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1. WO2010029196 - ANTIBACTERIAL PEPTIDE COMPOUNDS

Publication Number WO/2010/029196
Publication Date 18.03.2010
International Application No. PCT/ES2009/000445
International Filing Date 09.09.2009
IPC
C07K 7/62 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
50Cyclic peptides containing at least one abnormal peptide link
54with at least one abnormal peptide link in the ring
60the cyclisation occurring through the 4-amino group of 2,4-diamino-butanoic acid
62Polymyxins; Related peptides
A61K 38/12 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
12Cyclic peptides
A61P 31/04 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 38/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
12Cyclic peptides ; , e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
C07K 7/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04Linear peptides containing only normal peptide links
06having 5 to 11 amino acids
C07K 7/62
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
50Cyclic peptides containing at least one abnormal peptide link
54with at least one abnormal peptide link in the ring
60the cyclisation occurring through the 4-amino group of 2,4-diamino-butanoic acid
62Polymyxins; Related peptides
Y02A 50/30
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
50in human health protection, e.g. against extreme weather
30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Applicants
  • UNIVERSIDAD DE BARCELONA [ES]/[ES] (AllExceptUS)
  • RABANAL ANGLADA, Francesc [ES]/[ES] (UsOnly)
  • CAJAL VISA, Yolanda [ES]/[ES] (UsOnly)
  • GARCIA SUBIRATS, Maria [ES]/[ES] (UsOnly)
  • RODRÍGUEZ NUÑEZ, Montserrat [ES]/[ES] (UsOnly)
Inventors
  • RABANAL ANGLADA, Francesc
  • CAJAL VISA, Yolanda
  • GARCIA SUBIRATS, Maria
  • RODRÍGUEZ NUÑEZ, Montserrat
Agents
  • SEGURA CÁMARA, Pascual
Priority Data
P20080262610.09.2008ES
Publication Language Spanish (es)
Filing Language Spanish (ES)
Designated States
Title
(EN) ANTIBACTERIAL PEPTIDE COMPOUNDS
(ES) COMPUESTOS PEPTÍDICOS ANTIBACTERIANOS
(FR) COMPOSÉS PEPTIDIQUES ANTIBACTÉRIENS
Abstract
(EN) Compounds of formula (I), or retroenantiomers thereof unacylated at their N-terminal end and having the configuration of the aminoacid with the R2 side chain non-inverted when R2 is -CH(CH3)(OH), wherein R0 is CH3-(CH2)m-, CH3-O-(CH2CH2O)2CH2- or phenyl-(CH2)x-; m is an integer between 7 and 10; x is an integer between 1 and 3; R1, R3, R4, R7 and R8 are independently selected from the formula GF-(CH2)n-, wherein n is an integer between 1 and 4; and GF is -NH2, -NH-C(=NH)-NH2 or 4-imidazolyl; R2 is -CH(CH3)(OH), -CH(CH3)2, -CH2NH2 or -CH2OH; R5 and R6 are -(C1-C4-linear or branched alkyl, -(CH2)-R10, -CH2-CH2-S-CH3 or -CH2-CH2-S(=O)-CH3; R9 is H or Gly-spermide; and R10 is phenyl, 3-indolyl, 4-imidazolyl, 4-hydroxyphenyl, α- or β-naphthyl or 2-, 3- or 4-pyridyl, have been found to be useful in the treatment of bacterial infections.
(ES) Los compuestos de formula (I), o retroenantiόmeros de los mismos no acilados en su extremo N-terminal y con la configuraciόn del aminoácido con la cadena lateral R2 no invertida cuando R2 es -CH(CH3)(OH), donde: R0 es CH3-(CH2)m-, CH3-O-(CH2CH2O)2CH2- o fenil-(CH2)x-; m es un entero entre 7 y 10; x es un entero entre 1 y 3; R1, R3, R4, R7 y R8 se seleccionan independientemente de la formula GF-(CH2)n- donde n es un entero entre 1 y 4; y GF es -NH2, -NH-C(=NH)-NH2 o 4-imidazolilo; R2 es -CH(CH3)(OH), -CH(CH3)2, -CH2NH2 o -CH2OH; R5 y R6 son -(C1-C4-alquilo lineal o ramificado, -(CH2)-R10, -CH2-CH2-S-CH3 o -CH2-CH2-S(=O)-CH3; Rg es H o Gly-espermida; y R10 es fenilo, 3-indolilo, 4-imidazolilo, 4-hidroxifenilo, α o β- naftilo o 2-, 3- o 4-piridilo, se ha encontrado que son ύtiles en el tratamiento de infecciones bacterianas.
(FR) L'invention concerne des composés représentés par la formule (I), ou des rétroénantiomères de ces derniers non acylés à leur extrémité N terminale et présentant une configuration de l'acide aminé à chaîne latérale R2 non inversée lorsque R2 est -CH(CH3)(OH), où: R0 est CH3-(CH2)m-, CH3-O-(CH2CH2O)2CH2- ou phényl-(CH2)x-; m est un entier compris entre 7 et 10; x est un entier compris entre 1 et 3; R1, R3, R4, R7 et R8 sont sélectionnés indépendamment de la formule GF-(CH2)n- dans laquelle n est un entier compris entre 1 et 4; et GF est -NH2, -NH-C(=NH)-NH2 ou 4-imidazolyle; R2 est -CH(CH3)(OH), -CH(CH3)2, -CH2NH2 ou -CH2OH; R5 et R6 sont -(C1-C4-alkyle linéaire ou ramifié, -(CH2)-R10, -CH2-CH2-S-CH3 ou -CH2-CH2-S(=O)-CH3; Rg est H ou Glu-spermine; et R10 est phényle, 3-indolyle, 4-imidazolyle, 4-hydroxyphényle, α ou β- naphtyle ou 2-, 3- ou 4-pyridyle. Lesdits composés ou énantiomères se révèlent être utiles dans le traitement d'infections bactériennes.
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