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1. 发明申请

WO2019201848A1 2-METHYL-AZA-QUINAZOLINES 审中-公开
公开(公告)号：WO2019201848A1
公开(公告)日：2019-10-24
申请号：PCT/EP2019/059650
申请日：2019-04-15
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BAYER HEALTHCARE CHINA
发明人： WORTMANN, Lars , SAUTIER, Brice , EIS, Knut , BRIEM, Hans , BÖHNKE, Niels , VON NUSSBAUM, Franz , HILIG, Roman , BADER, Benjamin , SCHRÖDER, Jens , PETERSEN, Kirstin , LIENAU, Philip , WENGNER, Antje, Margret , MOOSMAYER, Dieter , WANG, Qiuwen
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00
摘要： The present invention covers 2-methyl-aza-quinazoline compounds of general formula (I) as described and 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 disorders, as a sole agent or in combination with other active ingredients

2. 发明公开

EP3781565A1 2-METHYL-AZA-QUINAZOLINES 无效
公开(公告)号：EP3781565A1
公开(公告)日：2021-02-24
申请号：EP19720074.4
申请日：2019-04-15
申请人： Bayer Pharma Aktiengesellschaft , Bayer Healthcare China
发明人： WORTMANN, Lars , SAUTIER, Brice , EIS, Knut , BRIEM, Hans , BÖHNKE, Niels , VON NUSSBAUM, Franz , HILIG, Roman , BADER, Benjamin , SCHRÖDER, Jens , PETERSEN, Kirstin , LIENAU, Philip , WENGNER, Antje, Margret , MOOSMAYER, Dieter , WANG, Qiuwen
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00

3. 发明申请

WO2018087126A1 AMIDO-SUBSTITUTED CYCLOHEXANE DERIVATIVES AS INHIBITORS OF TANKYRASE 审中-公开
标题翻译： AMIDO取代的环己烷衍生物作为TANKYRASE抑制剂
公开(公告)号：WO2018087126A1
公开(公告)日：2018-05-17
申请号：PCT/EP2017/078567
申请日：2017-11-08
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： BUCHGRABER, Philipp , EIS, Knut , WAGNER, Sarah , SÜLZLE, Detlev , BENDER, Eckhard , LI, Volkhart, Min-Jian , LIU, Ningshu , SIEGEL, Franziska , LIENAU, Philip
IPC分类号： C07D401/14 , A61K31/352 , A61K31/357 , A61K31/416 , A61K31/4188 , A61K31/426 , A61K31/4375 , A61K31/44 , A61K31/4439 , A61K31/47 , A61K31/498 , A61K31/519 , C07D213/72 , C07D213/81 , C07D311/18 , C07D215/48 , C07D215/54 , C07D319/18 , C07D231/54 , C07D401/12 , C07D241/44 , C07D471/04 , C07D487/04 , C07D277/56 , C07D513/04
摘要： The present invention relates to amido-substituted cyclohexane compounds of general formula (I), in which A, R 4 , R 6 , R 7 , R 8 , R 9 , R 10 and R 11 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.
摘要翻译：本发明涉及通式（I）的酰氨基取代的环己烷化合物，其中A，R 4，R 6，R 5，R 6， R 8，R 9，R 10和R 11的取代基为本文定义的化合物，制备所述化合物的方法，可用于制备所述化合物的中间体化合物，包含所述化合物的药物组合物和组合以及所述化合物用于制备用于治疗或预防疾病的药物组合物的用途，特别是的肿瘤，作为单独的药物或与其他活性成分组合。

