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1.发明申请N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS 审中-公开N-苯基 - （MORPHOLIN-4-YL或PIPERAZINYL）乙酰胺衍生物及其作为WNT信号通路的抑制剂的用途
公开(公告)号：WO2016131810A1
公开(公告)日：2016-08-25
申请号：PCT/EP2016/053235
申请日：2016-02-16
发明人： THEDE, Kai , BENDER, Eckhard , SCOTT, William , RICHTER, Anja , ZORN, Ludwig , LIU, Ningshu , MÖNNING, Ursula , SIEGEL, Franziska , GOLZ, Stefan , HÄGEBARTH, Andrea , LIENAU, Philip , PUEHLER, Florian , BASTING, Daniel , SCHNEIDER, Dirk , MÖWES, Manfred
IPC分类号： C07D213/73 , C07D231/12 , C07D403/04 , C07D239/26 , C07D239/34 , C07D239/42 , C07D213/40 , C07D213/61 , C07D213/64 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P35/00
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 L A represents *CH 2 ** or *Δ**; wherein indicates the point of attachment to the carbonyl group, and ** indicates the point of attachment to R 1 ; L B represents *N(H)-C(=O)** or *C(=O)-N(H)**; wherein * indicates the point of attachment to R 2 , and ** indicates the point of attachment to the phenyl group; R 1 represents a group selected from: (AA); wherein * indicates the point of attachment to L A , R 2 represents: (BB) wherein * indicates the point of attachment to R 3 , and ** indicates the point of attachment to L B R 3 represents a group selected from: (CC); wherein * indicates the point of attachment to R 2 ; R 4 and R 5 represent a hydrogen atom; and R 6 represents a halogen atom or group selected from: -CH 3 , -O-CH 3 , -O-CHF 2 , -O-CF 3 , 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.
摘要翻译： 本发明涉及通式（I）的Wnt信号通路抑制剂，其中LA代表* CH2 **或*Δ**; 其中表示与羰基的连接点，**表示与R1的连接点; LB表示* N（H）-C（= O）**或* C（= O）-N（H）**; 其中*表示与R2的连接点，**表示与苯基的连接点; R1表示选自以下的基团：（AA）; 其中*表示与LA的连接点，R2表示：（BB）其中*表示与R3的连接点，**表示与LB的连接点，R3表示选自以下的基团：（CC）; 其中*表示与R2的连接点; R4和R5代表氢原子; 并且R 6表示选自：-CH 3，-O-CH 3，-O-CHF 2，-O-CF 3和-O-环丙基的卤素原子或基团; 制备所述化合物的方法，药物组合物和包含所述化合物的组合以及所述化合物用于制备用于治疗或预防疾病，特别是高增殖性疾病的药物组合物作为唯一试剂的用途 或与其他活性成分组合。
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公开(公告)号：WO2015140196A1
公开(公告)日：2015-09-24
申请号：PCT/EP2015/055631
申请日：2015-03-18
发明人： THEDE, Kai , BENDER, Eckhard , SCOTT, William J. , RICHTER, Anja , ZORN, Ludwig , LIU, Ningshu , MÖNNING, Ursula , SIEGEL, Franziska , GOLZ, Stefan , HÄGEBARTH, Andrea , LIENAU, Philip , PUEHLER, Florian , BASTING, Daniel , SCHNEIDER, Dirk , MÖWES, Manfred , GEISLER, Jens
IPC分类号： C07D491/08 , C07D491/04 , C07D403/04 , C07D237/20 , C07D239/42 , C07D241/20 , C07D241/28 , C07D253/07 , A61K31/496 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/53 , A61P35/00
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.
摘要翻译： 本发明涉及如本文所述和定义的通式（I）的Wnt信号传导途径的抑制剂，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， 使用所述化合物制造用于治疗或预防疾病，特别是高增殖性疾病的药物组合物作为唯一试剂或与其它活性成分组合。
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公开(公告)号：WO2015074986A1
公开(公告)日：2015-05-28
申请号：PCT/EP2014/074722
申请日：2014-11-17
发明人： KLAR, Ulrich , WORTMANN, Lars , KETTSCHAU, Georg , GRAHAM, Keith , RICHTER, Anja , LIENAU, Philip , PUEHLER, Florian , PETERSEN, Kirstin , SIEGEL, Franziska , SÜLZLE, Detlev
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D519/00
摘要： The present invention relates to substituted thienopyrimidine compounds 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 and/or angiogenesis 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通式（I）的取代的噻吩并嘧啶化合物，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 用于制造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它活性成分组合的化合物。
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公开(公告)号：WO2015140195A1
公开(公告)日：2015-09-24
申请号：PCT/EP2015/055629
申请日：2015-03-18
发明人： THEDE, Kai , BENDER, Eckhard , SCOTT, William , RICHTER, Anja , ZORN, Ludwig , LIU, Ningshu , MÖNNING, Ursula , SIEGEL, Franziska , GOLZ, Stefan , HÄGEBARTH, Andrea , LIENAU, Philip , PUEHLER, Florian , BASTING, Daniel , SCHNEIDER, Dirk , MÖWES, Manfred , GEISLER, Jens
IPC分类号： C07D401/14 , A61K31/427 , A61K31/433 , A61K31/444 , A61K31/497 , A61K31/506 , C07D401/04 , C07D417/04 , C07D417/14
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.
