl compounds of the formula I ##STR1## in which R.sup.1 represents C.sub.3-14 -alkanoyl, benzoyl, the acyl radical of an .alpha.-aminocarboxylic acid that is other than glycine, L-alanine and derivatives thereof having a substituted amino group, and of which the .alpha.-amino group may be substituted by lower alkanoyl, lower alkoxycarbonyl or by benzyloxycarbonyl, or the acyl radical of a .beta.-aminocarboxylic acid or an .alpha.- or .beta.-hydroxycarboxylic acid,T represents a group NH that is unsubstituted or is substituted by lower alkyl, or oxygen,Y represents dimethylene that is unsubstituted or is substituted by free, etherified or amidated carboxy,W represents hydrogen, andZ represents a 1,2-dihydroxyethyl, 2-hydroxyethyl or hydroxymethyl group, in which at least one of the hydroxy groups is esterified by an aliphatic C.sub.8-30 -carboxylic acid or is etherified by an aliphaticC.sub.

Abstract: There are described sugar derivatives of the formula I ##STR1## that have immuno-stimulating action and that contain as inventive element at least one radical A.sup.1 or A.sup.2. These radicals A.sup.1 and A.sup.2, which may be constituents of the radicals R.sup.1, R.sup.2, R.sup.4, R.sup.6, R.sup.9, R.sup.10 or R.sup.12 according to formula I, are defined as follows:A.sup.1 represents lower alkanoyl that is substituted by aryl, heteroaryl or heteroarylthio and that may be additionally substituted by an ethylene radical which, with the above-mentioned aryl or heteroaryl substituent, forms a five-membered ring or represents ortho- or ortho/meta-substituted aroyl. A.sup.2 represents lower alkoxy substituted by aryl, heteroaryl or heteroarylthio.Also described are processes for the manufacture of the compounds of the formula I and novel intermediates.

Abstract: The invention relates to lipopeptides of the formula I, ##STR1## in which each of R.sub.a.sup.1 and R.sub.b.sup.1, independently of the other, represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 7 to 21 carbon atoms that is optionally substituted by oxygen functions, orone of the radicals R.sub.a.sup.1 --CO-- and R.sub.b.sup.1 --CO-- represents hydrogen and the other of the radicals R.sub.a.sup.1 --CO-- and R.sub.b.sup.1 --CO-- represents an acyl radical, wherein R.sub.a.sup.1 and R.sub.b.sup.1 have the meanings given above,R.sup.2 represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 1 to 21 carbon atoms that is optionally substituted by oxygen functions,n=0 or 1,As.degree. represents a radical of the formula --O--Kw--CO-- or --NH--Kw--CO-- wherein Kw represents an aliphatic hydrocarbon radical having a maximum of 12 carbon atoms,As.sup.1 represents a D- or L-.alpha.-amino acid,each of Z.sup.1 and Z.sup.

Abstract: There are described sugar derivatives of the formula I ##STR1## that have immuno-stimulating action and that contain as inventive element at least one radical A.sup.1 or A.sup.2. These radicals A.sup.1 and A.sup.2, which may be constituents of the radicals R.sup.1, R.sup.2, R.sup.4, R.sup.6, R.sup.9, R.sup.10 or R.sup.12 according to formula I, are defined as follows:A.sup.1 represents lower alkanoyl that is substituted by aryl, heteroaryl or heteroarylthio and that may be additionally substituted by an ethylene radical which, with the above-mentioned aryl or heteroaryl substituent, forms a five-membered ring or represents ortho- or ortho/meta-substituted aroyl. A.sup.2 represents lower alkoxy substituted by aryl heteroaryl or heteroarylthio.Also described are processes for the manufacture of the compounds of the formula I and novel intermediates.

Abstract: The compounds of the formula I ##STR1## in which each of R.sup.1, R.sup.4 and R.sup.6, independently of the others, represents hydrogen or lower alkanoyl, R.sup.2 represents C.sub.1-4 -alkyl, hydroxymethyl or phenyl, R.sup.3 represents hydrogen or methyl, R.sup.5 represents hydrogen or C.sub.1-3 -alkyl, R.sup.7 represents C.sub.1-3 -alkyl that is unsubstituted or substituted by hydroxy, mercapto or methylthio, R.sup.8 represents hydrogen or lower alkyl, X represents oxygen or the group NH, Y represents C.sub.1-4 -alkylidene, and each of R.sup.9 and R.sup.10, independently of the other, represents C.sub.11-17 -alkyl or C.sub.11-17 -alkenyl, and their salts, have an immunostimulating activeity.

Abstract: There are described hexopyranose compounds of the formula I and salts thereof having immunomodulatory action, which can be used, for example, in the form of pharmaceutical preparations, and also together with antibiotics, and processes for their manufacture. ##STR1## The variables are as described in the disclosure. The invention relates to the above-mentioned compounds as immunomodulators, especially as immunostimulants, their use as pharmacologically active substances, especially their use as immunomodulators, particularly as immunostimulants, and their use for the manufacture of pharmaceutical preparations, and to pharmaceutical preparations containing these compounds.

Abstract: Described are derivatives of pyranoses of the formula I, manufacturing processes and intermediates, and their use as medicaments. ##STR1## The pyranose moiety in the compounds of the formula I is derived especially from D-glucose, but alternatively from D-galactose or D-mannose.Characteristic of the compounds of the formula I is the lower alkyl or phenyl-lower alkyl radical R.sub.8, which carries an oxycarbonyl, mercaptocarbonyl or aminocarbonyl group, which is bonded to an aliphatic, cycloaliphaticaliphatic, cycloaliphatic or aromatic hydrocarbon radical R.sub.0, each of which is optionally substituted and which may be interrupted by oxycarbonyl, mercaptocarbonyl and/or iminocarbonyl and which, like the remaining radicals of the formula I, is defined in patent claim 1.

Abstract: Derivatives of 5-norbicyclomycin of the formula ##STR1## wherein R represents an unsubstituted or substituted monovalent hydrocarbon radical in which one, two or more carbon atoms can be replaced by heteroatoms, and X represents a bivalent group of the formula --O-- or --N(R')--, wherein R' has one of the meanings assigned to R, whilst R and R', if both have a meaning which is different from hydrogen, can also be linked to each other through a C--C bond or an oxygen, sulphur or nitrogen atom, and corresponding compounds, in which at least one hydroxyl group is protected, and salts of said compounds, provided they contain salt-forming groups, are useful as antibiotics, especially against Enterobacteriaceae, or as intermediates for the production of such antibiotics. They are obtained by condensing a corresponding 5-norbicyclomycin-5-one with a compound of the formula R--X--NH.sub.2 in which X and R have the above meaning.

Abstract: Bicyclomycin derivatives (i.e. compounds with the skeleton of the 5-methylene-2-oxa-7,9-diazabicyclo?4,2,2!decane) of the formula ##STR1## wherein R.sup.a to R.sub.d represent hydrogen atoms or hydroxyl protective groups, X represents a free or functionally modified carboxyl group, a substituted or unsubstituted hydrocarbon radical or a halogen atom, and n is 0 or 1, possess valuable antibiotic properties which are of importance in particular for combating infections caused by Enterobacteriaceae and Proteus species.