4. 发明申请

WO2017198341A8 MACROCYCLIC INDOLE DERIVATIVES 审中-公开
公开(公告)号：WO2017198341A8
公开(公告)日：2017-11-23
申请号：PCT/EP2017/000629
申请日：2017-05-17
申请人： BAYER AKTIENGESELLSCHAFT , BAYER PHARMA AKTIENGESELLSCHAFT , THE BROAD INSTITUTE, INC.
发明人： WAGNER, Sarah Anna Liesa Johannes , BUCHGRABER, Philipp , KLAR, Ulrich , CHRIST, Clara , FERNANDEZ-MONTALVAN, Amaury, Ernesto , MÖWES, Manfred , LIENAU, Philipp , EIS, Knut , SACK, Ulrike , MÖNNING, Ursula , SCHOLZ, Arne , KUHNKE, Joachim , THEDE, Kai , WERBECK, Nicolas , SERRANO-WU, Michael H. , LEMKE, Chris , MCKINNEY, David , FITZGERALD, Mark , NASVESCHUK, Christopher , LAZARSKI, Kiel , FERRARA, Steven, James , FURST, Laura , WEI, Guo , MCCARREN, Patrick, Ryan
IPC分类号： C07D487/14 , C07D487/04 , C07D498/04 , C07D498/14 , C07D498/20 , A61K31/4162 , A61P35/00
摘要： The present invention relates to macrocyclic indole derivatives of general formula (I) : (I), in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A and L 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 disorders, as a sole agent or in combination with other active ingredients.

5. 发明申请

WO2016062688A1 1-PHENYL-4,5-DIHYDRO-3H-2,3-BENZODIAZEPINE DERIVATIVES 审中-公开
标题翻译： 1-苯基-4,5-二氢-3H-2,3-苯并二氮杂衍生物
公开(公告)号：WO2016062688A1
公开(公告)日：2016-04-28
申请号：PCT/EP2015/074214
申请日：2015-10-20
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： SIEGEL, Stephan , CLEVE, Arwed , HAENDLER, Bernard , EIS, Knut
IPC分类号： C07D243/02 , A61K31/551 , A61P25/00 , A61P35/00
CPC分类号： C07D243/02
摘要： Es werden Bromodomänen-proteininhibitorische, insbesondere BET-proteininhibitorische bevorzugt BRD4-inhibitorische Carboxamide der allgemeinen Formel (I) in der R 1 , R 2 , R 3 , R 4 und R 5 die in der Beschreibung angegebenen Bedeutungen haben, pharmazeutische Mittel enthaltend die erfindungsgemäßen Verbindungen sowie deren prophylaktische und therapeutische Verwendung bei hyper-proliferativen Erkrankungen, insbesondere bei Tumorerkrankungen beschrieben. Des weiteren wird die Verwendung von BET- Proteininhibitoren bei benignen Hyperplasien, atherosklerotische Erkrankungen, Sepsis, Autoimmunerkrankungen, Gefäßerkrankungen, viralen Infektionen, HIV-assoziierten Nierenerkrankungen, neurodegenerativen Erkrankungen, inflammatorischen Erkrankungen, atherosklerotischen Erkrankungen, Herzinsuffizienz, Muskeldystrophien wie zum Beispiel die fazioskapulohumerale Muskeldystrophie und bei der männlichen Fertihtätskontrolle beschrieben.
摘要翻译：有溴基结构域-proteininhibitorische，特别是BET-proteininhibitorische含有该新型化合物的通式（I），其中R1，R2，R3，R4和R5具有在说明书中给出的含义，优选BRD4抑制羧酰胺，药物组合物和它们的预防和在过度增殖疾病的治疗用途，特别是所描述的肿瘤疾病。此外，使用在良性增生BET蛋白抑制剂，动脉粥样硬化性疾病，败血症，自身免疫性疾病，血管疾病，病毒感染，HIV相关的肾病，神经变性疾病，炎性疾病，动脉粥样硬化疾病，心脏衰竭，肌肉萎缩症如面肩肱型肌营养不良症和阳Fertihtätskontrolle说明。

