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Solid dispersion comprising a tetrazol derivative as active ingredient
专利权人:
03
发明人:
JUN YOUNG CHOI,YOUNG KEUN CHOI,YONG IL KIM,JAE HYUN PARK,JONG SOO WOO
申请号:
ARP130104460
公开号:
AR093706A1
申请日:
2013.12.03
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
Claim 1: An amorphous solid dispersion comprising a tetrazole derivative of the formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient, wherein, R¹ is quinoline, isoquinoline, quinoxaline, pyridine, pyrazine, naphthalene, phenyl, thiophene, furan, 4-oxo-4H-chromene or cinoline, which is unsubstituted or substituted by C₁₋₅ alkyl,Hydroxy, alcoxi c8321e 83318325;halogen, trifluoromethyl, nitro or amino; R² to R⁵ and R⁸ to R¹¹ are -each independently- H, hydroxyl, halogen, nitro, C₁₋₅ alkyl or C₁₋₅ alkoxy;R⁶ and R⁷ are each independently H, hydroxyl, halogen, nitro, C₁₋₅ alkylene or C₁₋₅ alkoxy;e. C8310a and r8311a can be connected with each other to form a ring of 4 to 8 members; m and N are 0 to 4 members respectively; X is c832222;O or S. claim 2: non substantial solid scattering of claim 1, wherein the derivative of tetrazole is a compound of formula (2) or (3). 13. Claim 3: the non viscous solid dispersion of claim 1, the solid dispersion further comprising a water-soluble polymer. 11. Claim 4: amorphate solid dispersion in claim 3, in which the soluble polymer is selected from Hebron, hydroxypropyl cellulose, polyethylene, propylene propanol, diethyl aminoacetate, polyethylene and mixtures thereof.Reivindicación 1: Una dispersión sólida amorfa que comprende un derivado de tetrazol de la fórmula (1) o una sal farmacéuticamente aceptable del mismo como ingrediente activo, donde, R¹ es quinolina, isoquinolina, quinoxalina, piridina, pirazina, naftaleno, fenilo, tiofeno, furano, 4-oxo-4H-cromeno o cinolina, que está insustituido o sustituido por alquilo C₁₋₅, hidroxilo, alcoxi C₁₋₅, halógeno, trifluorometilo, nitro o amino; R² a R⁵ y R⁸ a R¹¹ son -cada uno en forma independiente- H, hidroxilo, halógeno, nitro, alquilo C₁₋₅ o alcoxi C₁₋₅; R⁶ y R⁷ son -cada uno en forma independiente H, hidroxilo, halógeno, nitro, alquileno C₁₋₅ o alcoxi C₁₋₅; y R⁶ y R⁷ pueden estar conectados para formar un anillo de 4 a 8 miembros; m y n son -cada uno en fo
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