CELL-REACTIVE COMPOSTATIN ANALOGUES, LONG-ACTING COMPSTATIN ANALOGUES OR COMPUTED EFFECT ANALOGUES OF TARGETED ACTION AND RELATED COMPOSITIONS AND METHODS Russian patent published in 2019 - IPC C07K7/08 A61K38/10 A61K47/60 A61P37/00 

FIELD: biotechnology.

SUBSTANCE: according to certain aspects, the present invention provides cell-reactive analogues of compstatin and a composition containing cell-reactive analogues of compstatin. Long-acting compstatin analogue contains a clearance-reducing fragment attached to two fragments of the compstatin analogue, wherein each fragment of the compstatin analogue contains a cyclic peptide elongated with a lysine residue or a sequence containing a lysine residue on the N-terminal, a C-terminal or on both ends, wherein said lysine residue is separated from the cyclic part of said peptide by a rigid or flexible spacer containing a fragment of oligo(ethylene glycol), and wherein said cyclic peptide comprises an amino acid sequence presented in any of SEQ ID NOs: 3–36, 71, 72, 73 or 74; said clearance lowering moiety contains a linear polymer, wherein said linear polymer is polyethylene glycol (PEG) with average molecular weight from about 30 kDa to about 40 kDa, wherein each end of said linear polymer is bound to one of fragments of carbamate analogue carbamate, wherein (i) said spacer contains -(CH₂)_m- and -(O-CH₂-CH₂-)_n, connected covalently, where m ranges from 1 to 10, and n ranges from 1 and 10; and/or (ii) said spacer contains 8-amino-3,6-dioxoctanoic acid (AEEAc) or 11-amino-3,6,9-trioxaundecanoic acid.

EFFECT: cell-reactive analogues of compstatin are intended for treating a complement-mediated disorder, for example, for inhibiting complement-mediated cell, tissue or organ damage.

1 cl, 12 tbl, 13 dwg, 7 ex