Beecham Group Plc

Harry Ferres

John P Clayton

Desmond John Best

Adrian Victor Kemmenoe

Richard A Smith

Andrew J Garman

Frank P Harrington

A fibrinolytically active protein conjugate comprising at least one optionally blocked fibrinolytic enzyme linked by way of a site other than the catalytic site responsible for fibrinolytic activity to at least one human protein. Processes from making the conjugates and pharmaceutical compositions containing them are also described.

Novel fibrinolytic enzyme compounds

A class of substituted aminoalkyl esters of methicillin have good oral absorption properties.

Penicillin compositions

A class of esters of the penicillin, nafcillin have the general formula: ##STR1## wherein A is a C.sub.1 -C.sub.6 alkylene group substituted with one or two groups of formula --NR.sup.1 R.sup.2 and optionally further substituted with one or more methyl or ethyl groups, wherein R.sup.1 and R.sup.2 are the same or different and each is a C.sub.1 -C.sub.6 alkyl group or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a saturated 5- or 6- membered heterocyclic ring. Upon oral administration, the esters are absorbed into the bloodstream where they are hydrolyzed to release the antibacterially active parent penicillin, nafcillin.

Penicillin esters and their preparation

New penicillin antibiotics are disclosed which are effective antibacterial agents and which belong to the class of .alpha.-(heterocyclic acylamino) penicillins and their salts and esters together with pharmaceutical compositions containing the same and their method of administration. The new compounds are characterized by having an amino substituent on the heterocyclic ring which is linked through an acylamino group to the .alpha.-carbon atom of the penicillin side chain. Procedure for preparing the new penicillins is described as well as the antibacterial activity of exemplary compounds against typical microorganisms.

Penicillins

A class of substituted aminocycloalkyl esters of penicillins have improved pharmacokinetic properties and are hydrolysed to the antibacterially active penicillin.

3-Substituted aminocycloalkyl esters of penicillin antibiotics

Lactonyl esters of Penicillins of the formula ##STR1## WHEREIN R.sup.1 is an antibacterially active penicillin-completing side chain; R is hydrogen, methyl or phenyl; and Ra, Rb, Rc, Rd are hydrogen, lower alkyl, lower alkoxy, halo, and nitro, provided that when R is hydrogen and R.sup.1 is D-.alpha.-aminophenylacetamido and Ra, Rb, Rc, and Rd are not all hydrogen are disclosed to possess antibacterial properties.

Lactonyl esters of penicillins

The invention provides penicillins of formula (I) their pharmaceutically acceptable salts and esters, a process for their preparation and intermediates from which they may be prepared. ##EQU1##

Mono-esters of .alpha.-carboxypenicillins and their preparation are described including intermediates for the mono-esters. The mono-esters are esterified on the .alpha.-carboxy group. They are well absorbed orally and de-esterified in vivo to give high serum concentrations of the parent .alpha.-carboxypenicillins.

Penicillin monoesters, their production and intermediates thereof

This invention relates to a novel class of esters of penicillins and cephalosporins which, upon oral administration are absorbed into the bloodstream where they are split by enzymic action to release the antibacterially active parent penicillin or cephalosporin.

Penicillin esters

The phthalide ester of 6-[D(-)a-aminophenylacetamido] penicillanic acid and intermediates therefor are described. The phthalide penicillin ester is orally administered to obtain high serum concentrations of the parent penicillin.

Phthalide penicillin ester intermediates

Aminoacylpenicillins are disclosed which possess a broad spectrum of antibacterial activity.

New penicillins and their salts and esters particularly active against Gram-negative organisms such as Pseudomonas spp., and their preparation and administration. The penicillins are active against clinically important organisms against which well-known broad spectrum penicillins are inactive and may generally be designated as aminoacyldipeptide penicillins of unusual structure and properties.

3-CROTONOLACTONE 3-BISCROTONO-LACTANE PENICILLINS WHICH POSSESS ANTIBACTERIAL ACTIVITY ARE DISCLOSED.

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Horsham, United Kingdom

Harry Ferres