Microencapsulated 3-piperidinyl-substituted...

Details Microencapsulated 3-piperidinyl-substituted... Microencapsulated 3-piperidinyl-substituted...

A - Human Necessities

61

K

A61K 31/505 (2006.01) A61K 9/16 (2006.01) A61K 31/517 (2006.01) A61K 31/519 (2006.01)

Patent

CA 2175370

A pharmaceutical composition comprising biodegradable and biocompatible microparticle containing a 1,2-benzazole of the formula (I), or a pharmaceutically acceptable acid addition salt thereof, wherein R is hydrogen or C1-6alkyl; R1 and R2 independently are hydrogen, halo, hydroxy, C1- 6alkyloxy and C1-6alkyl; X is O or S; Alk is C1-4alkanediyl; and R3 is hydrogen or C1-6alkyl; Z is -S-, -CH2, or -CR4=CR5-; where R4 and R5 independently are hydrogen or C1-6alkyl; A is a bivalent radical -CH2-CH2-, - CH2-CH2-CH2- or -CR6=CR7-; wherein R6 and R7 are hydrogen, halo, amino or C1- 6alkyl; and R8 is hydrogen or hydroxyl; within a polymeric matrix.

Composition pharmaceutique comportant, dans une matrice polymère, des microparticules biodégradables et biocompatibles renfermant un 1,2-benzazole de la formule (I), ou son sel d'addition d'acide pharmaceutiquement acceptable, dans laquelle R représente hydrogène ou alkyle C¿1-6?; R?1¿ et R?2¿, indépendamment l'un de l'autre, représentent hydrogène, halo, hydroxy, alkyloxy C¿1-6? ou alkyle C¿1-6?; X représente O ou S; Alk représente alcanediyle C¿1-4?; et R?3¿ représente hydrogène ou alkyle C¿1-6?; Z représente -S-, -CH¿2?-, ou -CR?4¿=CR?5¿-; où R?4¿ et R?5¿, indépendamment l'un de l'autre, représentent hydrogène ou alkyle C¿1-6?; A représente un radical bivalent -CH¿2?-CH¿2?-, -CH¿2?-CH¿2?-CH¿2?- ou -CR?6¿=CR?7¿-; où R?6¿ et R?7¿ représentent hydrogène, halo, amino ou alkyle C¿1-6?; et R?8¿ représente hydrogène ou hydroxyle.

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