PROCESS TO OBTAIN EXTRACTS, FRACTIONS AND ISOLATED COMPOUNDS FROM COPAIFER SPECIES AND THEIR USE FOR THE TREATMENT OF URINARY LITHIASIS IN HUMAN BEINGS AND ANIMALS - Patent Articles

PROCESS TO OBTAIN EXTRACTS, FRACTIONS AND ISOLATED COMPOUNDS FROM COPAIFER SPECIES AND THEIR USE FOR THE TREATMENT OF URINARY LITHIASIS IN HUMAN BEINGS AND ANIMALS
Publication Number: WO/2005/110446 International Application No.: PCT/BR2005/000052
Publication Date: 24.11.2005 International Filing Date: 12.04.2005
Chapter 2 Demand Filed: 15.02.2006

Int. Class.7: A61K 35/78, A61P 13/04
Applicants: BRUNHAROTO, Aurita Rodrigues Flores [BR/BR]; Rua S?o Luis, 519, Apto. 100, Centro, 17500-001 Marilia - SP (BR).
BRUNHAROTO JR., Claudino [BR/BR]; Rua S?o Luis, 519, Apto. 100, Centro, 17500-001 Marilia - SP (BR) (US Only).
BRUNHAROTO, Luis Paulo Flores [BR/BR]; Rua S?o Luis, 519, Apto. 100, Centro, 17500-001 Marilia - SP (BR) (US Only).
BASTOS, Jairo Kenupp [BR/BR]; Avenida Caramuru, 1280, Apto. 61, Republica, 14030-00 Ribeir?o Preto - SP (BR) (US Only).
CARVALHO, Jos? Carlos Tavares [BR/BR]; Rua Alfredo Leite da Silva, 1415, Boa Esperan?a, 37130-000 Alfenas - MG (BR) (US Only).
Inventors: BRUNHAROTO, Aurita Rodrigues Flores [BR/BR]; Rua S?o Luis, 519, Apto. 100, Centro, 17500-001 Marilia - SP (BR).
BRUNHAROTO JR., Claudino [BR/BR]; Rua S?o Luis, 519, Apto. 100, Centro, 17500-001 Marilia - SP (BR).
BRUNHAROTO, Luis Paulo Flores [BR/BR]; Rua S?o Luis, 519, Apto. 100, Centro, 17500-001 Marilia - SP (BR).
BASTOS, Jairo Kenupp [BR/BR]; Avenida Caramuru, 1280, Apto. 61, Republica, 14030-00 Ribeir?o Preto - SP (BR).
CARVALHO, Jos? Carlos Tavares [BR/BR]; Rua Alfredo Leite da Silva, 1415, Boa Esperan?a, 37130-000 Alfenas - MG (BR).
Agent: ADVOCACIA PIETRO ARIBONI S/C; Rua Guararapes, 1909, 7o Andar, Brooklin Novo, 04561-004 S?o Paulo - SP (BR).
Priority Data: PI 0401631-9 22.04.2004 BR

Abstract:
Process to obtain and use extracts, fractions and isolated compounds from the Copaifer species for the treatment of urinary lithiasis in human beings and animals, which comprises the following steps: a) drying of aerial parts, leaves and branches from Copaifer species in a circulating hot air stove at 40 ?C; b) milling of the dry material in a knife mill until a fine powder is obtained; c) extraction by cold or hot maceration in water or hydro-alcohol solution 7:3 in ethanol; d) filtration of extracts through filtration canvas to separate the plant cake; e) lyophilization of the water extract; f) concentration of hydro-alcohol extract in concentrators under reduced pressure; g) fractioning of crude extracts, obtained from the aerial parts of Copaifera species or from crude copaiba oil, by filtration processes in packing columns with stationary phases based on silica gel; or; h) obtainment of fractions rich in the active principles by liquid-liquid partition processes from the hydro-alcohol extract from the branches of the Copaifera species, using hexane, chloroform and n-butanol in sequence; i) fractioning of the fraction in hexane by using a liquid column containing silica gel and elution with hexane and hexane-ethyl acetate mixtures in increasing polarity order to isolate sesquiterpenes; i) fractioning of the fraction in chloroform by using a liquid column containing silica gel and elution with hexane, dichloromethane and methanol in increasing polarity order to isolate diterpenes of the types chlerodane, labdane and low polarity derivatives from cinnamic acid; k) fractioning of the butanol extract by using a liquid column containing silica gel and modified with the addition of acetic acid and elution with mixtures of dichloromethane and methanol to isolate acid diterpenes and polar derivatives from cinnamic acid.