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31. 发明申请

US20220017516A1 LOX INHIBITORS 有权
公开(公告)号：US20220017516A1
公开(公告)日：2022-01-20
申请号：US17293970
申请日：2019-11-15
申请人： THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
发明人： Mohammed ALJARAH , Dan NICULESCU-DUVAZ , Leo LEUNG , Deborah SMITHEN , Michael BROWN , Lawrence Christopher DAVIES , Caroline SPRINGER
IPC分类号： C07D471/08 , C07D487/08 , C07D295/088 , C07D487/04 , C07D239/48 , C07D295/108 , C07D487/10 , A61P35/00
摘要： The disclosure relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, Formula (I) 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.

32. 发明授权

US11161839B2 2-quinolone derived inhibitors of BCL6 有权
公开(公告)号：US11161839B2
公开(公告)日：2021-11-02
申请号：US16616906
申请日：2018-05-25
申请人： Cancer Research Technology Limited , The Institute of Cancer Research: Royal Cancer Hospital
发明人： Benjamin Richard Bellenie , Kwai Ming Jack Cheung , Owen Alexander Davis , Swen Hoelder , Rosemary Huckvale , Matthew Garth Lloyd
IPC分类号： C07D413/14 , C07D401/14 , C07D471/04 , C07D471/10 , C07D491/10 , C07D405/14 , C07D401/12 , A61P35/00
摘要： 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.

33. 发明申请

US20210163497A1 BCL6 INHIBITORS 有权
公开(公告)号：US20210163497A1
公开(公告)日：2021-06-03
申请号：US17046650
申请日：2019-04-12
申请人： Cancer Research Technology Limited , The Institute of Cancer Research: Royal Cancer Hospital
发明人： Benjamin Richard Bellenie , Kwai Ming Jack Cheung , Owen Alexander Davis , Swen Hoelder , Rosemary Huckvale , Gavin Collie , Mirco Meniconi , Alfie Brennan , Matthew Garth Lloyd
IPC分类号： C07D498/04 , C07D498/20 , C07D513/04 , C07D519/00 , C07D498/14 , C07D471/04 , A61P35/00
摘要： 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.

34. 发明申请

US20210040078A1 Methylamine Derivatives as Lysysl Oxidase Inhibitors for the Treatment of Cancer 有权
公开(公告)号：US20210040078A1
公开(公告)日：2021-02-11
申请号：US16908487
申请日：2020-06-22
申请人： The Institute of Cancer Research: Royal Cancer Hospital
发明人： Caroline SPRINGER , Richard MARAIS , Dan NICULESCU-DUVAZ , Leo LEUNG , Deborah SMITHEN , Cedric CALLENS , Haoran TANG
IPC分类号： C07D417/12 , C07D333/34 , C07D277/36 , C07D263/46 , C07D409/12 , A61P35/00 , C07D277/26 , C07D333/18 , C12Q1/37
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.

35. 发明申请

US20200095314A1 ENHANCEMENT OF PROSTATE CANCER TREATMENT 审中-公开
公开(公告)号：US20200095314A1
公开(公告)日：2020-03-26
申请号：US16574828
申请日：2019-09-18
申请人： Fondazione per l'Istituto Oncologico di Ricerca (IOR) , The Institute of Cancer Research: Royal Cancer Hospital
发明人： Andrea Alimonti , Arianna Calcinotto , Johann de Bono
IPC分类号： C07K16/24 , A61K31/4166 , A61K31/506 , G01N33/574 , C12Q1/6886 , A61K39/395
摘要： The present invention provides a method of treatment of prostate cancer, comprising administering a therapeutically effective amount of an inhibitor of IL-23 and/or an inhibitor of IL-23R to a mammalian patient in need thereof. The prostate cancer may be castration resistant prostate cancer (CRPC). The inhibitor may, for example, be an anti-IL-23 antibody, such as risankizumab, guselkumab or tildrakizumab. The method of treatment may further comprise administration of androgen deprivation therapy, such as enzalutamide. Also provided is a method of predicting the development of resistance to androgen deprivation therapy (ADT) in a prostate cancer in a mammalian patient and a related screening method.

