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1. 发明授权

US11608330B2 Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer 有权
公开(公告)号：US11608330B2
公开(公告)日：2023-03-21
申请号：US17221549
申请日：2021-04-02
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 , A61P35/00 , C07D263/46 , C07D277/26 , C07D277/36 , C07D333/18 , C07D333/34 , C07D409/12 , 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.

2. 发明申请

US20230012116A1 COUMARIN DERIVATIVE FOR THERAPY OR PROPHYLAXIS OF A CELL PROLIFERATIVE DISORDER 有权
公开(公告)号：US20230012116A1
公开(公告)日：2023-01-12
申请号：US17850463
申请日：2022-06-27
申请人： The Institute of Cancer Research: Royal Cancer Hospital , The Royal Marsden NHS Foundation Trust
发明人： Udai Banerji
IPC分类号： A61K31/506 , A61P35/00 , A61K9/00
摘要： The present invention provides a medicament for the treatment or prevention of a cell proliferative disorder, the medicament comprising as an active ingredient a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the medicament is used in such a manner that: (a) said compound or salt is administered twice weekly for 3 weeks,
(b) administration of said compound or salt is paused for the following 1 week, and
(c) steps (a) and (b) are subsequently repeated at least once.

3. 发明申请

US20210010085A1 MATERIALS AND METHODS FOR STRATIFYING AND TREATING CANCERS 有权
公开(公告)号：US20210010085A1
公开(公告)日：2021-01-14
申请号：US16637975
申请日：2018-08-10
申请人： The Institute of Cancer Research Royal Cancer Hospital , The Royal Marsden NHS Foundation Trust
发明人： Alex Lee , Paul Huang , Maggie Cheang , Robin Jones
IPC分类号： C12Q1/6886 , A61K31/506 , C07K16/28 , A61P35/00
摘要： The present invention relates to materials and methods for stratifying and treating cancers and to methods of identifying/selecting patients for treatment of cancer with tyrosine kinase inhibitors. Gene expression profiles, TP53 mutations and FGFR1 and PDGFRA expression are used to identify/select/stratify the cancers and patients.

4. 发明授权

US10807974B2 Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer 有权
公开(公告)号：US10807974B2
公开(公告)日：2020-10-20
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 Niculescu-Duvaz , Leo Leung , Deborah Smithen , Cedric Callens , Haoran Tang
IPC分类号： C07D417/12 , A61P35/00 , C07D333/18 , C07D277/26 , C12Q1/37 , C07D333/34 , C07D277/36 , C07D263/46 , C07D409/12
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.

5. 发明授权

US08796293B2 Purine and deazapurine derivatives as pharmaceutical compounds 有权
公开(公告)号：US08796293B2
公开(公告)日：2014-08-05
申请号：US12298462
申请日：2007-04-25
申请人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
发明人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
IPC分类号： A61K31/519 , A61K31/44 , C07D471/04 , C07D473/34
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： The invention provides 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 C1-4alkylene 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 α 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, R3R4, R6 and R8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.

6. 发明申请

US20110269808A1 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] - 乙醇的组合物作为蛋白激酶的调节剂
公开(公告)号：US20110269808A1
公开(公告)日：2011-11-03
申请号：US13180127
申请日：2011-07-11
申请人： Steven John WOODHEAD , David Charles REES , Martyn FREDERICKSON , Kyla Merriom GRIMSHAW
发明人： Steven John WOODHEAD , David Charles REES , Martyn FREDERICKSON , Kyla Merriom GRIMSHAW
IPC分类号： C07D231/12 , C07C215/32 , C07C213/00 , A61K31/415 , A61P35/00
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]-ethanok 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] - 乙酮新方法中间体和方法的方法用于制造新型工艺中间体。

7. 发明授权

US07956011B2 Materials and methods for the photodirected synthesis of oligonucleotide arrays 有权
标题翻译：寡核苷酸阵列的光定向合成的材料和方法
公开(公告)号：US07956011B2
公开(公告)日：2011-06-07
申请号：US11913650
申请日：2006-05-04
申请人： Pawel Jerzy Serafinowski , Peter Bryan Garland
发明人： Pawel Jerzy Serafinowski , Peter Bryan Garland
IPC分类号： C40B50/00 , C40B50/12 , C40B50/18 , C07H21/00 , C40B40/00 , C40B40/06 , C40B40/10 , C40B60/10 , C12Q1/68
CPC分类号： B82Y30/00 , B01J19/0046 , B01J2219/00286 , B01J2219/00439 , B01J2219/00497 , B01J2219/00527 , B01J2219/00585 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00612 , B01J2219/00626 , B01J2219/00641 , B01J2219/00659 , B01J2219/00675 , B01J2219/00677 , B01J2219/00711 , B01J2219/00713 , B01J2219/00722 , B01J2219/00725 , B01J2219/00729
摘要： Materials and methods for photodirected synthesis of oligonucleotide arrays on a solid substrate by photodirected synthesis are disclosed which employ a film formed from (i) a photoacid generator that on photolysis generates acid that is capable of directly removing the protecting group of the linker molecules or oligonucleotides and (ii) a polymer substantially lacking electronegative heteroatoms that are capable of hydrogen bonding with photogenerated acid. Methods of synthesizing an oligomer arrays are also described that use a film that restricts diffusion of reactants and products on the substrate during synthesis of the array and which includes a precursor of a deprotecting reagent. The method involves removing one or more of the non-required products of the deprotection reaction from the reactive array elements at which they are produced during the reaction, in order to displace the deprotection reaction towards completion.
摘要翻译：公开了通过光导合成在固体基质上光聚合合寡核苷酸阵列的材料和方法，其采用由（i）光解产生剂形成的膜，光致酸发生剂在光解产生能够直接除去连接分子或寡核苷酸的保护基团的酸和（ii）能够与光生酸氢键合的基本上不含电负性杂原子的聚合物。还描述了合成低聚物阵列的方法，其使用在阵列合成期间限制反应物和产物在基底上的扩散并且包括脱保护试剂的前体的膜。该方法包括从反应中产生它们的反应性阵列元素中去除脱保护反应的一种或多种非必需产物，以便使脱保护反应完全移位。

8. 发明授权

US07696204B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US07696204B2
公开(公告)日：2010-04-13
申请号：US12089677
申请日：2006-10-11
申请人： Edward McDonald , Jonathan M Large , Stephen J Shuttleworth
发明人： Edward McDonald , Jonathan M Large , Stephen J Shuttleworth
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Pyrimidines of formula (I): wherein R1 to R4, X and Y are defined in the specification are inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的嘧啶：其中R1至R4，X和Y在本说明书中定义为P13K的抑制剂，因此可用于治疗与P13激酶例如癌症相关的异常细胞生长，功能或行为引起的疾病和病症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

9. 发明申请

US20100022564A1 PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 有权
公开(公告)号：US20100022564A1
公开(公告)日：2010-01-28
申请号：US12298462
申请日：2007-04-25
申请人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
发明人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： The invention provides 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 C1-4alkylene 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 α 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, R3R4, R6 and R8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.

10. 发明申请

US20220372028A1 Methylamine Derivatives as Lysysl Oxidase Inhibitors for the Treatment of Cancer 有权
公开(公告)号：US20220372028A1
公开(公告)日：2022-11-24
申请号：US17221549
申请日：2021-04-02
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.

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