6. 发明申请

WO2014128093A1 SUBSTITUTED-IMIDAZO[1,2-B]PYRIDAZINES AS MKNK1 INHIBITORS 审中-公开
标题翻译：作为MKNK1抑制剂的替代 - 咪唑并[1,2-B]吡啶
公开(公告)号：WO2014128093A1
公开(公告)日：2014-08-28
申请号：PCT/EP2014/053056
申请日：2014-02-18
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： EIS, Knut , PÜHLER, Florian , ZORN, Ludwig , SCHULZE, Volker , SÜLZLE, Detlev , LIENAU, Philip , WENGNER, Antje, Margret , PETERSEN, Kirstin , BÖMER, Ulf
IPC分类号： C07D487/04 , C07D491/04 , A61K31/5025 , A61P35/00 , A61P29/00 , A61P37/00
CPC分类号： A61K31/5025 , A61K9/0019 , A61K9/19 , A61K9/20 , A61K9/48 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D487/04 , C07D491/04 , C07D519/00 , C07F7/1856
摘要： The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): (Ia) (Ib) (Ic) (Id) in which A, Y, R1, R2, R3, R4 and n are as defined in the claims, 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 a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译：本发明涉及通式（I）：（Ia）（Ib）（Ic）（Id）的酰氨基取代的咪唑并哒嗪化合物，其中A，Y，R 1，R 2，R 3，R 4和n如权利要求，制备所述化合物的方法，可用于制备所述化合物的中间体化合物，包含所述化合物的药物组合物和组合，以及所述化合物用于制备用于治疗或预防疾病的药物组合物的用途，特别是高增殖和/或血管生成障碍，作为唯一的药剂或与其它活性成分组合。

7. 发明申请

WO2014118135A1 AMIDOIMIDAZOPYRIDAZINES AS MKNK-1 KINASE INHIBITORS 审中-公开
标题翻译： AMIDOIMIDAZOPYRIDAZINES作为MKNK-1激酶抑制剂
公开(公告)号：WO2014118135A1
公开(公告)日：2014-08-07
申请号：PCT/EP2014/051554
申请日：2014-01-28
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： ZORN, Ludwig , EIS, Knut , SCHULZE, Volker , SÜLZLE, Detlev , PÜHLER, Florian , LIENAU, Philip , BÖMER, Ulf , PETERSEN, Kirstin , HÄGEBARTH, Andrea
IPC分类号： C07D487/04 , C07D491/04 , A61K31/5025 , A61P35/00 , A61P29/00 , A61P37/00
CPC分类号： C07D487/04 , A61K31/5025 , A61K31/513 , A61K45/06 , C07D491/04 , C07D491/048
摘要： The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I) : in which A, R1, R2, R3, R4 and n are as defined in the claims, 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 a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译：本发明涉及通式（I）的酰氨基取代的咪唑并哒嗪化合物：其中A，R1，R2，R3，R4和n如权利要求中所定义，涉及制备所述化合物的方法，可用于制备所述化合物，包含所述化合物的药物组合物和组合以及所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其他活性成分组合。

8. 发明申请

WO2012104428A1 (5S,8S)-3-(4'-CHLOR-3'-FLUOR-4-METHYLBIPHENYL-3-YL)-4-HYDROXY-8-METHOXY-1-AZASPIRO[4.5]DEC-3-EN-2-ON (VERBINDUNG A) ZUR THERAPIE 审中-公开
标题翻译：（5S，8S）-3-（4'-氯-3'-氟-4-甲基联苯-3-基）-4-羟基-8-甲氧基-1-氮杂螺[4.5]癸-3-烯-2- 酮（化合物A）治疗
公开(公告)号：WO2012104428A1
公开(公告)日：2012-08-09
申请号：PCT/EP2012/051895
申请日：2012-02-03
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , LIU, Ningshu , THEDE, Kai , LIENAU, Philip , SCHOLZ, Arne , HILGER, Christoph-Stephan , BÖMER, Ulf , NAJJAR, Maher , EIS, Knut , FISCHER, Reiner , MORADI, Wahed, Ahmed
发明人： LIU, Ningshu , THEDE, Kai , LIENAU, Philip , SCHOLZ, Arne , HILGER, Christoph-Stephan , BÖMER, Ulf , NAJJAR, Maher , EIS, Knut , FISCHER, Reiner , MORADI, Wahed, Ahmed
IPC分类号： A61K31/4015 , A61K45/06
CPC分类号： C07D209/54 , A61K31/4015 , A61K45/06
摘要： Die Erfindung betrifft (5s,8s)-3-(4'-Chlor-3'-fluor-4-methylbiphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-on zu therapeutischen Zwecken, Pharmazeutische Mittel und deren Verwendung in der Therapie, insbesondere zur Prophylaxe und Therapie von Tumorerkrankungen.
摘要翻译：本发明涉及（5S，8S）-3-（4'-氯-3'-氟-4-甲基联苯-3-基）-4-羟基-8-甲氧基-1-氮杂螺[4.5]癸-3-烯 -2-酮用于治疗目的，药物制剂和它们在治疗肿瘤性疾病的预防和治疗中的用途，尤其如此。