36. 发明授权

US09512486B2 Materials, methods, and systems for treating cancer 有权
标题翻译：用于治疗癌症的材料，方法和系统
公开(公告)号：US09512486B2
公开(公告)日：2016-12-06
申请号：US13960537
申请日：2013-08-06
申请人： The Institute of Cancer Research: Royal Cancer Hospital
发明人： Sabera Nazneen Rahman
IPC分类号： C12Q1/68 , A61K31/502
CPC分类号： C12Q1/6886 , A61K31/502 , C12Q2600/156
摘要： Aspects of the invention relate to methods of treatment, and to kits and systems for the same including materials for determining that an individual is susceptible to cancer and if warranted treating the patient of cancer or initiating a monitoring strategy and/or taking a preventive action. Therapeutic and preventive interventions include, treating the patient with a PARR inhibitors and/or laprascopic oophorectomy. The invention also relates to systems and methods of genotyping an individual, and to methods of identifying a patent with a higher than normal likelihood of developing cancer and/or genetically related individuals or groups at heighten risk for developing cancer, particularly ovarian cancer.
摘要翻译：本发明的方面涉及治疗方法以及用于确定个体易患癌症的材料以及如果需要治疗癌症患者或启动监测策略和/或采取预防措施的药物和系统。治疗和预防性干预措施包括用PARR抑制剂和/或拉普拉西奥卵巢切除术治疗患者。本发明还涉及对个体进行基因分型的系统和方法，以及鉴定具有高于正常发生癌症和/或遗传相关个体或群体的可能性的专利的方法，以增加发展癌症，特别是卵巢癌的风险。

37. 发明申请

US20140303177A1 ORTHO-CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E.G., PURINES) AS PROTEIN KINASES INHIBITORS 有权
标题翻译：作为蛋白激酶抑制剂的ORTHO凝聚的吡啶和吡嗪衍生物（E.G.，PURINES）
公开(公告)号：US20140303177A1
公开(公告)日：2014-10-09
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： C07D471/04 , A61K31/52 , A61K31/4545 , C07D487/04 , A61K31/519 , C07D473/34 , 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 R 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是氢且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

US08809336B2 Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors 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：US08809336B2
公开(公告)日：2014-08-19
申请号：US14017814
申请日：2013-09-04
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： A61K31/497 , A61K31/52 , A61K31/519
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 R1 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 Q2 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R1或Q1的碳原子连接的C 1-4亚烷基链，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是氢且G是NR 2 R 3时，则Q2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。

39. 发明授权

US08541461B2 Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators 失效
标题翻译：包含吡唑衍生物作为蛋白激酶调节剂的药物组合
公开(公告)号：US08541461B2
公开(公告)日：2013-09-24
申请号：US11993823
申请日：2006-06-21
申请人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
发明人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
IPC分类号： A61K31/415
CPC分类号： A61K45/06 , A61K31/415 , A61K31/454 , A61K2300/00
摘要： The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound 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 patient packs, pharmaceutical kits and packs and compositions containing the combinations, methods for preparing the combinations and their use in combination therapy as anticancer agents.
摘要翻译：本发明提供包含辅助化合物（例如一种，两种或多种辅助化合物）和具有蛋白激酶B抑制活性的式（I）化合物的组合的组合：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团具有在R1和NR2R3之间延伸的5个原子的最大链长度，以及在E和NR 2 R 3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被氧或氮取代原子; 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，条件是当存在的羟基不相对于NR 2 R 3基团位于碳原子α时，条件是存在时的氧代基位于相对于NR 2 R 3基团的碳原子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。还提供了包含组合的患者包装，药物盒和包装和组合，用于制备组合的方法及其在联合治疗中作为抗癌剂的用途。

40. 发明授权

US08497294B2 Compositions comprising (S)-2-amino-1-(4-chlorophenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol as modulator of protein kinases 有权
标题翻译：包含（S）-2-氨基-1-（4-氯苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇作为蛋白激酶调节剂的组合物
公开(公告)号：US08497294B2
公开(公告)日：2013-07-30
申请号：US13180127
申请日：2011-07-11
申请人： Steven John Woodhead , David Charles Rees , Kyla Merriom Grimshaw
发明人： Steven John Woodhead , David Charles Rees , Kyla Merriom Grimshaw
IPC分类号： A61K31/415 , C07D231/12
CPC分类号： A61K31/415 , C07C215/32 , C07C247/10 , C07C309/30 , C07D231/12 , A61K2300/00
摘要： The invention provides a composition comprising (S)2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R)2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S)2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, novel process intermediates and methods for making the novel process intermediates.
摘要翻译：本发明提供包含（S）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的组合物，其中组合物基本上不含的（R）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇或该组合物含有（S）和（（S）对映异构体占优势。还提供了制备（S）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的方法，新工艺中间体和制备新工艺中间体的方法。

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