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    • 52. 发明申请
    • SUBSTITUTED BENAMIDINES AS ANTIBACTERIAL AGENTS
    • 取代的抗生素作为抗菌剂
    • WO2009040507A1
    • 2009-04-02
    • PCT/GB2008/003208
    • 2008-09-22
    • PROLYSIS LTDHAYDON, David, JohnCOLLINS, IanCZAPLEWSKI, Lloyd, George
    • HAYDON, David, JohnCOLLINS, IanCZAPLEWSKI, Lloyd, George
    • A61P31/04A61K31/4245A61K31/427A61K31/429A61K31/433C07D285/08C07D271/06C07D277/34C07D277/64
    • C07D277/34A61K31/4245A61K31/427A61K31/429A61K31/433C07D271/07C07D277/64C07D285/08C07D417/12
    • Compounds of formula (IA) or (IB) have antibacterial activity : wherein W is =C(H)- or =N-; R 3 is a radical of formula -(Alk 1 ) m -(Z 1 ) p -(Alk 2 ) n -Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z1 is -O-, -S-, -S(O)-, -S(O 2 )-, -NH-, -N(CH 3 )-, -N(CH 2 CH 3 )-, -C(-O)-, -0-(C=O)-, -C(=O)-O-, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; AIk 1 and AIk 2 are optionally substituted C 1 -C 6 alkylene, C 2 -C 6 alkenylene, or C 2 -C 6 alkynylene radicals, which may optionally terminate with or be interrupted by -O-, -S-, -S(O)-, -S(O 2 )-, -NH-, -N(CH 3 )-, Or -N(CH 2 CH 3 )-; and Q is hydrogen, halogen, nitrile, or hydroxyl, or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; R 4 and R 5 are optional substituents; and R 2 , R 6 and R 7 are independently hydrogen or a radical of formula -(Alk 3 ) x - (Z 2 )y-(Alk 4 ) z -H wherein x, y and z are independently 0 or 1, Z 2 is -O-, -S-, -S(O)-, -S(O 2 )-, - NH-, -N(CH 3 )-, -N(CH 2 CH 3 )-, -C(-O)-, -0-(C=O)- or -C(=O)-O-; AIk 3 and AIk 4 are optionally substituted C 1 -C 3 alkylene, C 2 -C 3 alkenylene, or C 2 -C 3 alkynylene radicals, which may optionally terminate with or be interrupted by -O-, -S-, -S(O)-, -S(O 2 )-, -NH-, -N(CH 3 )-, or - N(CH 2 CH 3 )-.
    • 式(IA)或(IB)的化合物具有抗菌活性:其中W为= C(H) - 或= N-; R3是式 - (Alk1)m-(Z1)p-(Alk2)nQ的基团,其中m,p和n独立地为0或1,条件是m,p和n中的至少一个为1, (O) - , - S(O 2) - , - NH - , - N(CH 3) - , - N(CH 2 CH 3) - , - (C = O) - , - C(= O)-O-,或具有3至6个环原子的任选取代的二价单环碳环或杂环基; 或具有5至10个环原子的任选取代的二价双环碳环或杂环基; Alk1和Alk2是任选取代的C 1 -C 6亚烷基,C 2 -C 6亚烯基或C 2 -C 6亚炔基,其可以任选地被-O - , - S - , - S(O) - , - S( O,-N(CH 3) - 或 - N(CH 2 CH 3) - ; Q为氢,卤素,腈或羟基,或任选取代的具有3至6个环原子的单环碳环或杂环基; 或具有5至10个环原子的任选取代的双环碳环或杂环基; R4和R5是任选的取代基; 并且R2,R6和R7独立地为氢或式 - (Alk3)x-(Z2)y-(Alk4)zH的基团,其中x,y和z独立地为0或1,Z2为-O - , - S- , - (O) - , - S(O 2) - , - NH-, - N(CH 3) - , - N(CH 2 CH 3) - , - 或-C(= O)-O-; Alk3和Alk4是任选取代的C 1 -C 3亚烷基,C 2 -C 3亚烯基或C 2 -C 3亚炔基,其可以任选地被-O - , - S - , - S(O) - , - S( O,-N(CH 3) - 或-N(CH 2 CH 3) - 。
    • 53. 发明申请
    • ANTIBACTERIAL AGENTS
    • 抗菌剂
    • WO2009037485A1
    • 2009-03-26
    • PCT/GB2008/003200
    • 2008-09-22
    • PROLYSIS LTDHAYDON, David, JohnCOLLINS, IanCZAPLEWSKI, Lloyd, George
    • HAYDON, David, JohnCOLLINS, IanCZAPLEWSKI, Lloyd, George
    • C07D285/08A61K31/433A61P33/00
    • C07D285/08
    • Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is =CH- or =N-; Ri and R2 are independently selected from hydrogen, fluoro and chloro, provided that Ri and R2 are not each hydrogen when W is =CH-; n is 0 or 1; X is -O-, -S-, or -CH 2 -; and Q is (i) a phenyl radical, a naphthyl radical, a monocyclic carbocyclic or heteroaryl radical having 3 to 6 ring atoms, or a bicyclic heteroaryl radical having 5 to 10 ring atoms, any of which radicals being optionally substituted; or (ii) an optionally substituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl, or C 2 -C 6 alkynyl radical, which may optionally be interrupted by -O-, -S-, -S(O)-, -S(O 2 )-, -NH-, -N(CH 3 )-, -N(CH 2 CH 3 )-, - C-K=Oh or -C(=O)-O-.
