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Found 2 translations.
| Name | Current message text |
|---|---|
| h English (en) | [[Vildagliptin]] (Galvus)(''Figure 6'') was first synthesized in May 1998 and was named after Edwin B. Villhauer. It was discovered when researchers at [[Novartis]] examined adamantyl [[Derivative (chemistry)|derivative]]s that had proven to be very [[potency (pharmacology)|potent]]. The [[adamantyl]] group worked as a [[steric bulk]] and slowed intramolecular cyclization while increasing chemical stability. Furthermore, the primary [[metabolite]]s were highly active. To avoid additional [[Chiral (chemistry)|chiral]] center a [[hydroxylation]] at the [[adamantyl]] ring was carried out (''Figure 6''). The product, [[vildagliptin]], was even more stable, undergoing intramolecular cyclization 30-times slower, and having high [[DPP-4 inhibitor]]y activity and longer-lasting [[pharmacodynamic]] effect. |
| h Japanese (ja) | [[Vildagliptin/ja|ビルダグリプチン]]（ガルバス）(''図6'')は1998年5月に初めて合成され、Edwin B. Villhauerにちなんで命名された。[[Novartis/ja|]]の研究者が、非常に[[potency (pharmacology)/ja|効能]]が高いことが証明されていたアダマンチル[[Derivative (chemistry)/ja|誘導体]]を調べたときに発見された。[[adamantyl/ja|アダマンチル]]基は[[steric bulk/ja|立体バルク]]として働き、化学的安定性を高めながら分子内環化を遅らせた。さらに、一次[[metabolite/ja|代謝物]]は高活性であった。さらなる[[Chiral (chemistry)/ja|キラル]]中心を避けるために、[[adamantyl/ja|アダマンチル]]環での[[hydroxylation/ja|ヒドロキシル化]]が行われた（''図6''）。生成物である[[vildagliptin/ja|ビルダグリプチン]]はさらに安定であり、分子内環化反応は30倍遅く、高い[[DPP-4 inhibitor/ja|DPP-4阻害剤]]活性と[[pharmacodynamic/ja|薬力学的]]効果がより長く持続した。 |