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1. 发明公开

EP1539716A1 BENZODIAZEPINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：苯并二氮杂衍生物和含有它们的药物组合物
公开(公告)号：EP1539716A1
公开(公告)日：2005-06-15
申请号：EP03748279.1
申请日：2003-09-22
申请人： Arrow Therapeutics Limited
发明人： CARTER, MalcolmArrow Therapeutics Limited , HENDERSON, ElisaArrow Therapeutics Limited , KELSEY, RichardArrow Therapeutics Limited , WILSON, LaraArrow Therapeutics Limited , CHAMBERS, PhilArrow Therapeutics Limited , TAYLOR, DebraArrow Therapeutics Limited , TYMS, StanArrow Therapeutics Limited
IPC分类号： C07D243/24 , C07D409/12 , C07D405/12 , C07D413/12 , C07D403/12 , C07D401/12 , A61K31/5513 , A61P31/12
CPC分类号： C07D401/12 , C07D243/24 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: - R1 represents C1-6 alkyl, aryl or heteroaryl; - R2 represents hydrogen or C1-6 alkyl; - each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, -CO2RI, -CONRIRII, -NH-CO-RI, -S(O)RI, -S(O)2RI, -NH-S(O)2RI, -S(O)NRIRII or -S(O)2NRIRII wherein each RI and RII is the same or different and represents hydrogen or C1-6 alkyl; - n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; - R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)-C(O)-, heteroaryl-C(O)-C(O)-, carbocyclyl-C(O)-C(O)-, heterocyclyl-C(O)-C(O)- or, -XR6; - X represents -CO-, -S(O)- or -S(0)2-; and - R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C 1-6hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C 1-6 hydroxyalkyl)-, aryl-(C 1-6alkyl)-O-, heteroaryl-(C 1-6alkyl)-O-, carbocyclyl-(C1-6 alkyl)-O-, heterocyclyl-(C1-6 alkyl)-O- or -NRIRII wherein each RI and RII is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl- (C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

2. 发明授权

EP1844004B1 QUINAZOLINE DERIVATES AS ANTIVIRAL AGENTS 有权
标题翻译：喹唑啉衍生物作为抗病毒剂
公开(公告)号：EP1844004B1
公开(公告)日：2009-06-24
申请号：EP06709585.1
申请日：2006-01-30
申请人： Arrow Therapeutics Limited
发明人： COCKERILL, George, Stuart, Arrow Therapeutics Ltd. , FLACK, Stephen Sean, Arrow Therapeutics Limited , MATHEWS, Neil, Arrow Therapeutics Limited , SALTER, James Iain, Arrow Therapeutics Limited
IPC分类号： C07C255/61 , C07D239/94 , C07D403/14 , A61P31/14 , A61K31/5377 , A61K31/517
CPC分类号： C07C255/61 , C07D239/94
摘要： Compounds of formula (I) are found to be active in inhibiting replication of flaviviridae Formula (I) wherein: X represents a direct bond or a moiety -L-NR-, wherein R is hydrogen or C1-C4 alkyl, and L represents a C1-C4 alkylene, C6-C10 aryl or 5- to 10- membered heteroaryl moiety; either R1 and R2, together with the N atom to which they are attached, form a 5- to 10- membered heterocyclyl group or a 5- to 10- membered heteroaryl group, or R1 represents hydrogen, C6-C10 aryl, C1-C4 alkyl or C1-C4 hydroxyalkyl and R2 represents C6-C10 aryl, C1-C4 alkyl or C1-C4 hydroxyalkyl; and R3 represents a C6-C10 aryl, C3-C6 carbocyclyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl moiety, said aryl, carbocyclyl, heteroaryl and heterocyclyl groups being unsubstituted or substituted by 1, 2 or 3 substituents selected from halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxy, thiol, -NH2, C1-C4 hydroxyalkyl, C1-C4 thioalkyl and C1-C4 aminoalkyl substituents.

3. 发明公开

EP1991533A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：喹唑啉衍生物FOR USE作为抗病毒剂
公开(公告)号：EP1991533A1
公开(公告)日：2008-11-19
申请号：EP06794697.0
申请日：2006-10-09
申请人： Arrow Therapeutics Limited
发明人： MATHEWS, Neil , THOMAS, Alexander, James, Floyd , SPENCER, Keith, Charles , DENNISON, Helena , BARNES, Michael, Christopher , CHANA, Surinder, Singh , JENNENS, Lyn , PILKINGTON, Christopher, John
IPC分类号： C07D239/94 , A61K31/517 , A61P31/14
CPC分类号： C07D239/94
摘要： Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses (Ia), wherein R1 and R2 are the same or different and represent hydrogen, halogen, -L-O-R3, -L-O-L-A or -L-O-L´-A´, wherein each L is the same or different and represents a direct bond or a C1-C4 alkylene group; L´ represents a direct bond or a C2-C4 alkylene group; R3 represents hydrogen, C1-C4 alkyl or C1-C4 haloalkyl; A represents a 5- to 10-membered heterocyclyl group; and A´ represents a C6-C1 aryl group; wherein at least one of R1 and R2 is -L-O-R3, -L-O-L-A or -L-O-L´-A´.

