NUCLEOSIDE PHOSPHONATE CONJUGATES AS ANTI HIV AGENTS

Serbia

PATENT NO 51799
SERIAL NO

P20110303

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Abstract

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The compound of the following formula, wherein R1 and R2 are selected from the following table: R1 R2 EstarAla OPh cPentAla OCH2CF3 EtAla OPh 3-furan-4HAla OPh cButPhe (B) OPh EtPhe (A) OPh EtAla (B) OPh EtPhe OPh sBu ) Phe OPh cBuPhe OCH2CF3 iBuAla (A) OPh EtPhe OPh sBu (R) Ala (B) OPh CH2cPrAla (A) OPh CH2cPrPhe (B) OPh nBuPhe (A) OPh nBuPhe OPh CH2cPrPhe OPh CH2cBuAla OPh 3-pentABA (B) OPh eTab (A) OPh Etal OPh CH2cBuMet OPh ETR1 R2 EstarPro OPh BnPhe (B) OPh iBuPhe (A) OPh iBuPhe OPh iPrPhe OPh NPRA OPh CH2cPrPhe OPh Etal OPh eTab OPh nPentPhe Phe nPrPhe Phe Etal Ala etch OPh MeGly OPh iPrABA OPh nBuPhe OPh AliiAla OPh nPentGly OPh iBuABA OPh iBuAla OPh nBuCHA CHA MePhe Phe AliiABA ABA nPentGly Gly iBuGly Gly iPrPhe OPh iBuAla OPh nPrPhe OPh nBuABA OPh nPrABA OPh Etal Ala Bn R1 R2 EstarPhe OPh nBuABA ABA nPrABA ABA Etal Ala NPRA OPh IPRA OPh BnAla Ala nBuAla Ala iBuABA ABA nBuABA ABA iPrAla OPh iBuABA OPh MeABA OPh iPrABA ABA iBugde Ala represents L-alanine, Phe represents L-phenylalanine n, Met represents L-methionine, ABA represents (S) -2-aminobutyric acid, Pro represents L-proline, CHA represents 2-amino-3- (S) cyclohexyl-propionic acid, Gly represents glycine; R1 or R2 are amino acid carboxylic the groups are esterified as indicated in the ester column, gdecPent is a cyclopent ester; Et is ethyl ester, 3-furan-4H is (R) tetrahydrofuran-3-yl ester; cBut is a cyclobutane ester; sBu (S) is (S) secButyl ester; sBu (R) is (R) secButyl ester; iBu isobutyl ester; CH2cPr is methylcyclopropane ester, nBu is n-butyl ester; CH2cBu is a methylcyclobutane ester; 3-pent is 3-pentyl ester; nPent is nPentyl ester; iPr is isopropyl ester, nPr is nPropyl ester; allyl is an allyl ester; Me is methyl ester; Bn is a benzyl ester; wherever A or B in parentheses denote one stereoisomer on phosphorus, where the less polar isomer is designated as (A) and the polar isomer as (B), or a pharmacologically acceptable salt or solvate thereof. The application contains 11 more claims.

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