Global Patent Index - EP 0000473 A1

EP 0000473 A1 19790207 - Process for preparing aminoglycoside derivatives, novel derivatives obtained and pharmaceutical compositions containing such derivatives.

Title (en)

Process for preparing aminoglycoside derivatives, novel derivatives obtained and pharmaceutical compositions containing such derivatives.

Title (de)

Verfahren zur Herstellung von Amino-glucosidderivaten, erhaltene Derivate und diese enthaltende pharmazeutische Zusammensetzungen.

Title (fr)

Procédé de préparation de dérivés amino-glucosides, dérivés obtenus et compositions pharmaceutiques les contenant.

Publication

EP 0000473 A1 19790207 (EN)

Application

EP 78100207 A 19780621

Priority

US 80983977 A 19770624

Abstract (en)

This invention relates to a process for preparing 2 min -hydroxy-2 min - desamino-4,6-di-O-(aminoglycosyl) -1,3-diaminocyclitols having a 6 min -amino function and pharmaceutically acceptable acid addition salts thereof, to novel compounds and salts obtained by this process; and to novel antibacterially active compositions comprising such novel compounds or salts. The process comprises reacting the corresponding N-protected (except the 2 min -amino)-4,6-di-O- (aminoglycosyl)-1,3,-diaminocyclitol with hydrogen peroxide in the presence of tungstate ion, followed by cleavage of the thereby formed 2 min -oximino derivative and by reduction of the resulting 2 min -oxo derivative and by removal of the N-protecting groups. The preferred group of novel compounds obtained by this process are the 1-N- ( omega -amino- alpha - hydroxyalkanoyl) -2 min -hydroxy-2 min - desamino-4,6-di-O- (aminoglycosyl)- 1,3-diaminocyclitols. The compounds obtained by the process of this invention exhibit antibacterial activity

IPC 1-7

C07H 15/22; A61K 31/70

IPC 8 full level

A61K 31/70 (2006.01); A61K 31/7028 (2006.01); A61K 31/7034 (2006.01); A61K 31/7036 (2006.01); A61P 31/04 (2006.01); C07H 15/234 (2006.01); C07H 15/236 (2006.01)

CPC (source: EP)

A61P 31/04 (2018.01); C07H 15/234 (2013.01); Y02P 20/55 (2015.11)

Citation (search report)

  • [X] FR 2201872 A1 19740503 - SCHERICO LTD [CH]
  • [X] FR 2289202 A1 19760528 - PFIZER [PA]
  • FR 2293941 A1 19760709 - BRISTOL MYERS CO [US]
  • FR 2218879 A2 19740920 - BRISTOL MYERS CO [US]
  • [X] REAGENTS FOR ORGANIC SYNTHESIS; Fieser and Fieser, vol. 1, Wiley 1967 New York. Page 475
  • [X] STICKSTOFFVERBINDUNGEN I, Band 10, Teil 4, Houben-Weyl G.Thieme Verlag, Stuttgart 1968. Page 269
  • [X] THE JOURNAL OF ANTIBIOTICS 29(4) (1976) pages 319-353.
  • THE JOURNAL OF ANTIBIOTICS 27 (11) (1974) pages 851-858.

Designated contracting state (EPC)

BE CH DE FR GB NL SE

DOCDB simple family (publication)

EP 0000473 A1 19790207; EP 0000473 B1 19810311; DE 2860513 D1 19810409; DK 283478 A 19781225; IT 1097278 B 19850831; IT 7824904 A0 19780623; JP S5412347 A 19790130

DOCDB simple family (application)

EP 78100207 A 19780621; DE 2860513 T 19780621; DK 283478 A 19780623; IT 2490478 A 19780623; JP 7633778 A 19780623