SPI-ESTEROID SYSTEMS WITH NEUROACTIVE AND ANTI-INFLAMMATORY EFFECTS

Argentina Patent

APP PUB NO AR-089491-A1
SERIAL NO

P120105012

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Abstract

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These molecular entities have anti-glutamatergic and anti-inflammatory action, usable in the treatment of chronic and acute inflammatory diseases, neurodegenerative, neuropsychiatric and neurological. Claim 1: Spiro-steroid systems with neuroactive and anti-inflammatory effects derived from diosgenin, hecogenin and solasodine with spirostanic rings fused to their structure, for use as drugs in medicine, of the group of general formula (1), (2), ( 3) and (4) in all their configurations and natural conformations, where for the compounds of general formulas (1), (2), (3) and (4), R¹, R² and R⁴ represents H, hydroxyl group, ketal, alkoxy, alkanoyloxy, alkenyloxy and alkoxycarbonyloxy (preferably alkyl groups of up to 8 straight or branched chain carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and octyl, and the chain isomers of all of the above) ; R¹, R² and R⁴ also represent an amino group, preferably substituted with alkylamino, dialkylamino, alkenylamino, dialkenylamino, aminocarbonyloxy, alkylamino and dialkylamino groups. The alkyl groups will preferably have up to 8 straight or branched chain carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and octyl, and the chain isomers of all of the foregoing; R¹, R² and R⁴ also represent amido, thiols, sulfinyls, sulfonamides and sulfonyl groups. The sulfonyls groups are preferably substituted with alkylaryls, alkanoyloxyaryls, alkenyloxyaryls and alkenylaryls. The alkyl groups will preferably have up to 8 straight or branched chain carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and octyl, and the chain isomers of all of the foregoing; R¹, R² and R⁴ also represent cyano, thiocyan, isothiocyano groups, preferentially substituted with alkyl, azidoalkyl, alkanoyloxyalkyl, arylalkyl, heteroarylalkyl, arylalkyl, heteroarylalkyl, arylalkyl, arylalkylalkyl, alkanoyloxy-alkylaryloxy, alkylalkyl-alkylaryloxy-alkylaryloxy-alkylalkyl-alkylaryloxy-alkylaryloxy-alkylaryloxy-alkylaryloxy-alkylaryl-alkylaryloxy-alkylalkyl-alkylaryloxy-alkylaryl-alkylaryloxy-alkylaryloxy-alkylaryloxy-alkylaryloxy-alkylaryloxy-alkylaryloxylalkyl groups. Cyanoalkynyl substituents may in turn be substituted by heteroarylalkyls, hydroxyalkyls, alkoxyalkyls, aminoalkyls and acyloaminoalkyls. The alkyl groups will preferably have up to 8 straight or branched chain carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and octyl, and the chain isomers of all of the foregoing; R¹, R² and R⁴ also represent a phosphoryl group, preferably substituted with alkylaryls, alkanoyloxyaryls, alkenyloxyaryls and alkenyryls. The alkyl groups will preferably have up to 8 straight or branched chain carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and octyl, and the chain isomers of all of the foregoing; for the compounds of general formula (1), (2), (3) and (4), R³ represents H and hydroxyl group; for the compounds of the general formula (1), (2), (3) and (4), R⁵ represents H and hydroxyl, ketal, amino, thiols and cyano groups; for the compounds of the general formula (1), (2), (3) and (4), R⁶ represents a methyl group, lipid chains derived from mono and polyunsaturated fatty acids of up to 24 carbon atoms, protein binding site; for the compounds of general formula (3) and (4), Rˣ represents alkyl groups of up to 8 straight or branched chain carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and octyl, and the isomers string of all the above, when x is different from zero; for the compounds of general formula (3) and (4), Rˣ also represents alkylaryl, alkanoyloxyaryls, alkenyloxyaryls and alkenylaryls groups. The alkyl groups will preferably have up to 8 straight or branched chain carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and octyl, and the chain isomers of all of the above, when x is different from zero.

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Patent Owner(s)

Patent OwnerAddress
CT DE INVESTIGACIÓN Y DESARROLLO DE MEDICAMENTOSCU

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Inventor(s)

Inventor Name Address
YAMILA VERDECIA REYES CU
ESTAEL OCHOA RODRIGUEZ CU
LAURA GARCIA PUPO CU
YANIER NUEZ FIGUEREDO CU
JUAN ENRIQUE TACORONTE MORALES CU

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