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公开(公告)号：US20220153745A1
公开(公告)日：2022-05-19
申请号：US17516542
申请日：2021-11-01
发明人： Dirk BROHM , Melanie HEROULT , Marie-Pierre COLLIN , Walter HÜBSCH , Mario LOBELL , Klemens LUSTIG , Sylvia GRÜNEWALD , Ulf BÖMER , Verena VÖHRINGER
IPC分类号： C07D487/04 , C07D409/14 , C07D409/04 , A61P35/00 , A61K31/53 , A61K31/5355 , A61K31/5377 , A61K31/541
摘要： This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(=0)-NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR9R10, —C(=0)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
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公开(公告)号：US20190016724A1
公开(公告)日：2019-01-17
申请号：US15900725
申请日：2018-02-20
发明人： Dirk BROHM , Melanie HEROULT , Marie-Pierre COLLIN , Walter HÜBSCH , Mario LOBELL , Klemens LUSTIG , Sylvia GRÜNEWALD , Ulf BÖMER , Verena VÖHRINGER
IPC分类号： C07D487/04 , A61K31/541 , A61K31/5377 , A61K31/53 , A61K31/5355
摘要： This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(═O)-NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR9R10, —C(═O)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
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公开(公告)号：US20130158000A1
公开(公告)日：2013-06-20
申请号：US13715553
申请日：2012-12-14
发明人： Dirk BROHM , Melanie HEROULT , Marie-Pierre COLLIN , Walter HÜBSCH , Mario LOBELL , Klemens LUSTIG , Sylvia GRÜNEWALD , Ulf BÖMER
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/53 , A61K31/5355 , A61K31/5377 , A61K31/541
摘要： This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
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公开(公告)号：US20130190290A1
公开(公告)日：2013-07-25
申请号：US13748043
申请日：2013-01-23
发明人： Frank SÜßMEIER , Mario LOBELL , Sylvia GRÜNEWALD , Michael HÄRTER , Bernd BUCHMANN , Joachim TELSER , Hannah JÖRIßEN , Melanie HEROULT , Antje KAHNERT , Klemens LUSTIG , Niels LINDNER
IPC分类号： C07D487/04 , A61K31/4439 , A61K31/5377 , A61K31/4188 , A61K31/496 , A61K45/06
CPC分类号： C07D487/04 , A61K31/4188 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K45/06
摘要： The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
摘要翻译： 本申请涉及新颖的1-苯基-1H-咪唑并[1,2-b]吡唑衍生物，其制备方法，其用于治疗和/或预防疾病及其用于制备药物的用途 治疗和/或预防新生血管形成起作用的疾病，特别是血管生成障碍和过度增殖性疾病，例如肿瘤性疾病和肿瘤病症。 这样的治疗可以作为单一疗法进行，也可以与其他药物组合进行或进一步的治疗措施。
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公开(公告)号：US20170037028A1
公开(公告)日：2017-02-09
申请号：US15106814
申请日：2014-12-16
发明人： Iring HEISLER , Thomas MÜLLER , Holger SIEBENEICHER , Bernd BUCHMANN , Arwed CLEVE , Judith GÜNTHER , Marcus KOPPITZ , Melanie HEROULT , Roland NEUHAUS , Heike PETRUL , Maria QUANZ-SCHÖFFEL
IPC分类号： C07D401/12 , A61K31/473 , C07D401/14 , A61K31/5377 , C07D471/04 , C07D413/14 , C07D417/14 , C07D495/10 , C07D405/14 , A61K31/496 , A61K31/4709 , C07D409/14
CPC分类号： C07D401/12 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/5377 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/10
摘要： The present invention relates to chemical compounds that selectively inhibit glucose transporter 1 (GLUT1), to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
摘要翻译： 本发明涉及选择性抑制葡萄糖转运蛋白1（GLUT1）的化合物，制备所述化合物的方法，药物组合物和包含所述化合物的组合，用于制备药物组合物的用途，用于治疗或预防 疾病，以及可用于制备所述化合物的中间体化合物。
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6.发明申请公开(公告)号：US20180333418A1
公开(公告)日：2018-11-22
申请号：US15534033
申请日：2015-12-08
发明人： Peter ELLINGHAUS , Melanie HEROULT
IPC分类号： A61K31/53 , C12Q1/6886 , A61K31/506 , A61K31/496 , A61K31/498 , A61K31/4184 , A61P35/00
CPC分类号： A61K31/53 , A61K31/4184 , A61K31/496 , A61K31/4965 , A61K31/498 , A61K31/506 , A61P35/00 , C12Q1/6886 , C12Q2600/106
摘要： The current invention is based on a pan FGFR inhibitor for use in the treatment of cancer in a subject, wherein the subject is one for whom the sum of FGFR1, FGFR2 and/or FGFR3 mRNA in a tumor tissue sample from the subject has been found to be overexpressed.
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7.发明申请公开(公告)号：US20180164317A1
公开(公告)日：2018-06-14
申请号：US15577625
申请日：2016-05-25
IPC分类号： G01N33/574 , A61K31/551 , A61K31/497 , A61K31/381 , A61K31/17 , A61K31/215 , A61P35/00
CPC分类号： G01N33/5743 , A61K31/17 , A61K31/215 , A61K31/381 , A61K31/497 , A61K31/551 , A61P35/00
摘要： The present invention refers to a method and kit for stratification of melanoma patients by determining the OCR and levels of PPARGC1A, PPARGC1B and MITF RNA, derived cDNA, or corresponding protein. Especially, the invention is related to stratification kits to determine whether a patient with melanoma will respond to treatment with a BET inhibitor. In a further aspect, the invention is related to the use of a BET inhibitor for the treatment of melanoma in a patient by stratifying a sample of body fluid or tumor tissue in vitro and determining whether a patient suffering from melanoma will respond to treatment with a BET inhibitor.
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公开(公告)号：US20170210738A1
公开(公告)日：2017-07-27
申请号：US15328455
申请日：2015-07-22
发明人： Bernd BUCHMANN , Iring HEISLER , Thomas MÜLLER , Arwed CLEVE , Melanie HEROULT , Roland NEUHAUS , Heike PETRUL , Maria QUANZ-SCHÖFFEL
IPC分类号： C07D417/14 , C07D413/14 , C07D401/14 , C07D401/12 , A61K31/4709
CPC分类号： C07D417/14 , A61K31/4709 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention relates to chemical compounds of formula (I) that selectively inhibit glucose transporter 1 (GLUT1), to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
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