摘要翻译： 本发明涉及如本文所述和定义的通式（I）的Wnt信号传导途径的抑制剂，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， 使用所述化合物制造用于治疗或预防疾病，特别是高增殖性病症的药物组合物作为唯一试剂或与其它活性成分组合。
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5.发明申请AMIDO-SUBSTITUTED IMIDAZOPYRIDAZINES USEFUL IN THE TREATMENT OF HYPER-PROLIFERATIVE AND/OR ANGIOGENESIS DISORDERS 审中-公开用于治疗高血压和/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
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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公开(公告)号：WO2015004024A1
公开(公告)日：2015-01-15
申请号：PCT/EP2014/064347
申请日：2014-07-04
发明人： KLAR, Ulrich , WORTMANN, Lars , KETTSCHAU, Georg , GRAHAM, Keith , RICHTER, Anja , LIENAU, Philip , PUEHLER, Florian , PETERSEN, Kirstin , SIEGEL, Franziska , SÜLZLE, Detlev
IPC分类号： C07D519/00 , A61K31/519 , A61P35/04
CPC分类号： C07D471/04 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D519/00 , A61K2300/00
摘要： The present invention relates to substituted pyrazolopyridine compounds 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 and/or angiogenesis 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通式I的取代吡唑并吡啶化合物，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 制造用于治疗或预防疾病，特别是过度增殖和/或血管生成障碍的药物组合物，作为唯一试剂或与其它活性成分组合。
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7.发明申请1,3,4-THIADIAZOL-2-YL-BENZAMIDE DERIVATIVES AS INHIBITORSOF THE WNT SIGNALLING PATHWAY 审中-公开1,3,4-THIADIAZOL-2-YL-BENZAMIDE DERIVATIVES作为抑制剂WNT信号通路
公开(公告)号：WO2016131808A1
公开(公告)日：2016-08-25
申请号：PCT/EP2016/053231
申请日：2016-02-16
发明人： THEDE, Kai , BENDER, Eckhard , SCOTT, William , RICHTER, Anja , ZORN, Ludwig , LIU, Ningshu , MÖNNING, Ursula , SIEGEL, Franziska , GOLZ, Stefan , HÄGEBARTH, Andrea , LIENAU, Philip , PUEHLER, Florian , BASTING, Daniel , SCHNEIDER, Dirk , MÖWES, Manfred , GEISLER, Jens
IPC分类号： C07D417/12 , C07D417/14 , A61K31/454 , A61K31/496 , A61P35/00 , A61P37/02
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.
摘要翻译： 本发明涉及如本文所述和定义的通式（I）的Wnt信号传导途径的抑制剂，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， 使用所述化合物制造用于治疗或预防疾病，特别是高增殖性病症的药物组合物作为唯一试剂或与其它活性成分组合。
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8.发明申请3-CARBAMOYLPHENYL-4-CARBOXAMIDE AND ISOPHTALAMIDE DERIVATIVES AS INHIBITORS OF THE WNT SIGNALLING PATHWAY 审中-公开作为WNT信号通路的抑制剂的3-羰基苯基-4-羧酰胺和异佛尔酮二胺衍生物
公开(公告)号：WO2016131794A1
公开(公告)日：2016-08-25
申请号：PCT/EP2016/053211
申请日：2016-02-16
发明人： THEDE, Kai , BENDER, Eckhard , SCOTT, William , RICHTER, Anja , ZORN, Ludwig , LIU, Ningshu , MÖNNING, Ursula , SIEGEL, Franziska , GOLZ, Stefan , HÄGEBARTH, Andrea , LIENAU, Philip , PUEHLER, Florian , BASTING, Daniel , SCHNEIDER, Dirk , MÖWES, Manfred
IPC分类号： C07D401/14 , C07D213/73 , C07D213/75 , C07D401/12 , A61K31/435 , A61P35/00 , C07C15/04
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: R 1 represents a group selected from: C 1 -C 3 -alkoxy-C 2 -C 5 -alkyl-, (A), (B), (C), (D), (E), (F), (G) or (H); wherein * indicates the point of attachment to the rest of the molecule; R 2 represents a group selected from: (I), (J) or (K); wherein * indicates the point of attachment to the rest of the molecule.
