DERIVATIVES OF IMIDAZO-[1,5-A]-PYRIDINE AS INHIBITORS OF SERINE PROTEASES AND PHARMACEUTICAL COMPOSITION Russian patent published in 2001 - IPC

Abstract RU 2175327 C2

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to inhibitor of serine proteases which is a derivative of imidazo-[1,5-a] -pyridine containing structural unit (link) of the general formula (I) where R1 and R2 mean hydrogen atom; R3 and R4 mean independently hydrogen atom, (1-6C)-alkyl or in common they form =CH-NR5R6 being R5 and R6 mean (1-6C)-alkyl; X means hydrogen atom, R7, acetyl, Ртс, R7 = SO2, N-protective group where R7 means (1-12C)-alkyl or (1-14C)-aryl; P3 means a bond, D-Tig, Atc, D-amino acid with hydrophobic side chain; P2 means Pro, Gly, Val, Jle, 2,4-Me-P20, 3,3-Dmp, Jlc, Thr, Hyp, 2,2-Dmt or 5,5-Dmt; or P2 means a bond when P3 means a bond also and X means R7-SO2-; or P2 and P3 in common mean the structure that is similar to dipeptide of the formula (II) which in positions labeled by asterisks can be condensed with benzene ring and where R9 is hydrogen atom; or its pharmaceutically acceptable salt. Invention describes a pharmaceutical composition also. EFFECT: valuable biochemical properties of compounds. 5 cl

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RU 2 175 327 C2

Authors

Khenrikus Karl Jozef Ottenkhejm

Anton Ehgbert Peter Adang

Jakobus Al'Bertus Marija Peters

Dates

2001-10-27Published

1996-05-29Filed