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US 5,288,716 AGranted
Use of pyridoxine derivatives in the prevention and treatment of hyperlipidaemia and atherosclerosis
OwnerUlrich Speckinventor
Life of this patent
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Abstract
A method for prevention of atherosclerosis or for treatment of hyperlipidaemia or atherosclerosis comprises administering one of more pyridoxine derivatives to a host in need thereof.
Claims20
A compound according to formula I ##STR16## wherein a) R.sub.1 is hydrogen and
- R.sub.2 is ##STR17## wherein R.sub.3 and R.sub.4 are independently hydrogen, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, (hydroxy or C.sub.1-4 -alkoxy)-C.sub.1-6 -alkyl or C.sub.6-14 -aryl or substituted aryl, or
- b) R.sub.1 is hydrogen and R.sub.2 is ##STR18## or
- R.sub.1 and R.sub.2 together are ##STR19## both radicals ##STR20## being derived from a natural amino acid, a natural amine, or a respective amide, R.sub.5 and R.sub.6 being the appropriate groups to form said radicals derived from natural amino acids, amines or respective amides,
- and X is hydrogen, ##STR21## or --PO.sub.4 H.sub.2, R.sub.3
- being independently a group defined for R.sub.3 above;
- or a pharmacologically acceptable salt of said compound;
- with the provisos that:
- R.sub.3 and R.sub.4 are not both H when X is H or PO.sub.4 H.sub.2,
- when R.sub.1 and R.sub.2 are .dbd.N--CHR.sub.5 R.sub.6, then .dbd.N--CHR.sub.5 R.sub.6 is not derived from glutamic acid, aspartic acid, or an S-containing amino acid when X is PO.sub.4 H.sub.2 ;
- when one of R.sub.3 and R.sub.4 is H and the other is alkyl, then X is not PO.sub.4 H.sub.2 ;
- when one of R.sub.3 and R.sub.4 is H and X is H, then the other of R.sub.3 and R.sub.4 is not butyl;
- when X is H or PO.sub.4 H.sub.2 and R.sub.1 and R.sub.2 together are ##STR22## then R.sub.5 and R.sub.6 are not (H, phenethyl) or (H, benzyl);
- when one of R.sub.3 and R.sub.4 is H and X is PO.sub.4 H.sub.2, then the other of R.sub.3 and R.sub.4 is not tryptamine;
- when R.sub.1 and R.sub.2 are --NCHR.sub.5 R.sub.6, then --NHCHR.sub.5 R.sub.6 is not derived from aspartic acid when X is H;
- and
- when X is H, R.sub.1 and R.sub.2 are not together ##STR23##
13 more elements
A method for prevention of atherosclerosis and/or for treatment of hyperlipidemia or atherosclerosis comprising administering to a host in need thereof an effective amount of a compound or a mixture of compounds according to formula (I) ##STR24## wherein a) R.sub.1 is hydrogen and R.sub.2 is ##STR25## wherein R.sub.3 and R.sub.4 are independently hydrogen, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, (hydroxy or C.sub.1-4 -alkoxy)-C.sub.1-6 -alkyl or C.sub.6-14 -aryl or substituted aryl or
- b) R.sub.1 is hydrogen and R.sub.2 is ##STR26## or
- R.sub.1 and R.sub.2 together are ##STR27## both radicals ##STR28## and ##STR29## being derived from a
- natural amino acids, a natural amine, or a respective amide, R.sub.5 and R.sub.6 being the appropriate groups to form said radicals derived from natural amino acids, amines or respective amides,
- and X is hydrogen, ##STR30## R.sub.3 being independently a group defined for R.sub.3 above;
- or a pharmacologically acceptable salt selected from the group consisting of sulfate, pyrosulfate, bisulfate, sulfite, bisulfite phosphate, monohydrogen phosphate, dihydrogen phosphate, metaphosphate, pyrophosphate, chloride, bromide, iodide, acetate, propionate, decanoate, caprylate, acrylate, formate, isobutyrate, caproate, heptanoate, propionate, malonate, succinate, suberate, sebacate, fumarate, maleate, butyne-1,4-dioate, hexyne-1,6-dioate, benzoate, chlorobenzoate, methylbenzoate, dinitrobenzoate, hydroxybenzoate, methoxybenzoate, phthalate, terephthalate, benezenesulfonate, toluenesulfonate, chlorobenzenesulfonate, xylenesulfonate, phenylacetate, phenylpropionate, glycolate, malate, tartrate, methanesulfonate, propanesulfonate, naphthalene-1-sulfonate and naphthalene-2-sulfonate, salts of said compound. with the provisos that:
- when one of R.sub.1 and R.sub.2 is H and the other is NR.sub.3 R.sub.4 and both R.sub.3 and R.sub.4 are H or one of R.sub.3 and R.sub.4 is H and the other is alkyl, then X is not PO.sub.4 H.sub.2 ;
- when X is H and one of R.sub.1 and R.sub.2 is H and the other is NR.sub.3 R.sub.4 and both R.sub.3 and R.sub.4 are H or one of R.sub.3 and R.sub.4 is H and the other is alkyl, then the resultant compound is not coadministered with clofibric acid or an ester or salt thereof;
- that when R.sub.1 and R.sub.2 are .dbd.N'CHR.sub.5 R.sub.6, then .dbd.NCHR.sub.5 R.sub.6 is not derived from glutamic or aspartic acid when X is PO.sub.4 H.sub.2.
5 more elements
Dependencies are inferred from the claim text.