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1. 发明申请

US20230030983A1 FGFR/PD-1 COMBINATION THERAPY FOR THE TREATMENT OF CANCER 有权
公开(公告)号：US20230030983A1
公开(公告)日：2023-02-02
申请号：US17655519
申请日：2022-03-18
申请人： ASTEX THERAPEUTICS LTD
发明人： Jayaprakash KARKERA , Suso Jesus PLATERO , Raluca VERONA , Matthew V. LORENZI
IPC分类号： A61K39/395 , G01N33/574 , A61K31/498 , C12Q1/6886 , A61K45/06 , C07K16/28
摘要： 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.

2. 发明授权

US10716787B2 Combinations 有权
公开(公告)号：US10716787B2
公开(公告)日：2020-07-21
申请号：US15955149
申请日：2018-04-17
申请人： ASTEX THERAPEUTICS LTD
发明人： Eleonora Jovcheva , Timothy Pietro Suren Perera
IPC分类号： A61K31/4985 , A61K31/5025 , A61K31/498 , A61K45/06
摘要： 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.

3. 发明授权

US09757364B2 Naphthyridine derivative compounds 有权
公开(公告)号：US09757364B2
公开(公告)日：2017-09-12
申请号：US15339148
申请日：2016-10-31
申请人： ASTEX THERAPEUTICS LIMITED
发明人： Patrick René Angibaud , Michel Obringer , Julien Jérémie Joseph Marin , Matthieu Jeanty
IPC分类号： A61K31/4375 , A61K31/506 , A61K31/4545 , A61K31/444
CPC分类号： A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/506 , A61K45/06 , C07D471/04
摘要： The invention relates to new naphthyridine 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.

4. 发明授权

US09439896B2 Quinolines as FGFR kinase modulators 有权
标题翻译：喹啉作为FGFR激酶调节剂
公开(公告)号：US09439896B2
公开(公告)日：2016-09-13
申请号：US14354773
申请日：2012-10-26
申请人： ASTEX THERAPEUTICS LIMITED
发明人： Valerio Berdini , Patrick Rene Angibaud , Steven John Woodhead , Gordon Saxty
IPC分类号： C07D215/38 , A61K31/47 , C07D401/14 , C07D413/14 , C07D401/04 , C07D407/14 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D405/14
CPC分类号： A61K31/4709 , A61K31/47 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D215/38 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/14
摘要： The invention relates to new quinoline 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. Formula (I)
摘要翻译：本发明涉及式（I）的新的喹啉衍生物化合物，包含所述化合物的药物组合物，所述化合物的制备方法以及所述化合物在治疗疾病中的用途。癌症。式（I）

5. 发明申请

US20160031856A1 SUBSTITUTED QUINOXALINES AS FGFR KINASE INHIBITORS 有权
标题翻译：作为FGFR激酶抑制剂的替代喹喔啉
公开(公告)号：US20160031856A1
公开(公告)日：2016-02-04
申请号：US14816565
申请日：2015-08-03
申请人： ASTEX THERAPEUTICS LTD
发明人： 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分类号： C07D403/04 , C07D401/14 , C07D403/14
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14
摘要： 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.
摘要翻译：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。

7. 发明授权

US08779147B2 3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators 有权
标题翻译： 3,4-二取代的1H-吡唑化合物及其作为细胞周期蛋白依赖性激酶和糖原合成酶激酶-3调节剂的用途
公开(公告)号：US08779147B2
公开(公告)日：2014-07-15
申请号：US13289373
申请日：2011-11-04
申请人： Valerio Berdini , Michael Alistair O'Brien , Maria Grazia Carr , Theresa Rachel Early , Adrian Liam Gill , Gary Trewartha , Alison Jo-Anne Woolford , Andrew James Woodhead , Paul Graham Wyatt
发明人： Valerio Berdini , Michael Alistair O'Brien , Maria Grazia Carr , Theresa Rachel Early , Adrian Liam Gill , Gary Trewartha , Alison Jo-Anne Woolford , Andrew James Woodhead , Paul Graham Wyatt
IPC分类号： C07D401/12
CPC分类号： C07D231/38 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C04B35/632 , C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04
摘要： The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.
摘要翻译：本发明提供式（O）的化合物或其盐或互变异构体或其N-氧化物或溶剂合物，以及其与其它抗癌剂的组合，用于预防或治疗疾病状态和病症，例如由细胞周期蛋白介导的癌症依赖性激酶和糖原合成酶激酶-3。

