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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：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：US20150306102A1
公开(公告)日：2015-10-29
申请号：US14371567
申请日：2013-01-08
发明人： Lars BÄRFACKER , William SCOTT , Andrea HÄGEBARTH , Hartmut REHWINKEL , Oliver POLITZ , Roland NEUHAUS , Ulf BÖMER
IPC分类号： A61K31/519 , A61K45/06 , C07D487/04
CPC分类号： A61K31/519 , A61K45/06 , C07D487/04
摘要： Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
摘要翻译： 作为Pi3K / Akt途径的有效抑制剂的式（I）化合物，其制备方法及其作为药物的用途。
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![AMINOALCOHOL SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS](/abs-image/US/2015/03/19/US20150080374A1/abs.jpg.150x150.jpg)
4.发明申请AMINOALCOHOL SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS 有权用于治疗与增生性疾病有关的高血压病和疾病的氨基二醇替代的2,3-二氢吲哚并[1,2-C]喹唑啉衍生物公开(公告)号：US20150080374A1
公开(公告)日：2015-03-19
申请号：US14553280
申请日：2014-11-25
发明人： William Scott , Ningshu LIU , Manfred MÖWES , Andrea HÄGEBARTH , Ursula MÖNNING , Ulf BÖMER
IPC分类号： C07D487/04 , A61K45/06 , C07D471/04 , A61K31/5386 , A61K31/519 , A61K31/541 , A61K31/5377 , C07D498/08
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K45/06 , C07D471/04 , C07D498/08
摘要： This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及新的2,3-二氢咪唑并[1,2-c]喹唑啉化合物，含有这些化合物的药物组合物以及这些化合物或组合物用于磷脂酰肌醇-3-激酶（PI3K）抑制和治疗与磷脂酰肌醇 - 3-激酶（PI3K）活性，特别是治疗高增殖和/或血管生成障碍，作为唯一的药剂或与其它活性成分组合。
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公开(公告)号：US20170217949A1
公开(公告)日：2017-08-03
申请号：US15488155
申请日：2017-04-14
发明人： Ulrich LÜCKING , Rolf BOHLMANN , Arne SCHOLZ , Gerhard SIEMEISTER , Mark Jean GNOTH , Ulf BÖMER , Dirk KOSEMUND , Philip LIENAU , Gerd RÜHTER , Carsten SCHULTZ-FADEMRECHT
IPC分类号： C07D417/12 , A61K31/53 , C07D413/12 , C07D405/12 , C07B59/00 , C07D401/12 , C07D251/16 , C07D405/04
CPC分类号： A61K31/53 , C07B59/002 , C07B2200/05 , C07C381/10 , C07D251/16 , C07D251/22 , C07D251/42 , C07D251/44 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to 4-aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group of general formula (I) or (Ia) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I) or (Ia).
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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：US20220388982A1
公开(公告)日：2022-12-08
申请号：US17869674
申请日：2022-07-20
发明人： Ulrich BOTHE , Holger SIEBENEICHER , Nicole SCHMIDT , Reinhard NUBBEMEYER , Ulf BÖMER , Judith GÜNTHER , Holger STEUBER , Martin LANGE , Christian STEGMANN , Andreas SUTTER , Alexandra RAUSCH , Christian FRIEDRICH , Peter HAUFF
IPC分类号： C07D401/12 , C07F7/18 , A61P19/02 , A61K31/4439 , C07D405/14
摘要： The present application relates to novel substituted indazoles, to processes for preparation thereof, to the use thereof alone or in combinations 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 and endometriosis-associated pain and other endometriosis-associated symptoms such as dysmenorrhoea, dyspareunia, dysuria and dyschezia, of lymphoma, rheumatoid arthritis, spondyloarthritis (especially psoriatic spondyloarthritis and Bekhterev's disease), lupus erythematosus, multiple sclerosis, macular degeneration, COPD, gout, fatty liver disorders, insulin resistance, neoplastic disorders and psoriasis.
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公开(公告)号：US20190047980A1
公开(公告)日：2019-02-14
申请号：US16063370
申请日：2016-12-15
发明人： Volker SCHULZE , Tobias HEINRICH , Florian PRINZ , Julien LEFRANC , Jens SCHRÖDER , Anne MENGEL , Wilhelm BONE , Joszef BÁLINT , Antje Margret WENGNER , Knut EIS , Horst IRLBACHER , Marcus KOPPITZ , Ulf BÖMER , Benjamin BADER , Hans BRIEM , Philip LIENAU , Clara CHRIST , Detlef STÖCKIGT , Roman HILLIG
IPC分类号： C07D401/12 , A61P35/00 , C07D401/14 , C07D487/08 , C07D471/08 , C07D451/14 , C07D409/14 , C07D405/14
摘要： The present invention covers heteroarylbenzimidazole compounds of general formula (I) in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for 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 hyperproliferative and/or inflammatory disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：US20160297811A1
公开(公告)日：2016-10-13
申请号：US14896426
申请日：2014-06-03
发明人： Hartmut SCHIROK , Volker SCHULZE , Dirk KOSEMUND , Hans BRIEM , Benjamin BADER , Ulf BÖMER , Antje Margret WENGNER , Gerhard SIEMEISTER , Philip LIENAU
IPC分类号： C07D471/04 , A61K31/496 , A61K31/5377 , A61K45/06
CPC分类号： C07D471/04 , A61K31/496 , A61K31/5377 , A61K45/06
摘要： The present invention relates to substituted triazolopyridine compounds of general formula (I); in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, 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：US20230064809A1
公开(公告)日：2023-03-02
申请号：US17780814
申请日：2020-11-24
发明人： Norbert SCHMEES , Lars WORTMANN , Dennis KIRCHHOFF , Thi Thanh Uyen NGUYEN , Nicolas WERBECK , Ulf BÖMER , Kirstin PETERSEN , Christina KOBER , Detlef STÖCKIGT , Christian LECHNER , Rienk OFFRINGA
IPC分类号： A61K31/4709 , C07D471/10 , C07D487/10 , A61K31/5377 , A61K31/496 , A61P37/04 , A61P35/00 , A61K45/06
摘要： The present invention covers aminoquinolone compounds of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, m, n, o and p are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.
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