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1. 发明申请

WO2009156735A3 NEW THERAPEUTIC AGENTS 审中-公开
标题翻译：新的治疗剂
公开(公告)号：WO2009156735A3
公开(公告)日：2010-11-18
申请号：PCT/GB2009001599
申请日：2009-06-25
申请人： CANCER REC TECH LTD , GOLDING BERNARD THOMAS , RIEDINGER CHRISTIANE , GRIFFIN ROGER JOHN , HARDCASTLE IAN ROBERT , VALEUR ERIC , WATSON ANNA FRANCES , NOBLE MARTIN
发明人： GOLDING BERNARD THOMAS , RIEDINGER CHRISTIANE , GRIFFIN ROGER JOHN , HARDCASTLE IAN ROBERT , VALEUR ERIC , WATSON ANNA FRANCES , NOBLE MARTIN
IPC分类号： C07D209/48 , A61K31/4035 , A61P35/00 , C07D401/06 , C07D403/06
CPC分类号： C07D209/49 , A61K31/4035 , A61K31/4402 , A61K45/06 , C07D209/48 , C07D401/06 , C07D403/06
摘要： A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
摘要翻译：式（I）化合物或式（II）化合物或其药学上可接受的盐，其中R 1 -R 7和X如说明书中所定义，以及这些化合物在治疗中的用途，特别是在治疗癌症或作为 MDM2蛋白与p53相互作用的抑制剂。

2. 发明申请

WO2009050159A1 COMBINATION OF FLUTICASONE FUROATE WITH 4- [ (4-CHL0R0PHENYL)METHYL] -2- ({ (2R)-I- [4-(4-{ [3-(HEXAHYDR0-LH-AZEPIN-L-YL) PROPYL ] OXY} PHENYL) BUTYL] -2-PYRROLIDINYL}METHYL) -1 (2H) - PHTHALAZ INONE 审中-公开
标题翻译：氟磷酸酯与4- [（4-氯苯基）甲基] -2 - （{（2R）-1- [4-（4 - {[3-（十六氢化-4-羟基 - 丙酸叔丁酯）丙基]氧化物的组合 }苯基）丁基] -2-吡咯烷基}甲基）-1（2H） - PHTHALAZ INONE
公开(公告)号：WO2009050159A1
公开(公告)日：2009-04-23
申请号：PCT/EP2008/063781
申请日：2008-10-14
申请人： GLAXO GROUP LIMITED , BONE, Gavin , BROWN, Richard Orlando , GORE, Paul Martin , HANCOCK, Ashley Paul , HODGSON, Simon Teanby , KINDON, Leanda Jane , NOBLE, Martin Philip
发明人： BONE, Gavin , BROWN, Richard Orlando , GORE, Paul Martin , HANCOCK, Ashley Paul , HODGSON, Simon Teanby , KINDON, Leanda Jane , NOBLE, Martin Philip
IPC分类号： A61K31/502 , A61K31/58 , A61K45/06 , A61P29/00 , A61P37/08
CPC分类号： A61K45/06 , A61K31/502 , A61K31/58 , A61K2300/00
摘要： The present invention provides aqueous pharmaceutical compositions which comprise a compound which is 4-[(4-chlorophenyl)methyl]-2-({(2/ R )-1-[4-(4-{[3-(hexahydro-1 H -azepin- 1-yl)propyl]oxy}phenyl)butyl]-2-pyrrolidinyl}methyl)-1 (2 H )-phthalazinone (I) or a pharmaceutically acceptable salt thereof, and to their use in the treatment of various inflammatory and/or allergic diseases such as allergic rhinitis.
摘要翻译：本发明提供了包含4 - [（4-氯苯基）甲基] -2 - （{（2 / R）-1- [4-（4 - {[3-（六氢-1H- - 氮杂-1-基）丙基]氧基}苯基）丁基] -2-吡咯烷基}甲基）-1（2H） - 酞嗪酮（I）或其药学上可接受的盐，并且用于治疗各种炎症和 /或过敏性疾病如过敏性鼻炎。

