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公开(公告)号:WO2019043103A1
公开(公告)日:2019-03-07
申请号:PCT/EP2018/073357
申请日:2018-08-30
发明人: DE MAN, Adrianus Petrus Antonius , UITDEHAAG, Joost Cornelis Marinus , STERRENBURG, Jan Gerard , DE WIT, Joeri Johannes Petrus , VAN CAUTER, Freek , SEEGERS, Nicole Wilhelmina Cornelia , VAN DOORNMALEN, Antonius Maria , BUIJSMAN, Rogier Christian , ZAMAN, Guido Jenny Rudolf
IPC分类号: C07D405/04 , C07D409/04 , C07D409/14 , C07D417/04 , A61K31/4178 , A61P35/00 , A61P25/00 , A61P31/00 , A61P37/00
CPC分类号: C07D409/04 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D405/04 , C07D409/14 , C07D417/04
摘要: The invention relates to a compound of Formula (I) : Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The invention also relates to the use of the compounds of Formula (I) for the treatment or prevention of diseases cancer, infections, central nervous system disease or disorder, and immune-related disorders, either as a single agent or in combination with other therapies.
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公开(公告)号:WO2015155042A1
公开(公告)日:2015-10-15
申请号:PCT/EP2015/056839
申请日:2015-03-30
发明人: DE MAN, Adrianus Petrus Antonius , BUIJSMAN, Rogier Christian , STERRENBURG, Jan Gerard , UITDEHAAG, Joost Cornelis Marinus , DE WIT, Joeri Johannes Petrus , ZAMAN, Guido Jenny Rudolf
IPC分类号: C07D471/22 , A61K31/519 , A61P35/00
CPC分类号: C07D471/14 , C07D471/22
摘要: The invention relates to a compound of Formula (I) wherein, R 1 and R 2 independently are selected from the group consisting of optionally substituted (6-10C)aryl and (1-5C)heteroaryl groups. The compounds can be used in pharmaceutical compositions, in particular in the treatment of cancer.
摘要翻译: 本发明涉及式(I)化合物,其中R1和R2独立地选自任选取代的(6-10C)芳基和(1-5C)杂芳基。 该化合物可用于药物组合物,特别是用于治疗癌症。
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公开(公告)号:WO2018011227A1
公开(公告)日:2018-01-18
申请号:PCT/EP2017/067447
申请日:2017-07-11
发明人: DE MAN, Adrianus Petrus Antonius , UITDEHAAG, Joost Cornelis Marinus , STERRENBURG, Jan Gerard , DE WIT, Joeri Johannes Petrus , SEEGERS, Nicole Wilhelmina Cornelia , VAN DOORNMALEN, Antonius Maria , BUIJSMAN, Rogier Christian , ZAMAN, Guido Jenny Rudolf
IPC分类号: C07D401/12 , C07D405/12 , C07D453/02 , C07D471/04 , C07D209/18 , A61K31/404 , A61P35/00
摘要: The invention relates to a compound of Formula I : Formula I, or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of tryptophan 2,3-dioxygenase. The invention also relates to the use of the compounds of Formula (I) for the treatment or prevention of cancer and central nervous system disease or disorder, either as a single agent or in combination with other therapies.
摘要翻译: 本发明涉及式I的化合物或其药学上可接受的对映体或其盐。 本发明还涉及式(I)化合物作为色氨酸2,3-双加氧酶的选择性抑制剂的用途。 本发明还涉及式(I)化合物用于治疗或预防癌症和中枢神经系统疾病或病症的用途,作为单一药物或与其他疗法组合。 p>
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公开(公告)号:WO2017153459A1
公开(公告)日:2017-09-14
申请号:PCT/EP2017/055419
申请日:2017-03-08
发明人: DE MAN, Adrianus Petrus Antonius , UITDEHAAG, Joost Cornelis Marinus , STERRENBURG, Jan Gerard , DE WIT, Joeri Johannes Petrus , SEEGERS, Nicole Wilhelmina Cornelia , VAN DOORNMALEN, Antonius Maria , BUIJSMAN, Rogier Christian , ZAMAN, Guido Jenny Rudolf
IPC分类号: C07D233/32 , C07D403/06 , C07D405/06 , A61K31/4166 , A61K31/4178 , A61K31/4995 , A61P37/00 , A61P35/00 , A61P25/00 , A61P31/00
摘要: The invention relates to a compound of Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The invention also relates to the use of the compounds of Formula (I) for the treatment or prevention of diseases cancer, infections, central nervous system disease or disorder, and immune-related disorders, either as a single agent or in combination with other therapies.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的对映体或其盐。 本发明还涉及式(I)化合物作为吲哚胺2,3-双加氧酶的选择性抑制剂的用途。 本发明还涉及式(I)化合物用作治疗或预防疾病癌症,感染,中枢神经系统疾病或病症以及免疫相关病症的用途,作为单一药物或与其他疗法组合 p>
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公开(公告)号:WO2016166255A1
公开(公告)日:2016-10-20
申请号:PCT/EP2016/058292
申请日:2016-04-14
发明人: DE ROOS, Jeroen , UITDEHAAG, Joost, Cornelis, Marinus , DE MAN, Adrianus, Petrus, Antonius , BUIJSMAN, Rogier, Christiaan , ZAMAN, Guido, Jenny, Rudolf
IPC分类号: C12Q1/68
CPC分类号: C12Q1/6886
摘要: The present invention provides a method for identifying a tumor - in a human individual or in an animal - that is susceptible to treatment with a TTK inhibitor, said method comprising: a] providing a sample of a tumor; b] determining the presence of a mutated CTNNB1 gene in said tumor sample, wherein said mutation is located in exon 3 of CTNNB1 and whereby the presence of a mutated CTNNB1 gene indicates that the tumor is susceptible to treatment with a TTK inhibitor. In an alternative aspect, step b] of the above defined method is replaced by the step of determining the presence of a mutated CTNNB1 protein in said tumor sample, wherein said mutation is located in exon 3 of CTNNB1 and whereby the presence of a mutated CTNNB1 protein indicates that the tumor is susceptible to treatment with a TTK inhibitor. In a further alternative, step b] comprises determining an altered expression of a CTNNB1 regulated gene, whereby an altered expression of a CTNNB1 regulated gene indicates that the tumor is susceptible to treatment with a TTK inhibitor.
摘要翻译: 本发明提供了用于鉴定易于用TTK抑制剂治疗的人个体或动物中的肿瘤的方法,所述方法包括:a]提供肿瘤样品; b]确定所述肿瘤样品中突变的CTNNB1基因的存在,其中所述突变位于CTNNB1的外显子3中,由此突变的CTNNB1基因的存在表明肿瘤易于用TTK抑制剂治疗。 在另一方面,上述定义的方法的步骤b]由所述肿瘤样品中确定突变的CTNNB1蛋白的存在的步骤代替,其中所述突变位于CTNNB1的外显子3中,由此存在突变的CTNNB1 蛋白质表明肿瘤易于用TTK抑制剂治疗。 在另一替代方案中,步骤b]包括测定CTNNB1调节基因的改变的表达,由此CTNNB1调节基因的改变的表达表明肿瘤易于用TTK抑制剂治疗。
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