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1. 发明申请

WO2019057852A1 USE OF KAP1 AS A BIOMARKER FOR DETECTING OR MONITORING ATR INHIBITION IN A SUBJECT 审中-公开
公开(公告)号：WO2019057852A1
公开(公告)日：2019-03-28
申请号：PCT/EP2018/075535
申请日：2018-09-20
申请人： BAYER AKTIENGESELLSCHAFT , BAYER PHARMA AKTIENGESELLSCHAFT
发明人： GOLFIER, Sven , WENGNER, Antje, Margret , BEHNKE, Anna , SCHUBERT, Sabine
IPC分类号： G01N33/50 , G01N33/68
CPC分类号： G01N33/5011 , G01N33/68 , G01N2440/14
摘要： The present invention covers a method for detecting or monitoring ATR inhibition in a subject, the method comprising quantifying the amount of pKAP1 protein phosphorylated at serine 824 in a sample from said subject. It also covers the use of pKAP1 protein phosphorylated at serine 824 as a biomarker for detecting or monitoring ATR inhibition in a subject, the use comprising quantifying the amount of pKAP1 protein phosphorylated at serine 824 in a sample obtained from said subject.

2. 发明申请

WO2014198645A1 COMBINATIONS FOR THE TREATMENT OF CANCER COMPRISING A MPS-1 KINASE INHIBITOR AND A MITOTIC INHIBITOR 审中-公开
标题翻译：用于治疗包含MPS-1激酶抑制剂和MITOTIC抑制剂的癌症的组合
公开(公告)号：WO2014198645A1
公开(公告)日：2014-12-18
申请号：PCT/EP2014/061772
申请日：2014-06-06
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： WENGNER, Antje, Margret , SIEMEISTER, Gerhard
IPC分类号： A61K31/337 , A61K31/437 , A61K31/475 , A61K33/24 , A61P35/00
CPC分类号： A61K31/437 , A61K31/337 , A61K31/475 , A61K33/24 , A61K2300/00
摘要： The present invention relates to a combination comprising an Mps-1 kinase inhibitor and a mitotic inhibitor. The present invention also relates to the use of said combination for the treatment of cancer, in particular of pancreatic cancer, glioblastoma, ovarian cancer, non-small cell lung carcinoma, breast cancer and/or gastric cancer.
摘要翻译：本发明涉及包含Mps-1激酶抑制剂和有丝分裂抑制剂的组合。本发明还涉及所述组合用于治疗癌症，特别是胰腺癌，胶质母细胞瘤，卵巢癌，非小细胞肺癌，乳腺癌和/或胃癌的用途。

3. 发明申请

WO2014128093A1 SUBSTITUTED-IMIDAZO[1,2-B]PYRIDAZINES AS MKNK1 INHIBITORS 审中-公开
标题翻译：作为MKNK1抑制剂的替代 - 咪唑并[1,2-B]吡啶
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
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： EIS, Knut , PÜHLER, Florian , ZORN, Ludwig , SCHULZE, Volker , SÜLZLE, Detlev , LIENAU, Philip , WENGNER, Antje, Margret , PETERSEN, Kirstin , BÖMER, Ulf
IPC分类号： C07D487/04 , C07D491/04 , A61K31/5025 , A61P35/00 , A61P29/00 , A61P37/00
CPC分类号： A61K31/5025 , A61K9/0019 , A61K9/19 , A61K9/20 , A61K9/48 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D487/04 , C07D491/04 , C07D519/00 , C07F7/1856
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2018172250A1 2-METHYL-QUINAZOLINES 审中-公开
公开(公告)号：WO2018172250A1
公开(公告)日：2018-09-27
申请号：PCT/EP2018/056824
申请日：2018-03-19
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： WORTMANN, Lars , SAUTIER, Brice , EIS, Knut , BRIEM, Hans , BÖHNKE, Niels , VON NUSSBAUM, Franz , HILLIG, Roman , BADER, Benjamin , SCHRÖDER, Jens , PETERSEN, Kirstin , LIENAU, Philip , WENGNER, Antje, Margret , MOOSMAYER, Dieter , WANG, Qiuwen , SCHICK, Hans
IPC分类号： C07D403/12 , C07D405/14 , C07D401/12 , C07D403/04 , C07D405/10 , C07D405/12 , C07D409/12 , C07D409/14 , C07D239/94 , C07D417/12 , C07D487/04 , C07D495/04 , A61P35/00 , A61K31/517
摘要： The present invention describes 2-methyl-quinazoline compounds of general formula (I), 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. The 2-methyl substituted quinazoline compounds of general formula(I) effectively and selectively inhibit the Ras-Sos interaction without significantly targeting the EGFR receptor. They are therefore useful for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, such as cancer as a sole agent or in combination with other active ingredients.

