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PROCESS TO OBTAIN DIBENZYLBUTYROLACTONIC, TETRAHYDROFURANIC LIGNANS AND THEIR SYNTHETIC AND SEMI-SYNTHETIC DERIVATIVES, THEIR ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES, TOPICAL AND/OR SYSTEMIC FORMULATIONS CONTAINING SAID LIGNANS AND THEIR RESPECTIVE THERAPEUTIC METHOD

OfficeEPO
Document type:Patent
Inventor(s): Márcio Luís Andrade E Silva; Jairo Kenupp Bastos; Paulo Marcos Donate; Sergio De Albuquerque; Rosangela Da Silva
Applicant:Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Year: 2006
Application Number:EP 20060721642
IPC: A61K 31/341 A61K 31/36 A61P 29/00 C07D 307/12 C07D 407/06 C07D 407/10 C07D 407/12 C07D 407/14
Abstract

The present invention refers to a process to obtain dibenzylbutyrolactonic lignans from (-)-cubebin, isolated from a Piperaceae, especially Piper cubeba, and from (-)-methylpluviatolide, isolated from a Rutacea, especially Zanthoxylum naranjillo; their synthetic and semi-synthetic derivatives and tetrahydrofuranic lignans, such as galgravin and veragensin, isolated from Nectandra megapotamica, as well as the analgesic and anti-inflammatory activities of said lignans, and the topical and/or systemic formulations where lignans represent 60 to 80% of the formulation. The invention also refers to a therapeutic method using topic and/or systemic formulations based on said lignans for the treatment of inflammation and/or pain. More specifically, it refers to a process to obtain synthetic and semi-synthetic derivatives of (-)-cubebin, such as: (-)-O-acetyl cubebin; (-)-O-methyl cubebin; (-)-O-(N,N-dimethylamino-ethyl)-cubebin; (-)-hinokinin; (-)-6,6'-dinitroinokinin; (-)-O-benzyl cubebin; (-)-6,6'-diaminohinokinin and other synthetic derivatives which may be obtained, and synthetic and semi-synthetic derivatives of (-)-methylpluviatolide, such as (-)-6,6'-dinitromethylpluviatolide and (-)-6,6'-diaminomethylpluviatolide, to be used in the manufacture of medicine that has analgesic and anti-inflammatory activity. The present invention also refers to the process to obtain the substances galgravin and veragensin isolated from Nectandra megapotamica, as well as their synthetic and semi-synthetic derivatives with substituents on the aromatic rings that may be obtained.


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)