公开(公告)号：US20170114070A1

公开(公告)日：2017-04-27

申请号：US15127782

申请日：2015-03-18

申请人： Bayer Pharma Aktiengesellschaft

发明人： Kai THEDE ,  Eckhard BENDER ,  William SCOTT ,  Anja GIESE ,  Ludwig ZORN ,  Ningshu LIU ,  Ursula MÖNNING ,  Franziska SIEGEL ,  Stefan GOLZ ,  Andrea HÄGEBARTH ,  Philip LIENAU ,  Florian PUEHLER ,  Daniel BASTING ,  Dirk SCHNEIDER ,  Manfred MÖWES ,  Jens GEISLER

IPC分类号： C07D491/08 ,  A61K31/501 ,  C07D403/04 ,  A61K31/506 ,  C07D237/20 ,  A61K31/5377 ,  C07D241/20 ,  C07D253/07 ,  A61K31/53 ,  C07D239/42 ,  A61K31/497 ,  A61K31/541 ,  A61K45/06 ,  C07C233/54 ,  C07D295/15 ,  C07C233/25 ,  C07C205/45 ,  C07C229/64 ,  C07D241/24 ,  C07C205/59 ,  C07D401/04

CPC分类号： C07D491/08 ,  A61K9/0007 ,  A61K9/0019 ,  A61K9/0056 ,  A61K9/08 ,  A61K9/10 ,  A61K9/19 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2063 ,  A61K9/4858 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K45/06 ,  C07C205/45 ,  C07C205/59 ,  C07C229/64 ,  C07C233/25 ,  C07C233/54 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D241/24 ,  C07D241/28 ,  C07D253/07 ,  C07D295/15 ,  C07D401/04 ,  C07D403/04 ,  A61K2300/00

摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and 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 a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20180042931A1

公开(公告)日：2018-02-15

申请号：US15552251

申请日：2016-02-16

申请人： Bayer Pharma Aktiengesellschaft

发明人： Kai THEDE ,  Eckhard BENDER ,  William J. SCOTT ,  Anja GIESE ,  Ludwig ZORN ,  Ningshu LIU ,  Ursula MÖNNING ,  Franziska SIEGEL ,  Stefan GOLZ ,  Andrea HÄGEBARTH ,  Philip LIENAU ,  Florian PÜHLER ,  Daniel BASTING ,  Dirk SCHNEIDER ,  Manfred MÖWES

IPC分类号： A61K31/5377 ,  A61K45/06 ,  C07D239/26 ,  C07D213/40 ,  C07D231/12 ,  C07D239/34 ,  C07D239/42 ,  C07D213/64 ,  C07D213/73 ,  C07D213/61

CPC分类号： A61K31/5377 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D231/12 ,  C07D239/26 ,  C07D239/34 ,  C07D239/42 ,  C07D403/04

摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) wherein LA represents *CH2** or *Δ**; wherein indicates the point of attachment to the carbonyl group, and ** indicates the point of attachment to R1; LB represents *N(H)—C(═O)** or *C(═O)—N(H)**; wherein * indicates the point of attachment to R2, and ** indicates the point of attachment to the phenyl group; R1 represents a group selected from: (AA); wherein * indicates the point of attachment to LA, R2 represents: (BB) wherein * indicates the point of attachment to R3, and ** indicates the point of attachment to LB R3 represents a group selected from: (CC); wherein * indicates the point of attachment to R2; R4 and R5 represent a hydrogen atom; and R6 represents a halogen atom or group selected from: —CH3, —O—CH3, —O—CHF2, —O—CF3, and —O-cyclopropyl; to methods of 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 disorder, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20180028507A1

公开(公告)日：2018-02-01

申请号：US15552228

申请日：2016-02-16

申请人： Bayer Pharma Aktiengesellschaft

发明人： Kai THEDE ,  Eckhard BENDER ,  William J. SCOTT ,  Anja GIESE ,  Ludwig ZORN ,  Ningshu LIU ,  Ursula MÖNNING ,  Franziska SIEGEL ,  Stefan GOLZ ,  Andrea HÄGEBARTH ,  Philip LIENAU ,  Florian PÜHLER ,  Daniel BASTING ,  Dirk SCHNEIDER ,  Manfred MÖWES

IPC分类号： A61K31/435 ,  C07D401/14 ,  C07D213/75 ,  C07D401/12 ,  C07C237/44 ,  C07D213/73

CPC分类号： A61K31/435 ,  C07C237/44 ,  C07D213/73 ,  C07D213/75 ,  C07D401/12 ,  C07D401/14

摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and 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 a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients, in which: R1 represents a group selected from: C1-C3-alkoxy-C2-C3-alkyl-, (A), (B), (C), (D), (E), (F), (G) or (H); wherein * indicates the point of attachment to the rest of the molecule; R2 represents a group selected from: (I), (J) or (K); wherein * indicates the point of attachment to the rest of the molecule.

