TRICYCLIC HETEROCYCLIC COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS Russian patent published in 2021 - IPC C07D471/16 C07D491/22 C07D498/16 A61K31/53 A61K31/5395 A61P31/18 

Abstract RU 2749043 C2

FIELD: biochemistry.

SUBSTANCE: invention relates to a compound or a pharmaceutically acceptable salt thereof having Formula (I), in which A is -CH(R2)-; X is a 5-membered monocyclic heteroaryl containing 2 ring heteroatoms representing N, or -N(R5)C(O)-; Y is selected from -О-, -N(R5)- or -CH(R3)- or -A-Y- is -C(R2)=CH-; Z is -С(=О), -CH(R4)- or a bond in such a way that: (i) when Y is -О- or -N(R5)-, then Z is -С(=O), (ii) when Y is -CH(R3)-, then Z is a bond or -CH(R4), and (iii) when -А-Y- is -C(R2)=CH-, then Z is a bond; R1 represents a phenyl group which is substituted by 1 to 3 groups, each of which is independently selected from halogen; R2 is selected from Н, -O-(C1-C6alkyl); R3 is selected from Н; in each case R4 is independently selected from Н; in each case R5 independently represents Н or C1-C6alkyl; R7A is Н; R7B is Н or R7A and R7B together with their common carbon atom to which they are attached, combine to form a spirocyclic 4-7-membered monocyclic heterocycloalkyl group containing 1 heteroatom, which is O; and R8 is selected from C1-C6alkyl, -(C16alkylene)-О-(С16alkyl) and -(C16alkylene)-С37cycloalkyl. invention also relates to individual compounds, a pharmaceutical composition, a method for inhibiting HIV integrase in a subject, a method for treating HIV infection or treating, preventing or delaying the onset or progression of AIDS in a subject.

EFFECT: new compounds of Formula (I) have been obtained that inhibit HIV integrase and which can find use in the treatment of HIV infection.

(I)

16 cl, 1 tbl, 22 ex

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RU 2 749 043 C2

Authors

Graham, Thomas, H.

Yu, Tao

Waddell, Sherman, T.

Mccauley, John, A.

Dates

2021-06-03Published

2017-12-01Filed