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1. WO2000043414 - TRIPEPTIDE COMPOUNDS USEFUL AS SELECTIVE INHIBITORS OF AMINOPEPTIDASE A AND CORRESPONDING PHARMACEUTICAL COMPOSITIONS

Publication Number WO/2000/043414
Publication Date 27.07.2000
International Application No. PCT/FR2000/000112
International Filing Date 19.01.2000
Chapter 2 Demand Filed 31.07.2000
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 5/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
C07K 5/065 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
065the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61P 13/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
02of urine or of the urinary tract, e.g. urine acidifiers
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
C07K 5/06034
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06008with the first amino acid being neutral
06017and aliphatic
06034the side chain containing 2 to 4 carbon atoms
C07K 5/06078
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06008with the first amino acid being neutral
06078and aromatic or cycloaliphatic
Applicants
  • INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) [FR/FR]; 101, rue de Tolbiac F-75013 Paris, FR (AllExceptUS)
  • CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) [FR/FR]; 3, rue Michel-Ange F-75016 Paris, FR (AllExceptUS)
  • ROQUES, Bernard [FR/FR]; FR (UsOnly)
  • FOURNIE-ZALUSKI, Marie-Claude [FR/FR]; FR (UsOnly)
  • BISCHOFF, Laurent [FR/FR]; FR (UsOnly)
  • DAVID, Christelle [FR/FR]; FR (UsOnly)
  • LLORENS-CORTES, Catherine [FR/FR]; FR (UsOnly)
Inventors
  • ROQUES, Bernard; FR
  • FOURNIE-ZALUSKI, Marie-Claude; FR
  • BISCHOFF, Laurent; FR
  • DAVID, Christelle; FR
  • LLORENS-CORTES, Catherine; FR
Agents
  • MONCHENY, Michel; Cabinet Lavoix 2, place d'Estienne d'Orves F-75441 Paris Cedex 09, FR
Priority Data
99/0058720.01.1999FR
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) TRIPEPTIDE COMPOUNDS USEFUL AS SELECTIVE INHIBITORS OF AMINOPEPTIDASE A AND CORRESPONDING PHARMACEUTICAL COMPOSITIONS
(FR) COMPOSES TRIPEPTIDIQUES UTILES A TITRE D'INHIBITEURS SELECTIFS DE L'AMINOPEPTIDASE A ET COMPOSITIONS PHARMACEUTIQUES CORRESPONDANTES
Abstract
(EN)
The invention concerns a compound of general formula (I) wherein: R1 represents an alkyl, alkenyl or alkynyl chain, or a cycloalkyl, or (cycloalkyl)alkyl group substituted by at least a COOH, SO3H, PO3H2 or tetrazolyl group; R2 represents an alkyl chain, or an aryl, arylalkyl, cycloalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl group substituted or not by at least a OH, OR, SR', NH2,NHR', guanidinyl, COOH, CONH2 group, or a halogen atom; R3 represents a hydrogen atom or a methyl group; R4 represents a) an alkyl chain, an aryl, alrylalkyl, cycloalkyl, (cycloalkyl)alkyl, (heteroalkyl)alkyl, heterocycloalkyl or (heterocycloalkyl)alkyl group substituted by at least a CONH2, SO3H, SO2NH2, PO3H2 or tetrazolyl group; b) a C2-C6 alkyl chain, an aryl, arylalkyl, cycloalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl group substituted by at least a CO2H group capable of being protected as described above; or c) R3 and R4 can together form a heterocyclic compound, with 5 to 6 links, substituted by at least a CO2H, CONH2, SO3H, SO2NH2 or PO3H2 group; X represents a CONH or CH2NH; and Z represents a OH, OCH2-C6H5 or NR''R''' group.
(FR)
La présente invention a pour objet un composé de formule générale (I), dans laquelle R1 représente une chaîne alkyle, alkényle ou alkynyle, ou un groupement cycloalkyle, ou (cycloalkyle)alkyle substituée par au moins un groupement COOH, SO3H, PO3H2, ou tétrazolyle; R2 représente une chaîne alkyle, ou un groupement aryle, arylalkyle, cycloalkyle, (cycloalkyle)alkyle, (héteroarly)alkyle substituée ou non par au moins un groupement OH, OR, SR', NH2, NHR', guanidinyle, COOH, CONH2, ou un atome d'halogène; R3 représente un atome d'hydrogène ou un groupement méthyle; R4 représente: a) une chaîne alkyle, un groupement aryle, arylalkyle, cycloalkyle, (cycloalkyl)alkyle, (hétéroaryl)alkyle, hétérocycloalkyle ou (hétérocycloalkyl)alkyle substituée par au moins un groupement CONH2, SO3H, SO2NH2, PO3H2 ou tétrazolyle; b) une chaîne alkyle en C2 à C6, un groupement aryle, arylalkyle, cycloalkyle, (cycloalkyl)alkyle, (hétéroaryl)alkyle, hétérocycloalkyle ou (hétérocycloalkyl)alkyle substituée par au moins un groupement CO2H pouvant être protégés comme décrit ci-dessus; ou c) R3 et R4 peuvent constituer ensemble un composé hétérocyclique, à 5 ou 6 chaînons, substitué par au moins un groupement CO2H, CONH2, SO3H, SO2NH2 ou PO3H2; X représente un groupement CONH ou CH2NH, et Z représente un groupement OH, OCH2-C6H5 ou NR''R'''.
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