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公开(公告)号:US20230165845A1
公开(公告)日:2023-06-01
申请号:US17996775
申请日:2021-04-24
申请人: Dr. Falk Pharma GmbH , Zedira GmbH
发明人: Roland Greinwald , Martin Hils , Wolfgang Mohr , Ralf Pasternack , Bernhard Tewes , Rudolf Wilhelm
IPC分类号: A61K31/4439 , A61P1/16 , A61P13/12 , A61K9/00
CPC分类号: A61K31/4439 , A61P1/16 , A61P13/12 , A61K9/0053
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.
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公开(公告)号:US20240317708A1
公开(公告)日:2024-09-26
申请号:US18573802
申请日:2022-06-30
申请人: ZEDIRA GMBH
发明人: Ralf PASTERNACK , Christian BÜCHOLD , Martin HILS , Martin STIELER , Uwe GERLACH
IPC分类号: C07D401/12 , A61K31/4375 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4748 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/502 , A61K31/506 , A61K31/5377 , C07D213/75 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D513/04
CPC分类号: C07D401/12 , A61K31/4375 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4748 , A61K31/497 , A61K31/4995 , A61K31/501 , A61K31/502 , A61K31/506 , A61K31/5377 , C07D213/75 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D513/04
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, in particular transglutaminase 2.
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3.
公开(公告)号:US09434763B2
公开(公告)日:2016-09-06
申请号:US14415374
申请日:2013-07-12
申请人: ZEDIRA GMBH
发明人: Christian Buchold , Uwe Gerlach , Martin Hils , Ralf Pasternack , Johannes Weber
IPC分类号: A61K45/06 , C07K5/093 , A61K38/07 , C07K1/06 , C07K5/113 , A61K38/06 , C07K5/10 , C07D213/75 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D493/10 , C07D401/06 , C07K5/02 , C07K5/083 , C07K5/117
CPC分类号: C07K5/1021 , A61K38/06 , A61K38/07 , A61K45/06 , C07D213/75 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D493/10 , C07K1/068 , C07K5/0202 , C07K5/081 , C07K5/0819 , C07K5/1002 , C07K5/1024
摘要: The invention relates to pyridinone derivatives of general formula (I) as inhibitors of tissue transglutaminase, to methods for producing the pyridinone derivatives, to pharmaceutical compositions containing said pyridinone derivatives and to their use for the prophylaxis and treatment of diseases associated with tissue transglutaminase.
摘要翻译: 本发明涉及作为组织转谷氨酰胺酶抑制剂的通式(I)的吡啶酮衍生物,制备吡啶酮衍生物的方法,含有所述吡啶酮衍生物的药物组合物及其用于预防和治疗与组织转谷氨酰胺酶有关的疾病的用途。
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公开(公告)号:US20240270715A1
公开(公告)日:2024-08-15
申请号:US18394766
申请日:2023-12-22
申请人: ZEDIRA GMBH
发明人: Ralf PASTERNACK , Christian BÜCHOLD , Martin HILS , Martin STIELER , Uwe GERLACH
IPC分类号: C07D401/12 , A61K31/4439
CPC分类号: C07D401/12 , A61K31/4439
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, in particular transglutaminase 2.
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公开(公告)号:US20210147478A1
公开(公告)日:2021-05-20
申请号:US17047704
申请日:2019-04-17
申请人: Zedira GmbH
发明人: Martin Hils , Ralf Pasternack , Christian Büchold
摘要: The invention relates to a compound of general formula (I) as novel inhibitor of blood coagulation factor XIII, methods for synthesis thereof and to use thereof for the prophylaxis or treatment of diseases associated with blood coagulation factor XIII.
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公开(公告)号:US11472838B2
公开(公告)日:2022-10-18
申请号:US17047704
申请日:2019-04-17
申请人: Zedira GmbH
发明人: Martin Hils , Ralf Pasternack , Christian Büchold
摘要: The invention relates to a compound of general formula (I) as novel inhibitor of blood coagulation factor XIII, methods for synthesis thereof and to use thereof for the prophylaxis or treatment of diseases associated with blood coagulation factor XIII.
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公开(公告)号:US11072634B2
公开(公告)日:2021-07-27
申请号:US16473265
申请日:2018-01-02
申请人: Zedira GmbH
发明人: Martin Hils , Ralf Pasternack , Christian Büchold
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.
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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
CPC分类号: C07K5/1021 , C07K1/02 , C07K1/042 , C07K1/067 , C07K5/06104 , C07K5/0808 , C07K5/0819 , C07K5/1016 , C07K5/1024 , C07K5/1027 , C07K7/06
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。
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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
发明人: Martin Hils , Ralf Pasternack , Christian Büchold
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.
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公开(公告)号:US20160137990A1
公开(公告)日:2016-05-19
申请号:US14650987
申请日:2013-12-10
申请人: ZEDIRA GMBH
发明人: Martin Hils , Ralf Pasternack , Christian Buchold , Johannes Weber , Andreas Heine , Gerhard Klebe , Martin Stieler
CPC分类号: C12N9/1044 , C07K2299/00 , C12Y203/02013 , G16B5/00 , G16B15/00
摘要: The present invention relates to crystal forms of blood coagulation factor XIIIa, crystal structure information obtained from them, methods of preparing such crystal forms, their use for the identification and/or design of inhibitors of blood coagulation factor XIIIa activity and methods for identifying, optimizing and designing compounds which should have the ability to interact with or inhibit blood coagulation factor XIIIa.
摘要翻译: 本发明涉及凝血因子XIIIa的结晶形式,从中获得的晶体结构信息,制备这种晶型的方法,其用于鉴定和/或设计凝血因子XIIIa活性抑制剂的用途和用于鉴定,优化的方法 并设计应具有与凝血因子XIIIa相互作用或抑制能力的化合物。
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