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公开(公告)号:US20230030983A1
公开(公告)日:2023-02-02
申请号:US17655519
申请日:2022-03-18
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Jayaprakash KARKERA , Suso Jesus PLATERO , Raluca VERONA , Matthew V. LORENZI
IPC: A61K39/395 , G01N33/574 , A61K31/498 , C12Q1/6886 , A61K45/06 , C07K16/28
Abstract: Provided herein are combination therapies for the treatment of cancer. In particular, the disclosed methods are directed to treatment of cancer in a patient comprising administering an antibody that blocks the interaction between PD-1 and PD-L1 and an FGFR inhibitor, wherein the antibody that blocks the interaction between PD-1 and PD-L1 and the FGFR inhibitor are administered if one or more FGFR variants are present in a biological sample from the patient.
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公开(公告)号:US10716787B2
公开(公告)日:2020-07-21
申请号:US15955149
申请日:2018-04-17
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Eleonora Jovcheva , Timothy Pietro Suren Perera
IPC: A61K31/4985 , A61K31/5025 , A61K31/498 , A61K45/06
Abstract: The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor.The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer.The FGFR inhibitor (N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof) and the cMet inhibitor can be administered simultaneously, separately or sequentially.The invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to the invention.
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公开(公告)号:US20160031856A1
公开(公告)日:2016-02-04
申请号:US14816565
申请日:2015-08-03
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Gordon SAXTY , Christopher William MURRAY , Valerio BERDINI , Gilbert Ebai BESONG , Christopher Charles Frederick HAMLETT , Steven John WOODHEAD , Yannick Aime Eddy LIGNY , Patrick René ANGIBAUD
IPC: C07D403/04 , C07D401/14 , C07D403/14
CPC classification number: C07D403/04 , C07D401/14 , C07D403/14
Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Abstract translation: 本发明涉及新的喹喔啉衍生物化合物,包含所述化合物的药物组合物,用于制备所述化合物的方法和所述化合物在治疗疾病中的用途。 癌症。
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公开(公告)号:US20210169877A1
公开(公告)日:2021-06-10
申请号:US17125261
申请日:2020-12-17
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Diego Fernando Domenico BROGGINI
Abstract: The invention relates to pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, or a pharmaceutically acceptable salt thereof or a solvate thereof; to processes for the preparation of said compositions and to the use of said compositions for the manufacture of a medicament for the prophylaxis of or the treatment, in particular the treatment, of diseases, e.g. cancer
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公开(公告)号:US20210038598A1
公开(公告)日:2021-02-11
申请号:US16931728
申请日:2020-07-17
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Eleonora JOVCHEVA , Timothy Pietro Suren PERERA
IPC: A61K31/4985 , A61K31/498 , A61K31/5025 , A61K45/06
Abstract: The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5 -dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3 -(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor.
The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer.
The FGFR inhibitor (N-(3,5 -dimethoxyphenyl)-N-(1-methylethyl)-N-[3 -(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof) and the cMet inhibitor can be administered simultaneously, separately or sequentially.
The invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to the invention.-
公开(公告)号:US10519137B2
公开(公告)日:2019-12-31
申请号:US15810521
申请日:2017-11-13
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Gordon Saxty , Christopher William Murray , Valerio Berdini , Gilbert Ebai Besong , Steven John Woodhead , Michael Reader , Laurence Anne Mevellec , Patrick René Angibaud , Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Berthold Wroblowski , Alexandra Papanikos , Olivier Alexis Georges Querolle , Isabelle Noëlle Constance Pilatte , Pascal Ghislain André Bonnet , Werner Constant Johan Embrechts , Rhalid Akkari , Lieven Meerpoel
IPC: C07D231/10 , C07D231/12 , A61K31/415 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D491/113 , C07D401/14 , C07F9/6524
Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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公开(公告)号:US10144731B2
公开(公告)日:2018-12-04
申请号:US15105306
申请日:2014-12-17
Inventor: Thomas Glanmor Davies , Alison Jo-anne Woolford , Hendrika Maria Gerarda Willems , David Norton , Thomas Daniel Heightman , Jeffrey K. Kerns
IPC: C07D249/18 , C07D417/10 , C07D281/02 , C07D291/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/14 , C07D419/10 , C07D419/14 , C07D471/04 , C07D513/04 , C07D515/04
Abstract: The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
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公开(公告)号:US09902714B2
公开(公告)日:2018-02-27
申请号:US15128345
申请日:2015-03-26
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Wim Vermeulen , Steven Anna Hostyn , Filip Albert Celine Cuyckens , Russell Mark Jones , Diego Fernando Domenico Broggini
IPC: C07D403/04 , A61K31/4985 , A61K31/5513 , C07D403/14 , A61P35/00
CPC classification number: C07D403/14 , A61K31/4985 , A61K31/5513
Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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公开(公告)号:US09464071B2
公开(公告)日:2016-10-11
申请号:US14505020
申请日:2014-10-02
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Gordon Saxty , Christopher William Murray , Valerio Berdini , Gilbert Ebai Besong , Christopher Charles Frederick Hamlett , Christopher Norbert Johnson , Steven John Woodhead , Michael Reader , David Charles Rees , Laurence Anne Mevellec , Patrick René Angibaud , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Johan Erwin Edmond Weerts , Timothy Pietro Suren Perera , Ronaldus Arnodus Hendrika Joseph Gilissen , Berthold Wroblowski , Jean Fernand Armand Lacrampe , Alexandra Papanikos , Olivier Alexis Georges Querolle , Elisabeth Thérèse Jeanne Pasquier , Isabelle Noëlle Constance Pilatte , Pascal Ghislain André Bonnet , Werner Constant Johan Embrechts , Rhalid Akkari , Lieven Meerpoel
IPC: A61K31/415 , C07D231/10 , C07D231/12 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D491/113
CPC classification number: C07D403/04 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D491/113 , C07F9/6524
Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Abstract translation: 本发明涉及新的喹喔啉衍生物化合物,包含所述化合物的药物组合物,用于制备所述化合物的方法和所述化合物在治疗疾病中的用途。 癌症。
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公开(公告)号:US20160250187A1
公开(公告)日:2016-09-01
申请号:US15010831
申请日:2016-01-29
Applicant: Astex Therapeutics Ltd , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
Inventor: Valerio BERDINI , Gordon SAXTY , Marinus Leendert VERDONK , Steven John WOODHEAD , Paul Graham WYATT , Robert George BOYLE , Hannah Fiona SORE , David Winter WALKER , Ian COLLINS , Robert DOWNHAM , Robin Arthur Ellis CARR
IPC: A61K31/415 , A61K31/454 , A61K31/4439 , A61K31/5377 , A61K31/4155 , A61K9/20 , A61K31/4178 , A61K31/497 , A61K31/551 , A61K31/4545 , A61K9/00 , A61K9/48 , A61K45/06 , A61K31/496
CPC classification number: A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
Abstract translation: 本发明提供了具有蛋白激酶B抑制活性的式(I)化合物:其中A是含有1至7个碳原子的饱和烃连接基团,该连接基团具有在R1和NR2R3之间延伸的最大链长度为5个原子,以及 在E和NR2R3之间延伸的4个原子的最大链长度,其中连接基团中的一个碳原子可以任选地被氧或氮原子取代; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代,氟和羟基的取代基,条件是存在的羟基相对于NR 2 R 3基团不位于碳原子α,条件是 存在时的氧代基相对于NR2R3基团位于碳原子α; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且R 2,R 3,R 4和R 5如权利要求中所定义。 还提供含有化合物的药物组合物,制备化合物的方法及其作为抗癌剂的用途。
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