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1. 发明申请

WO2018178679A1 COMBINATION OF ISOINDOLINONE DERIVATIVES WITH SGI-110 审中-公开
公开(公告)号：WO2018178679A1
公开(公告)日：2018-10-04
申请号：PCT/GB2018/050832
申请日：2018-03-28
申请人： ASTEX THERAPEUTICS LIMITED , CANCER RESEARCH TECHNOLOGY LIMITED
发明人： CHESSARI, Gianni , LYONS, John Francis
IPC分类号： C07D401/06 , A61K31/4035 , A61K31/708 , C07D403/06 , C07D405/06 , C07D405/10 , C07D405/12 , C07H19/207 , C07C403/12 , C07D209/46 , A61P35/00
摘要： The invention provides a combination comprising: (i) a compound of formula (Io) : (Io) or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims; and (ii) a compound which is SGI-110 (SGI-110) or a tautomer or a solvate or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions containing the combinations and medical uses of the combinations.

2. 发明公开

EP1756082A1 5-MORPHOLINYLMETHYLTHIOPHENYL PHARMACEUTIAL COMPOUNDS AS P38 MAP KINASE MODULATORS 审中-公开
标题翻译：作为P38 MAP激酶调节剂的5-吗啉基甲基噻吩基药物化合物
公开(公告)号：EP1756082A1
公开(公告)日：2007-02-28
申请号：EP05732791.8
申请日：2005-04-13
申请人： Astex Therapeutics Limited
发明人： GILL, Adrian Liam , CARR, Maria Grazia , LYONS, John Francis , THOMPSON, Neil Thomas , REES, David Charles
IPC分类号： C07D333/36 , C07D409/12 , C07D417/12 , A61K31/381 , A61P35/04
CPC分类号： C07D333/36 , C07D409/12 , C07D417/12
摘要： The invention provides compounds of the formula (I) or a salt, solvate or N-oxide thereof, wherein:R1 and R2 are the same or different and each is selected from hydrogen, saturated C1-3 hydrocarbyl, halogen and cyano; X is selected from C=O, C=S, C(=O)NH, C(=S)NH, C(=O)O, C(=O)S, C(=S)O and C(=S)S; R3 is selected from aryl and heteroaryl groups each having from 5 t0 12 ring members and being unsubstituted or substituted by one or more substituent groups R10 as defined in the claims; R4 and R5 are the same or different and are selected from hydrogen and methyl; or one of R4 and R5 is selected from hydroxymethyl and ethyl and the other is hydrogen; and R6 and R7 are the same or different and are selected from hydrogen and methyl. The compounds of the formula (I) hayed activity as p38 MAP kinase and Taf kinase inhibitors.
摘要翻译：本发明提供了式（I）化合物或其盐，溶剂化物或N-氧化物，其中：R 1和R 2相同或不同，并且各自选自氢，饱和C 1-3烃基，卤素和氰基; X选自C = O，C = S，C（= O）NH，C（= S）NH，C（= O）O，C（= O）S，C（= S）O和C S）S; R3选自各自具有5至10个环成员且未被取代或被一个或多个如权利要求所定义的取代基R10取代的芳基和杂芳基; R4和R5相同或不同，选自氢和甲基; 或者R 4和R 5中的一个选自羟甲基和乙基，另一个是氢; R6和R7相同或不同，选自氢和甲基。式（I）化合物具有p38 MAP激酶和Taf激酶抑制剂的活性。

