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1. WO1996041800 - ISOLATION OF NATURALLY OCCURRING ISOFLAVANONE AND SOME CLINICAL USES THEREOF

Publication Number WO/1996/041800
Publication Date 27.12.1996
International Application No. PCT/AP1996/000002
International Filing Date 24.04.1996
Chapter 2 Demand Filed 05.11.1996
IPC
C07D 311/38 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo pyrans, not hydrogenated in the carbocyclic ring
22with oxygen or sulfur atoms directly attached in position 4
26with aromatic rings attached in position 2 or 3
34with aromatic rings attached in position 3 only
382, 3-Dihydro derivatives, e.g. isoflavanones
C07D 311/40 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo pyrans, not hydrogenated in the carbocyclic ring
22with oxygen or sulfur atoms directly attached in position 4
26with aromatic rings attached in position 2 or 3
40Separation, e.g. from natural material; Purification
CPC
C07D 311/38
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
22with oxygen or sulfur atoms directly attached in position 4
26with aromatic rings attached in position 2 or 3
34with aromatic rings attached in position 3 only
382,3-Dihydro derivated, e.g. isoflavanones
C07D 311/40
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
22with oxygen or sulfur atoms directly attached in position 4
26with aromatic rings attached in position 2 or 3
40Separation, e.g. from natural material; Purification
Applicants
  • CHAVUNDUKA, Gordon, Lloyd [ZW]/[ZW] (AllExceptUS)
  • UNIVERSITY OF ZIMBABWE [ZW]/[ZW] (AllExceptUS)
  • ZIMBABWE NATIONAL TRADITIONAL HEALERS ASSOCIATION (ZINATHA) [ZW]/[ZW] (AllExceptUS)
  • MASHAVA, Peter [ZW]/[MW]
Inventors
  • MASHAVA, Peter
Common Representative
  • MASHAVA, Peter, N.
Priority Data
89/9512.06.1995ZW
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ISOLATION OF NATURALLY OCCURRING ISOFLAVANONE AND SOME CLINICAL USES THEREOF
(FR) ISOLEMENT DE L'ISOFLAVANONE NATURELLE ET QUELQUES EMPLOIS CLINIQUES DE CETTE SUBSTANCE
Abstract
(EN)
The compound of formula (II), designated as 'PMZ-1', was isolated from $i(Bolusanthus speciosus (Bolus) Harms). PMZ-1 is active against HIV-1RF (EC50 = 0.1 $g(m)M) and HIV-1IIIB (EC50 = 0.2 $g(m)M) with cytotoxic concentrations (IC50) of 30 to 50 $g(m)M respectively. PMZ-1 has a broad therapeutic index (TI > 300). The compound shows good activity when tested in the fresh human peripheral blood mononuclear cells (PBMC's, EC50 < 1 $g(m)M) and monocytes/macrophages (Mono/MAC's, EC50 < 1 $g(m)M) assays. It inhibited protease enzymatic activity (ID50 = 3.8 $g(m)M) and integrase enzymatic activity (ID50 = 40 $g(m)M). It shows activity against breast cancer.
(FR)
Le composé représenté par la formule (II), désigné par 'PMZ-1', a été isolé à partir de $i(Bolusanthus speciosus (Bolus) Harms). Le PMZ-1 présente une activité contre le VIH-1RF (EC50 = 0,1 $g(m)M) et le VIH-1IIIB (EC50 = 0,2 $g(m)M), avec des concentrations cytotoxiques (IC50) de 30 à 50 $g(m)M respectivement. LePMZ-1 présente un large indice thérapeutique (IT > 300). Ce composé fait preuve d'une activité satisfaisante quand il est essayé dans les cellules mononucléaires fraîches du sang humain périphérique (PBMC, EC < 1 $g(m)M) et dans les dosages monocytes-macrophages (mono-mac, EC50 < 1 $g(m)M). Il a inhibé l'activité enzymatique de la protéase (ID50 = 3,8 $g(m)M) et de l'intégrase (ID50 = 40 $g(m)M). Il manifeste une activité contre le cancer du sein.
Also published as
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