US 9,808,535 B2
Conjugates for protection from nephrotoxic active substances
Armin Kuebelbeck, Bensheim (DE); Gregor Larbig, Gelnhausen (DE); Stefan Arnold, Muenster (DE); Walter Mier, Bensheim (DE); and Uwe Haberkorn, Schwetzingen (DE)
Assigned to MERCK PATENT GMBH, Darmstadt (DE)
Appl. No. 14/889,553
Filed by Merck Patent GmbH, Darmstadt (DE)
PCT Filed Apr. 16, 2014, PCT No. PCT/EP2014/001025
§ 371(c)(1), (2) Date Nov. 6, 2015,
PCT Pub. No. WO2014/180533, PCT Pub. Date Nov. 13, 2014.
Claims priority of application No. 13002431 (EP), filed on May 7, 2013.
Prior Publication US 2016/0114054 A1, Apr. 28, 2016
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 47/48 (2006.01); A61K 51/08 (2006.01); A61K 31/192 (2006.01); A61K 31/385 (2006.01)
CPC A61K 47/48315 (2013.01) [A61K 31/192 (2013.01); A61K 31/385 (2013.01); A61K 51/08 (2013.01)] 7 Claims
OG exemplary drawing
 
1. A conjugate containing at least one kidney-selective carrier molecule and at least one active compound which has a protective action for the kidney against nephrotoxic active compounds,
wherein the at least one kidney-selective carrier molecule is
an oligopeptide comprising multiple monomeric peptides comprising more than 50% (based on the number of amino acid units) of sequence sections selected from the group consisting of -(KKEEE)-, -(RREEE)-, -(KKKEEE)- and -(KKKEE)-, wherein
(i) the peptide or oligopeptide overall has a chain length of 15 to 100 amino acid units;
(ii) the peptide or oligopeptide comprises at least 50% (based on the number of amino acid units) of amino acids K and E, or R and E, respectively; and
(iii) the oligopeptide comprises at least 3 consecutive sequence sections; wherein the at least one active compound is selected from the group consisting of lipoic acid, resveratrol, caffeic acid, luteolin, quercetin, rutin, cyanidin, xanthohumol, ascorbic acid, nicotinic acid, amifostin, alliin, thiols, tocopherols, carotinoids, butylhydroxytoluene (BHT), pifithrin-μ, pifithrin-α, MDL 28170 and NS3694, and combinations thereof.