5. 发明申请

WO2014195274A1 SUBSTITUTED TRIAZOLOPYRIDINES 审中-公开
标题翻译：取代三唑并吡啶
公开(公告)号：WO2014195274A1
公开(公告)日：2014-12-11
申请号：PCT/EP2014/061410
申请日：2014-06-03
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： SCHIROK, Hartmut , SCHULZE, Volker , KOSEMUND, Dirk , BRIEM, Hans , BADER, Benjamin , BÖMER, Ulf , WENGNER, Antje, Margret , SIEMEISTER, Gerhard , LIENAU, Philip
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , A61K31/496 , A61K31/5377 , A61K45/06
摘要： The present invention relates to substituted triazolopyridine compounds of general formula (I); in which R 1 , R 2 , R 3 , R 4 , and R 5 are as given in the description and in the claims, 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：本发明涉及通式（I）的取代三唑并吡啶化合物; 其中R 1，R 2，R 3，R 4和R 5如在说明书和权利要求书中给出的，涉及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，用于制备药物组合物的所述化合物用于治疗或预防疾病，以及可用于制备所述化合物的中间体化合物。

6. 发明申请

WO2021013693A1 ANTIBODY DRUG CONJUGATES (ADCS) WITH NAMPT INHIBITORS 审中-公开
公开(公告)号：WO2021013693A1
公开(公告)日：2021-01-28
申请号：PCT/EP2020/070149
申请日：2020-07-16
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BAYER AKTIENGESELLSCHAFT
发明人： BÖHNKE, Niels , GRIEBENOW, Nils , SOMMER, Anette , HAMMER, Stefanie , BERNDT, Sandra , STELTE-LUDWIG, Beatrix , BEIER, Rudolf , MAHLERT, Christoph , GREVEN, Simone , GIESE, Anja , GÜNTHER, Judith , BARAK, Naomi , BÖMER, Ulf , DIETZ, Lisa , JÖRISSEN, Hannah , ERKELENZ, Michael , ROTTMANN, Antje , WENGNER, Antje, Margret , FERNANDEZ-MONTALVAN, Amaury, Ernesto
IPC分类号： A61K47/68 , A61P35/00
摘要： Conjugate of a binder having formula (AA) wherein AB stands for a binder, Z' stands for a linker, D stands for an active component which is a NAMPT inhibitor and its use as pharmaceuticals.

7. 发明申请

WO2019025440A1 COMBINATION OF ATR KINASE INHIBITORS AND PD-1/PD-L1 INHIBITORS 审中-公开
公开(公告)号：WO2019025440A1
公开(公告)日：2019-02-07
申请号：PCT/EP2018/070729
申请日：2018-07-31
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BAYER AKTIENGESELLSCHAFT
发明人： WENGNER, Antje, Margret
IPC分类号： A61K45/06 , C07D471/04
摘要： The present invention covers combinations of at least two components, component A and component B, comprising component A being an inhibitor of ATR kinase, particularly an inhibitor of ATR kinase selected from VX-803, VX-970, AZD-6738, a compound of general formula (I) described herein, a compound of general formula (lb) described herein and Compound A described infra, and component B being a PD-1/PD-L1 inhibitor described herein. 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 disease, particurlarly for the treatment of a hyper-proliferative disease.

8. 发明申请

WO2018153968A1 AN INHIBITOR OF ATR KINASE FOR USE IN A METHOD OF TREATING A HYPER-PROLIFERATIVE DISEASE 审中-公开
公开(公告)号：WO2018153968A1
公开(公告)日：2018-08-30
申请号：PCT/EP2018/054361
申请日：2018-02-22
申请人： BAYER AKTIENGESELLSCHAFT , BAYER PHARMA AKTIENGESELLSCHAFT
发明人： WENGNER, Antje, Margret , SIEMEISTER, Gerhard , HÄNDLER, Bernard , GOLFIER, Sven , SCHLICKER, Andreas , LIU, Li
IPC分类号： C12Q1/6886
摘要： The present invention covers 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H- pyrazol-5-yl)-1,7-naphthyridine (in the following called "Compound A"), an inhibitor of ATR kinase, for use in a method of treating a hyper-proliferative disease in a subject. Preferably the hyper-proliferative disease or the subject is characterized by one or more biomarker(s) selected from a) one or more functional mutation(s) in one or more gene(s)/protein(s) selected from APC, ATG5, ARID1A, ATM, ATR, ATRIP, ATRX, BAP1, BARD1, BLM, BRAF, BRCA1, BRCA2, BRIP1, CCND1, CCNE1, CCNE2, CDC7, CDK12, CHEK1, CHEK2, DCLRE1A, DCLRE1B, DCLRE1C, DYRK1A, EGFR, ERBB2, ERBB3, ERCC2, ERCC3, ERCC4, ERCC5, FAM175A, FANCA, FANCB, FANCC, FANCD2, FANCE, FANCF, FANCG, FANCI, FANCL, FANCM, FBXO18, FBXW7, FEN1, GEN1, HDAC2, H2AFX, HRAS, KRAS, LIG4, MDC1, MLH1, MLH3, MRE11A, MSH2, MSH3, MSH6, MYC, NBN, NRAS, PALB2, PARP1, PARP2, PARP3, PARP4, PCNA, PIK3CA, PMS2, POLA1, POLB, POLH, POLL, POLN, POLQ, PRKDC, PTEN, RAD9A, RAD17, RAD18, RAD50, RAD51, RAD52, RAD54B, RAD54L, RB1, REV3L, RPA1, RPA2, SLX4, TDP1, TDP2, TMPRSS2, TMPRSS2-ERG, TOPBP1, TOP2A, TOP2B, TP53, TP53BP1, TRRAP, UBE2N, UIMC1, USP1, WDR48, WRN, XPA, XRCC1, XRCC2, XRCC3, XRCC4 and/or XRCC6 gene/protein; and/or b) the activation of the ALT pathway; and/or c) microsatellite instability. The present invention also covers a kit comprising Compound A together with means to detect one or more of the aforementioned biomarker(s) and a method for identifying a subject having a hyper- proliferative disease disposed to respond favorably to Compound A, wherein the method comprises the detection of one or more of the aforementioned biomarker(s). Further, the invention covers a method of determining whether a subject having a hyper-proliferative disease will respond to the treatment with Compound A, wherein the method comprises the detection of one or more of the aforementioned biomarker(s) in a sample of the subject.

