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Title:
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 RESPECTIV
Document Type and Number:
WIPO Patent Application WO2006113981
Kind Code:
A3
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.

Inventors:
SILVA MARCIO LUIS ANDRADE E (BR)
BASTOS JAIRO KENUPP (BR)
DONATE PAULO MARCOS (BR)
ALBUQUERQUE SERGIO DE (BR)
SILVA ROSANGELA DA (BR)
Application Number:
PCT/BR2006/000084
Publication Date:
December 14, 2006
Filing Date:
April 28, 2006
Export Citation:
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Assignee:
FUNDACAO DE AMPARO A PESQUISA (BR)
SILVA MARCIO LUIS ANDRADE E (BR)
BASTOS JAIRO KENUPP (BR)
DONATE PAULO MARCOS (BR)
ALBUQUERQUE SERGIO DE (BR)
SILVA ROSANGELA DA (BR)
International Classes:
C07D407/10; C07D407/12; A61K31/36; A61P29/00; C07D407/14
Domestic Patent References:
WO2003080600A12003-10-02
Other References:
DA SILVA FILHO A.A. ET AL.: "Tetrahydrofuran lignans from Nectandra megapotamica with trypanocidal activity", JOURNAL OF NATURAL PRODUCTS, vol. 67, no. 1, 2004, pages 42 - 45, XP003004499
See also references of EP 1917260A4
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