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1. 发明申请

US20200063212A1 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：US20200063212A1
公开(公告)日：2020-02-27
申请号：US16488033
申请日：2018-02-22
申请人： Bayer Aktiengesellschaft , Bayer Pharma Aktiengesellschaft
发明人： Antje Margret WENGNER , Gerhard SIEMEISTER , Bernard HÄNDLER , Sven GOLFIER , Andreas SCHLICKER , Li LIU
IPC分类号： C12Q1/6886 , A61K31/5377 , A61P35/00
摘要： The present invention covers 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyra-zol-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, ER-CC5, 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, TM-PRSS2, TMPRSS2-ERG, TOPBP1, TOP2A, TOP2B, TP53, TP53BP1, TRRAP, UBE2N, UIMC1, USP1, WDR48, WRN, XPA, XR-CC1 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 afore-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.

2. 发明申请

US20210404012A1 INHIBITOR OF ATR KINASE FOR USE IN A METHOD OF TREATING A HYPER-PROLIFERATIVE DISEASE 有权
公开(公告)号：US20210404012A1
公开(公告)日：2021-12-30
申请号：US17164336
申请日：2021-02-01
申请人： Bayer Aktiengesellschaft , Bayer Pharma Aktiengesellschaft
发明人： Antje Margret WENGNER , Gerhard SIEMEISTER , Bernard HÄNDLER , Sven GOLFIER , Andreas SCHLICKER , Li LIU
IPC分类号： C12Q1/6886 , A61P35/00 , A61K31/5377
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.

3. 发明申请

US20180162940A1 ANTI-CEACAM6 ANTIBODIES AND USES THEREOF 审中-公开
公开(公告)号：US20180162940A1
公开(公告)日：2018-06-14
申请号：US15561013
申请日：2016-03-21
申请人： Bayer Pharma Aktiengesellschaft
发明人： Jörg WILLUDA , Mark TRAUTWEIN , Uwe GRITZAN , Christoph FREIBERG , Frank DITTMER , Dorian SCHÖNFELD , Julian Marius GLÜCK , Jessica PINKERT , Eva-Maria GUTIERREZ , Sven GOLFIER , Simon HOLTON , Philip BECKHOVE , Yingzi GE
IPC分类号： C07K16/28 , A61P35/00
摘要： The present invention provides recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for human and Macaca fascicularis CEACAM6 (Carcinoembryonic antigen-related cell adhesion molecule 6, CD66c, Non-specific crossreacting antigen, NCA, NCA-50/90), and which do not significantly cross-react with the closely related human CEACAM1, human CEACAM3, and human CEACAM5. The invention further provides methods to generate this kind of antibodies. The antibodies, accordingly, can be used to treat cancer and other disorders and conditions associated with expression of the CEACAM6. The invention also provides nucleic acid sequences encoding the foregoing antibodies, vectors containing the same, pharmaceutical compositions and kits with instructions for use.

4. 发明申请

US20200157214A1 ANTI-CEACAM6 ANTIBODIES AND USES THEREOF 审中-公开
公开(公告)号：US20200157214A1
公开(公告)日：2020-05-21
申请号：US16776329
申请日：2020-01-29
申请人： Bayer Pharma Aktiengesellschaft
发明人： Jörg WILLUDA , Mark TRAUTWEIN , Uwe GRITZAN , Christoph FREIBERG , Frank DITTMER , Dorian SCHÖNFELD , Julian Marius GLÜCK , Jessica PINKERT , Eva-Maria GUTIERREZ , Sven GOLFIER , Simon HOLTON , Philip BECKHOVE , Yingzi GE
IPC分类号： C07K16/28 , A61P35/00
摘要： The present invention provides recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for human and Macaca fascicularis CEACAM6 (Carcinoembryonic antigen-related cell adhesion molecule 6, CD66c, Non-specific crossreacting antigen, NCA, NCA-50/90), and which do not significantly cross-react with the closely related human CEACAM1, human CEACAM3, and human CEACAM5. The invention further provides methods to generate this kind of antibodies.The antibodies, accordingly, can be used to treat cancer and other disorders and conditions associated with expression of the CEACAM6. The invention also provides nucleic acid sequences encoding the foregoing antibodies, vectors containing the same, pharmaceutical compositions and kits with instructions for use.

