PRODRUG FORMING COMPOUNDS Russian patent published in 2018 - IPC C07J41/00 C07J43/00 A61K31/56 A61K31/568 A61P5/30 A61P5/26 A61P5/34 

Abstract RU 2667942 C2

FIELD: chemistry.

SUBSTANCE: invention describes prodrug compounds having a general structure: active agent - (acid)-(linker) - SO2NR1R2 :

where R1 represents H, C1-C12alkyl or C1-C12alkylC6-C10aryl; hAr represents C6-C10 aryl or 5-7 membered monocyclic heterocyclic ring or 7-10 membered bicyclic heterocyclic ring containing 1-4 heteroatoms selected from N, O and S; R2 represents H or C1-C12alkyl; R1 and R2 can be combined to form a 3-7-membered ring containing up to one heteroatom; each R3 and R4 independently represents H or C1-C12alkyl; X and Y represents H; Z represents O; and the active agent is androgen, estrogen or progestin.

EFFECT: compounds having this general structure (1) have a higher activity when administered orally than the unmodified parent molecule.

17 cl, 3 tbl

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RU 2 667 942 C2

Authors

Nikish Klaus

Santamma Bindu

Akhmed Gulzar

Mis Frederik

Elger Valter

Virma Ralf

Nair Kharesh

Dates

2018-09-27Published

2014-07-11Filed