Triterpene derivatives and pharmaceuticals for treating...

C - Chemistry – Metallurgy – 07 – J

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C07J 63/00 (2006.01) A61K 31/56 (2006.01) C07J 71/00 (2006.01)

Patent

CA 2226346

A pharmaceutical composition for treating a hepatic disorder, comprising a triterpene derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof is disclosed: (see formula I) wherein R1 represents a hydroxyl group, alkoxy, alkylcarbonyloxy, or aralkyloxy; R2 represents alkyl, -- CH2OR5, wherein R5 represents a hydrogen atom, alkyl, aralkyl, or alkylcarbonyl, formyl, -COOR6, wherein R6 represents a hydrogen atom or alkyl, or -CH2N(R7)R8; or R1 and R2 combine with each other to form -O-CR9(R10)-OCH2- wherein R9 and R10, which may be the same or different, represent a hydrogen atom, alkyl, or aryl; R3 and R4, which may be the same or different, represent a hydrogen atom, a hydroxyl group, alkyl, hydroxyalkyl, formyl, -COOR11, wherein R11 represents a hydrogen atom or alkyl, or -OR12, wherein R12 represents alkyl, aralkyl, C1-6 alkylcarbonyl, arylcarbonyl, alkenyl, alkenylcarbonyl, or arylalkenylcarbonyl which may be optionally substituted; or R3 and R4 combine with each other to form a methylene group; and ~ represents a single or double bond, provided that, when ~ represents a double bond, R4 is absent.

Ce médicament pour les maladies du foie comprend un dérivé triterpène représenté par la formule générale (I), où un sel de celui-ci acceptable sur le plan pharmacologique. Dans cette formule R<1> represente hydroxy, alcoxy, alkylcarbonyloxy ou aralkyloxy; R<2> represente alkyle, -CH2OR5 (ou R<5> represente hydrogène, alkyle, aralkyle ou akylcarbonyle), formyle, -COOR<6> (où R<6> represente hydrogène ou alkyle) ou -CH2N(R<7>)R<8>, ou bien R<1> et R<2> sont liés l'un à l'autre pour former -O-CR<9>(R<10>)-OCH2- (où R<9> et R<10> sont identiques ou différents et représentent chacun hydrogène, alkyle ou aryle); R<3> et R<4> sont identiques ou différents et représentent chacun hydrogène, hydroxy, alkyle, hydroxyalkyle, formyle, -COOR<11> (où R<11> represente hydrogène ou alkyle) ou -OR<12> (où R<12> represente alkyle, aralkyle, C1-6 alkylcarbonyle, arylcarbonyle, alcényle, alcénylcarbonyle ou arylalcénylcarbonyle éventuellement substitué, ou bien R<3> et R<4> ensemble forment méthylène; et <u>- - -</u> represente une liaison simple ou double, à condition que lorsque <u>---</u> est une liaison double, R<4> est absent.

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