4. 发明公开

EP1727550A1 PHARMACEUTICAL COMPOSITION COMPRISING A BENZODIAZEPINE DERIVATIVE AND AN INHIBITOR OF THE RSV FUSION PROTEIN 有权
标题翻译： WITH A苯并二氮杂衍生物和药物组合物中的RSV融合蛋白的抑制剂
公开(公告)号：EP1727550A1
公开(公告)日：2006-12-06
申请号：EP05718061.4
申请日：2005-03-18
申请人： Arrow Therapeutics Limited
发明人： POWELL, Kenneth, Arrow Therapeutics Limited , KELSEY, Richard, Arrow Therapeutics Limited , CARTER, Malcolm, Arrow Therapeutics Limited , ALBER, Dagmar, Arrow Therapeutics Limited , WILSON, Lara, Arrow Therapeutics Limited , HENDERSON, Elisa, Arrow Therapeutics Limited , CHAMBERS, Phil, Arrow Therapeutics Limited , TAYLOR, Debra, Arrow Therapeutics Limited , TYMS, Stan, Arrow Therapeutics Limited , DOWDELL, Verity, Arrow Therapeutics Limited
IPC分类号： A61K31/5513
CPC分类号： A61K45/06 , A61K31/5513 , A61K2300/00
摘要： A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.

5. 发明公开

EP1520020A2 TRANSPOSON 审中-公开
标题翻译：转座子
公开(公告)号：EP1520020A2
公开(公告)日：2005-04-06
申请号：EP03743429.7
申请日：2003-03-05
申请人： Arrow Therapeutics Limited
发明人： MASKELL, Duncan J.,Centre for Veterinary Science , CHARLES, Ian, George , ALLEN, Andy , OWEN, Paul
IPC分类号： C12N15/10 , C12N15/90 , C12Q1/68 , C12Q1/70 , C12N1/21 , A61K39/02
CPC分类号： C12N15/1082 , C12N15/90
摘要： A transposon which comprises an RNA polymerase recognition site and a homing endonuclease recognition site. The transposon may be used in methods for the identification of an essential gene or a conditional essential gene of an organism. Genes identified in such methods are useful as substrates for use in screening for antibacterials, antiparasitics, fungicides, pesticides and herbicides.

6. 发明公开

EP1370669A2 METHOD FOR HOMOLOGOUS RECOMBINATION USING THE GENES BET AND EXO, BUT NOT GAM, OF THE LAMBDA RECOMBINATION SYSTEM 审中-公开
标题翻译：和方法同源重组拉姆达重组BET的基因EXO但不GAM
公开(公告)号：EP1370669A2
公开(公告)日：2003-12-17
申请号：EP02753587.1
申请日：2002-03-18
申请人： Arrow Therapeutics Limited
发明人： CHARLES, Ian George , WHEELER, Kerry
IPC分类号： C12N15/90
CPC分类号： C12N15/102 , A61K2039/522 , Y02A50/484
摘要： A method for replacing a target nucleotide/polynucleotide sequence of a bacterial chromosome with a different nucleotide/polynucleotide sequence, which method comprises: (a) providing a bacterium which is capable of expressing: (1) the gamma genes exo or a functional equivalent thereof and bet or a functional equivalent thereof, but not the gamma gene gam or a functional equivalent thereof; or (2) the gamma gene bet or a functional equivalent thereof and gam or a functional equivalent thereof; (b) providing a polynucleotide construct which comprises: (i) a sequence which corresponds to a first sequence flanking the left hand side of the target sequence; (ii) a second sequence corresponding to a sequence flanking the right hand side of the target sequence; and (iii) positioned between (i) and (ii), the donor sequence; and (c) introducing the polynucleotide construct into the bacterium, thereby to replace the target nucleotide sequence with the sequence different from that of the target nucleotide sequences. The method can be used in the preparation of attenuated bacteria and in the identification of essential genes.