4. 发明公开

EP2073804A2 HYDROXY-SUBSTITUTED BENZOIC ACID AMIDE COMPOUNDS FOR USE IN THERAPY 有权
标题翻译：羟基取代基苯甲酸酯 - 维生素D维生素DER BEHANDLUNG VON SCHMERZEN
公开(公告)号：EP2073804A2
公开(公告)日：2009-07-01
申请号：EP07824166.8
申请日：2007-10-12
申请人： Astex Therapeutics Limited
发明人： LYONS, John Francis , THOMPSON, Neil Thomas
IPC分类号： A61K31/4035 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P29/00 , A61P29/02 , A61P9/10 , A61P25/02 , A61P25/28 , A61P43/00 , A61P31/12 , A61P31/10 , A61P33/00
CPC分类号： A61K31/4035 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , Y02A50/411 , A61K2300/00
摘要： The invention also provides the use of a compound of the formula (VI) for the manufacture of a medicament for the prophylaxis or treatment of a fungal, protozoal, viral or parasitic disease state or condition (other than a disease state or condition due to Plasmodium falciparum) or for use in the prophylaxis or treatment of Ewing's sarcoma, atherosclerosis or lupus erythematosus.
摘要翻译：本发明提供化合物在制备用于治疗疼痛的药物中的用途，其中所述化合物为式（Ⅵ）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 其中双环基团选自结构C1，C5和C6：其中n，R1，R2a，R3，R4a，R8和R10如权利要求中所定义。本发明还提供了式（VI）化合物在制备用于预防或治疗真菌，原生动物，病毒或寄生虫病状态或疾病（除了由于疟原虫导致的疾病状态或疾病之外）恶性疟原虫）或用于预防或治疗尤文氏肉瘤，动脉粥样硬化或红斑狼疮。

5. 发明公开

EP1845974A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：EP1845974A1
公开(公告)日：2007-10-24
申请号：EP06700912.6
申请日：2006-01-20
申请人： Astex Therapeutics Limited
发明人： CURRY, Jayne Elizabeth , LYONS, John Francis , SQUIRES, Matthew Simon , THOMPSON, Neil Thomas , THOMPSON, Kyla Merriom , WYATT, Paul Graham
IPC分类号： A61K31/415 , A61K31/4155 , A61P35/00 , A61K33/24 , A61K31/70 , A61K31/047 , A61K31/505 , A61K31/337 , A61K38/01 , A61K39/395 , A61K31/4745 , A61K31/475
CPC分类号： A61K33/24 , A61K31/047 , A61K31/337 , A61K31/415 , A61K31/4155 , A61K31/4745 , A61K31/505 , A61K31/70 , A61K31/7068 , A61K38/01 , A61K39/395 , A61K45/06 , A61K47/545 , A61K47/6805 , A61K2300/00
摘要： The invention provides a combination of a cytotoxic compound or signalling inhibitor and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO 2 , C-O, NR g (C-O) or 0(C-O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R 1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C 1-4 hydrocarbyloxy, amino, mono- or di-C 1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO 2 ; R 2 is hydrogen; halogen; C 1-4 alkoxy (e.g. methoxy); or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy); R 3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R 4 is hydrogen or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy).

6. 发明公开

EP3601251A1 COMBINATION OF ISOINDOLINONE DERIVATIVES WITH SGI-110 审中-公开
公开(公告)号：EP3601251A1
公开(公告)日：2020-02-05
申请号：EP18715917.3
申请日：2018-03-28
申请人： Astex Therapeutics Limited , Cancer Research Technology Limited
发明人： CHESSARI, Gianni , LYONS, John Francis
IPC分类号： C07D401/06 , A61K31/4035 , A61K31/708 , C07D403/06 , C07D405/06 , C07D405/10 , C07D405/12 , C07H19/207 , C07C403/12 , C07D209/46 , A61P35/00

7. 发明授权

EP2073804B1 HYDROXY-SUBSTITUTED BENZOIC ACID AMIDE COMPOUNDS FOR USE IN THE TREATMENT OF PAIN 有权
标题翻译：羟基取代的苯甲酸酰胺化合物用于治疗疼痛
公开(公告)号：EP2073804B1
公开(公告)日：2017-09-13
申请号：EP07824166.8
申请日：2007-10-12
申请人： Astex Therapeutics Limited
发明人： LYONS, John Francis , THOMPSON, Neil Thomas
IPC分类号： A61K31/4035 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P29/00 , A61P29/02 , A61P9/10 , A61P25/02 , A61P25/28 , A61P43/00 , A61P31/12 , A61P31/10 , A61P33/00
CPC分类号： A61K31/4035 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , Y02A50/411 , A61K2300/00
摘要： The invention also provides the use of a compound of the formula (VI) for the manufacture of a medicament for the prophylaxis or treatment of a fungal, protozoal, viral or parasitic disease state or condition (other than a disease state or condition due to Plasmodium falciparum) or for use in the prophylaxis or treatment of Ewing's sarcoma, atherosclerosis or lupus erythematosus.
摘要翻译：本发明还提供了式（VI）化合物在制备用于预防或治疗真菌，原生动物，病毒或寄生虫疾病状态或病症（除由于疟原虫引起的疾病状态或病症之外的药物恶性疟原虫）或用于预防或治疗尤因肉瘤，动脉粥样硬化或红斑狼疮。

