Abstract: The invention relates to novel acyl derivatives of rifamycins of the formula ##STR1## and the salts thereof, in which the structural elements --A.sub.1 --A.sub.2 --, --A.sub.3 --A.sub.4 -- and --A.sub.5 --A.sub.6 -- each denote ethylene or vinylene or the elements --A.sub.1 --A.sub.2 -- and --A.sub.3 --A.sub.4 -- each denote ethylene and --A.sub.5 --A.sub.6 -- denotes vinylene; X represents >C(R.sub.6)-- or >N-- and R.sub.6 denotes hydrogen or alkyl; alk denotes an aliphatic hydrocarbon radical; R.sub.1 denotes hydrogen or acyl; R.sub.2 denotes acyl, or alkyl which is optionally substituted by an aromatic radical, and R.sub.3 and R.sub.3 ' represent a common bond, or R.sub.3 denotes hydrogen or acyl, and R.sub.3 ' is hydrogen; R.sub.4 denotes hydrogen, cycloalkyl or aryl; R.sub.5 denotes hydrogen or acetyl; R.sub.7 denotes hydrogen or alkyl, which can be used as active compounds in medicaments, the preparation and use thereof, and pharmaceutical products and the preparation thereof.

Abstract: The invention relates to the preparation of substituted azacyclohexyl derivatives of rifamycins of the formula ##STR1## and salts thereof in which R.sub.1 is hydrogen or trialkylacetyl, R.sub.2 is hydrogen or acetyl and R.sub.3 is alkyl, which exhibit valuable pharmacological properties.

Abstract: Compounds of the general formula: ##STR1## in which R is a lower alkyl group, and R.sub.1 is a tri-lower alkylmethylcarbonyl group, the structure elements --A.sub.1 --A.sub.2 --, A.sub.3 --A.sub.4 -- or A.sub.5 --A.sub.6 -- each represent ethylene or vinylene, or the elements --A.sub.1 --A.sub.2 -- and --A.sub.3 --A.sub.4 -- each represent ethylene and --A.sub.5 --A.sub.6 -- represents vinylene, their optical isomers and their salts exhibit valuable pharmaceutical properties.

Abstract: The invention relates to a process for the preparation of a compound of formula ##STR1## or a salt thereof, wherein R.sub.1 is hydrogen or trialkylacetyl, R.sub.2 is hydrogen or acetyl and R.sub.3 is alkyl, which process comprises cyclising a compound of formula ##STR2## wherein R.sub.1 is trialkylacetyl and, if desired, converting a compound of formula I obtainable by said process or in another manner, or a salt thereof, into another compound of formula I or a salt thereof, or converting a resultant free compound of formula I into a salt and/or a resultant salt into the free compound of formula I or into another salt.

Abstract: The invention relates to novel substituted azacyclohexyl derivatives of formula ##STR1## and salts of thereof in which the structural elements --A.sub.1 -A.sub.2, --A.sub.3 -A.sub.4 -- and --A.sub.5 -A.sub.6 -- are each ethylene or vinylene or the elements --A.sub.1 -A.sub.2 -- and --A.sub.3 -A.sub.4 -- are each ethylene and --A.sub.5 -A.sub.6 -- is vinylene, X is >CR.sub.6 -- or >N-- and R.sub.6 is alkyl or hydrogen, alk is an aliphatic hydrocarbon radical or a bond, R.sub.1 is hydrogen or acyl, R.sub.2 is hydrogen or acetyl, R.sub.3 and R.sub.4 together are a bond or each is hydrogen, R.sub.5 is hydrogen, a cycloaliphatic hydrocarbon radical, aryl or heteroaryl and R.sub.7 is hydrogen or alkyl, with the proviso that when --A.sub.1 -A.sub.2 --, --A.sub.3 -A.sub.4 -- and --A.sub.5 -A.sub.6 -- are each vinylene, X is >N--, R.sub.1 is hydrogen or trialkylacetyl, R.sub.2 is hydrogen or acetyl, R.sub.3 and R.sub.4 together are a bond and alk is methylene, R.sub.

