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31. 发明申请

US20200216818A1 VACCINIA VIRUS FOR GENE-DIRECTED ENZYME PRODRUG THERAPY 审中-公开
公开(公告)号：US20200216818A1
公开(公告)日：2020-07-09
申请号：US16592187
申请日：2019-10-03
申请人： The Institute of Cancer Research: Royal Cancer Hospital
发明人： Richard Marais , Caroline Springer , Serena Tommasini
IPC分类号： C12N7/00 , C12N9/48 , A61K31/136 , A61K35/768 , A61K47/54 , A61K31/135 , A61K38/48
摘要： Methods of making vaccinia viruses for gene-directed prodrug therapy are disclosed and their use in the treatment of disease is provided. In particular, the anti-tumour effects of vaccinia viruses that are modified to express a prodrug activating enzyme are disclosed.

32. 发明申请

US20190164717A1 X-Ray Micro-Beam Production and High Brilliance X-Ray Production 审中-公开
公开(公告)号：US20190164717A1
公开(公告)日：2019-05-30
申请号：US16308780
申请日：2017-06-14
申请人： The Institute of Cancer Research: Royal Cancer Hospital
发明人： Stefan BARTZSCH , Uwe OELFKE
IPC分类号： H01J35/26 , H01J35/14 , H01J35/10 , G21K1/02 , G21K1/087
摘要： An x-ray micro-beam radiation production system is provided having: a source of accelerated electrons, an electron focusing component configured to focus the electrons provided by the source, and a target which produces x-rays when electrons impinge thereon from the source. The electron focusing component is configured to focus the electrons provided by the source such that they impinge at a focal spot having a width δ formed on a surface of the target. The focusing component is configured to move the electron beam relative to the target such that the focal spot moves across the target surface in the width direction, and/or the target is movable relative to the focusing component such that the focal spot moves across the target surface in the width direction, the surface velocity of the focal spot across the target surface in the width direction being greater than vt where: formula (I), k, ρ and c denoting respectively the heat conductivity, the density and the heat capacity of the target material, and d denoting the electron penetration depth in the target material. v t = π   k 4  ρ   c · δ d 2 , ( I )

33. 发明申请

US20190152966A1 Methylamine Derivatives as Lysysl Oxidase Inhibitors for the Treatment of Cancer 审中-公开
公开(公告)号：US20190152966A1
公开(公告)日：2019-05-23
申请号：US15999458
申请日：2017-02-17
申请人： THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
发明人： Caroline SPRINGER , Richard MARAIS , Dan NICULES-CU-DUVAZ , Leo LEUNG , Deborah SMITHEN , Cedric CALLENS , Haoran TANG
IPC分类号： C07D417/12 , A61P35/00 , C07D333/18 , C07D277/26 , C12Q1/37
CPC分类号： C07D417/12 , A61P35/00 , C07D263/46 , C07D277/26 , C07D277/36 , C07D333/18 , C07D333/34 , C07D409/12 , C12Q1/37 , C12Y304/21
摘要： Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

34. 发明申请

US20170365053A1 SCORING OF TUMOR INFILTRATION BY LYMPHOCYTES 审中-公开
公开(公告)号：US20170365053A1
公开(公告)日：2017-12-21
申请号：US15527284
申请日：2015-11-24
申请人： THE INSTITUTE OF CANCER RESEARCH ROYAL CANCER HOSPITAL
发明人： Yinyin Yuan
IPC分类号： G06T7/00 , G01N33/574
CPC分类号： G06T7/0012 , G01N33/57415 , G01N2800/52 , G06T2207/30068 , G06T2207/30096
摘要： A method of providing a prognosis in a cancer patient comprising analysing a tumour image to calculate a metric of immune infiltration for the tumour, and a method of analysing a tumour image.

35. 发明申请

US20160130564A1 VACCINIA VIRUS FOR GENE-DIRECTED ENZYME PRODRUG THERAPY 审中-公开
标题翻译： VACCINIA病毒用于基因型ENZYME PRODRUG疗法
公开(公告)号：US20160130564A1
公开(公告)日：2016-05-12
申请号：US14898284
申请日：2014-06-18
申请人： THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
发明人： Richard Marais , Caroline Springer , Serena Tommasini
IPC分类号： C12N7/00 , C12N9/48 , A61K31/136 , A61K35/768 , A61K47/48
CPC分类号： C12N7/00 , A61K31/135 , A61K31/136 , A61K35/768 , A61K38/48 , A61K47/542 , C12N9/485 , C12N2710/24132 , C12N2710/24143 , C12Y304/16 , C12Y304/17021
摘要： Methods of making vaccinia viruses for gene-directed prodrug therapy are disclosed and their use in the treatment of disease is provided. In particular, the anti-tumor effects of vaccinia viruses that are modified to express a prodrug-activating enzyme are disclosed.
摘要翻译：公开了用于基因导向的前药治疗的痘苗病毒的方法，并提供其在治疗疾病中的用途。特别地，公开了修饰以表达前体药物活化酶的痘苗病毒的抗肿瘤作用。

