Publication number: 20180086792
Abstract: Synthetic analogs of general formula (I-A), (I-A) a-Ile-b-c-d-e-f-Lys-Lys-g-h-i-j-Ile-k-Lys-NH2 where a is Gly, Lys or ?-Ala; b is Met, Leu, Nle, Ile, Trp, Val or Phe; c is Ser, Lys, Arg or Orn; d is Ser, Lys, Arg or Orn; e is Leu, Nle, Ile, Trp, Val or Phe; f is Met, Leu, Nle, Ile, Trp, Val or Phe; g is Leu, Nle, Ile or Trp; h is Lys, Arg, Orn or Ala; i is Lys, Arg, Orn or Ala; j is Ile, Leu, Nle or His; k is Lys, Arg, Orn or Ala; where amino acids in all positions may be in D-configuration, and their use for the treatment of topical infections caused by pathogenic bacteria or yeasts.
Type:
Application
Filed:
April 8, 2016
Publication date:
March 29, 2018
Applicants:
USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., FYZIOLOGICKY USTAV AV CR, V.V.I.
Inventors:
Vaclav CEROVSKY, Ondrej NESUTA, Vlasta DUDKOVA, Hana SYCHROVA, Marie KODEDOVA
Publication number: 20170096433
Abstract: Helquat derivatives of general formula I, in which substituents R1 and R2 are independently selected from a group comprising H and C1 to C4 alkyl, up to three of S1,2, S1?,2?, S3,4 and S3?,4? are present, each of S1,2, S1?,2?, S3,4 and S3?,4? independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2?, and 4? are substituted with a substituent R3 of general formula II, wherein R4 is substituted or unsubstituted heteroaryl, T1 and T2 are independent linkers that bridge atoms N5 with C8 and N5? with C8?, wherein T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X1)? and (X2)? independently represent anions of pharmaceutically acceptable salts.
Type:
Application
Filed:
May 26, 2015
Publication date:
April 6, 2017
Applicants:
USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., VYSOKA SKOLA CHEMICKO-TECHNOLOGICKA V PRAZE
Inventors:
Filip TEPLY, Miroslav HAJEK, Erika KUZMOVA, Jaroslav KOZAK, Veronika KOMARKOVA, Pavla HUBALKOVA, Paul Eduardo REYES-GUTIERREZ, Michael JIRASEK, Manoj R. SONAWANE, Vishwas D. JOSHI, Lukas SEVERA, Jana NOVOTNA