Leo Pharmaceutical Products, Ltd.

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

Leo Pharmaceutical Products Ltd. A/s

Lovens Kemiske Fabrik Produktionsaktieselskab

Wagn O Godtfredsen

Welf Von Daehne

Erling Knud Frederiksen

Schneur Rachlin

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

The invention relates to the use of certain vitamin D analogues for the treatment of acne. The analogues have only moderate activity on the calcium metabolism when compared to 1,25-(OH).sub.2 D.sub.3, but retain the ability to activate receptors for 1,25-(OH).sub.2 D.sub.3 not associated with calcium absorption or bone calcium mobilization.

Use of vitamin-D analogues in the treatment of acne

Use of the treatment of acne

This invention relates to pharmaceutical compositions for treatment of alopecia comprising a compound of formula, in the form of the free base or acid addition salts thereof, in association with a pharmaceutical carrier adapted for topical application to mammalian skin. The compounds used have general formula ##STR1## in which the R.sub.1 -substituted cyanoguanidyl radical is placed in the 3- or 4-position of the pyridine ring, and in which R.sub.1 stands for a straight or branched, saturated or unsaturated, aliphatic hydrocarbon radical having from 1 to 8 carbon atoms, a cycloalkyl or cycloalkenyl radical having from 3 to 7 carbon atoms, or an aryl or an aralkyl radical. R.sub.2 stands for hydrogen, halogen, hydroxy, lower alkyl or alkoxy radicals. The present compositions find applications both in the human and veterinary use.

Topical preparation for treatment of alopecia

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

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

The invention relates to a new series of penicillin esters and salts thereof, to methods of their preparation and to intermediates in the production of the esters of the general formula ##STR1## in which R.sub.1 and R.sub.2 represent an alkyl radical having from 1 to 6 carbon atoms, a cycloalkyl or cycloalkylalkyl radical the cycloalkyl part having from 3 to 10 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom represent a heterocyclic ring with from 4 to 8 carbon atoms; R.sub.3 represents radicals known from natural, biosynthetic, and semisynthetic penicillins; and pharmaceutically acceptable salts thereof. The new compounds are efficiently absorbed from the gastrointestinal tract and after the absorption they are rapidly transformed into the corresponding free penicillins and amidinopenicillanic acids, whereby a broad-spectrum infection can be combated.

Penicillin esters, salts thereof and methods for their preparation

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

New penicillin esters and their salts together with methods for, and intermediates in the preparation thereof, the esters having the formula: ##EQU1## in which formula the asterisk indicates the possibility of an asymmetric carbon atom, n indicates an integer from 0 to 5, R.sup.1 represents a group, which together with --CO-- forms the side chain of any of the known semisynthetic, biosynthetic, and natural penicillins; R.sup.2 has any of the following meanings: hydrogen, an aliphatic, an aromatic, a heterocyclic group, and an aromatically substituted aliphatic group; each of R.sup.3, R.sup.4, and R.sup.5 represents hydrogen, or a lower aliphatic group with the provision that R.sup.2 and R.sup.5 together with the carbon atom between them can form a 5-, 6-, or 7-membered carbocyclic ring, and either R.sup.3 and R.sup.4, or R.sup.4 and R.sup.5 together with the nitrogen atom can form a ring system.

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Vaerlose, Denmark

Wagn O Godtfredsen