Abstract: 3-W-Rifamycin SV and S compound, wherein W is a piperazin-1-yl radical of the formula ##STR1## wherein R.sup.1 and R.sup.2 are C.sub.1 -C.sub.4 alkyl and R.sup.3, R.sup.4 and R.sup.5 are hydrogen or C.sub.1 -C.sub.4 alkyl, or R.sup.2 together with R.sup.3 or R.sup.3 together with R.sup.4 are buta-1,3-dien-1,4-ylene, trimethylene or tetramethylene, each of which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl, and R.sup.1, R.sup.4 and R.sup.5 or R.sup.1, R.sup.2 and R.sup.5 are hydrogen or C.sub.1 -C.sub.4 alkyl, and salts thereof, have long-term antituberculotic and antimicrobial activity.

Abstract: Compounds of the formula ##STR1## in which R represents lower alkyl, R.sub.1 represents tri-lower alkylmethylcarbonyl, and one of the radicals R.sub.2 and R.sub.3 represents tri-lower alkylmethylcarbonyl and the other represents hydrogen, and salts thereof, exhibit hypo-lipidaemic properties.

Abstract: Rifamycin derivatives of formula ##STR1## wherein R is a radical of the formula ##STR2## in which R.sub.1 is an unsubstituted or substituted biphenylyl radical, and wherein X--X, Y--Y and Z--Z are each vinylene of the formula CH.dbd.CH, or wherein X--X and Y--Y are each ethylene of the formula CH.sub.2 --CH.sub.2 and Z--Z is ethylene or vinylene, and processes for the preparation thereof are described. These compounds can be used as antibacterial and antiviral medicaments.

Abstract: 3-Hydroxyrifamycin S and its new analogues with an etherified or esterified 3-hydroxyl group of the formula ##STR1## in which each of R and R' represents a hydrogen atom, or R' represents acetyl and R represents hydrogen, an optionally substituted hydrocarbyl or the acyl radical of a carboxylic acid, and also the corresponding compounds of the SV series, are obtained by a novel process in which 3-bromorifamycin S is treated with a reagent ROH, in which R has the meanings mentioned above, or with a salt thereof, in a neutral to weakly basic medium. The final products are primarily suitable as antibiotics for combating microbial infections and/or as intermediates for the manufacture of the same.

Abstract: Antibiotically active compounds derived from rifamycin S or from the corresponding hydroquinone, rifamycin SV, or from derivatives at least partially hydrogenated in positions 16, 17; 18, 19; 28, 29, such as the 16, 17; 18, 19--tetrahydro- or the 16, 17; 18, 19; 28, 29--hexahydro derivatives, which contain in position 3 a free or an aliphatically substituted amino group. The hydrocarbon radicals of the aliphatically substituted amino group can also be interrupted in their carbon chain by heteroatoms and/or be substituted by functional groups.A special group of these new compounds is represented by 3-amino derivatives as defined above, in which the amino group is a particular type of N-aza-cyclo-aliphatic radical unsubstituted by functional groups, and which has, in addition to the antibiotic action against sensitive microorganisms also an antibacterial activity against certain types of resistant microorganisms.

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: Antibiotically active compounds derived from rifamycin S or from the corresponding hydroquinone, rifamycin SV, or from derivatives at least partially hydrogenated in positions 16, 17; 18, 19; 28, 29, such as the 16, 17; 18, 19-tetrahydro-or the 16, 17; 18, 19; 28, 29-hexahydro derivatives, which contain in position 3 a free or an aliphatically substituted amino group. The hydrocarbon radicals of the aliphatically substituted amino group can also be interrupted in their carbon chain by heteroatoms and/or be substituted by functional groups.A special group of these new compounds is represented by 3-amino derivatives as defined above, in which the amino group is a particular type of N-aza-cyclo-aliphatic radical unsubstituted by functional groups, and which has, in addition to the antibiotic action against sensitive microorganisms also an antibacterial activity against certain types of resistant microorganisms.

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.

Abstract: Antibiotically active compounds derived from rifamycin S or from the corresponding hydroquinone, rifamycin SV, or from derivatives at least partially hydrogenated in positions 16, 17; 18, 19; 28, 29, such as the 16, 17; 18, 19 - tetrahydro- or the 16, 17; 18, 19; 28, 29 - hexahydro derivatives, which contain in position 3 a free or an aliphatically substituted amino group. The hydrocarbon radicals of the aliphatically substituted amino group can also be interrupted in their carbon chain by heteroatoms and/or be substituted by functional groups.A special group of these new compounds is represented by 3-amino derivatives as defined above, in which the amino group is a particular type of N- aza - cyclo - aliphatic radical unsubstituted by functional groups, and which has, in addition to the antibiotic action against sensitive microorganisms also an antibacterial activity against certain types of resistant microorganisms.