Leo Pharmaceutical Products Ltd. A/s

Leo Pharmaceutical Products Ltd. A/s (lovens Kemiske Fabrik

Leo Pharmaceutical Products, Ltd.

Lovens Kemiske Fabrik Produktionsaktieselskab

Other

Leo Pharmaceutical Products Ltd. A/s (lovens Kemiske Produktionsaktiensel

Welf Von Daehne

Wagn O Godtfredsen

Poul Rodbroe Rasmussen

Martin John Calverley

Claus Aage Svensgaard Bretting

Tore Duvold

Gunnar Grue-S&oslash;rensen

Mogens P Kran-Nielsen

Erling Knud Frederiksen

Erik I Hansen

Schneur Rachlin

Novel 17,20-dihydrofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.

Fusidic acid derivatives

Vitamin D analogues

The invention is directed to compounds, compositions and method of preparation of compounds of formulae I and II:

Tetracyclic triterpenes as cholesterol-lowering and anti-atherosclerosis agents

Crystalline 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate napsylate. The product may be prepared by reacting 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate or a salt thereof with 2-naphthalenesulfonic acid or salt thereof.

Crystalline 1,1-dioxopenicillanoyloxymethyl

Method for preparing 6-.beta.-halopenicillanic acids

The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R.sub.2 represents a primary amino or a carboxy group; R.sub.3 is a hydrogen atom, or a lower alkyl, aryl or aralkyl radical, and A stands for a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group. The present invention provides new compounds useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.

Antibacterial beta-lactams, pharmaceuticals thereof and methods of using

The present invention relates to a crystalline hydrate of a salt of the antimicrobial agent 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate with p-toluenesulfonic acid, more particularly the mono- and dihydrate. The hydrates are easily obtained in a crystalline state devoid of organic solvent residues, they show good stability on storage, they are effectively absorbed and hydrolyzed in vivo, and they are thus specifically suitable for medical treatment of patients, in particular for oral administration.

Crystalline penicillin derivative tosylate hydrates

This invention relates to penicillanic acid derivatives of the formula I ##STR1## in which X stands for chlorine, bromine or iodine, to pharmaceutically acceptable, non-toxic salts of the compounds of formula I, to pharmaceutically acceptable, easily hydrolyzable esters thereof, including salts of such esters, to pharmaceutical compositions containing the compounds of the invention and dosage units thereof, to methods for the preparation of the compounds of the invention, and to methods of using the said new compounds in the human and veterinary therapy. The 6.beta.-halopenicillanic acids of formula I are potent inhibitors of .beta.-lactamases from a variety of gram-positive and gram-negative bacteria, making the 6.beta.-halopenicillanic acids as well as their salts and easily hydrolyzable esters valuable in human and veterinary medicine.

Substantially pure dicyclohexyl ammonium 6-.beta.-bromo-penicillanate

Derivatives of penicillanic acid

Processes for preparing .beta.-lactams

.beta.-Lactam compounds, antibacterial compositions thereof and method

The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a five- to ten-membered azacycloalkyl or azabicycloalkyl residue attached via the nitrogen atom and optionally being substituted by one or two, the same or different, lower alkyl groups; R.sub.2 represents a hydrogen atom or a lower alkyl, aryl, or aralkyl radical; and A represents a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.

6-Amidinopenicillanic acid derivatives including the radical of a

Fusidic acid derivatives which possess anti-bacterial, antimicrobial and pharmacokinetic properties. These derivatives include, for example, 3.alpha.,11.alpha.-dihydroxy-16.beta.-(2'-methlyphenyl) thiofusida-13(17),24-dien-21-oic acid and pharmaceutically acceptable, non-toxic salts or easily hydrolysable esters thereof.

The present invention relates to a new series of fusidic acid derivatives, to salts and easily hydrolysable esters thereof, to the preparation of these compounds, and to pharmaceutical compositions containing the compounds, the new fusidic acid derivatives having the general formula: ##STR1## in which the dotted line between C-24 and C-25 indicates that the carbon atoms in question are connected by either a double bond or a single bond, and in which Q.sub.1 represents oxygen or one of the groupings ##STR2## Z being a hydroxy group, a halogen atom, an alkylsulfonyloxy or arylsulfonyloxy group, such as methanesulfonyloxy or p-toluenesulfonyloxy, an azido or a nitro group, Q.sub.2 is oxygen or the grouping ##STR3## and R.sub.1 stands for a straight or branched alkyl radical having from 1 to 6 carbon atoms, such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl or the known isomers of pentyl and hexyl, a phenyl or a heterocyclyl radical having 5 to 6 ring atoms and containing nitrogen, oxygen and/or sulfur atoms, these radicals being optionally substituted with halogen, nitro, lower alkyl or lower alkoxy radicals. The present compounds show both in vitro and in vivo interesting antimicrobial and pharmacokinetic properties.

16-S-acyl derivatives of fusidic acid

The invention relates to a new series of fusidic acid derivatives, to salts and easily hydrolyzable esters thereof, to the preparation of these compounds and to pharmaceutical compositions containing the compounds, the new compounds having the general formula: ##STR1## in which Q.sub.1 and Q.sub.2 stand for the group ##STR2## or oxygen, A represents oxygen or sulphur, and R.sub.1 stands for a straight or branched alkyl radical having from 1 to 12 carbon atoms, R.sub.1 can further be an alkenyl or alkynyl radical having from 3 to 6 carbon atoms, a cycloalkyl radical having from 3 to 7 carbon atoms in the alicyclic ring, an aralkyl or aryl radical, R.sub.1 can also be a heterocyclic radical having 5 or 6 ring atoms and containing oxygen, sulphur and/or nitrogen atoms, R.sub.1 optionally being further substituted, and in which formula I the dotted line between C-24 and C-25 indicates that the carbon atoms in question are connected by either a double bond or a single bond, and the asterix at C-20 indicates that the compounds exist in two diastereomeric forms, and thus the invention comprises the pure diastereomers as well as mixtures of these. The compounds of the present invention possess antibacterial properties and show further interesting antimicrobial and pharmacokinetic properties.

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Welf Von Daehne