    • 式(IA)或(IB)的化合物具有抗菌活性:其中W为= CH-或= N-; R 1和R 2独立地选自氢,氟和氯,条件是当W = CH-时,R 1和R 2不是氢。 n为0或1; X是-O - , - S-或-CH 2 - ; Q为(i)具有3〜6个环原子的苯基,萘基,单环碳环或杂芳基,或环原子数为5〜10的双环杂芳基,其中任意一个为任选被取代的基团; 或(ⅱ)任选被-O - , - S - , - S(O) - , - S(O 2))间隔的任选取代的C 1 -C 6烷基,C 2 -C 6烯基或C 2 -C 6炔基, - , - NH - , - N(CH 3) - , - N(CH 2 CH 3) - , - CK =噢或-C(= O)-O-。
    • 56. 发明申请
    • EMULATION COMPONENT FOR DATA BACKUP APPLICATIONS
    • 用于数据备份应用的仿真组件
    • WO2007041849A1
    • 2007-04-19
    • PCT/CA2006/001670
    • 2006-10-12
    • STORAGE APPLIANCE CORPORATIONCOLLINS, IanLI, EricCHOWDHARY, YousufBRUNET, Jeffrey
    • COLLINS, IanLI, EricCHOWDHARY, YousufBRUNET, Jeffrey
    • G06F9/455G06F12/16
    • G06F3/065G06F3/0605G06F3/0632G06F3/0676G06F3/0677G06F11/1451G06F11/1458G06F11/1461
    • An emulation component for a data backup system is provided. The emulation component represents a storage device, such as a flash memory device or a partition of a disk drive, as if it were an auto-launch device, that will trigger applications to execute automatically. Accordingly, other computing systems, such as personal computers, interact with the storage device, through the emulation component, as if the storage device were the auto-launch device. Because the emulation component makes this representation, merely connecting the emulation component between the storage device and the computing system can cause a backup application stored on the storage device to automatically execute on the computing system. A data backup appliance including an emulation component and a storage device is also provided. The backup system can also include an interface for connecting another removable device, such as a disk drive, for storing backup content from the data source.
