Novel using dipeptidyl peptidase iv inhibitors

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention proposes a pharmaceutical composition used in treatment of patients suffering from cerebrospinal sclerosis. The composition comprises as an active component inhibitor of dipeptidyl peptidase IV (DPIV) of the general formula (I): wherein A means a residue of amino acid comprising at least one functional group in by-side chain; B means oligopeptide comprising up to 20 amino acids in its chain length, or polyethylene glycol of molecular mass up to 20000 g/mole, or optionally substituted organic amine, amide, alcohol, acid or aromatic compound comprising from 8 to 50 carbon atoms representing substituted or optionally substituted phenyl, benzyl, naphthyl, biphenyl and wherein a substitute can mean replacing with one or some groups of alkyl, alkenyl, alkynyl, mono- or multivalent acyl, alkanoyl, alkoxyalkanoyl or alkoxyalkyl as by-side groups; C means group of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine bound by amide bond with the group A. In animal model study administration of inhibitor DPIV as isoleucylthiazolidine fumarate in the dose 1 mg/kg resulted to the absence of clinical symptoms of disease. In other experiments this inhibitor caused accelerating recovery and shoed anti-inflammatory effect also.

EFFECT: valuable medicinal and biochemical properties of inhibitors.

4 cl, 8 dwg, 14 ex

 

The text descriptions are given in facsimile form.

1. Pharmaceutical composition for treatment of multiple sclerosis, characterized in that as the active ingredient contains a therapeutically effective amount of an inhibitor of the enzymatic activity of dipeptidylpeptidase IV (DPIV), General formula

including all stereoisomers, pharmaceutically acceptable salts and prodrug,

where a represents the residue of an amino acid having at least one functional group in the side chain;

In the mean moiety covalently associated with at least one functional group in the side chain and represents

Oligopeptide having a chain length of up to 20 amino acids,

polyethylene glycol having a molecular weight of up to 20,000 g/mol,

optionally substituted organic amine, amide, alcohol, acid, or an aromatic compound having from 8 to 50 carbon atoms, and a represents a substituted or optionally substituted phenyl group, benzyl, naphthyl, biphenyl, and the Deputy can mean the substitution of one or several groups of alkyl, alkenyl, quinil, mono - or polyvalent acyl, alkanoyl, alkoxyalkanols or alkoxyalkyl as side groups;

With is a group of thiazolidine, pyrrolidine, cianergoline, hydroxyproline, dihydrobromide, or piperidine, linked by an amide bond with A.

2. The pharmaceutical composition according to claim 1, characterized in that a represents an amino acid, preferably α-amino acid, mainly natural α-amino acid having at least one functional group in the side chain, selected from the group consisting of threonine, tyrosine, serine, arginine, lysine, aspartic acid, glutamic acid or cysteine.

3. The pharmaceutical composition according to claim 1, characterized in that it is in a form for parenteral or oral administration.

4. The pharmaceutical composition according to claim 1, characterized in that the pharmaceutically acceptable salt is selected from the group sotoyama the salt of hydrochloric, Hydrobromic, perchloric, sulfuric, nitric, phosphoric, acetic, propionic, glycolic, lactic, succinic, maleic, fumaric, malic, tartaric, citric, benzoic, almond, methansulfonate, hydroxyethanesulfonic, benzosulfimide, oxalic, pambou, 2-naphthalenesulfonates, para-toluensulfonate, cyclohexanesulfamic, salicylic, some saccharine or triperoxonane acid.



 

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3 cl, 3 tbl, 3 ex

FIELD: medicine, pharmaceuticals.

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FIELD: organic chemistry, medicine.

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EFFECT: valuable medicinal property of compounds.

4 cl, 1 tbl, 9 ex

FIELD: organic chemistry, medicine.

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EFFECT: valuable medicinal property of compounds.

4 cl, 1 tbl, 9 ex

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EFFECT: valuable medicinal property of compounds.

4 cl, 1 tbl, 9 ex

FIELD: medicine.

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18 cl, 1 tbl

FIELD: organic chemistry, medicine, pharmacy.

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EFFECT: valuable medicinal properties of compound and pharmaceutical composition.

28 cl, 1 tbl, 417 ex

FIELD: organic chemistry, medicine, pharmacy.

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28 cl, 1 tbl, 417 ex

FIELD: organic chemistry, medicine, pharmacy.

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EFFECT: valuable medicinal and pharmacological properties of compounds and drug.

7 cl, 3 tbl, 27 ex

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19 cl, 2 dwg, 1 tbl, 15 ex

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1 ex, 1 tbl

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34 cl, 2 tbl, 7 dwg, 4 ex

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8 dwg, 2 ex, 5 tbl

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EFFECT: higher efficiency.

2 ex, 2 tbl

FIELD: medicine.

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1 ex

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EFFECT: improved and valuable medicinal properties of drug.

33 cl, 42 dwg, 10 tbl, 12 ex

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2 ex

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EFFECT: higher efficiency of therapy.

46 cl, 1 ex, 1 tbl

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