Method for producing prodrug from amidoxime and n-hydroxyguanidine carboxylic acid esters
AssigneeDritte Patentportfolio Beteiligungsgesellschaft mbH & Co. KG
InventorsBernd CLEMENT, Christiane WOLTER-REEH, Helen SCHENK
Life of this patent
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Abstract
The invention relates to a method for improving the bioavailability of pharmaceutical substances and for allowing the pharmaceutical substances to permeate the blood-brain barrier, the pharmaceutical substances having at least one or more amidine, guanidine, N-hydroxyamidine (amidoxime) or N-hydroxyguanidine functions. The invention also relates to medicaments containing the correspondingly modified pharmaceutical substances.
Claims17
A method of producing a prodrug for a medicinal substance, the medicinal substance having at least one functional group selected from the group consisting of an amidine, guanidine, N-hydroxyamidine (amidoxime) and N-hydroxyguanidine function, the method comprising substituting the at least one functional group of the medicinal substance with a partial structure of formula (I) or (II):
- to thereby produce the prodrug, wherein n is an integer of 0 to 12, and R1 is selected from the group consisting of hydrogen, an alkyl radical and aryl radical.
A method of improving at least one property selected from the group consisting of solubility, bioavailability and capacity to pass the blood-brain barrier of a medicinal substance, the method comprising substituting at least one functional group selected from the group consisting of an amidine, guanidine, N-hydroxyamidine (amidoxime) and N-hydroxyguanidine function in the medicinal substance with a partial structure of formula (I) or (II):
- to thereby obtain a prodrug of the medicinal substance, the prodrug having at least one of improved solubility, improved bioavailability and increased capacity to pass the blood-brain barrier as compared to the medicinal substance, wherein n is an integer of 0 to 12 and R1 is selected from the group consisting of hydrogen, an alkyl radical and aryl radical.
Dependencies are inferred from the claim text.