摘要翻译： 本发明涉及如本文所述和定义的通式（I）的Wnt信号传导途径的抑制剂，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， 使用所述化合物制造用于治疗或预防疾病，特别是高增殖性疾病的药物组合物作为唯一试剂或与其它活性成分组合，其中：R1表示选自以下的基团：C1 （A），（B），（C），（D），（E），（F），（G）或（H） 其中*表示与分子的其余部分连接的点; R2表示选自：（I），（J）或（K）的基团; 其中*表示与分子的其余部分连接的点。
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公开(公告)号：WO2014147182A2
公开(公告)日：2014-09-25
申请号：PCT/EP2014/055616
申请日：2014-03-20
发明人： THEDE, Kai , SCOTT, William Johnston , BENDER, Eckhard , GOLZ, Stefan , HÄGEBARTH, Andrea , LIENAU, Philip , PUEHLER, Florian , BASTING, Daniel , SCHNEIDER, Dirk , MÖWES, Manfred
IPC分类号： C07D491/08
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 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 hyper-proliferative 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 - 甲酰胺与制备所述化合物的方法， 可用于制备所述化合物的化合物，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，特别是高增殖性疾病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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10.发明申请3-ACETYLAMINO-1-(PHENYL-HETEROARYL-AMINOCARBONYL OR PHENYL-HETEROARYL-CARBONYLAMINO)BENZENE DERIVATIVES FOR THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS 审中-公开用于治疗过度增殖性疾病的3-乙酰氨基-1-（苯基 - 杂芳基 - 氨基羰基或苯基 - 杂芳基 - 羰基氨基）苯衍生物
公开(公告)号：WO2014147021A3
公开(公告)日：2014-09-25
申请号：PCT/EP2014/055300
申请日：2014-03-17
发明人： THEDE, Kai , BENDER, Eckhard , SCOTT, William J. , RICHTER, Anja , ZORN, Ludwig , LIU, Ningshu , MÖNNING, Ursula , SIEGEL, Franziska , GOLZ, Stefan , HÄGEBARTH, Andrea , LIENAU, Philip , PUEHLER, Florian , BASTING, Daniel , SCHNEIDER, Dirk , MÖWES, Manfred
IPC分类号： C07D213/75 , C07D498/08 , C07D277/46 , C07D277/56 , C07D333/38 , C07D213/82 , C07D263/34 , C07D207/34 , C07D285/135 , C07D271/06 , C07D231/14 , C07D271/07 , C07D401/12 , C07D417/12 , C07D487/08 , C07D271/113 , A61K31/4418 , A61P35/00
摘要： The present invention relates to substituted N-(phenyl-heteroaryl) -3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-phenyl-heteroaryl-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 such as cancer, wherein i.a.: L A represents an optionally substituted methylene or ethylene group; L B represents -N(H)-C(=0)- or -C(=0)-N(H)-; R 1 represents an optionally substituted 5- to 8-membered heterocycloalkyl, 4- to 10-membered heterocycloalkenyl, aryl, heteroaryl or -N(R7)(Ci-C6-alkyl) group; R 2 represents an optionally substituted 5- or 6-membered heteroaryl group; R 3 represents an optionally substituted phenyl group.
摘要翻译： 本发明涉及通式（I）的取代的N-（苯基 - 杂芳基）-3-乙酰氨基 - 苯甲酰胺和N- [3-（乙酰氨基）苯基] - 苯基 - 杂芳基 - 甲酰胺， 如本文所述和定义，涉及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在制备用于治疗或预防疾病的药物组合物中的用途 如癌症，其中ia：L表示任选取代的亚甲基或亚乙基; L表示-N（H）-C（= O） - 或-C（= O）-N（H） - ; R 1表示任选取代的5-至8-元杂环烷基，4-至10-元杂环烯基，芳基，杂芳基或-N（R 7）（C 1 -C 6 - 烷基）基团; R 2表示任选取代的5元或6元杂芳基; R 3表示任选取代的苯基。
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