    • 提供了一种用于数据备份系统的仿真组件。 仿真组件表示存储设备,例如闪存设备或磁盘驱动器的分区,就像它是自动启动设备一样,将触发应用程序自动执行。 因此,诸如个人计算机的其他计算系统通过仿真组件与存储设备交互,就像存储设备是自动发射设备一样。 由于仿真组件做出这种表示,只需将存储设备和计算系统之间的仿真组件连接起来就可以使存储在存储设备上的备份应用程序在计算系统上自动执行。 还提供了包括仿真组件和存储设备的数据备份设备。 备份系统还可以包括用于连接另一个可移动设备(如磁盘驱动器)的接口,用于从数据源存储备份内容。
    • 59. 发明申请
    • PYRIMIDOTHIOPHENE COMPOUNDS HAVING HSP90 INHIBITORY ACTIVITY
    • 具有HSP90抑制活性的吡咯烷酮化合物
    • WO2006079789A1
    • 2006-08-03
    • PCT/GB2006/000219
    • 2006-01-23
    • VERNALIS R & D LTDCANCER RESEARCH TECHNOLOGY LTDTHE INSTITUTE OF CANCER RESEARCHMATTHEWS, Thomas, PeterCHEUNG, Kwai, MingCOLLINS, IanMCDONALD, EdwardBROUGH, Paul, AndrewDRYSDALE, Martin, James
    • MATTHEWS, Thomas, PeterCHEUNG, Kwai, MingCOLLINS, IanMCDONALD, EdwardBROUGH, Paul, AndrewDRYSDALE, Martin, James
    • C07D495/04A61K31/519A61P35/00
    • C07D495/04
    • Compounds of formula (I) are HSP90 inhibitors, of utility in the treatment of, for example, cancers: wherein R 1 is -(Alk 1 ) p -(Z)r(Alk 2 ) s -Q wherein AIk 1 and AIk 2 are optionally substituted divalent C 1 C 3 alkylene or C 2 -C 3 alkenylene radicals, p, r and s are independently 0 or 1 , Z is -O-, -S-, -(C=O)-, -(C=S)-, -SO 2 -, -C(=O)O-, -C(=O)NR A , -C(=S)NRA-, -SO 2 NR A -NR A C(=O)-, -NR A SO 2 - or -NR A - wherein R A is hydrogen or C 1 -C 6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is optionally substituted aryl or heteroaryl; R 3 is hydrogen, an optional substituent, or an optionally substituted (C 1 -C- 6 )alkyl, aryl or heteroaryl radical; and R 4 is (i) a carboxylic ester, carboxamide or sulfonamide group, or (ii) a -CN group, or (iii) an optionally substituted C 1 -C 6 alkyl, aryl, heteroaryl, aryl(C 1 -C 6 alkyl)-, or heteroaryl(C 1 -C 6 alkyl)- group, or (iv) a group of formula -C(=O)R 5 wherein R 5 is hydroxyl, optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C 1 -C 6 alkyl)-, aryl(C 1 -C 6 alkoxy)-, heteroaryl(C 1 -C 6 alkyl)-, or heteroaryl(C 1 -C- 6 alkoxy)-, or (v) a group of formula -C(=O)NHR 6 wherein R 6 is primary, secondary, tertiary or cyclic amino, or hydroxyl, optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C 1 -C 6 alkyl)-, aryl(C 1 -C 6 alkoxy)-, heteroaryl(C 1 -C 6 alkyl)-, or heteroaryKC 1 -C 6 aikoxy)-.
    • 式(I)化合物是HSP90抑制剂,其可用于治疗例如癌症:其中R 1是 - (Alk 1)p < /(Z)r(Alk 2)其中Alk 1和Alk 2是 任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烷基,p,r和s 独立地是0或1,Z是-O - , - S - , - (C = O) - , - (C = S) - , - SO 2 - , - C(= O) O-,-C(= O)NR A,-C(= S)NRA,-SO 2 NR A, C(= O) - , - NR S - SO 2 - 或-NR A - 其中R 0 A是氢或C 1 -C 6烷基,Q是氢或任选取代的碳环或杂环基; R 2是任选取代的芳基或杂芳基; R 3是氢,任选的取代基或任选取代的(C 1 -C 6 -C 6 - )烷基,芳基或杂芳基; 和R 4是(i)羧酸酯,羧酰胺或磺酰胺基,或(ii)-CN基,或(iii)任选取代的C 1 -C 烷基,芳基,杂芳基,芳基(C 1 -C 6 -C 6烷基) - 或杂芳基(C 1 -C 12 - -C(= O)R 5,其中R 5是(C 1 -C 6)烷基) - ,或(iv)式-C 羟基,任选取代的C 1 -C 6烷基,C 1 -C 6烷氧基,芳基,芳氧基, 杂芳基,杂芳氧基,芳基(C 1 -C 6烷基) - ,芳基(C 1 -C 6 - 烷氧基) - ,杂芳基(C 1 -C 6烷基) - 或杂芳基(C 1 -C 6 - 其中R 6为伯,仲,叔或环状氨基,或(v)式-C(= O)NHR 6基团,其中R 6为伯,仲,叔或环状氨基,或 羟基,任选取代的C 1 -C 6烷基,C 1 -C 6烷氧基,芳基,芳氧基, 杂芳基,杂芳氧基,芳基(C 1 -C 6烷基) - ,芳基(C 1 -C 6烷氧基) - ,杂芳基(C 1 -C 6烷基) - 或杂芳基K > 1 -C 6 烷氧基) - 。