公开(公告)号：US20170273980A1

公开(公告)日：2017-09-28

申请号：US15512494

申请日：2015-09-17

申请人： Bayer Pharma Aktiengesellschaft

发明人： Anne MENGEL ,  Hans-Georg LERCHEN ,  Manfred MÖWES ,  Thomas MÜLLER ,  Lars BÄRFACKER ,  Marion HITCHCOCK ,  Arwed CLEVE ,  Joachim KUHNKE ,  Hans BRIEM ,  Gerhard SIEMEISTER ,  Wilhelm BONE ,  Amaury Ernesto FERNANDEZ-MONTALVAN ,  Jens SCHRÖDER ,  Ursula MÖNNING ,  Simon HOLTON

IPC分类号： A61K31/506 ,  C07D403/14 ,  C07D401/14

CPC分类号： A61K31/506 ,  C07D401/14 ,  C07D403/14

摘要： Compounds of formula (I) as defined herein and their use as pharmaceuticals.

公开(公告)号：US20180044306A1

公开(公告)日：2018-02-15

申请号：US15552249

申请日：2016-02-16

申请人： Bayer Pharma Aktiengesellschaft

发明人： Kai THEDE ,  Eckhard BENDER ,  William J. SCOTT ,  Anja GIESE ,  Ludwig ZORN ,  Ningshu LIU ,  Ursula MÖNNING ,  Franziska SIEGEL ,  Stefan GOLZ ,  Andrea HÄGEBARTH ,  Philip LIENAU ,  Florian PÜHLER ,  Daniel BASTING ,  Dirk SCHNEIDER ,  Manfred MÖWES ,  Jens GEISLER

IPC分类号： C07D285/135 ,  C07D417/04 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/496

CPC分类号： C07D285/135 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and 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 a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20170107212A1

公开(公告)日：2017-04-20

申请号：US15127780

申请日：2015-03-18

申请人： Bayer Pharma Aktiengesellschaft

发明人： Kai THEDE ,  Eckhard BENDER ,  William SCOTT ,  Anja GIESE ,  Ludwig ZORN ,  Ningshu LIU ,  Ursula MÖNNING ,  Franziska SIEGEL ,  Stefan GOLZ ,  Andrea HÄGEBARTH ,  Philip LIENAU ,  Florian PUEHLER ,  Daniel BASTING ,  Dirk SCHNEIDER ,  Manfred MÖWES ,  Jens GEISLER

IPC分类号： C07D417/14 ,  A61K31/5377 ,  C07D417/04 ,  A61K45/06 ,  C07D409/04 ,  A61K31/497 ,  A61K31/506 ,  C07D401/04 ,  A61K31/496

CPC分类号： C07D417/14 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D409/04 ,  C07D417/04

摘要： The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and 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 a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20160052898A1

公开(公告)日：2016-02-25

申请号：US14778603

申请日：2014-03-20

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Kai THEDE ,  William Johnston SCOTT ,  Eckhard BENDER ,  Stefan GOLZ ,  Andrea HÄGEBARTH ,  Philip LIENAU ,  Florian PUEHLER ,  Daniel BASTING ,  Dirk SCHNEIDER ,  Manfred MÖWES ,  Anja RICHTER ,  Ludwig ZORN ,  Ningshu LIU ,  Ursula MÖNNING ,  Franziska SIEGEL

IPC分类号： C07D295/15 ,  C07D491/08 ,  C07D498/08 ,  C07D333/24 ,  C07D307/54 ,  C07D491/107 ,  C07D267/10 ,  C07D211/42 ,  C07D211/46 ,  C07C237/40 ,  C07D207/12 ,  C07D231/10 ,  C07D265/30

CPC分类号： C07D295/15 ,  C07C233/54 ,  C07C233/80 ,  C07C237/40 ,  C07C237/42 ,  C07C237/44 ,  C07C271/24 ,  C07C317/44 ,  C07C317/48 ,  C07C317/50 ,  C07C323/63 ,  C07C2601/02 ,  C07D205/04 ,  C07D207/12 ,  C07D211/42 ,  C07D211/44 ,  C07D211/46 ,  C07D231/10 ,  C07D231/12 ,  C07D265/30 ,  C07D267/10 ,  C07D295/145 ,  C07D295/26 ,  C07D307/54 ,  C07D333/24 ,  C07D413/12 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107 ,  C07D498/08

摘要： The present invention relates to substituted N-biphenyl-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-biphenyl-carboxamides of general formula (I) as described and 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 a hyperproliferative disorder, as a sole agent or in combination with other active ingredients.

摘要翻译： 本发明涉及如本文所述和定义的取代的N-联苯-3-乙酰氨基 - 苯甲酰胺和通式（I）的N- [3-（乙酰氨基）苯基] - 联苯 - 甲酰胺，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特别是过度增殖性疾病的药物组合物作为唯一试剂或在 与其他活性成分组合。