DPP4 INHIBITOR AND PHARMACEUTICAL USE THEREOF
    7.
    发明申请
    DPP4 INHIBITOR AND PHARMACEUTICAL USE THEREOF 审中-公开
    DPP4抑制剂及其药物用途

    公开(公告)号:US20080175837A1

    公开(公告)日:2008-07-24

    申请号:US11927051

    申请日:2007-10-29

    摘要: The present invention provides a Dpp4 inhibitor which comprises a leucine derivative of the following formula (1) or a methionine derivative of the following formula (2): wherein each R1 and R3 represents a hydrogen atom (H) and an L-amino acid residue; R2 represents a hydroxyl group (OH), alkoxy group having 1 to 6 carbon atoms, amino group (NH2), alkylamino group having 1 to 6 carbon atoms, glycine residue, β-alanine residue, L-amino acid (except for proline, alanine and phenylalanine) residue or L-amino-acid amide (except for proline amide, alanine amide and phenylalanine amide) residue; and R4 represents a hydroxyl group (OH), alkoxy group having 1 to 6 carbon atoms, amino group (NH2), alkylamino group having 1 to 6 carbon atoms, glycine residue, β-alanine residue, L-amino acid (except for proline and alanine) residue or L-amino-acid amide (except for proline amide and alanine amide) residue. These derivatives also act as autophagy regulators.

    摘要翻译: 本发明提供一种Dpp4抑制剂,其包含下式(1)的亮氨酸衍生物或下式(2)的甲硫氨酸衍生物:其中R 1和R 3表示氢原子(H)和L-氨基酸残基 ; R2表示羟基(OH),碳原子数1〜6的烷氧基,氨基(NH2),碳原子数1〜6的烷基氨基,甘氨酸残基,β-丙氨酸残基,L-氨基酸(脯氨酸, 丙氨酸和苯丙氨酸)残基或L-氨基酸酰胺(脯氨酸酰胺,丙氨酸酰胺和苯丙氨酸酰胺除外)残基; R 4表示羟基(OH),碳原子数1〜6的烷氧基,氨基(NH 2),碳原子数1〜6的烷基氨基,甘氨酸残基,β-丙氨酸残基,L-氨基酸(脯氨酸 和丙氨酸)残基或L-氨基酸酰胺(除脯氨酰胺和丙氨酸酰胺除外)残基。 这些衍生物也作为自噬调节剂。

    COMPOSITION FOR AMELIORATION/PREVENTION OF ADVERSE SIDE EFFECT IN STEROID THERAPY
    10.
    发明申请
    COMPOSITION FOR AMELIORATION/PREVENTION OF ADVERSE SIDE EFFECT IN STEROID THERAPY 审中-公开
    用于治疗或预防非甾体类药物不良反应的组合物

    公开(公告)号:US20090291928A1

    公开(公告)日:2009-11-26

    申请号:US12483846

    申请日:2009-06-12

    CPC分类号: A61K31/198 A23L33/175

    摘要: Provided is a composition containing isoleucine, leucine and valine as active ingredients for improving or suppressing side effects associated with a steroid treatment and a composition for suppressing muscular atrophy-related gene. The composition improves or suppresses side effects in a steroid treatment such as muscular atrophy, muscular pain, arthritic pain, impaired glucose tolerance, decreased bone metabolism, impaired immunity, loss of appetite, body weight loss, fatigability and the like, and further suppresses muscular atrophy associated with various diseases. In addition, the composition suppresses muscular atrophy associated with promoted expression of muscular atrophy-related gene associated with glucocorticoid excess or renal failure pathology and the like. Therefore, the composition is effective form improving the QOL of patients.

    摘要翻译: 本发明提供含有异亮氨酸,亮氨酸,缬氨酸作为改善或抑制类固醇治疗副作用的有效成分的组合物和抑制肌萎缩相关基因的组合物。 该组合物改善或抑制类固醇治疗中的副作用,例如肌肉萎缩,肌肉疼痛,关节炎疼痛,葡萄糖耐量降低,骨代谢减少,免疫力下降,食欲不振,体重减轻,疲劳等,并进一步抑制肌肉 与各种疾病相关的萎缩。 此外,该组合物抑制与促进与糖皮质激素过量或肾衰竭病理学相关的肌肉萎缩相关基因的表达相关的肌肉萎缩等。 因此,组合物有效地改善了患者的生活质量。