TETRAHYDROQUINOLINE DERIVATIVES AND BASED PHARMACEUTICAL COMPOSITION FOR HIV INFECTION TREATMENT AND PREVENTION Russian patent published in 2009 - IPC C07D215/38 C07D471/04 A61K31/44 A61K31/47 A61P31/12 

FIELD: chemistry.

SUBSTANCE: present invention refers to tetrahydroquinoline derivatives, described by formula (I) where t is equal to 0, 1 or 2; each R independently represents H, alkyl, alkenyl, alkinyl, halogenalkyl, cycloalkyl; n is equal to 0; R² is chosen from the group consisting of H, alkyl, halogenalkyl, cycloalkyl, -R^acycloalkyl, alkenyl, alkinyl, -R^aAy, -R^aOR⁵; where R² is not substituted with amine or alkylamine; R³ represents H; each R⁴ independently represents halogen, halogenalkyl, alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, -A'y, -NHAy, -Het, -NHHet, -OR¹⁰, -NR⁶R⁷, -R^aNR⁶R⁷, -C(O)NR⁶R⁷, -C(O)Ay, -C(O)Het; m is equal to 0, 1 or 2; each R⁵ independently represents H; p is equal to 0 or 1; Y represents NR¹⁰-, -O-, -C(O)NR¹⁰-, -NR¹⁰C(O)-, -C(O)- , - -NR¹⁰C(O)N(R¹⁰)-; X represents -N(R¹⁰)₂, -R^aN(R¹⁰)₂, -AyN(R¹⁰)₂, -R^aAyN(R¹⁰)₂, -AyR^aN(R¹⁰)₂, -R^aAyR^aN(R¹⁰)₂, -Het, -R^aHet, -HetN(R¹⁰)₂, -R^aHetN(R¹⁰)₂, -HetR^aN(R¹⁰)₂, - R^aHetR^aN(R¹⁰)₂; each R^a independently represents alkylen, optionally substituted with with one or more alkyl; each R¹⁰ independently represents H, alkyl, cycloalkyl, alkenyl, alkinyl, cycloalkenyl, -R^acycloalkyl; each R⁶ and R⁷ is independently chosen from H, alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, -R^acycloalkyl, -R^aNR⁸R⁹; each R⁸ and R⁹ is independently chosen from H or alkyl; each Ay independently represents optionally substituted aryl group; and each Het independently represents optionally substituted 4-, 5- or 6-merous heterocyclil or heteroaryl group where heteroatoms are chosen from N and O; or its pharmaceutically acceptable salt, or ester. Besides, there are disclosed pharmaceutical composition based on compound of formula (I), its application and methods of production.

EFFECT: new compound manifesting protective action against HIV-infection on target cell by chemoquine receptor and influencing binding of natural ligand or chemoquine and target cell receptor, such as CXCR4 and/or CCR5.

53 cl, 2 tbl, 105 ex