公开(公告)号：WO2018153969A1

公开(公告)日：2018-08-30

申请号：PCT/EP2018/054362

申请日：2018-02-22

Applicant: BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： WENGNER, Antje,Margret ,  SCHOLZ, Arne

IPC: A61K45/06 ,  A61K31/5377 ,  A61K33/24 ,  A61P35/00

CPC classification number: A61K33/24 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  A61K2300/00

Abstract: The present invention covers combinations of at least two components, component A and component B, component A being an ATR kinase inhibitor, and component B being radium-223, particularly a pharmaceutically acceptable salt of radium-223. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a hyper-proliferative disease, particurlarly for the treatment of prostate cancer as well as bone metastases thereof.

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：WO2016059011A1

公开(公告)日：2016-04-21

申请号：PCT/EP2015/073609

申请日：2015-10-13

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： KOSEMUND, Dirk ,  LÜCKING, Ulrich ,  SIEMEISTER, Gerhard ,  SCHOLZ, Arne ,  LIENAU, Philip

IPC: C07D405/04 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D405/04 ,  A61K31/506 ,  C07D239/42

Abstract: The present invention relates to fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group of general formula (I) 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). R 2 represents the group (a).

Abstract translation: 本发明涉及含有本文所述和定义的通式（I）的砜基的氟化苯并呋喃基 - 嘧啶衍生物及其制备方法，其用于治疗和/或预防病症，特别是高增殖性 疾病和/或病毒诱导的传染病和/或心血管疾病。 本发明还涉及可用于制备所述通式（I）化合物的中间体化合物。 R2表示组（a）。

公开(公告)号：WO2014076111A1

公开(公告)日：2014-05-22

申请号：PCT/EP2013/073683

申请日：2013-11-13

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： LÜCKING, Ulrich ,  BÖHNKE, Niels ,  SCHOLZ, Arne ,  LIENAU, Philip ,  SIEMEISTER, Gerhard ,  BÖMER, Ulf ,  KOSEMUND, Dirk ,  BOHLMANN, Rolf

IPC: C07D401/12 ,  A61K31/506 ,  A61P9/00 ,  A61P35/00

CPC classification number: C07D401/12 ,  A61K31/506

Abstract: The present invention relates to disubstituted N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfoximine group of general formula (I) 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).

Abstract translation: 本发明涉及含有本文所述和定义的通式（I）的亚磺酰亚胺基的二取代的N-（吡啶-2-基）嘧啶-4-胺衍生物及其制备方法及其用于治疗和/ 或预防疾病，特别是高增殖性疾病和/或病毒诱导的传染病和/或心血管疾病的疾病。 本发明还涉及可用于制备所述通式（I）化合物的中间体化合物。

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：WO2016150903A1

公开(公告)日：2016-09-29

申请号：PCT/EP2016/056112

申请日：2016-03-21

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： SCHOLZ, Arne

IPC: A61K31/53 ,  A61K45/06 ,  A61P35/00

CPC classification number: A61K31/53 ,  A61K45/06

Abstract: The present invention relates to 4-(4-Fluoro-2-methoxyphenyl)-N- {3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A), more particularly (+)-4-(4-Fluoro-2-methoxyphenyl)-N- {3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A'), for use in treating lymphoma, preferably diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma, follicular lymphoma, diffuse large B-cell lymBurkitt's lymphoma, adult T-cell lymphoma (ATL) and Hodgkin's lymphoma, more preferably DLBCL and ATL.

Abstract translation: 本发明涉及4-（4-氟-2-甲氧基苯基）-N- {3 - [（S-甲基亚氨基亚氨基）甲基]苯基} -1,3,5-三嗪-2-胺（化合物A），更多 特别是（+） - 4-（4-氟-2-甲氧基苯基）-N- {3 - [（S-甲基亚氨基亚氨基）甲基]苯基} -1,3,5-三嗪-2-胺（化合物A'）， 用于治疗淋巴瘤，优选弥漫性大B细胞淋巴瘤（DLBCL），套细胞淋巴瘤，滤泡淋巴瘤，弥漫性大B细胞淋巴细胞淋巴瘤，成人T细胞淋巴瘤（ATL）和霍奇金淋巴瘤，更优选DLBCL和ATL。

公开(公告)号：WO2016150902A1

公开(公告)日：2016-09-29

申请号：PCT/EP2016/056108

申请日：2016-03-21

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： SCHOLZ, Arne

IPC: A61K31/53 ,  A61P35/00 ,  A61K45/06

CPC classification number: A61K31/53 ,  A61K45/06

Abstract: The present invention relates to the use of 4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S- methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A), more particularly (+)-4-(4- Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A´), for treating gastric cancer, preferably gastric cancers in which cells have an amplification of the C-MYC gene.