3. 发明申请

WO2007039761A3 CRYSTAL STRUCTURE OF CD44 AND ITS USE 审中-公开
标题翻译： CD44的晶体结构及其用途
公开(公告)号：WO2007039761A3
公开(公告)日：2007-06-21
申请号：PCT/GB2006003734
申请日：2006-10-06
申请人： MEDICAL RES COUNCIL , JACKSON DAVID G , BANERJI SUNEALE , NOBLE MARTIN , DAY ANTHONY J
发明人： JACKSON DAVID G , BANERJI SUNEALE , NOBLE MARTIN , DAY ANTHONY J
IPC分类号： C07K14/705 , C12N15/09 , G01N33/68
CPC分类号： G01N33/6872 , C07K14/70585 , C07K2299/00 , G01N2333/70585 , G01N2500/00
摘要： The invention provides the crystal structure of the CD44 protein molecule. The structure is set out in Tables 1 to 4. The structure may be used in to model the interaction of compounds such as pharmaceuticals with this protein, and to determine the structure of related molecules.
摘要翻译：本发明提供了CD44蛋白分子的晶体结构。该结构列于表1至4中。该结构可用于模拟化合物（例如药物）与该蛋白质的相互作用，并确定相关分子的结构。

4. 发明申请

WO2002059125A1 CYCLIN DEPENDENT KINASE INHIBITING PURINE DERIVATIVES 审中-公开
标题翻译： CYCLIN依赖性激酶抑制嘌呤衍生物
公开(公告)号：WO2002059125A1
公开(公告)日：2002-08-01
申请号：PCT/GB2002/000272
申请日：2002-01-22
申请人： CANCER RESEARCH CAMPAIGN TECHNOLOGY LIMITED , GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , GOLDING, Bernard, Thomas , HARDCASTLE, Ian, Robert , NEWELL, David, Richard , JEWSBURY, Philip, John , BOYLE, Francis, Thomas , ENDICOTT, Jane, Anne , NOBLE, Martin, Edward, Mantyla
发明人： GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , GOLDING, Bernard, Thomas , HARDCASTLE, Ian, Robert , NEWELL, David, Richard , JEWSBURY, Philip, John , BOYLE, Francis, Thomas , ENDICOTT, Jane, Anne , NOBLE, Martin, Edward, Mantyla
IPC分类号： C07D473/18
CPC分类号： C07D473/24 , A61K31/52 , C07D473/18 , C07D473/32
摘要： The present invention relates to a series of CDK-inhibiting purine derivatives of structural formula (I), or a pharmaceutically acceptable salt and/or prodrug form thereof, wherein: X is O, S or CHR x where R x is H or C 1-14 alkyl; D is NZ 1 Z 2 where Z 1 is selected from H, C 1-4 alkyl, C 1-4 hydroxyalkyl, an unsubstituted or substituted aryl or heteroaryl, and an unsubstituted or substituted aralkyl or heteroaralkyl group, and Z 2 is selected from an unsubstituted or substituted aryl or heteroaryl, and an unsubstituted or substituted aralkyl or heteroaralkyl group; A is selected from H, C 1-4 alkyl, C 1-4 alkoxy, hydroxy, CH 2 (CH 2 ) n OH (n=1-4), and NR al R a2 where R al and R a2 are each independently H or C 1-4 alkyl; B is selected from H, halo, C 1-4 alkyl, C 1-4 alkoxy, CF 3 , an optionally substituted aryl or an optionally substituted aralkyl, and a hydroxy group that may undergo a C=O tautomeric rearrangement; and Y comprises an unsubstituted or substituted 4- to 8-membered carbocyclic or heterocyclic ring, optionally forming part of a larger fused ring structure, or consists of an optionally substituted linear or branched hydrocarbon chain. These purine derivatives are potential chemotherapeutic agents and, accordingly, the present invention also relates to the use of these compounds in the treatment of tumours or other cell proliferation disorders and pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及结构式（I）的一系列CDK抑制性嘌呤衍生物或其药学上可接受的盐和/或前药形式，其中：X是O，S或CHR x，其中Rx是H或C 1-14烷基 ; D是NZ1Z2，其中Z1选自H，C1-4烷基，C1-4羟基烷基，未取代或取代的芳基或杂芳基，以及未取代或取代的芳烷基或杂芳烷基，Z2选自未取代或取代的芳基或杂芳基和未取代或取代的芳烷基或杂芳烷基; A选自H，C1-4烷基，C1-4烷氧基，羟基，CH2（CH2）nOH（n = 1-4）和NRalRa2，其中Ral和Ra2各自独立地为H或C1-4烷基; B选自H，卤素，C 1-4烷基，C 1-4烷氧基，CF 3，任选取代的芳基或任选取代的芳烷基，以及可经历C = O互变异构重排的羟基; 并且Y包含未取代或取代的4至8元碳环或杂环，任选地形成较大稠环结构的一部分，或由任选取代的直链或支链烃链组成。这些嘌呤衍生物是潜在的化学治疗剂，因此，本发明还涉及这些化合物在治疗肿瘤或其它细胞增殖障碍中的用途以及包含这些化合物的药物组合物。

