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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

Document type:Patente
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)
Deposit date: April 2006, 28
INPI register:
US11/912,645
IPC: A61P 29/00 C07D 407/14 A61K 31/357 C07D 407/12 A61K 31/36 C07D 307/02 C07D 317/46
Abstract

The present invention refers to a process to obtain dibenzylbutyrolactonic lignans form (-)- cubebin, insolate from a Piperaceae, especially Piper cubeba, and from (-)-methylpluviatolide insolated form a Rutacea, especially Zanthoxylum naranjillo; their synthetic and semisyntheti derivatives and tetrahydrofuranic lignans, such as glagravin and veragensin, insolated form Nectandra meapotamica, as well as the analgesic and anti-inflammatory activities of said lignans, and the topical and/or systemic formulatins where lignans present 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-acet l cubebin; - -O-meth l cubebin - -O- N N-dimeth lamino-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 ot obtain the substances glagravin and veragensin islated 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)