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PROCESS TO OBTAIN SYNTHETIC AND SEMI-SYNTHETIC LIGNAN DERIVATIVES, THEIR ANTIPARASITIC ACTIVITIES AND CORRESPONDING PHARMACEUTICAL FORMULATIONS, INCLUDING THE THERAPEUTIC METHOD USING SAID LIGNAN FOR THE TREATMENT OF PARASITOSIS

OfficeEPO
Document type:Patent
Inventor(s): Márcio Luís Andrade E Silva; Rosângela Da Silva; Vanderlei Rodrigues; Olavo Dos Santos Pereira Júnior; Ademar Alves Da Silva Filho; Paulo Marcos Donate; Sérgio De Albuquerque; Jairo Kenupp Bastos
Applicant:Acef S/A; Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Year: 2006
Application Number:EP 20060761026
IPC: A61K 31/59 A61P 33/02 C07D 321/00 C07D 407/10 C07D 407/14 C07J 75/00
Abstract

The invention refers to a process to obtain synthetic and semi-synthetic derivatives of lignans, especially dibenzylbutyrolactonic, tetrahydrofuranic, aryltetralynic, furofuranic and dibenzocyclooctanic lignans obtained by means of partial synthesis and/or full synthesis or also by isolation from plant extracts. It refers to a process to obtain synthetic and semi-synthetic derivatives of (-)-cubebin, such as: (-)-O-acetylcubebin; (-)-O-methylcubebin; (-)-O-N,N-(dimethylamino-ethyl)-cubebin; (-)-hinokinin; (-)-6,6'-dinitroinokinine; (-)-O-benzylcubebin; (-)-6,6'-diaminoinokinin, (-)-6,6'-dinitroinokinin, as well as to obtain dibenzocyclooctanic lignans from dibenzylbutyrolactoinic lignans by means of structural modifications in the positions 7, 7', 8, 8', 9' and in the aromatic rings (introduction and/or substitution of functional groups such as: -OH, -CO2H, -CO2CH3, -NO2, -NH2, -OCH3, -OAc, -SO2CH3, -SO2NH2, prenyl and halogens). The invention also refers to a therapeutic method, since the substances described are used in the manufacture of medicine that presents antiparasitic activity.


Grantee:Márcio Luís Andrade e Silva
Principal Investigator:Márcio Luís Andrade e Silva
Institution: Universidade de Franca (UNIFRAN). Pró-Reitoria Adjunta de Pesquisa e Pós-Graduação
Support Opportunities: Research Grants - Young Investigators Grants

Grantee:Márcio Luís Andrade e Silva
Principal Investigator:Márcio Luís Andrade e Silva
Institution: Universidade de Franca (UNIFRAN). Pró-Reitoria Adjunta de Pesquisa e Pós-Graduação
Support Opportunities: Research Grants - Support for Intellectual Property Rights and Licensing (PAPI/Nuplitec)