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    • 37. 发明申请
    • ADAMANTYL O-GLUCURONIDE DERIVATIVES AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV FOR THE TREATMENT OF DIABETES
    • 作为DIPEPTIDYL PEPTIDASE IV抑制剂的ADAMANTYL O-GLUCURONIDE衍生物用于治疗糖尿病
    • WO2009068531A3
    • 2010-09-10
    • PCT/EP2008066159
    • 2008-11-25
    • NOVARTIS AGHASSIEPEN ULRICHKITTELMANN MATTHIAS
    • HASSIEPEN ULRICHKITTELMANN MATTHIAS
    • C07H7/033A61K31/7056A61P3/10C07H15/24C07H15/26
    • C07H15/26B41J2/17593
    • The present invention relates to a compound The instant invention relates to a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B), wherein R' represents (formula) and R' represents hydrogen, hydroxy, C1-C7alkoxy, C1-C8-alkanoyloxy, or R5R4N-CO-O-, where R4 and R5 independently are C1-C7alkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C1-C7alkyl, C1-C7alkoxy, halogen and trifluoromethyl and where R4 additionally is hydrogen; or R4 and R5 together represent C3-C6alkylene; in free form or in form of a pharmaceutically acceptable acid addition salt. Compounds of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B) inhibit DPP-IV (dipeptidyl- peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin- dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
    • 本发明涉及化合物本发明涉及式(IA),(IB),(XA),(XB),(YA)或(YB)的化合物,其中R'表示(式)和R' 表示氢,羟基,C 1 -C 7烷氧基,C 1 -C 8 - 烷酰氧基或R 5 R 4 N-CO-O-,其中R 4和R 5独立地是C 1 -C 7烷基或未被取代或被选自C 1 -C 7烷基, C7烷氧基,卤素和三氟甲基,R4另外是氢; 或者R 4和R 5一起代表C 3 -C 6亚烷基; 游离形式或药学上可接受的酸加成盐的形式。 式(I A),(I B),(X A),(X B),(Y A)或(Y B)的化合物抑制DPP-IV(二肽基肽酶-IV)活性。 因此,它们被指示用作抑制DPP-IV的药物和用于治疗由DPP-IV介导的病症,例如非胰岛素依赖性糖尿病,关节炎,肥胖症,骨质疏松症和进一步的葡萄糖耐量降低的病症。