5. 发明申请

WO2008145951A1 PROTEIN LAYERS AND THEIR USE IN ELECTRON MICROSCOPY 审中-公开
标题翻译：蛋白质层及其在电子显微镜中的应用
公开(公告)号：WO2008145951A1
公开(公告)日：2008-12-04
申请号：PCT/GB2008/001437
申请日：2008-04-23
申请人： ISIS INNOVATION LIMITED , SINCLAIR, John, Charles , NOBLE, Martin, Edward, Mäntylä
发明人： SINCLAIR, John, Charles , NOBLE, Martin, Edward, Mäntylä
IPC分类号： C07K14/00 , C07K14/47 , C07K19/00 , G01N1/28 , H01J37/20
CPC分类号： C07K14/001 , C07K14/24 , C07K14/47 , C07K19/00 , C07K2319/00 , H01J37/20 , H01J37/295 , H01J2237/201
摘要： Protein layers (1) repeating regularly in two dimensions comprise protein protomers (2) which each comprise at least two monomers (5), (6) genetically fused together. The monomers (5), (6) are monomers of respective oligomer assemblies (3), (4) into which the monomers are assembled to assembly of the protein layer. The first oligomer assembly (3) belongs to a dihedral point group of order O, where O equals (3), (4) or (6) and has a set of O rotational symmetry axes of order (2). The second oligomer assembly (4) has a rotational symmetry axis of order (2). Due to the symmetry of the oligomer assemblies (3), (4), the rotational symmetry axes of each second oligomer assembly (4) is aligned with one of said set of O rotational symmetry axes of a first oligomer assembly (3) with (2) protomers being arranged symmetrically therearound. Thus, an 2-fold fusion between the oligomer assemblies (3), (4) is produced and the arrangements of the rotational symmetry axes of the oligomer assemblies (3), (4) cause the protein layer to repeat regularly. The protein layer has many uses, for example to support molecular entities for biosensing, x-ray crystallography or electron microscopy.
摘要翻译：在二维中规则重复的蛋白质层（1）包含蛋白质反转录剂（2），其每个包含至少两个基因融合在一起的单体（5），（6）。单体（5），（6）是各自的低聚物组件（3），（4）的单体，其中单体组装成蛋白质层的组装。第一低聚物组件（3）属于阶数为O的二面点组，其中O等于（3），（4）或（6），并具有一组O旋转对称轴（2）。第二低聚物组件（4）具有顺序（2）的旋转对称轴。由于低聚物组件（3），（4）的对称性，每个第二低聚物组件（4）的旋转对称轴线与第一低聚物组件（3）的所述一组O旋转对称轴线之一与（ 2）检测器在其周围对称布置。因此，产生低聚物组件（3），（4）之间的2倍融合，并且低聚物组件（3），（4）的旋转对称轴的布置使得蛋白质层定期重复。蛋白质层具有许多用途，例如支持用于生物传感，X射线晶体学或电子显微镜的分子实体。

6. 发明申请

WO2007039761A2 CRYSTAL STRUCTURE OF CD44 AND ITS USE 审中-公开
标题翻译： CD44的晶体结构及其用途
公开(公告)号：WO2007039761A2
公开(公告)日：2007-04-12
申请号：PCT/GB2006/003734
申请日：2006-10-06
申请人： MEDICAL RESEARCH COUNCIL , JACKSON, David, G. , BANERJI, Suneale , NOBLE, Martin , DAY, Anthony, J.
发明人： JACKSON, David, G. , BANERJI, Suneale , NOBLE, Martin , DAY, Anthony, J.
IPC分类号： C07K14/475 , C07K14/71 , C07K16/28 , A61K39/395 , A61P25/00
CPC分类号： G01N33/6872 , C07K14/70585 , C07K2299/00 , G01N2333/70585 , G01N2500/00
摘要： The invention provides the crystal structure of the CD44 protein molecule. The structure is set out in Tables 1 to 4. The structure may be used in to model the interaction of compounds such as pharmaceuticals with this protein, and to determine the structure of related molecules.
摘要翻译：本发明提供了CD44蛋白分子的晶体结构。该结构在表1至表4中列出。该结构可以用于模拟化合物如药物与该蛋白质的相互作用并确定相关分子的结构。

7. 发明申请

WO9902162A9 CYCLIN DEPENDENT KINASE INHIBITING PURINE DERIVATIVES 审中-公开
标题翻译：周期蛋白依赖性激酶抑制嘌呤衍生物
公开(公告)号：WO9902162A9
公开(公告)日：1999-07-29
申请号：PCT/GB9802025
申请日：1998-07-10
申请人： CANCER RES CAMPAIGN TECH , GRIFFIN ROGER JOHN , CALVERT ALAN HILARY , CURTIN NICOLA JANE , NEWELL DAVID RICHARD , GOLDING BERNHARD THOMAS , ENDICOTT JANE ANNE , NOBLE MARTIN EDWARD MANTYLA , BOYLE FRANCIS THOMAS , JEWSBURY PHILIP JOHN
发明人： GRIFFIN ROGER JOHN , CALVERT ALAN HILARY , CURTIN NICOLA JANE , NEWELL DAVID RICHARD , GOLDING BERNHARD THOMAS , ENDICOTT JANE ANNE , NOBLE MARTIN EDWARD MANTYLA , BOYLE FRANCIS THOMAS , JEWSBURY PHILIP JOHN
IPC分类号： A61K31/52 , A61K31/522 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P35/00 , A61P43/00 , C07D473/18 , C07D473/24 , C07D473/26 , C07D473/30 , C07D473/40 , C07H15/26 , C07H17/02 , A61K31/70
CPC分类号： C07H15/26 , C07D473/18 , C07D473/30 , C07D473/40
摘要： A range is disclosed of purine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDKs) and which thereby c an provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to be different to that of known CDK inhibitors such as olomoucine and roscovitine. In formula (I), in preferred embodiments: X is O, S or CHRx where Rx is H or C1-4 alkyl; D is H, halo or NZ1Z2 where Z1 and Z2 are each independently H or C1-4 alkyl or C1-4 hydroxyalkyl; A is selected from H, C1-4 alkyl, C1-4 alkoxy, hydroxy, CH2(CH2)nOH (n=1-4), and NRa1Ra2 where Ra1 and Ra2 are each independently H or C1-4 alkyl; B is selected from H, C1-4 alkyl, C1-4 alkoxy, CF3, an optionally substituted aryl (e.g. phenyl) or an optionally substituted aralkyl (e.g. benzyl), and an hydroxy group that provides a C=O tautomer; and Y is or includes an optionally substituted 4- to 8-membered carbocyclic or heterocyclic ring; or comprises an optionally substituted linear or branched hydrocarbon chain.
摘要翻译：公开了可作为细胞周期蛋白依赖性激酶（CDK）抑制剂并由此提供用于治疗肿瘤或其他细胞增殖性疾病的有用治疗化合物的嘌呤衍生物（I）的范围。本发明的化合物以似乎不同于已知CDK抑制剂例如奥罗莫星和罗可嘌呤的方式与CDK分子结合。在式（I）中，在优选的实施方案中：X是O，S或CHR x，其中R x是H或C 1-4烷基; D是H，卤素或NZ1Z2，其中Z1和Z2各自独立地是H或C1-4烷基或C1-4羟烷基; A选自H，C1-4烷基，C1-4烷氧基，羟基，CH2（CH2）nOH（n = 1-4）和NRa1Ra2，其中Ra1和Ra2各自独立地为H或C1-4烷基; B选自H，C 1-4烷基，C 1-4烷氧基，CF 3，任选取代的芳基（例如苯基）或任选取代的芳烷基（例如苄基），和提供C = O互变异构体的羟基; 且Y是或包括任选取代的4至8元碳环或杂环; 或包含任选取代的直链或支链烃链。

8. 发明申请

WO2004033487A1 PROTEIN LATTICE 审中-公开
标题翻译：蛋白质
公开(公告)号：WO2004033487A1
公开(公告)日：2004-04-22
申请号：PCT/GB2003/004306
申请日：2003-10-08
申请人： ISIS INNOVATION LIMITED , SINCLAIR, John, Charles , NOBLE, Martin, Edward, Mantyla
发明人： SINCLAIR, John, Charles , NOBLE, Martin, Edward, Mantyla
IPC分类号： C07K1/00
CPC分类号： C07K19/00 , C07K14/001 , C07K14/24 , C07K14/47 , C07K2319/00
摘要： Protein lattice (1) having a regular structure with a repeating unit repeating in three dimensions may have many uses, for example to support an array of macromolecular entities for x-ray crystallography. The repeating unit comprises protein protomers (2) which each comprise at least two monomers (5, 6) fused together. The monomers (5, 6) are each monomers of a respective oligomer assembly (3, 4) into which the monomers are assembled for assembly of the protomers into the lattice. The first oligomer assembly (3) has a set of rotational symmetry axes extending in three dimensions. In said protomers (2), further monomers (6) fused to said first monomers (5) are monomers of respective further oligomer assemblies (4) which have a rotational symmetry axis of the same order as a respective one of said set of rotational symmetry axes of said first oligomer assembly (3). Thus, the repeating unit includes protomers (2) with the first monomers (5) of the protomers (2) being assembled into said first oligomer assembly (3) and, in respect of respective ones of said set of rotational symmetry axes, with further monomers (6) of the protomers (2) fused to respective first monomers (3) being assembled into respective further oligomer assemblies (4). As a result of the symmetry of the oligomer assemblies (3, 4) said rotational symmetry axis of said respective further oligomer assemblies (4) is aligned with the respective rotational symmetry axis of said first oligomer assembly (3). Thus, an N-fold fusion between the oligomer assemblies (3, 4) is produced and the rotational symmetry axes of the oligomer assemblies (3, 4) define the symmetry of the lattice.
摘要翻译：具有在三维重复的重复单元的规则结构的蛋白质晶格（1）可以具有许多用途，例如用于支持用于x射线晶体学的大分子实体的阵列。重复单元包括蛋白质反转录剂（2），每种蛋白质包含至少两种融合在一起的单体（5,6）。单体（5,6）各自是各自的低聚物组件（3,4）的单体，其中组装单体以将反型体组装成晶格。第一低聚物组件（3）具有一组三维延伸的旋转对称轴。在所述检测器（2）中，与所述第一单体（5）熔合的另外的单体（6）是各自另外的低聚物组件（4）的单体，其具有与所述一组旋转对称中的相应一个相同顺序的旋转对称轴所述第一低聚物组件（3）的轴线。因此，重复单元包括反转剂（2），其中反萃剂（2）的第一单体（5）被组装到所述第一低聚物组合物（3）中，并且相对于所述一组旋转对称轴中的相应组与各自的第一单体（3）熔合的反射体（2）的单体（6）被组装成各自的另外的低聚物组件（4）。由于低聚物组件（3,4）的对称性，所述各个另外的低聚物组件（4）的所述旋转对称轴线与所述第一低聚物组件（3）的相应旋转对称轴线对齐。因此，产生低聚物组件（3,4）之间的N折融合，并且低聚物组件（3,4）的旋转对称轴限定了晶格的对称性。

9. 发明申请

WO9950251A3 CYCLIN DEPENDENT KINASE INHIBITORS 审中-公开
标题翻译： CYCLIN依赖性激酶抑制剂
公开(公告)号：WO9950251A3
公开(公告)日：2000-02-03
申请号：PCT/GB9900830
申请日：1999-03-29
申请人： CANCER RES CAMPAIGN TECH , GRIFFIN ROGER JOHN , CALVERT ALAN HILARY , CURTIN NICOLA JANE , NEWELL DAVID RICHARD , GOLDING BERNARD THOMAS , ENDICOTT JANE ANNE , NOBLE MARTIN EDWARD MANTYLA , BOYLE FRANCIS THOMAS , JEWSBURY PHILIP JOHN
发明人： GRIFFIN ROGER JOHN , CALVERT ALAN HILARY , CURTIN NICOLA JANE , NEWELL DAVID RICHARD , GOLDING BERNARD THOMAS , ENDICOTT JANE ANNE , NOBLE MARTIN EDWARD MANTYLA , BOYLE FRANCIS THOMAS , JEWSBURY PHILIP JOHN
IPC分类号： A61K31/505 , A61K31/52 , A61K31/522 , A61P35/00 , A61P43/00 , C07D239/48 , C07D239/50 , C07D473/00 , C07D473/18 , C07D473/24 , C07D473/30 , C07D473/32 , C07D473/36 , C07D519/00 , C07H19/167
CPC分类号： C07D239/48 , C07D239/50 , C07H19/167
摘要： A range is disclosed of pyrimidine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDK's) and which thereby can provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to differ from that of known CDK inhibitors such as olomoucine and roscovitine.
摘要翻译：公开了可以作为细胞周期蛋白依赖性激酶（CDK's）抑制剂的嘧啶衍生物（I）的范围，由此可以提供用于治疗肿瘤或其它细胞增殖病症的有用的治疗化合物。本发明的化合物以与已知的CDK抑制剂如奥洛莫斯和罗斯考维胺似乎不同的方式结合CDK分子。

10. 发明申请

WO2009156735A2 NEW THERAPEUTIC AGENTS 审中-公开
标题翻译：新的治疗剂
公开(公告)号：WO2009156735A2
公开(公告)日：2009-12-30
申请号：PCT/GB2009/001599
申请日：2009-06-25
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , GOLDING Bernard, Thomas , RIEDINGER Christiane , GRIFFIN Roger John , HARDCASTLE Ian, Robert , VALEUR Eric , WATSON Anna, Frances , NOBLE Martin
发明人： GOLDING Bernard, Thomas , RIEDINGER Christiane , GRIFFIN Roger John , HARDCASTLE Ian, Robert , VALEUR Eric , WATSON Anna, Frances , NOBLE Martin
CPC分类号： C07D209/49 , A61K31/4035 , A61K31/4402 , A61K45/06 , C07D209/48 , C07D401/06 , C07D403/06
摘要： A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
摘要翻译：式（I）化合物或式（II）化合物或其药学上可接受的盐，其中R 1 -R 7和X如说明书中所定义，以及这些化合物在治疗中的用途，特别是在治疗癌症或作为 MDM2蛋白与p53相互作用的抑制剂。

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