Use as medicine of a compound restoring active principles in vivo
A method for delivering at least an active principal A to a human or animal, by administering, in vivo, an active compound of general formula A′ V′ C′, that is capable of restoring at least the entity A by cleavage, in vivo, of the corresponding attachments between A′ and V′, wherein V is a biogenic vectorization compound of general formula X-R-Y, where R represents an aliphatic, cyclic or alicyclic, saturated or unsaturated hydrocarbon chain of 2 to 10 carbon atoms, and X and Y are each a free acid, amine or alcohol function; and A and C are two respectively different active principles, one of which has a chemical function complementary to the function of X, capable of reacting with the latter to give an ionic A′ - - - V′ or covalent A′—V′ attachment that can be cleaved in vivo, and the other of which has a chemical function complementary to the function of Y, capable of reacting with the latter to give an ionic V′ - - - C′ or covalent V′—C′ attachment.
1 . A method for delivering at least an active principal A to a human or animal, comprising administering, in vivo, an active compound of general formula A′ V′ C′, capable of restoring at least the entity A by cleavage, in vivo, of the corresponding attachments between A′ and V′, wherein:
V is a biogenic vectorization compound of general formula X-R-Y, where:
R represents an aliphatic, cyclic or alicyclic, saturated or unsaturated hydrocarbon chain of 2 to 10 carbon atoms, which is optionally substituted with C1 to C5 alkyl groups and/or with hydroxyl groups, and
X and Y are each a free acid, amine or alcohol function, and
A and C are two respectively different active principles, one of which comprises a chemical function complementary to the function X, capable of reacting with the latter to give an ionic A′ - - - V′ or covalent A′—V′ attachment which can be cleaved in vivo, and the other of which comprises a chemical function complementary to the function Y, capable of reacting with the latter to give an ionic V′ - - - C′ or covalent V′—C′ attachment.
2 . The method according to claim 1 , wherein the V′ - - - C′ or V′—C′ attachment can be cleaved in vivo, and said active compound is also capable of restoring the entities V′ and C by said cleavage in vivo.
3 . The method according to claim 1 , wherein the functions of X and Y are respectively different.
4 . The method according to claim 1 , wherein the functions of X and Y are identical.
5 . The method according to claim 3 , wherein the function of X is an acid or amine function, and the function of Y is an alcohol function.
6 . The method according to claim 4 , wherein the functions of X and Y are each an acid function.
7 . The method according to claim 6 , wherein the attachment A′—V′ is covalent and of the amide type.
8 . The method according to claim 6 , wherein the attachment V′ - - - C′ is ionic and of the salt type.
9 . The method according to claim 1 , wherein the active compound has as a general formula A′—V′—C′, the attachments A′—V′ and V′—C′ each being of the amide or ester type.
10 . The method according to claim 1 , wherein the active compound has as a general formula A′ - - - V′ - - - C′, the attachments A′ - - - V′ and V′ - - - C′ being of the ionic type and respectively different, and each being an attachment of the salt or acid/base type.
11 . The method according to claim 1 , wherein the active compound has as a general formula A′ - - - V′—C′, the attachment A′ - - - V′ being of the ionic type and the attachment V′—C′ being of the covalent type.
12 . The method according to claim 1 , wherein the active principles A and C have an approximately equal plasmatic half-life.
13 . The method according to claim 1 , wherein the active principles A and C belong to the same therapeutic class or respectively different therapeutic classes.
14 . The method according to claim 1 , wherein the active principles make it possible to treat two systematically and respectively associated pathologies.
15 . The method according to claim 1 , wherein the biogenic vectorization compound is metabolizable and/or biodegradable and/or atoxic in human or animals.
16 . A process to achieve an active compound AVC for delivering at least one active principle A to a target human or animal which can be used as a medicine, comprising:
a) choosing an active principle A as a function of at least one target which is a therapeutic object, and of the presence or absence on this active principle of free and accessible chemical functions capable of being chemical functions complementary to those of a biogenic vectorization compound;
b) choosing the biogenic vectorization compound as a function of the complementary chemical functions of the selected active principles A and C and of the qualities of the biogenic vectorization compound, said biogenic vectorization compound being at least one of metabolizable, biodegradable, and atoxic with respect to humans or to animals, at a physiological dose;
c) validating the possibility of synthesizing potential compounds AVC; and
d) choosing a final active compound from among the potential compounds, by sorting as a function of the results of the assays of cleavage as a function of the targeted sites of release, and then as a function of the results of toxicity assays.
17 . The process according to claim 16 , wherein at step c, the synthetic methods selected are those used for the formation of double salts, diesters, diamides, ester salts, amide salts or ester amides.
18 . The process according to claim 16 , wherein the biogenic vectorization compound is a compound of general formula X-R-Y, wherein:
R represents an aliphatic, cyclic or alicyclic, saturated or unsaturated hydrocarbon chain of 2 to 10 carbon atoms, which is optionally substituted with C1 to C5 alkyl groups and/or with hydroxyl groups, and
X and Y are each a free acid, amine, or alcohol function.
19 . The process according to claim 16 , wherein the active principles chosen at step a) are a sulphamide chosen among sulphamethoxazole and a trimethoprim.
20 . The process according to claim 16 , wherein the active principles chosen at step a) are selected from the group consisting of:
ranitidine and metronidazole;
a nonsteroidal anti-inflammatory agent and penicillamine;
metformin and arginine; and
an anti-hypertensive agent chosen among quinapril, benazepril and captopril, and a diuretic chosen among hydrochlorothiazide.