5. 发明申请

US20200181261A1 ANTI-CEACAM6 ANTIBODIES AND USES THEREOF 审中-公开
公开(公告)号：US20200181261A1
公开(公告)日：2020-06-11
申请号：US16776326
申请日：2020-01-29
申请人： Bayer Pharma Aktiengesellschaft
发明人： Jörg WILLUDA , Mark TRAUTWEIN , Uwe GRITZAN , Christoph FREIBERG , Frank DITTMER , Dorian SCHÖNFELD , Julian Marius GLÜCK , Jessica PINKERT , Eva-Maria GUTIERREZ , Sven GOLFIER , Simon HOLTON , Philip BECKHOVE , Yingzi GE
IPC分类号： C07K16/28 , A61P35/00
摘要： The present invention provides recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for human and Macaca fascicularis CEACAM6 (Carcinoembryonic antigen-related cell adhesion molecule 6, CD66c, Non-specific crossreacting antigen, NCA, NCA-50/90), and which do not significantly cross-react with the closely related human CEACAM1, human CEACAM3, and human CEACAM5. The invention further provides methods to generate this kind of antibodies.The antibodies, accordingly, can be used to treat cancer and other disorders and conditions associated with expression of the CEACAM6. The invention also provides nucleic acid sequences encoding the foregoing antibodies, vectors containing the same, pharmaceutical compositions and kits with instructions for use.

6. 发明申请

US20160237160A1 ANTI-TWEAKR ANTIBODIES AND USES THEREOF 审中-公开
标题翻译：抗微生物抗体及其用途
公开(公告)号：US20160237160A1
公开(公告)日：2016-08-18
申请号：US14898455
申请日：2014-06-12
申请人： BAYER PHARMA AKTIENGESELLSCHAFT
发明人： Christian VOTSMEIER , Stefanie HAMMER , Uwe GRITZAN , Sandra BERNDT , Dmitry ZUBOV , Lars LINDEN , Sven CHRISTIAN , Axel HARRENGA , Jörg BIRKENFELD , Christoph FREIBERG , Sven GOLFIER , Andrea EICKER , Simone GREVEN , Beatrix STELTE-LUDWIG , Marian RASCHKE
IPC分类号： C07K16/28 , A61K49/00 , A61K31/44 , A61K31/4745 , A61K31/282 , A61K31/513 , A61K47/48 , A61K39/395
CPC分类号： C07K16/2878 , A61K31/282 , A61K31/44 , A61K31/4745 , A61K31/513 , A61K39/39558 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K49/0032 , A61K49/0058 , A61K2039/505 , A61K2039/507 , C07K16/2863 , C07K2317/21 , C07K2317/24 , C07K2317/34 , C07K2317/54 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/622 , C07K2317/73 , C07K2317/75 , C07K2317/77 , C07K2317/92
摘要： The present invention provides recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for the TWEAKR (TNFRSF12A, FN14). The antibodies, accordingly, can be used to treat tumors and other disorders and conditions associated with expression of the TWEAKR. The invention also provides nucleic acid sequences encoding the foregoing antibodies, vectors containing the same, pharmaceutical compositions and kits with instructions for us.
摘要翻译：本发明提供重组抗原结合区和包含特异于TWEAKR（TNFRSF12A，FN14）的抗原结合区的抗体和功能片段。因此，抗体可用于治疗与TWEAKR表达相关的肿瘤和其它病症和病症。本发明还提供编码前述抗体的核酸序列，含有该抗体的载体，药物组合物和具有我们说明书的试剂盒。

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