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公开(公告)号：US20210317128A1
公开(公告)日：2021-10-14
申请号：US16759262
申请日：2018-10-18
发明人： Marcus KOPPITZ , Holger SIEBENEICHER , Nico BRÄUER , Elisabeth POOK , Andrea ROTGERI , Roland NEUHAUS , Oliver Martin FISCHER , Jens NAGEL , Adam James DAVENPORT , James Lindsay CARR , Robert James TOWNSEND , Nina CONNELLY URSINYOVA , Shelley Anne PARROTT
IPC分类号： C07D487/14
摘要： The present invention covers substituted. Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R1, R2 and R3 are as defined herein, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic diseases, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20170226081A1
公开(公告)日：2017-08-10
申请号：US15328463
申请日：2015-07-22
发明人： Bernd BUCHMANN , Iring HEISLER , Thomas MÜLLER , Arwed CLEVE , Mélanie HÉROULT , Roland NEUHAUS , Heike PETRUL , Maria QUANZ-SCHÖFFEL
IPC分类号： C07D401/12 , C07D417/14 , C07D413/14 , A61K31/4709 , C07D401/14
CPC分类号： C07D401/12 , A61K31/136 , A61K31/337 , A61K31/4709 , A61K31/513 , A61K31/555 , A61K31/573 , A61K31/675 , A61K31/704 , C07D215/50 , C07D231/38 , C07D401/06 , C07D401/14 , C07D403/06 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , A61K2300/00
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.
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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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公开(公告)号：US20190388410A1
公开(公告)日：2019-12-26
申请号：US16428669
申请日：2019-05-31
发明人： Ulrich BOTHE , Antje Margret WENGNER , Holger SIEBENEICHER , Nicole SCHMIDT , Reinhard NUBBEMEYER , Ulf BÖMER , Judith GÜNTHER , Holger STEUBER , Martin LANGE , Christian STEGMANN , Andreas SUTTER , Roland NEUHAUS
IPC分类号： A61K31/4439 , A61K45/06 , A61P35/00 , A61K31/519
摘要： The present application relates to novel combinations of at least two components, component A and component B: component A is an IRAK4-inhibiting compound of the formula (I) as defined herein, or a diastereomer, an enantiomer, a metabolite, a salt, a solvate or a solvate of a salt thereof; component B is a BTK-inhibiting compound, or a pharmaceutically acceptable salt thereof; and, optionally, one or more components C which are pharmaceutical products; in which one or two of the above-defined compounds A and B are optionally present in pharmaceutical formulations ready for simultaneous, separate or sequential administration, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis, lymphoma, macular degeneration, COPD, neoplastic disorders and psoriasis.
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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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公开(公告)号：US20170197921A1
公开(公告)日：2017-07-13
申请号：US15118154
申请日：2015-02-10
发明人： Hartmut REHWINKEL , Olaf PANKNIN , Sven RING , Sonja ANLAUF , Holger SIEBENEICHER , Duy NGUYEN , Wolfgang SCHWEDE , Marcus BAUSER , Katja ZIMMERMANN , Stefan KAULFUSS , Roland NEUHAUS , Paul Matthew BLANEY
IPC分类号： C07D235/30 , A61K31/4439 , C07D401/12 , A61K31/4184 , A61K45/06
CPC分类号： C07D235/30 , A61K31/4184 , A61K31/4439 , A61K45/06 , C07D401/12
摘要： The present invention relates to benzimidazol-2-amines of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20150376196A1
公开(公告)日：2015-12-31
申请号：US14769921
申请日：2014-02-18
发明人： Norbert SCHMEES , Bernd BUCHMANN , Bernard HAENDLER , Roland NEUHAUS , Pascale LEJEUNE , Martin KRÜGER , Amaury Ernesto FERNANDEZ-MONTALVAN , Hermann KÜNZER , Hartmut REHWINKEL
IPC分类号： C07D487/14 , C07D519/00 , A61K31/5517
CPC分类号： C07D487/14 , A61K31/5517 , C07D519/00
摘要： BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, 4-substituted pyrrolo- and pyrazolodiazepines of the general formula I are described, in which X, Y, n, m, p, R1, R2, R3, R4 and R5 are each as defined in the description, as are pharmaceutical compositions comprising the inventive compounds, and the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. Also described is the use of the inventive compounds as BET protein inhibitors in benign hyperplasias, in atherosclerotic disorders, in sepsis, in autoimmune disorders, in vascular disorders, in viral infections, in neurodegenerative disorders, in inflammatory disorders and in male fertility control.
