专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明公开

US20230192700A1 PYRAZOLOPYRAZINES ACTING ON CANCERS VIA INHIBITION OF CDK12 审中-公开
公开(公告)号：US20230192700A1
公开(公告)日：2023-06-22
申请号：US17909636
申请日：2021-03-05
申请人： Bayer Aktiengesellschaft , Deutsches Krebsforschungszentrum
发明人： Markus BERGER , Bernd BUCHMANN , Kai THEDE , Philipp BUCHGRABER , Gerhard SIEMEISTER , Patrick STEIGEMANN , Antje Margret WENGNER , Ulf BÖMER , Naomi BARAK , Philip LIENAU
IPC分类号： C07D487/04 , A61K45/06 , A61P35/00 , C07D519/00
CPC分类号： C07D487/04 , A61K45/06 , A61P35/00 , C07D519/00
摘要： The present invention provides compounds of general formula (I) in which X, R1, R2 and R3 are as described and defined herein, 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 for the treatment and/or prophylaxis of diseases, in particular of hyperproliferative disorders such as cancer disorders, as a sole agent or in combination with other active ingredients.

2. 发明申请

US20230117034A1 PYRAZOLOTRIAZINES 有权
公开(公告)号：US20230117034A1
公开(公告)日：2023-04-20
申请号：US17784545
申请日：2020-12-09
申请人： Bayer Aktiengesellschaft , Deutsches Krebsforschungszentrum
发明人： Kai THEDE , Philipp BUCHGRABER , Gerhard SIEMEISTER , Patrick STEIGEMANN , Antje Margret WENGNER , Ulf BOEMER , Naomi BARAK , Philip LIENAU
IPC分类号： A61K31/53 , C07D487/04 , C07D519/00 , A61K45/06 , A61K31/5377 , A61K31/553 , A61K31/5386 , A61K31/541 , A61K31/551 , A61P35/00 , A61P11/00
摘要： The present invention provides compounds of general formula (I), in which X, R1, R2 and R3 are as described and defined herein, 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 for the treatment and/or prophylaxis of diseases, in particular of hyperproliferative disorders such as cancer disorders, as a sole agent or in combination with other active ingredients.

3. 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.

4. 发明申请

US20200375997A1 PREDICTIVE MARKERS FOR ATR KINASE INHIBITORS 审中-公开
公开(公告)号：US20200375997A1
公开(公告)日：2020-12-03
申请号：US16770462
申请日：2018-12-04
申请人： Bayer Aktiengesellschaft
发明人： Antje Margret WENGNER , Gerhard SIEMEISTER , Li LIU
IPC分类号： A61K31/5377 , C12Q1/6886 , A61P35/00
摘要： The present invention covers an ATR kinase inhibitor, particularly 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(H-pyrazol-5-yl)-1,7-naphthyridine (“Compound A”), for use in the treatment of a hyper-proliferative disease in a subject, wherein the hyper-proliferative disease or the subject is or has been characterized by one or more biomarker(s), wherein the biomarker(s) comprise(s) a) one or more functional mutations in one or more gene(s)/protein(s) selected from RBBP8, APOBEC3A, APOBEC3B, CLSPN, ERCC, HUS1, MAD2L2, PGBD5, POLD1, RAD1, TIMELESS and/or TIPIN; and/or b) the expression of a fusion gene encoding a fusion protein selected from EWSR-ERG, EWSR1-FLI1, SS18-SSX and/or SS18-SSX2 gene/protein.

5. 发明公开

US20240247015A1 PHOSPHORUS DERIVATIVES AS NOVEL SOS1 INHIBITORS 审中-公开
公开(公告)号：US20240247015A1
公开(公告)日：2024-07-25
申请号：US18286809
申请日：2022-04-13
申请人： BAYER AKTIENGESELLSCHAFT
发明人： Felix PAPE , Steffen GRESSIES , Timo STELLFELD , Jeremie Xavier G MORTIER , Atanas Marinov KAMBUROV , Benjamin BADER , Keith GRAHAM , Roman HILLIG , Jens SCHRODER , Christoph Philipp HETHEY , Matthias ARLT , Gerhard SIEMEISTER , Katrin NOWAK-REPPEL , Michael ERKELENZ
IPC分类号： C07F9/6584 , A61K31/675 , C07F9/6561 , C07F9/6568
CPC分类号： C07F9/6584 , A61K31/675 , C07F9/6561 , C07F9/65685
摘要： The present invention covers phosphorus derivatives of general formula (I), in which R1, R2, R3, R4, R5, R6, X1, X2, X3, X4 and Y are as defined herein, 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 for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, especially diseases associated with SOS1, as a sole agent or in combination with other active ingredients.

6. 发明申请

US20210369724A1 COMBINATION OF ATR KINASE INHIBITORS WITH 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE COMPOUNDS 有权
公开(公告)号：US20210369724A1
公开(公告)日：2021-12-02
申请号：US17285858
申请日：2019-10-09
申请人： Bayer Aktiengesellschaft
发明人： Antje Margret WENGNER , Gerhard SIEMEISTER , Sylvia GRÜNEWALD , Bernard HAENDLER , Ningshu LIU
IPC分类号： A61K31/5377 , A61P35/00
摘要： The present invention relates to combinations of: component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2) as defined herein, or a stereoisomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof; and component B: one or more ATR kinase inhibitor(s) as defined herein, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof; and, optionally, component C: one or more further pharmaceutical agent(s); and, optionally, in which either or both of components A and B in any of the above-mentioned combinations are in the form of a pharmaceutical composition which is ready for use to be administered simultaneously, concurrently, separately or sequentially. The components may be administered independently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route.

7. 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.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式