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公开(公告)号：US20230287003A1
公开(公告)日：2023-09-14
申请号：US17968159
申请日：2022-10-18
Applicant: Cancer Research Technology Limited , The Institute of Cancer Research: Royal Cancer Hospital
Inventor： Benjamin Richard Bellenie , Kwai Ming Jack Cheung , Owen Alexander Davis , Swen Hoelder , Rosemary Huckvale , Gavin Collie , Mirco Meniconi , Alfie Brennan , Matthew Garth Lloyd
IPC: C07D498/04 , A61P35/00 , C07D471/04 , C07D498/14 , C07D498/20 , C07D513/04 , C07D519/00
CPC classification number: C07D498/04 , A61P35/00 , C07D471/04 , C07D498/14 , C07D498/20 , C07D513/04 , C07D519/00
Abstract: The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity:
wherein X1, X2, R1, R2, R30, R31 and Ring A are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.-
公开(公告)号：US11512095B2
公开(公告)日：2022-11-29
申请号：US17046650
申请日：2019-04-12
Applicant: Cancer Research Technology Limited , The Institute of Cancer Research: Royal Cancer Hospital
Inventor： Benjamin Richard Bellenie , Kwai Ming Jack Cheung , Owen Alexander Davis , Swen Hoelder , Rosemary Huckvale , Gavin Collie , Mirco Meniconi , Alfie Brennan , Matthew Garth Lloyd
IPC: C07D498/04 , A61P35/00 , C07D471/04 , C07D498/14 , C07D498/20 , C07D513/04 , C07D519/00
Abstract: The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: wherein X1, X2, R1, R2, R30, R31 and Ring A are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
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公开(公告)号：US20210244706A1
公开(公告)日：2021-08-12
申请号：US17035179
申请日：2020-09-28
Inventor： Alan Ashworth , Stephen Jackson , Niall Martin , Graeme Cameron Murray Smith
IPC: A61K31/366 , A61K31/00 , A61K31/405 , A61K31/4184 , A61K31/4706 , A61K31/473 , A61K31/502 , A61K31/517 , A61K31/522 , A61K31/675
Abstract: The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.
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公开(公告)号：US20210206756A1
公开(公告)日：2021-07-08
申请号：US16616906
申请日：2018-05-25
Applicant: Cancer Research Technology Limited , The Institute of Cancer Research: Royal Cancer Hospital
Inventor： Benjamin R. Bellenie , Kwai Ming Jack Cheung , Owen Alexander Davis , Swen Hoelder , Rosemary Huckvale , Matthew Garth Lloyd
IPC: C07D413/14 , C07D401/14 , C07D471/04 , C07D401/12 , C07D471/10 , C07D491/10 , C07D405/14
Abstract: The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: Formula I wherein X1, X2, X3, R1, R2, R3, R4 and R5 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
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公开(公告)号：US10885679B2
公开(公告)日：2021-01-05
申请号：US16092431
申请日：2017-03-28
Applicant: The Institute of Cancer Research: Royal Cancer Hospital , Royal Marsden NHS Foundation Trust
Inventor： Matthew Blackledge , David Collins , Martin Leach
IPC: G06K9/00 , G06T11/00 , G01R33/483 , G01R33/56 , G01R33/563 , G06T7/00
Abstract: A method of producing a magnetic resonance (MR) image of a region of interest is provided. The method includes the steps of: acquiring an initial MR image of the region of interest, the initial MR image mapping values of an MR-sensitive, physical property at positions over the region; determining a corresponding map of the estimated uncertainties in the values of the MR-sensitive, physical property over the region; and calculating a weighted MR image of the region, the weighted MR image mapping values of a function which combines, at each position of the initial image, the respective value of the MR-sensitive, physical property and the respective estimated uncertainty, the function applying a higher weighting to positions with relatively low estimated uncertainties than to positions with relatively high estimated uncertainties.
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Patent Agency Ranking
公开(公告)号：US10674920B2
公开(公告)日：2020-06-09
申请号：US14417427
申请日：2013-07-24
Inventor： Jeffrey Colin Bamber , Martin Frenz , Michael Jaeger
Abstract: A method of imaging a region of interest of a body, the body having sites outside the region which can produce image clutter. The method includes: generating a first pattern of vibration within the body to produce a localised first displacement at the region and localised first displacements at the clutter-producing sites; while the body undergoes the first displacements, generating ultrasound signals from the region, and detecting the ultrasound signals to generate a first image of the region; generating a second pattern of vibration within the body to produce a localised second displacement at the region and localised second displacements at the clutter-producing sites; while the body undergoes the second displacements, generating ultrasound signals from the region, and detecting the ultrasound signals to generate a second image of the region; and combining the first and second images to produce a third image of the region. The first and second vibration patterns are selected such that the first and second displacements combine in the production of the third image to reduce or eliminate the clutter in the third image relative to the clutter in the first and second images.
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公开(公告)号：US09550764B2
公开(公告)日：2017-01-24
申请号：US14421503
申请日：2013-08-22
Inventor： Keith Jones , Matthew David Cheeseman , Spyridon Linardopoulos , Amir Faisal , Olivier Remi Barbeau , Andrew Kalusa
IPC: C07D417/10 , C07D417/14 , C07D417/04 , C07D413/04
CPC classification number: C07D417/14 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof for use in the treatment of cancer:
Abstract translation: 本发明提供了用于治疗癌症的式（I）化合物及其药学上可接受的盐，水合物和溶剂合物：
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公开(公告)号：US09283226B2
公开(公告)日：2016-03-15
申请号：US14180440
申请日：2014-02-14
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 , C07D231/12 , A61K31/5377 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10 , A61K31/4155 , A61K31/4178 , A61K31/454 , A61K31/496 , A61K31/497 , A61K45/06
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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公开(公告)号：US20150232462A1
公开(公告)日：2015-08-20
申请号：US14421503
申请日：2013-08-22
Inventor： Keith Jones , Matthew David Cheeseman , Spyridon Linardopoulos , Amir Faisal , Olivier Remi Barbeau , Andrew Kalusa
IPC: C07D417/14 , C07D413/04 , C07D417/04
CPC classification number: C07D417/14 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof for use in the treatment of cancer:
Abstract translation: 本发明提供了用于治疗癌症的式（I）化合物及其药学上可接受的盐，水合物和溶剂合物：
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公开(公告)号：US20140271662A1
公开(公告)日：2014-09-18
申请号：US14180440
申请日：2014-02-14
Applicant: Astex Therapeutics Ltd , Cancer Research Technology Limited , The Institute of Cancer Research: Royal Cancer Hospital
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: A61K31/5377 , A61K45/06 , A61K31/415 , C07D401/10 , A61K31/497 , A61K31/4155 , A61K31/496 , C07D403/10 , A61K31/4178 , C07D231/12 , A61K31/454
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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