摘要翻译： 描述了通式I中的β蛋白抑制特别是BRD2-，BRD3-和BRD4抑制性4-取代的吡咯并 - 吡唑并二氮杂，其中X，Y，n，m，p，R1，R2，R3，R4 和R5各自如说明书中所定义，以及包含本发明化合物的药物组合物，以及在过度增殖性疾病的情况下的预防和治疗用途，特别是在肿瘤性疾病的情况下。 还描述了本发明化合物作为良性增生中的BET蛋白抑制剂，动脉粥样硬化病症，败血症，自身免疫性疾病，血管病症，病毒感染，神经变性疾病，炎症性疾病和雄性生育控制中的用途。
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公开(公告)号：US20220241261A1
公开(公告)日：2022-08-04
申请号：US17544641
申请日：2021-12-07
发明人： Ulrich BOTHE , Antje Margret WENGNER , Holger SIEBENEICHER , Nicole SCHMIDT , Reinhard NUBBEMEYER , Ulf BÖMER , Judith GÜNTHER , Holger STEUBER , Martin LANGE , Christian STEGMANN , Andreas SUTTER , Roland NEUHAUS
IPC分类号： A61K31/4439 , A61K31/519 , A61K31/497 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/55 , A61K31/506 , A61K31/454 , A61K31/505 , A61P35/00 , A61K45/06
摘要： The present application relates to novel combinations of at least two components, component A and component B: component A is an IRAK4-inhibiting compound of the formula (I) as defined herein, or a diastereomer, an enantiomer, a metabolite, a salt, a solvate or a solvate of a salt thereof; component B is a BTK-inhibiting compound, or a pharmaceutically acceptable salt thereof; and, optionally, one or more components C which are pharmaceutical products; in which one or two of the above-defined compounds A and B are optionally present in pharmaceutical formulations ready for simultaneous, separate or sequential administration, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis, lymphoma, macular degeneration, COPD, neoplastic disorders and psoriasis.
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公开(公告)号：US20180201585A1
公开(公告)日：2018-07-19
申请号：US15744641
申请日：2016-07-12
发明人： Olaf PANKNIN , Sven RING , Katja ZIMMERMANN , Roland NEUHAUS
IPC分类号： C07D235/30 , A61K31/4184 , A61K45/06 , A61P35/00
CPC分类号： C07D235/30 , A61K31/4184 , A61K45/06 , A61P35/00
摘要： The present invention relates to benzimidazol-2-amines of general formula (I) in which R1, R2, R3, R4, R5, R6 and R7 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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10.发明申请公开(公告)号：US20170319549A1
公开(公告)日：2017-11-09
申请号：US15520384
申请日：2015-10-21
发明人： Hartmut REHWINKEL , Sonja ANLAUF , Duy NGUYEN , Olaf PANKNIN , Marcus BAUSER , Katja ZIMMERMANN , Stefan KAULFUSS , Roland NEUHAUS , Paul Matthew BLANEY , Gianna TOSCHI
IPC分类号： A61K31/4184 , C07D235/30
CPC分类号： A61K31/4184 , C07D235/30 , C07D401/04 , C07D403/04 , C07D413/04
摘要： The present invention relates to benzimidazol-2-amines of general formula (I) in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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