SYSTEMIC FORMULATION OF A PYRIDINONE DERIVATE FOR TG2-RELATED DISEASES

    公开(公告)号:US20230165845A1

    公开(公告)日:2023-06-01

    申请号:US17996775

    申请日:2021-04-24

    摘要: The present invention relates to a formulation in particular an oral formulation for the prophylaxis and treatment of TG2-related disorders like fibrosis in particular diabetic nephropathy and/or diabetic associated non-alcoholic steatohepatitis (NASH) and/or non-alcoholic steatohepatitis, and its use in the prophylaxis and/or treatment of fibrosis in particular nephropathy, NASH, idiopathic pulmonary fibrosis, and cystic fibrosis. Further, the present application relates also to the use of (S,E)-methyl-7-(1-(2-(2-ethylbutylamino)-2-oxoethyl)-2-oxo-1,2-dihydro-pyridin-3-ylamino)-6-(1-methyl-1H- imidazole-5-carboxamido)-7-oxohept-2-enoate as hepatoprotectant, i.e. as hepatoprotective agent. In addition the present invention relates to a pharmaceutical composition comprising (S,E)-methyl-7-(1-(2-(2-ethylbutylamino)-2-oxoethyl)-2-oxo-1,2- dihydro-pyridin-3-ylamino)-6-(1-methyl-1H-imidazole-5-carboxamido)-7-oxohept-2-enoate for use as hepatoprotective agent and for use in the protection of the liver against liver toxicity, the improvement of liver function, and/or in the prophylaxis or treatment of a liver disease or liver disorder.

    Michael systems as transglutaminase inhibitors
    8.
    发明授权
    Michael systems as transglutaminase inhibitors 有权
    迈克尔系统作为转谷氨酰胺酶抑制剂

    公开(公告)号:US08471063B2

    公开(公告)日:2013-06-25

    申请号:US12513476

    申请日:2007-11-08

    申请人: Kai Oertel

    发明人: Kai Oertel

    IPC分类号: A61K31/16

    摘要: Described herein are peptide derivatives and peptidomimetics as inhibitors for transglutaminases, methods for their preparation, pharmaceutical compositions containing said compounds as well as uses of said transglutaminase inhibitors in particular for the treatment of coeliac disease and transglutaminase dependent diseases.

    摘要翻译: 本文描述了作为转谷氨酰胺酶抑制剂的肽衍生物和肽模拟物,其制备方法,含有所述化合物的药物组合物以及所述转谷氨酰胺酶抑制剂特别用于治疗乳糜泻和转谷氨酰胺酶依赖性疾病的用途。

    INHIBITORS OF TRANSGLUTAMINASES
    9.
    发明申请

    公开(公告)号:US20190322700A1

    公开(公告)日:2019-10-24

    申请号:US16473265

    申请日:2018-01-02

    申请人: Zedira GmbH

    IPC分类号: C07K5/117 C07K5/097

    摘要: The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases.