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1. WO2001060845 - NOVEL ECHINOCANDIN DERIVATIVES, PREPARATION METHOD AND USE THEREOF AS FUNGICIDES

Publication Number WO/2001/060845
Publication Date 23.08.2001
International Application No. PCT/FR2001/000419
International Filing Date 14.02.2001
Chapter 2 Demand Filed 04.09.2001
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07K 7/56 2006.01
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
56the cyclisation not occurring through 2,4-diamino-butanoic acid
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61P 31/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
10Antimycotics
C07K 7/56
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
56the cyclisation not occurring through 2,4-diamino-butanoic acid
Applicants
  • AVENTIS PHARMA S.A. [FR]/[FR] (AllExceptUS)
  • COURTIN, Olivier [FR]/[FR] (UsOnly)
  • DUSSARAT, Arlette [FR]/[FR] (UsOnly)
  • MELON-MANGUER, Dominique [FR]/[FR] (UsOnly)
  • SCHIO, Laurent [FR]/[FR] (UsOnly)
Inventors
  • COURTIN, Olivier
  • DUSSARAT, Arlette
  • MELON-MANGUER, Dominique
  • SCHIO, Laurent
Agents
  • ROUSSEAU, Pierrick
Priority Data
00/0184415.02.2000FR
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) NOVEL ECHINOCANDIN DERIVATIVES, PREPARATION METHOD AND USE THEREOF AS FUNGICIDES
(FR) NOUVEAUX DERIVES DE L'ECHIOCANDINE, LEUR PROCEDE DE PREPARATION ET LEUR APPLICATION COMME FONGICIDES
Abstract
(EN)
The invention concerns compounds of general formula (I) wherein: R1 represents a hydrogen atom, a hydroxy radical, Ob or Ncd; A represents an oxygen atom, a CH2 radical or a NH radical; B represents the radical of a steroid; R3 represents a hydrogen atom, a methyl or hydroxyl radical; R4 represents a hydrogen atom or a hydroxyl radical; T represents a hydrogen atom, a methyl radical, a CH1CONH2, CH2C$m(Z)N radical, a (CH2)2NH2 or (CH2)2Nalk+X-radical; X being a halogen atom and alc an alkyl radical; Y represents a hydrogen atom, a hydroxyl radical or a halogen atom or a OSO3H radical; W represents a hydrogen atom or a OH radical; Z represents a hydrogen atom or a methyl radical. The compounds of formula (I) exhibit antifungal properties.
(FR)
L'invention a pour objet les composés de formule générale (I) dans lesquels: R1 représente un atome d'hydrogène, un radical hydroxy, Ob ou Ncd; A représente un atome d'oxygène, un radical CH2 ou un radical NH; B représente le reste d'un stéroïde; R3 représente un atome d'hydrogène, un radical méthyle ou hydroxyle; R4 représente un atome d'hydrogène ou un radical hydroxyle; T représente un atome d'hydrogène, un radical méthyle, un radical CH1CONH2, CH2C$m(Z)N, un radical (CH2)2NH2 ou (CH2)2Nalc+X-; X étant un atome d'halogène et alc un radical alkyle; Y représente un atome d'hydrogène, un radical hydroxyle ou un atome d'halogène ou un radical OSO3H; W représente un atome d'hydrogène ou un radical OH; Z représente un atome d'hydrogène ou un radical méthyle. Les composés de formule (I) sont doués de propriétés antifongiques.
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