Leo Pharmaceutical Products Ltd. A/s

Leo Pharmaceutical Products, Ltd.

Hans Jorgen Petersen

Ernst T Binderup

Sven Liisberg

The invention relates to a series of new compounds, to methods for preparing the compounds, to compositions containing said compounds which are useful in the human and veterinary medical practice, and to methods for treating patients suffering from certain illnesses with said compounds, the new compounds having the general formula I ##STR1## or the tautomeric forms thereof in which the R.sup.1 -substituted cyano-guanidyl radical is placed in the 2-, 3- or 4-position of the pyridine ring, and in which R.sup.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, an aryl or an aralkyl radical, and R.sup.2 stands for hydrogen, halogen, hydroxy, lower alkyl or alkoxy radicals; and in the case of the present compounds containing one or more asymmetric carbon atoms, also the stereoisomers thereof and racemic mixtures of same; and salts of the compounds of formula I with nontoxic, pharmaceutically acceptable acids. The new compounds of the invention have surprisingly shown to be highly potent hypotensive compounds giving rise to a pronounced reduction of the blood pressure. They have a low toxicity and consequently a high therapeutic ratio.

Antihypertensive pyridylguanidine compounds

The present invention relates to pivaloyloxymethyl D(-)-.alpha.-aminobenzylpenicillinate of the formula I in a novel and improved form, i.e. the crystalline form ##SPC1## To methods of producing said crystalline pivaloyloxymethyl D(-)-.alpha.-aminobenzylpenicillinate and to pharmaceutical preparations containing said crystalline pivaloyloxymethyl D(-)-.alpha.-aminobenzylpenicillinate. Crystalline pivaloyloxymethyl D(-)-.alpha.-aminobenzylpenicillinate has no bitter taste, is only slightly soluble in water, and is stable and readily absorbable.

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Herlev, Denmark

Hans Jorgen Petersen