9. 发明申请

WO2017055316A1 AMIDO-SUBSTITUTED AZOLE COMPOUNDS 审中-公开
标题翻译： AMIDO替代的AZOLE化合物
公开(公告)号：WO2017055316A1
公开(公告)日：2017-04-06
申请号：PCT/EP2016/073043
申请日：2016-09-28
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： EIS, Knut , ACKERSTAFF, Jens , WAGNER, Sarah , BUCHGRABER, Philipp , SÜLZLE, Detlev , BENDER, Eckhard , LI, Volkhart Min-Jian , LIU, Ningshu , SIEGEL, Franziska , LIENAU, Philip
IPC分类号： C07D403/12 , C07D233/90 , C07D405/12 , C07D413/12 , C07D471/10 , C07D495/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D233/90 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/10 , C07D495/10
摘要： The present invention relates to amido-substituted azole compounds of general formula (I), in which X 1 , X 2 , R 1 , R 2 , R 4 , R 5 , R 7 and R 8 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.
摘要翻译：本发明涉及通式（I）的酰胺取代的唑类化合物，其中X1，X2，R1，R2，R4，R5，R7和R8如本文所定义，与制备所述化合物的方法相关，可用于中间体化合物用于制备所述化合物，包含所述化合物的药物组合物和组合，以及所述化合物用于制备用于治疗或预防疾病，特别是赘生物的单一药物或与其它活性成分组合的药物组合物的用途。

10. 发明申请

WO2015104254A1 AMIDO-SUBSTITUTED IMIDAZOPYRIDAZINES USEFUL IN THE TREATMENT OF HYPER-PROLIFERATIVE AND/OR ANGIOGENESIS DISORDERS 审中-公开
标题翻译：用于治疗高血压和/或血管发生疾病的AMIDO取代的咪达唑胺
公开(公告)号：WO2015104254A1
公开(公告)日：2015-07-16
申请号：PCT/EP2015/050087
申请日：2015-01-06
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： SCHULZE, Volker , EIS, Knut , PUEHLER, Florian , ZORN, Ludwig , SÜLZLE, Detlev , LIENAU, Philip , WENGNER, Antje Margret , PETERSEN, Kirstin , BÖMER, Ulf
IPC分类号： C07D487/04 , C07D491/04 , C07D519/00 , A61K31/5025 , A61P35/00 , A61P37/00
CPC分类号： C07D519/00 , A61K31/5025 , A61K31/5377 , A61K45/06 , C07D487/04 , C07D491/04
摘要： The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): in which A, E, R2, R3, R4 and n are as defined in the claims, 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 a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译：本发明涉及通式（I）的酰氨基取代的咪唑并哒嗪化合物：其中A，E，R2，R3，R4和n如权利要求中所定义，涉及制备所述化合物的方法，可用于制备所述化合物，包含所述化合物的药物组合物和组合以及所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其他活性成分组合。

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