8. 发明授权

US08131527B1 FGFR pharmacophore compounds 有权
标题翻译： FGFR药效团化合物
公开(公告)号：US08131527B1
公开(公告)日：2012-03-06
申请号：US11963654
申请日：2007-12-21
申请人： Gordon Saxty , Valerio Berdini , David Richard Newell , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Andrew Madin , Christopher William Murray
发明人： Gordon Saxty , Valerio Berdini , David Richard Newell , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Andrew Madin , Christopher William Murray
IPC分类号： G06G7/58 , G01N23/00 , G01N23/83
CPC分类号： G06F19/706 , C40B30/02 , G01N2333/71 , G01N2500/04
摘要： The present invention relates to FGFR pharmacophores, and in particular to compounds which are capable of binding to FGFR with greater affinity than their binding to VEGFR and methods of identifying such compounds using the pharmacophore. The present invention further relates to compositions, methods and uses of the compounds and the pharmacophores disclosed herein.
摘要翻译：本发明涉及FGFR药效学，特别是涉及能够以比它们与VEGFR结合的亲和力更高的亲和力结合FGFR的化合物以及使用该药效团鉴别这些化合物的方法。本发明还涉及本文公开的化合物和药效团的组合物，方法和用途。

9. 发明授权

US08106057B2 Dihydroxyphenyl isoindolylmethanones 有权
标题翻译：二羟基苯基异吲哚甲酮
公开(公告)号：US08106057B2
公开(公告)日：2012-01-31
申请号：US12782996
申请日：2010-05-19
申请人： Gianni Chessari , Maria Grazia Carr , Miles Stuart Congreve , Robert Downham , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
发明人： Gianni Chessari , Maria Grazia Carr , Miles Stuart Congreve , Robert Downham , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
IPC分类号： A61K31/497 , A61K31/445 , A61K31/405
CPC分类号： C07D209/44 , C07D401/04 , C07D401/12
摘要： This invention provides methods for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I): and in particular, those of subgenus VIIa These compounds inhibit or modulate the activity of the heat shock protein Hsp90.
摘要翻译：本发明提供了治疗癌症，特别是淋巴或骨髓谱系造血肿瘤，前列腺癌，肺癌，胃肠道间质瘤，乳腺癌和黑素瘤的方法，其包括向哺乳动物施用化合物，盐，水合物，互变异构体或N-氧化物根据式（I）：特别是亚属VIIa的化合物这些化合物抑制或调节热休克蛋白Hsp90的活性。

10. 发明申请

US20110152244A1 PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES 有权
标题翻译：吡咯啉化合物及其用途
公开(公告)号：US20110152244A1
公开(公告)日：2011-06-23
申请号：US13060154
申请日：2009-08-20
申请人： Gilbert Besong , Christopher Thomas Brain , Clinton A. Brooks , Miles Stuart Congreve , Claudio Dagostin , Guo He , Ying Huo , Steven Howard , Yue Li , Yipin Lu , Paul Morteson , Troy Smith , Moo Sung , Steven Woodhead , Wojciech Wrona
发明人： Gilbert Besong , Christopher Thomas Brain , Clinton A. Brooks , Miles Stuart Congreve , Claudio Dagostin , Guo He , Ying Huo , Steven Howard , Yue Li , Yipin Lu , Paul Morteson , Troy Smith , Moo Sung , Steven Woodhead , Wojciech Wrona
IPC分类号： C07D487/04 , A61K31/497 , A61K31/519 , A61K31/551 , A61K31/5377 , A61K31/501 , C12N9/99 , A61P35/04 , A61P29/00
CPC分类号： C07D487/04 , A61K31/519 , C07D487/08
摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.
摘要翻译：所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。

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