8. 发明公开

EP2081891A2 PHARMACEUTICAL COMPOUNDS HAVING HSP90 INHIBITORY OR MODULATING ACTIVITY 审中-公开
标题翻译：药剂师VERBINDUNGEN MIT HSP90-HEMMENDER ODER MODULIERENDER WIRKUNG
公开(公告)号：EP2081891A2
公开(公告)日：2009-07-29
申请号：EP07824114.8
申请日：2007-10-12
申请人： Astex Therapeutics Limited
发明人： CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John Francis , THOMPSON, Neil Thomas
IPC分类号： C07D209/08 , C07D209/44 , C07D215/08 , C07D401/04 , C07D401/12 , C07D419/10 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10 , A61K31/438
CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18
摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (Vl0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R 1 : is„ hydrogen, hydroxy, or O-Rz; R2a is hydroxy, methoxy or O-Rz; provided that at least one of R1 and R2a is O-Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or; Lp is a bond, C=O, (C=O)O, (C=O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C=O or (C=O)O; and provided also that O-Rz does not contain an 0-0 moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims. The compounds of formula (Vl0) are pro-drugs of parent compounds wherein R1 and/or R2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.
摘要翻译：本发明提供一种用于医药的化合物，该化合物为式（VI0）化合物或其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团：选自结构式C1，C5和C6：其中n为0,1,2或3; R1是氢，羟基或O-Rz; R2a是羟基，甲氧基或O-Rz; 条件是R1和R2a中的至少一个是O-Rz; Rz是Lp-Rp1; SO3H; 葡萄糖苷酸残基; 单，二或三肽残基; 或Lp为键，C = O，（C = O）O，（C = O）NRp1或S（O）xNRp1; x为1或2; Rp1是氢或任选取代的含有0,1或2个碳环和0,1,2,3,4,5或6碳 - 碳多重键的C1〜25烃基，条件是当Lp为 C = O或（C = O）O; 并且还提供O-Rz不含有O-O部分; 并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，并且各自为基团Rp1; R3，R4a，R8和R10在权利要求中限定。式（VI0）化合物是其中R 1和/或R 2a是羟基的母体化合物的前药，其中母体化合物具有Hsp90抑制活性。

9. 发明公开

EP2046327A1 MEDICAL USE OF CYCLIN DEPENDENT KINASES INHIBITORS 审中-公开
标题翻译：激酶抑制剂细胞周期蛋白的医疗用途
公开(公告)号：EP2046327A1
公开(公告)日：2009-04-15
申请号：EP07766316.9
申请日：2007-07-20
申请人： Astex Therapeutics Limited
发明人： PIKE, Andrew , LYONS, John Francis
IPC分类号： A61K31/415 , A61K31/44 , A61P13/12 , A61P29/00 , A61P25/00 , A61P9/10 , A61P9/12 , A61P3/10
CPC分类号： A61K31/415 , A61K31/44
摘要： The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (0) : or a salt or tautomers or N-oxides or solvate thereof; wherein X is a group R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NR9(C=O) or O(C=O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy. The invention also provides the use of the compounds of the formula (0) for the treatment of stroke and for the treatment of polycystic kidney disease.

10. 发明公开

EP1933832A2 PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：与吡衍生物作为蛋白激酶调节剂的药物组合
公开(公告)号：EP1933832A2
公开(公告)日：2008-06-25
申请号：EP06755597.9
申请日：2006-06-21
申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , Cancer Research Technology Limited
发明人： THOMPSON, Neil Thomas , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle Dawn , LYONS, John Francis , THOMPSON, Kyla Merriom
IPC分类号： A61K31/415 , A61K31/454 , A61P35/00 , A61P37/00
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.

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