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1 601 984

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A1

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Application

4470002/04, 1988-08-01

(22)

Actual filing date

1988-08-01

(45)

Published

1995-02-09

(72)

Inventor

Tjukhteneva Z.I.Badovskaja L.A.Tlekhusezh M.A.Linchenko S.N.Bartashevich V.V.Mingalev A.N.Khan V.V.Uvarov A.V.Vas'Kov K.S.Medvedev O.S.Stoljarchuk A.A.Galenko-Jaroshevskij A.P.Ehgik'Jan A.L.Timoshenko Ja.G.Kubantsev A.V.Shejkh-Zade Ju.R.Budarin L.I.Kriss E.E.Arshinnikova L.L.Frantsuzova S.B.Tikhonova N.A.Galenko-Jaroshevskij P.A.Ljufi A.Ja.Onopriev V.V.Porotikov V.I.Bukej T.I.

DERIVATIVE OF 4-HYDROXYBUTYRIC ACID BENZYLAMIDE SHOWING LOCAL ANESTHETIC, ANTIARRHYTHMIC, ANTIANGIAL AND ANTINECROTIC ACTIVITY Russian patent published in 1995 - IPC

Abstract SU 1601984 A1

FIELD: organic chemistry. SUBSTANCE: products - 4-hydroxybutyric acid benzylamide derivatives of the general formula HO--CH2-CHY--CH2-C(O)-NH--CH2-C6H5 where Y - -NH-CH2-C6H5HX at HX: a) 0.5 x [CH2-C(O)OH]2; b) HCl; c) C6H5C(O)OH; d) 0.5 x HO-C(O)-CH(OH)--CH2--C(O)OH. Synthesis is carried out by reaction of 3-benzylamino-4-hydroxy-N-benzylbutaneamide with corresponding acid in inert solvent (ethanol) at 20-70 C. Yield, %; m. p. C; empirical formula; toxicity LD50, mg/kg: a) 95; 114-115; C22H28N2O6; 154; b) 90; 189-190; C18H23N2O2Cl; 11; c) 92; 119-120; no; 220; d) 95; 112-113; no; 129. Compounds a, b and c show antiangial activity additionally, and compounds a and b - antinecrotic one. Activity of new compounds is equal that of lidocaine and exceeds trimecaine (as anesthetic effect); they exceed effect of lithium hydroxybutyrate (as viability of ischemized tissue) and novocaine amide, quinidine, lithium hydroxybutyrate, isotine and ethiosine (as antiarrhythmic effect). EFFECT: enhanced activity of synthesized compounds. 4 cl, 23 tbl

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SU 1 601 984 A1

Authors

Tjukhteneva Z.I.

Badovskaja L.A.

Tlekhusezh M.A.

Linchenko S.N.

Bartashevich V.V.

Mingalev A.N.

Khan V.V.

Uvarov A.V.

Vas'Kov K.S.

Medvedev O.S.

Stoljarchuk A.A.

Galenko-Jaroshevskij A.P.

Ehgik'Jan A.L.

Timoshenko Ja.G.

Kubantsev A.V.

Shejkh-Zade Ju.R.

Budarin L.I.

Kriss E.E.

Arshinnikova L.L.

Frantsuzova S.B.

Tikhonova N.A.

Galenko-Jaroshevskij P.A.

Ljufi A.Ja.

Onopriev V.V.

Porotikov V.I.

Bukej T.I.

Dates

1995-02-09—Published

1988-08-01—Filed

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