SUBSTITUTED DERIVATIVES OF DIAMINO-1,3,5-TRIAZINE, METHODS OF THEIR SYNTHESIS, INTERMEDIATE COMPOUND, PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING Russian patent published in 2002 - IPC

Abstract RU 2186774 C2

FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention describes derivatives of diamino-1,3,5-triazine of the general formula (I) or their pharmaceutical acceptable acid additive salt or their stereochemically isomeric forms where R1 and R2 each means independently hydrogen atom, hydroxy-group, amino-group, C1-6-alkyloxy-group, C1-6-alkylcarbonyl, C1-6-alkyloxycarbonyl, phenyl substituted with cyano-group, mono- or di-(C1-6-alkyl)-aminocarbonyl, dihydro-2-(3H)-furanone, unsubstituted C1-6-alkyl or that substituted with one or two substituents each of that is taken independently among amino-group, imino-group, aminocarbonyl, aminocarbonylamino-group, hydroxy-group, hydroxy-C1-6-alkyloxy-group, carboxyl, mono- or di-(C1-6-alkyl)-amino-group, C1-6-alkyloxycarbonyl and thienyl; or R1 and R2 taken in common can form azido- and mono- or di-(C1-6-alkyl)- -amino-C1-4-alkylidene; R3 means hydrogen atom, phenyl substituted with cyano-group, C1-6-alkylcarbonyl, C1-6-alkyloxycarbonyl, unsubstituted C1-6-alkyl or that substituted with C1-6-alkyloxycarbonyl; R4 and R8 each means hydrogen atom; R5 and R7 each means hydrogen atom or cyano-group; R6 means cyano-group or aminocarbonyl; L means C3-10-alkenyl or C1-10-alkyl substituted with one or two substituents taken independently among C3-7-cycloalkyl, indolyl substituted with halogen atom, unsubstituted phenyl or phenyl substituted with 1-5 substituents each of that is taken independently among halogen atom, hydroxy-group, C1-6-alkyl, C1-6-alkyloxy-group, trihalogenmethyl, trihalogenmethyloxy-group, C1-6/ -alkylcarbonyl. Invention relates to also intermediate compounds of the formula (IV) used in synthesis, a pharmaceutical composition inhibiting replication of human immunodeficiency virus, method of its preparing and methods of synthesis of compounds of the formula (I). EFFECT: improved methods of synthesis, valuable medicinal properties of compounds and pharmaceutical composition. 17 cl, 6 tbl, 22 ex

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RU 2 186 774 C2

Authors

Kukla Majkl Dzhozef

Ljudovisi Donal'D V.

Zhansen Pol' Adrian Zhan

Geres Jan

Merel' Anri Ehmil' Lodevijk

Dates

2002-08-10Published

1997-09-30Filed