36. 发明申请

US20150182122A1 ULTRASONIC IMAGING 审中-公开
标题翻译：超声成像
公开(公告)号：US20150182122A1
公开(公告)日：2015-07-02
申请号：US14417427
申请日：2013-07-24
申请人： THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , UNIVERSITY OF BERN
发明人： Jeffrey Colin Bamber , Martin Frenz , Michael Jaeger
IPC分类号： A61B5/00 , A61B8/02 , G06T7/00 , A61B8/08
摘要： Method of ultrasound imaging in which vibration-induced localised (LOVIT) displacements code the ultrasound signal at the place of origin, enabling clutter cancellation. The require displacements can be induced by an acoustic radiation force (ARF) generated by an ultrasonic focused beam. One possibility for ARF-LOVIT is to acquire one photoacoustic (PA) image prior to the ARF push, and a second image immediately after the push when the non-zero displacement transient at the focus region is present. A difference image then highlights the signal from optically absorbing structures located inside the displacement region. Direct clutter, in contrast, originates from outside the imaged region where no displacement occurs, and is thus estimated. Echo clutter from acoustic scattering at echogenic structures inside the displacement region also shows up on the difference image, but at a different depth from where it was generated owing to the additional acoustic round-trip time as compared to PA signals.
摘要翻译：超声波成像方法，其中振动诱导的局部（LOVIT）位移在原点处对超声信号进行编码，从而实现杂波消除。要求位移可以由由超声波聚焦光束产生的声辐射力（ARF）引起。 ARF-LOVIT的一种可能性是在ARF推动之前获取一个光声（PA）图像，并且当存在在聚焦区域处的非零位移瞬变时紧接在推动之后的第二个图像。然后，差分图像突出了位于位移区域内的光学吸收结构的信号。相比之下，直接杂波源于没有位移发生的成像区域的外部，因此被估计。在位移区域内的回声结构的声散射的回波杂波也出现在差分图像上，但是与PA信号相比，由于额外的声学往返时间，与其产生的深度不同。

37. 发明授权

US09006430B2 Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein 有权
标题翻译：正构缩合的吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：US09006430B2
公开(公告)日：2015-04-14
申请号：US14310475
申请日：2014-06-20
申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
IPC分类号： C07D487/04 , C07D471/02 , C07D471/04 , C07D473/34 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, 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 may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.
摘要翻译：本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N = C（R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R或Q1的碳原子连接的C 1-4亚烷基链，以形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q2不是键; G为氢，NR2R3，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3时，则Q是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。

38. 发明授权

US12060360B2 Lysyl oxidase inhibitors 有权
公开(公告)号：US12060360B2
公开(公告)日：2024-08-13
申请号：US17712541
申请日：2022-04-04
申请人： The Institute of Cancer Research: Royal Cancer Hospital
发明人： Richard Marais , Caroline Springer , Dan Niculescu-Duvaz , Natalie Miller , Mohammed Aljarah , Alfonso Zambon , Leo Leung , Deborah Smithen , Michael Brown , Haoran Tang
IPC分类号： C07D471/08 , A61K31/439 , A61P35/00 , C07D487/08
CPC分类号： C07D487/08 , A61P35/00
摘要： This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.

39. 发明授权

US12018029B2 Hexahydropyrrolo[3,4-c]pyrrole derivatives useful as LOX inhibitors 有权
公开(公告)号：US12018029B2
公开(公告)日：2024-06-25
申请号：US16972335
申请日：2019-06-05
申请人： THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
发明人： Leo Leung , Kiri North , Deborah Smithen , Mohammed Aljarah , Michael Brown , Ben Ayers , Dan Niculescu-Duvaz , Caroline Springer
IPC分类号： A61P35/00 , C07D487/04
CPC分类号： C07D487/04 , A61P35/00
摘要： The disclosure relates to compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein X1 and X5 is each selected from CR1 or N; X2, X3 and X4 is each selected from CR1, CR2 or N, provided at least one of X2, X3 and X4 is CR2 and provided only one of X1, X2, X3, X4 and X5 can be N. R1, R2, R3, R4, R5, L1, L2 and L3 are as defined herein. Compounds according to Formula (I) are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer.

40. 发明公开

US20230277535A1 THERAPEUTIC COMPOSITIONS, COMBINATIONS, AND METHODS OF USE 审中-公开
公开(公告)号：US20230277535A1
公开(公告)日：2023-09-07
申请号：US17970192
申请日：2022-10-20
申请人： The Institute of Cancer Research: Royal Cancer Hospital
发明人： Udai Banerji
IPC分类号： A61K31/506 , A61P35/04
CPC分类号： A61K31/506 , A61P35/04
摘要： This invention relates to methods comprising administering a FAK inhibitor (e.g., VS-6063) in combination with a dual RAF/MEK inhibitor (e.g., CHS 126766) that are useful in the treatment of abnormal cell growth, such as cancer, in a subject such as humans.

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