Abstract translation: 本发明涉及4-（4-氟-2-甲氧基苯基）-N- {3 - [（S-甲基亚氨基亚氨基）甲基]苯基} -1,3,5-三嗪-2-胺（化合物A ），更特别是（+） - 4-（4-氟-2-甲氧基苯基）-N- {3 - [（S-甲基亚氨基）甲基]苯基} -1,3,5-三嗪-2-胺（化合物A '），用于治疗胃癌，优选其中细胞具有C-MYC基因扩增的胃癌。

公开(公告)号：WO2016150893A1

公开(公告)日：2016-09-29

申请号：PCT/EP2016/056089

申请日：2016-03-21

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： SCHOLZ, Arne

IPC: C07D251/22 ,  A61P35/00 ,  A61K31/53

CPC classification number: A61K31/53 ,  C07D251/22

Abstract: The present invention relates to the use of 4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A), more particularly (+)-4-(4-Fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine (compound A´), for treating multiple myeloma.

Abstract translation: 本发明涉及4-（4-氟-2-甲氧基苯基）-N- {3 - [（S-甲基亚氨基亚氨基）甲基]苯基} -1,3,5-三嗪-2-胺（化合物A ），更特别是（+） - 4-（4-氟-2-甲氧基苯基）-N- {3 - [（S-甲基亚氨基亚氨基）甲基]苯基} -1,3,5-三嗪-2-胺（化合物A '），用于治疗多发性骨髓瘤。

公开(公告)号：WO2015082378A1

公开(公告)日：2015-06-11

申请号：PCT/EP2014/076053

申请日：2014-12-01

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： LIU, Ningshu ,  SCHOLZ, Arne ,  HÄGEBARTH, Andrea

IPC: A61K45/06 ,  A61K31/519 ,  A61K31/5377 ,  A61K33/14 ,  A61P35/00 ,  A61P35/04 ,  A61K51/02

CPC classification number: A61K31/5377 ,  A61K31/519 ,  A61K33/14 ,  A61K45/06 ,  A61K51/00 ,  A61K51/02 ,  A61K2300/00

Abstract: The present invention relates to combinations of at least two components, component A and component B, component A being an inhibitor of PI3K kinase, and component B being a pharmaceutically acceptable salt of radium 223. Another aspect of the present invention relates to the use of such combinations as described supra for the preparation of a medicament for the treatment or prophylaxis of a disease, particurlarly for the treatment of cancer with bone metatases.

Abstract translation: 本发明涉及至少两种组分的组合，组分A和组分B，组分A是PI3K激酶的抑制剂，组分B是镭223的药学上可接受的盐。本发明的另一方面涉及使用 如上所述的用于制备用于治疗或预防疾病，特别是用于骨代谢治疗癌症的药物的上述组合。

公开(公告)号：WO2014060493A2

公开(公告)日：2014-04-24

申请号：PCT/EP2013/071661

申请日：2013-10-16

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： LÜCKING, Ulrich ,  BÖHNKE, Niels ,  SCHOLZ, Arne ,  LIENAU, Philip ,  SIEMEISTER, Gerhard ,  BÖMER, Ulf ,  KOSEMUND, Dirk ,  BOHLMANN, Rolf

IPC: C07D405/14 ,  C07D401/12 ,  A61K31/506 ,  A61P9/00 ,  A61P31/12 ,  A61P35/00

CPC classification number: C07D401/12 ,  A61K31/506 ,  A61K45/06 ,  C07D207/44 ,  C07D233/88 ,  C07D405/14 ,  A61K2300/00

Abstract: The present invention relates to N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group of general formula (I) 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).

Abstract translation: 本发明涉及含有本文所述和定义的通式（I）的砜基的N-（吡啶-2-基）嘧啶-4-胺衍生物及其制备方法及其用于治疗和/或 预防疾病，特别是高增殖性疾病和/或病毒诱导的传染病和/或心血管疾病。 本发明还涉及可用于制备所述通式（I）化合物的中间体化合物。