公开(公告)号：EP2807162A1

公开(公告)日：2014-12-03

申请号：EP13700765.4

申请日：2013-01-22

申请人： Bayer Pharma Aktiengesellschaft ,  Bayer Intellectual Property GmbH

发明人： SÜßMEIER, Frank ,  LOBELL, Mario ,  GRÜNEWALD, Sylvia ,  HÄRTER, Michael ,  BUCHMANN, Bernd ,  TELSER, Joachim ,  JÖRIßEN, Hannah ,  HEROULT, Melanie ,  KAHNERT, Antje ,  LUSTIG, Klemens ,  LINDNER, Niels

IPC分类号： C07D487/04 ,  A61K31/4188 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06

摘要： The present application relates to novel 1-phenyl-1
H -imidazo[1,2-b]pyrazole derivatives of the fomula (I), to processes for preparation thereof, to the use thereof for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially of angiogenic disorders and hyperproliferative disorders where neovascularization is involved, for example cancers and tumors. Such treatments can be effected as a monotherapy or else in combination with other medicaments or further therapeutic measures.

公开(公告)号：EP2791140A1

公开(公告)日：2014-10-22

申请号：EP12798738.6

申请日：2012-12-10

申请人： Bayer Pharma Aktiengesellschaft ,  Bayer Intellectual Property GmbH

发明人： BROHM, Dirk ,  HEROULT, Melanie ,  COLLIN, Marie-Pierre ,  HÜBSCH, Walter ,  LOBELL, Mario ,  LUSTIG, Klemens ,  GRÜNEWALD, Sylvia ,  BÖMER, Ulf ,  VÖHRINGER, Verena

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/53 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541

摘要： This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R
1 is hydrogen, chloro, methyl or methoxy, R
2 is hydrogen or methoxy, with the proviso that at least one of R
1 and R
2 is other than hydrogen, G
1 represents chloro, (C
1 -C
4 )-alkyl, (C
1 -C
4 )-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group -CH
2 -OR
3 , -CH
2 -NR
4 R
5 or -C(=0)- NR
4 R
6 , and G
2 represents chloro, cyano, (C
1 -C
4 )-alkyl, or the group - CR
8A R
8B -OH, -CH
2 -NR
9 R
10 , -C(=0)-NR
11 R
12 or -CH
2 -OR
15 , having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.

公开(公告)号：EP2791140B1

公开(公告)日：2016-06-15

申请号：EP12798738.6

申请日：2012-12-10

申请人： Bayer Pharma Aktiengesellschaft ,  Bayer Intellectual Property GmbH

发明人： BROHM, Dirk ,  HEROULT, Melanie ,  COLLIN, Marie-Pierre ,  HÜBSCH, Walter ,  LOBELL, Mario ,  LUSTIG, Klemens ,  GRÜNEWALD, Sylvia ,  BÖMER, Ulf ,  VÖHRINGER, Verena

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/53 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541

公开(公告)号：EP3229800A2

公开(公告)日：2017-10-18

申请号：EP15805493.2

申请日：2015-12-08

申请人： Bayer Pharma Aktiengesellschaft

发明人： ELLINGHAUS, Peter ,  HEROULT, Melanie

IPC分类号： A61K31/4184 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/506 ,  A61K31/53 ,  A61P35/00

CPC分类号： A61K31/53 ,  A61K31/4184 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/506

摘要： The current invention is based on a pan FGFR inhibitor for use in the treatment of cancer in a subject, wherein the subject is one for whom the sum of FGFR1, FGFR2 and/ or FGFR3 mRNA in a tumor tissue sample from the subject has been found to be overexpressed.

摘要翻译： 本发明基于泛FGFR抑制剂用于治疗受试者中的癌症，其中所述受试者是已经发现来自受试者的肿瘤组织样品中的FGFR1，FGFR2和/或FGFR3mRNA的总和的受试者 被过度表达。

公开(公告)号：EP3304080A1

公开(公告)日：2018-04-11

申请号：EP16724899.6

申请日：2016-05-25

申请人： Bayer Pharma Aktiengesellschaft

发明人： HAENDLER, Bernard ,  GELATO, Kathy Ann ,  SCHÖCKEL, Laura ,  HEROULT, Melanie

IPC分类号： G01N33/574

CPC分类号： G01N33/5743 ,  A61K31/17 ,  A61K31/215 ,  A61K31/381 ,  A61K31/497 ,  A61K31/551 ,  A61P35/00

摘要： The present invention refers to a method and kit for stratification of melanoma patients by determining the OCR and levels of PPARGC1A, PPARGC1B and MITF RNA, derived cDNA, or corresponding protein. Especially, the invention is related to stratification kits to determine whether a patient with melanoma will respond to treatment with a BET inhibitor. In a further aspect, the invention is related to the use of a BET inhibitor for the treatment of melanoma in a patient by stratifying a sample of body fluid or tumor tissue in vitro and determining whether a patient suffering from melanoma will respond to treatment with a BET inhibitor.

公开(公告)号：EP3172194A1

公开(公告)日：2017-05-31

申请号：EP15738705.1

申请日：2015-07-22

申请人： Bayer Pharma Aktiengesellschaft

发明人： BUCHMANN, Bernd ,  HEISLER, Iring ,  MÜLLER, Thomas ,  CLEVE, Arwed ,  HEROULT, Melanie ,  NEUHAUS, Roland ,  PETRUL, Heike ,  QUANZ-SCHÖFFEL, Maria

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D401/12 ,  C07D417/14 ,  A61P35/00 ,  A61K31/4709

CPC分类号： C07D417/14 ,  A61K31/4709 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

摘要： The present invention relates to chemical compounds of formula (I) that selectively inhibit glucose transporter 1 (GLUT1), to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

摘要翻译： 本发明涉及选择性抑制葡萄糖转运蛋白1（GLUT1）的式（I）化学化合物，制备所述化合物的方法，包含所述化合物的药物组合物和组合，涉及所述化合物用于制备用于 治疗或预防疾病，以及用于制备所述化合物的中间体化合物。