7. 发明公开

EP1218540A2 TRANSPOSON MEDIATED DIFFERENTIAL HYBRIDISATION 审中-公开
标题翻译：转座子介导的差异杂交
公开(公告)号：EP1218540A2
公开(公告)日：2002-07-03
申请号：EP00951684.0
申请日：2000-07-26
申请人： Arrow Therapeutics Limited
发明人： CHARLES, Ian George,Arrow Therapeutics Limited , MASKELL, Duncan John,University of Cambridge
IPC分类号： C12Q1/68 , C12N15/10
CPC分类号： C12Q1/6809 , C12N15/1082
摘要： A method for identifying an essential gene of an organism comprises: (i) providing a library of transposon mutants of the said organism; (ii) isolating polynucleotide sequences from the library which flank inserted transposons; (iii) hybridising the said polynucleotide sequences with a polynucleotide library from the said organism; and (iv) identifying a polynucleotide in the said polynucleotide library to which the said polynucleotide sequences do not hybridise, thereby to determine an essential gene of the organism.

8. 发明授权

EP1981876B1 TRIAZOLOANILINOPYRIMIDINE DERIVATIVES FOR USE AS ANTIVIRAL AGENTS 有权
标题翻译：用作抗病毒剂的三唑并茴酰胺嘧啶衍生物
公开(公告)号：EP1981876B1
公开(公告)日：2011-05-04
申请号：EP07704895.7
申请日：2007-01-11
申请人： Arrow Therapeutics Limited
发明人： MATHEWS, Neil , THOMAS, Alexander, James, Floyd , SPENCER, Keith, Charles , TIBERGHIEN, Nathalie , PILKINGTON, Christopher, John , JENNENS, Lyn , CHANA, Surinder , FRASER, Ian, John
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , A61K31/505 , A61P31/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14
摘要： A quinazoline derivative of formula (I), or a pharmaceutically acceptable salt thereof: formula (I) for use in treatment of prevention of a flaviviridae infection.
摘要翻译：式（I）的喹唑啉衍生物或其药学上可接受的盐：式（I）用于治疗黄病毒科感染的预防。

9. 发明公开

EP1981876A1 TRIAZOLOANILINOPYRIMIDINE DERIVATIVES FOR USE AS ANTIVIRAL AGENTS 有权
标题翻译： TRIAZOLOANILINOPYRIMIDINDERIVATE FOR USE作为抗病毒剂
公开(公告)号：EP1981876A1
公开(公告)日：2008-10-22
申请号：EP07704895.7
申请日：2007-01-11
申请人： Arrow Therapeutics Limited
发明人： MATHEWS, Neil , THOMAS, Alexander, James, Floyd , SPENCER, Keith, Charles , TIBERGHIEN, Nathalie , PILKINGTON, Christopher, John , JENNENS, Lyn , CHANA, Surinder , FRASER, Ian, John
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , A61K31/505 , A61P31/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14
摘要： A quinazoline derivative of formula (I), or a pharmaceutically acceptable salt thereof: formula (I) for use in treatment of prevention of a flaviviridae infection.

10. 发明公开

EP1928465A1 BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION 审中-公开
标题翻译：苯二氮类衍生物感染了丙型肝炎于治疗
公开(公告)号：EP1928465A1
公开(公告)日：2008-06-11
申请号：EP05784102.5
申请日：2005-09-19
申请人： Arrow Therapeutics Limited
发明人： DENNISON, Helena , WARNE, Justin , SPENCER, Keith , COCKERILL, George , LUMLEY, James
IPC分类号： A61K31/5513 , C07D243/24 , A61P31/14
CPC分类号： C07D243/24 , A61K31/5513
摘要： Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: - R1 represents C1-6 alkyl, aryl or heteroaryl; - R2 represents hydrogen or C1-6 alkyl; - each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, -CO2R', -CONR'R', -NH-C0-R', -S(O)R', -S(O)2R', -NH-S(O)2R', -S(O)NR'R' or -S(O)2NR'R', wherein each R' and R' is the same or different and represents hydrogen or C1-6 alkyl; - n is from 0 to 3; - R4 represents hydrogen or C1-6 alkyl; - R5 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, aryl-C(O)-C(O)-, heteroaryl-C(O)-C(O)-, carbocyclyl-C(O)-C(O)-, heterocyclyl-C(O)-C(O)- or -XR6; - X represents -CO-, -S(O)- or -S(O)2-; and - R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 alkyl)-O-, heteroaryl-(C1-6 alkyl)-O-, carbocyclyl-(C1-6 alkyl)-O-, heterocyclyl-(C1-6 alkyl)-O- or -NR'R' wherein each R' and R' is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

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