Title:
感染治療のための有機リン化合物の使用
Document Type and Number:
Japanese Patent JP2004505011
Kind Code:
A
Abstract:
Phosphinoyl, phosphinic acid or phosphonic acid derivatives (I), containing an amino or imino substituent linked to phosphorus via a nitrogen-containing spacer group, are used for the treatment of viral, bacterial, fungal or parasitic infections in humans or animals or as fungicides, bactericides or herbicides for use in plants. The use of organophosphorus compounds of formula (I), or their salts, esters, amides or ester salts, is claimed for the treatment of viral, bacterial, fungal or parasitic infections in humans or animals or as a fungicide, bactericide or herbicide for use in plants: [Image] R3, R4H; 1-26C alkyl, 1-26C hydroxyalkyl, aryl, acyl, aralkyl, 2-26C alkenyl, 2-26C alkynyl, cycloalkyl or heterocyclyl (all optionally substituted); or halo, OX3 or OX4; X3, X4H; 1-26C alkyl, 1-26C hydroxyalkyl, aryl, aralkyl, 2-26C alkenyl, 2-26C alkynyl, cycloalkyl or heterocyclyl (all optionally substituted); silyl; or a cation of an (in)organic base (especially a Group I-III non-transition metal, optionally substituted ammonium, ethylenediamine or aminoacid cation); B' : R1R2N-A- or R1-N=A-; A : alkyleneamine, alkenyleneamine, alkyleneimine or alkenyleneimine chain (all optionally substituted), in which the N atom is present in the chain linking the P atom of (I) to the N atom of R1R2N- or R1-N=; R1, R2H; alkyl, hydroxyalkyl, alkenyl, alkynyl, aryl, acyl, cycloalkyl, aralkyl or heterocyclyl (all optionally substituted); or halo, OX1 or OX2; and X1, X2H; or alkyl, hydroxyalkyl, alkenyl, alkynyl, aryl, acyl, cycloalkyl, aralkyl or heterocyclyl (all optionally substituted). - ACTIVITY : Antibacterial; fungicide; virucide; protozoacide; herbicide; dermatological; antiseborrheic; tuberculostatic; antiulcer; heptotropic; antiinflammatory; amebicide; coccidiostatic; cytostatic. N-(N-Benzoyl-N-hydroxy-aminomethyl)-aminomethyl-dimethyl-phosphine oxide (Ia) had MIC 420 nM against the malarial parasite Plasmopara falciparum in vitro. - MECHANISM OF ACTION : 1-Desoxy-D-xylulose-5-phosphate (DOXP) reductoisomerase inhibitor. (Ia) had IC50 80 nM against DOXP from Helicobacter pylori.
Inventors:
Hassan, Yommer
Application Number:
JP2001568435A
Publication Date:
February 19, 2004
Filing Date:
March 21, 2001
Export Citation:
Assignee:
JOMAA PHARMAKA GMBH
International Classes:
A61K31/662; A01N57/18; A01N57/20; A01N57/24; A61K31/66; A61K31/665; A61K31/675; A61P31/00; A61P31/04; A61P31/10; A61P31/12; A61P33/00; A61P33/06; C07F9/30; C07F9/38; C07F9/40; C07F9/53; C07F9/6533; C07F9/655; (IPC1-7): C07F9/30; A01N57/20; A01N57/24; A61K31/662; A61P31/00; A61P31/10; A61P31/12; A61P33/00; C07F9/40; C07F9/53; C07F9/6533; C07F9/655
Attorney, Agent or Firm:
Kenji Yoshitake
Yukitaka Nakamura
Konno Akio
Noritaka Yokota
Yukitaka Nakamura
Konno Akio
Noritaka Yokota