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2 238 950

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Application

2002111028/04, 2002-04-25

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Start date

2002-04-25

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Actual filing date

2002-04-25

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Published

2004-10-27

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Inventor

Evstigneeva R.P.Zheltukhina G.A.Zarubina T.V.Nebol'Sin V.E.Nosik D.N.Nosik N.N.

(73)

Holder

Nebol'Sin Vladimir Evgen'Evich

DERIVATIVES OF HEMIN AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, METHOD FOR PREPARING, APPLICATION AND PHARMACEUTICAL COMPOSITION Russian patent published in 2004 - IPC

Abstract RU 2238950 C2

FIELD: organic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to derivatives of hemin or their pharmaceutically acceptable salts that are inhibitors of proteolytic enzymes and representing compounds of the general formula (I):

wherein R1 and R2 are substituents that can represent amino acids, derivatives of amino acids, peptides consisting of 1-15 amino acid residues, derivatives of peptides consisting of 1-15 amino acid residue being α-carboxyl group of amino acids or peptides and side groups of amino acids or peptides can be modified being it is possible that R1 = R2 or R1 ≠ R2 is OH group; porphyrin carboxyl group can be modified with methyl or other (C2-C8)-ester or physiologically acceptable salt; Y- represents Cl-, CH3COO-; Me represents Fe with exception of compounds wherein Me means Fe3+; Y- means Cl-; R1 means -Leu-Leu-Val-Phe-OMe, R2 means -OH; R1 means -Val-Phe-OMe, R2 means -OH; R1 means -Leu-His-OMe, R2 means -OH; R1 means -Leu-His-Ala-OMe, R2 means -OH; R1 means -Leu-His-NH-C10H20-COOMe, R2 means -OH; R1 means -Leu-His-NH-C10H20-COOH, R2 means -OH; R1 means -Leu-His-NH-C10H20-COOMe, R2 means -Leu-His-NH-C10H20-COOMe; R1 means -Lys(Tfa)-Ala-Ala-OMe, R2 means -OH; R1 means -Val-Phe-OMe, R2 means -Leu-His-OMe; R1 means -Leu-Leu-Val-Phe-OMe, R2 means -Leu-His-OMe; R1 means -Leu-Lys(Tfa)-Leu-OMe; R2 means -OH; R1 means -Leu-Lys(Tfa)-Leu-OMe, R2 means -Leu-His-OMe; R1 means -Lys(Tfa)-Ala-Ala-OMe, R2 means -Ala-His-Lys(Cbz)-OMe; R1 means -Gly-OBzl, R2 means -Gly-OBzl; R1 means -His-OMe, R2 means -His-OMe; R1 means -Leu-His-OMe, R2 means -Leu-His-OMe; R1 means -leu-His-Leu-Gly-Cys(Bzl)-OBzl, R2 means -Leu-His-Leu-Cys(Bzl)-OBzl; R1 means -Leu-His-OMe, R2 means -OEt; R1 means -Leu-His-Leu-Gly-Cys(Bzl)-OBzl, R2 means -OEt; R1 means -OBzl, R2 means -OBzl; R1 means -OBzl, R2 means -OH; R1 means -Ala-OMe, R2 means -OBzl; R1 means -His-OMe, R2 means -OBzl; R1 means -Leu-His-OMe, R2 means -OBzl; R1 means -Leu-His-Leu-Gly-Cys(Bzl)-OBzl, R2 means -OBzl; R1 means -Leu-His-Ala-Lys(Cbz)-Gly-Cys(Bzl)-OBzl, R2 means -OBzl; R1 means -Leu-His-Lys(Cbz)-OMe, R2 means -OH; R means -Leu-His(Bzl)-Lys(Cbz)-OMe, R2 means -OH; R1 means -Leu-His-OMe, R2 means -OMe; R1 means -Leu-His(Bzl)-Lys(Cbz)-OMe, R2 means -OMe; R1 means -Ala-Leu-Ala-Phe-Ala-Cys(Bzl)-OMe, R2 means -Leu His-(Bzl)-Lys(Cbz)-OMe; R1 means -Ala-Leu-Ala-Phe-Ala-Cys(Bzl)-OBzl, R2 means -Leu-His(Bzl)-Lys(Cbz)-OMe; R1 means -Leu-His-Ala-Lys(Cbz)-Cys(Bzl)-)Bzl, R2 means -Leu-His(Bzl)-Lys(Cbz)-OMe; R1 means -Leu-His-OMe, R2 means -OMe; R1 means -Gly-Pro-Arg-Gly-Gly-OMe, R2 means -OH; R1 means -Arg-Pro-Pro-Gly-Phe-Ser(Bzl)-Phe-Arg-Gly-Gly-OMe, R2 means -OH. Also, invention relates two methods for preparing derivatives of hemin of the general formula (I), a pharmaceutical composition eliciting ability to inhibit activity of proteolytic enzymes and to application of derivatives of hemin of the formula (I) known early and designated above as inhibitors of activity of the following proteolytic enzymes: HIV proteinase, pepsin, trypsin and chymotrypsin.

EFFECT: improved preparing method, valuable biochemical and medicinal properties of compounds.

14 cl, 2 tbl, 2 dwg, 28 ex

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RU 2 238 950 C2

Authors

Evstigneeva R.P.

Zheltukhina G.A.

Zarubina T.V.

Nebol'Sin V.E.

Nosik D.N.

Nosik N.N.

Dates

2004-10-27—Published

2002-04-25—Filed

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