2-aminocarboxylic acids and their derivatives, processes for their preparation and their use as medicaments
AssigneeGodecke Aktiengesellschaft
InventorsUwe Trostmann, Johannes Hartenstein, Claus Rudolph, Christoph Schachtele, Hartmut Osswald, Gunter Weinheimer
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Abstract
The invention concerns 2-aminocarboxylic acids and derivatives of formula ##STR1## processes for their preparation, as well as medicaments containing them for the inhibition of protein kinase C and thus for the prevention and/or treatment of heart and blood vessel diseases, such as thromboses, arterioscleroses, hypertension, of inflammatory processes, allergies, cancers, and certain degenerative damages of the central nervous system.
Claims15
A compound of formula ##STR15## or a pharmaceutically acceptable salt thereof wherein:
- R.sup.1 is a straight or branched, saturated or unsaturated alkyl of from 1 to 20 carbon atoms,
- R.sup.2 and R.sup.3 are each independently hydrogen or a straight or branched alkyl of from 1 to 4 carbon atoms,
- R.sup.4 is benzyl, hydroxybenzyl, carboxyl, hydroxyalkyl, or alkoxycarbonyl wherein there are form 1 to 4 carbon atoms in the alkyl or alkoxy group;
- and
- R.sup.5 is hydrogen or a straight or branched alkyl of from 1 to 4 carbon atoms.
A compound named 2-[N-methyl-N-(3-octadecyloxy-2-hydroxypropyl)]-amino-3-hydroxypropionic acid hydrochloride.
A compound named 2-[N-methyl-N-(3-octyloxy-2-hydroxypropyl)]-amino-3-hydroxypropionic acid.
A compound named 2-[N-methyl-N-(3-octadecyloxy-2-hydroxypropyl)]-amino-3-hydroxypropionic acid ethyl ester.
A compound named (.+-.)-2-N-(3-octadecyloxy-2-hydroxypropyl)-aminoacetic acid hydrochloride.
A compound named 2-N-(3-octadecyloxy-2-hydroxypropyl)-amino-3-hydroxypropionic acid hydrochloride.
A compound named 2-N-(3-octadecyloxy-2-methoxypropyl)-aminopropionic acid ethyl ester oxalate.
A compound named 2-N-(3-octadecyloxy-2-methoxypropyl)-amino-3-hydroxybutyric acid.
A compound named 2-N-(octadecyloxy-2-hydroxypropyl)-aminomalonic acid diethyl ester.
A compound named 2-N-(3-octadecyloxy-2-hydroxypropyl)-amino-3-phenyl-propionic acid.
A pharmaceutical composition for the inhibition of a kinase selected from the group consisting of protein kinase C, cyclo-AMP-dependent kinase, cyclo-GMP-dependent kinase, and myosine light chain kinase comprising a therapeutically effective inhibiting amount of a compound of formula ##STR16## or a pharmaceutically acceptable salt thereof wherein:
- R.sup.1 is a straight or branched, saturated or unsaturated alkyl of from 1 to 20 carbon atoms,
- R.sup.2 and R.sup.3 are each independently hydrogen or a straight or branched alkyl of from 1 to 4 carbon atoms,
- R.sup.4 is hydrogen, methyl, benzyl, hydroxybenzyl, carboxyl, hydroxyalkyl, or alkoxycarbonyl, and
- R.sup.5 is hydrogen or a straight or branched alkyl of from 1 to 4 carbon atoms in combination with a pharmaceutically acceptable carrier.
A method of inhibiting a kinase selected from the group consisting of protein kinase C, cyclo-AMP-dependent kinase, cyclo-GMP-dependent kinase, and myosine light chain kinase in a patient suffering therefrom comprising administering to said patient a therapeutically effective inhibiting amount of a compound of formula ##STR17## or a pharmaceutically acceptable salt thereof wherein:
- R.sup.1 is a straight or branched, saturated or unsaturated alkyl of from 1 to 20 carbon atoms,
- R.sup.2 and R.sup.3 are each independently hydrogen or a straight or branched alkyl of from 1 to 4 carbon atoms,
- R.sup.4 is hydrogen, methyl, benzyl, hydroxybenzyl, carboxyl, hydroxyalkyl, or alkoxycarbonyl, and
- R.sup.5 is hydrogen or a straight or branched alkyl of from 1 to 4 carbon atoms in combination with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.