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

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： BUCHGRABER, Philipp ,  EIS, Knut ,  WAGNER, Sarah ,  SÜLZLE, Detlev ,  BENDER, Eckhard ,  LI, Volkhart, Min-Jian ,  LIU, Ningshu ,  SIEGEL, Franziska ,  LIENAU, Philip

IPC: 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

Abstract: 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.

Abstract translation: 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。

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

Applicant: BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC.

Inventor： 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: C07D487/14 ,  C07D487/04 ,  C07D498/04 ,  C07D498/14 ,  C07D498/20 ,  A61K31/4162 ,  A61P35/00

Abstract: 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.

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

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： SIEGEL, Stephan ,  CLEVE, Arwed ,  HAENDLER, Bernard ,  EIS, Knut

IPC: C07D243/02 ,  A61K31/551 ,  A61P25/00 ,  A61P35/00

CPC classification number: C07D243/02

Abstract: 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.

Abstract translation: 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。

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

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： EIS, Knut ,  PÜHLER, Florian ,  ZORN, Ludwig ,  SCHULZE, Volker ,  SÜLZLE, Detlev ,  LIENAU, Philip ,  WENGNER, Antje, Margret ,  PETERSEN, Kirstin ,  BÖMER, Ulf

IPC: C07D487/04 ,  C07D491/04 ,  A61K31/5025 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

CPC classification number: A61K31/5025 ,  A61K9/0019 ,  A61K9/19 ,  A61K9/20 ,  A61K9/48 ,  A61K31/5377 ,  A61K31/695 ,  A61K45/06 ,  C07D487/04 ,  C07D491/04 ,  C07D519/00 ,  C07F7/1856

Abstract: 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.

Abstract translation: 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。

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

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： ZORN, Ludwig ,  EIS, Knut ,  SCHULZE, Volker ,  SÜLZLE, Detlev ,  PÜHLER, Florian ,  LIENAU, Philip ,  BÖMER, Ulf ,  PETERSEN, Kirstin ,  HÄGEBARTH, Andrea

IPC: C07D487/04 ,  C07D491/04 ,  A61K31/5025 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K31/513 ,  A61K45/06 ,  C07D491/04 ,  C07D491/048

Abstract: 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.

Abstract translation: 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。

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

Applicant: 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

Inventor： LIU, Ningshu ,  THEDE, Kai ,  LIENAU, Philip ,  SCHOLZ, Arne ,  HILGER, Christoph-Stephan ,  BÖMER, Ulf ,  NAJJAR, Maher ,  EIS, Knut ,  FISCHER, Reiner ,  MORADI, Wahed, Ahmed

IPC: A61K31/4015 ,  A61K45/06

CPC classification number: C07D209/54 ,  A61K31/4015 ,  A61K45/06

Abstract: 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.

Abstract translation: 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。

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

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： EIS, Knut ,  ACKERSTAFF, Jens ,  WAGNER, Sarah ,  BUCHGRABER, Philipp ,  SÜLZLE, Detlev ,  BENDER, Eckhard ,  LI, Volkhart Min-Jian ,  LIU, Ningshu ,  SIEGEL, Franziska ,  LIENAU, Philip

IPC: C07D403/12 ,  C07D233/90 ,  C07D405/12 ,  C07D413/12 ,  C07D471/10 ,  C07D495/10 ,  A61K31/4164 ,  A61K31/4178 ,  A61P35/00

CPC classification number: C07D233/90 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/10 ,  C07D495/10

Abstract: 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.

Abstract translation: 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 。

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

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： SCHULZE, Volker ,  EIS, Knut ,  PUEHLER, Florian ,  ZORN, Ludwig ,  SÜLZLE, Detlev ,  LIENAU, Philip ,  WENGNER, Antje Margret ,  PETERSEN, Kirstin ,  BÖMER, Ulf

IPC: C07D487/04 ,  C07D491/04 ,  C07D519/00 ,  A61K31/5025 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D519/00 ,  A61K31/5025 ,  A61K31/5377 ,  A61K45/06 ,  C07D487/04 ,  C07D491/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2014147203A1

公开(公告)日：2014-09-25

申请号：PCT/EP2014/055657

申请日：2014-03-20

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： HITCHCOCK, Marion ,  MENGEL, Anne ,  BRIEM, Hans ,  EIS, Knut ,  SIEMEISTER, Gerhard ,  BONE, Wilhelm ,  FERNÁNDEZ-MONTALVÁN, Amaury, Ernesto ,  SCHRÖDER, Jens ,  HOLTON, Simon ,  PREUSSE, Cornelia ,  PÜTTER, Vera

IPC: C07D401/14 ,  A61K31/506 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04 ,  A61P35/00

CPC classification number: C07D403/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.

Abstract translation: 作为Bub1激酶抑制剂的式（I）化合物，其制备方法及其作为药物的用途。

公开(公告)号：WO2014076162A1

公开(公告)日：2014-05-22

申请号：PCT/EP2013/073793

申请日：2013-11-14

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： ZORN, Ludwig ,  EIS, Knut ,  SCHULZE, Volker ,  SÜLZLE, Detlev ,  PÜHLER, Florian ,  LIENAU, Philip ,  BÖMER, Ulf ,  PETERSEN, Kirstin ,  HÄGEBARTH, Andrea

IPC: C07D487/04 ,  A61K31/4355 ,  A61P35/00

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K45/06 ,  C07D519/00

Abstract: The present invention relates to amino-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.

Abstract translation: 本发明涉及通式（I）的氨基取代的咪唑并哒嗪化合物，其中A，R 1，R 2，R 3，R 4和n如权利要求中所定义，可用于制备所述化合物的方法， 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。