9. 发明申请

WO2017134231A1 COMPOUNDS, COMPOSITIONS AND METHODS FOR CANCER PATIENT STRATIFICATION AND CANCER TREATMENT 审中-公开
标题翻译：癌症患者分层和癌症治疗的化合物，组合物和方法
公开(公告)号：WO2017134231A1
公开(公告)日：2017-08-10
申请号：PCT/EP2017/052393
申请日：2017-02-03
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , THE BROAD INSTITUTE, INC. , DANA-FARBER CANCER INSTITUTE, INC.
发明人： WENGNER, Antje, Margret , EIS, Knut , LIENAU, Philip , SACK, Ulrike , LANGE, Martin , GREULICH, Heidi , MEYERSON, Matthew , DE WAAL, Luc , SCHENONE, Monica , BURGIN, Alex , LEWIS, Timothy, A. , WU, Xiaoyun
IPC分类号： A61K31/50 , A61K31/5375 , A61K45/00 , G01N33/68 , A61P35/00
CPC分类号： A61K31/50 , A61K31/5375 , A61K45/00 , G01N33/68 , G01N2333/4703 , G01N2333/916 , G01N2800/52
摘要： The present invention features improved Compounds, especially (I) methods of identifying patients having Cancer using biomarkers (e.g., PDE3A, SLFN12 and/or CREB3Ll) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., Compounds 1-6 disclosed herein).
摘要翻译：本发明特征在于改进的化合物，特别是（I）使用与药物敏感性相关并且因此治疗分层患者群体的生物标志物（例如，PDE3A，SLFN12和/或CREB3L1）鉴定患有癌症的患者的方法与本发明的试剂（例如本文公开的化合物1-6）进行比较。

10. 发明申请

WO2018153971A1 COMBINATION OF ATR KINASE INHIBITORS 审中-公开
公开(公告)号：WO2018153971A1
公开(公告)日：2018-08-30
申请号：PCT/EP2018/054364
申请日：2018-02-22
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： WENGNER, Antje, Margret , SIEMEISTER, Gerhard
IPC分类号： A61K31/5377 , A61K31/282 , A61K31/4745 , A61K31/513 , A61K31/555 , A61K33/24 , A61N5/10 , A61K45/06 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/282 , A61K31/4745 , A61K31/513 , A61K31/555 , A61K33/24 , A61K38/14 , A61K45/06 , A61N2005/1098 , A61P35/00 , A61K2300/00
摘要： The present invention covers combinations of at least two components, component A and component B, comprising component A being an ATR kinase inhibitor, particularly Compound A, and component B either being an anti-hyperproliferative, cytotoxic and/or cytostatic agent selected from: 5-FU, or a prodrug of 5-FU, such as 5'-deoxy-5-fluorouridine, capecitabine, BOF- A2, tegafur, UFT, or S-1; a platinum-based antineoplastic agent, such as oxaliplatin, cisplatin or carboplatin; a topoisomerase inhibitor, such as irinotecan, topotecan, camptothecin or SN-38; pharmaceutically acceptable salts of bleomycin such as bleomycin sulfate or bleomycin hydrochloride; or combinations thereof; or component B being ionizing radiation. 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 disease, particurlarly for the treatment of a hyper-proliferative disease.

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