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    • 8. 发明申请
    • 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS
    • 4-(4-吡啶基) - 苯甲酸酯及其作为岩石活性调节剂的用途
    • WO2009027392A1
    • 2009-03-05
    • PCT/EP2008/061135
    • 2008-08-26
    • ABBOTT GMBH & CO. KGMACK, HelmutTEUSCH, NicoleMÜLLER, Bernhard K.HORNBERGER, WilfriedJARVIS, Michael F.SAUER, Daryl
    • MACK, HelmutTEUSCH, NicoleMÜLLER, Bernhard K.HORNBERGER, WilfriedJARVIS, Michael F.SAUER, Daryl
    • C07D213/56C07D401/12C07D405/12C07D413/12C07D417/12A61K31/44A61K31/4427A61P9/00A61P25/00A61P35/00A61P29/00
    • C07D401/12C07D213/56C07D405/12C07D409/12C07D413/12C07D413/14C07D417/12
    • The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R 1 and R 2 are, independently of each other, hydrogen, hydroxy, cyano, C 1 -C 8 -alkyl, C 1 - C 8 -haloalkyl, C 1 -C 8 -alkoxy or C 1 -C 8 -haloalkoxy; R 3 , R 4 , R 5 and R 6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy, amino, C 1 -C 8 -alkylamino or di-(C 1 -C 8 -alkyl)-amino; R 7 is hydrogen, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, aryl or aryl-C 1 -C 8 -alkyl; R 8 is a group of the formula -X-W, where X is a single bond, C 1 -C 4 -alkylene or C 1 -C 4 -alkylene-O-, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R 9 is a group of the formula -Y-Z, where Z is hydrogen, halogen, OR 11 , NR 12 R 13 , S(O) m -R 14 , phenyl which may carry 1, 2, 3 or 4 substituents R 15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C 1 C 4 -alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.
    • 本发明涉及式(I)的新型4-(4-吡啶基) - 苯甲酰胺。 化合物I具有有价值的治疗特性,特别适用于治疗对Rho激酶(ROCK)的调节作用的疾病。 R 1和R 2彼此独立地为氢,羟基,氰基,C 1 -C 8 - 烷基,C 1 -C 8 - 卤代烷基,C 1 -C 8 - 烷氧基或C 1 -C 8 - 卤代烷氧基; R3,R4,R5和R6彼此独立地为氢,羟基,卤素,氰基,C1-C8-烷基,C1-C8-卤代烷基,C1-C8-烷氧基,C1-C8-卤代烷氧基,氨基,C1- C 8 - 烷基氨基或二 - (C 1 -C 8 - 烷基) - 氨基; R 7是氢,C 1 -C 8 - 烷基,C 1 -C 8 - 卤代烷基,芳基或芳基-C 1 -C 8 - 烷基; R8是式-XW的基团,其中X是单键,C1-C4-亚烷基或C1-C4-亚烷基-O-,其中三个最后提及的基团中的亚烷基可以是直链或支链的,并且可以 部分或完全卤化和/或可以被羟基取代和/或可被氧原子中断; 并且W是选自苯基和5-或6-元饱和,部分不饱和或芳族杂环的环状基团,其含有作为环成员1,2或3的选自O,S和N的杂原子和任选的1或2个羰基 ; R9是式-YZ的基团,其中Z是氢,卤素,OR11,NR12R13,S(O)m -R14,可以携带1,2,3或4个取代基R15或5-或6-元的苯基 饱和,部分不饱和或芳族杂环; Y是可部分或完全卤化和/或可被羟基和/或苯环取代的直链或支链C 1 -C 4亚烷基; 或者Z为苯基或上述5-或6-元杂环的情况下,Y也可以是单键。
    • 9. 发明申请
    • A SELF CLEANING PILL COUNTING DEVICE, AND CLEANING METHOD
    • 自清洁药丸计数装置和清洁方法
    • WO2008040124A1
    • 2008-04-10
    • PCT/CA2007/001760
    • 2007-10-02
    • TRAMAR PRODUCTSFAY, BrentJARVIS, Michael
    • FAY, BrentJARVIS, Michael
    • A61J7/02
    • A61J7/02B08B5/02B08B5/04B08B9/00B24C1/003
    • A pills counting device provided with cleaning means and comprising in combination, a tray comprising: a base member having an upper surface for receiving a bulk quantity of pills; a trough member alongside the base member and provided with a depression having opposite ends and at least one surface for receiving a load of a counted quantity of pills from said bulk quantity, one of said opposite ends further defining a spout for the unloading said counted quantity of pills in a pills container, a lid member having a lower surface, said lid member being mounted on the base member and being movable between two extreme positions, that is: a first position where the lower surface of the lid member is away from the upper surface of the base member and the surface of the depression of the trough member; a second position where the lower surface of the lid member is close and above the upper surface of the base member and the surface of the depression of the trough member to thereby create a cavity; at least one port provided in the tray and/or in the lid member and adapted to be connected in fluid communication with the cavity and with an air intake of a vacuum device that can be remotely controlled; being understood that when the lid is in the second position and a vacuum is applied to said at least one port, an air stream is established between said surfaces to entrain toward the vacuum device particles that may be present on said surfaces to clean said surfaces. A cleaning method using aforesaid pills counting device.
    • 一种具有清洁装置并且包括组合的药丸计数装置,其包括:基部构件,具有用于接收大量药丸的上表面; 槽底部件,与底座部件一起设置,并设置有具有相对端部的凹部和至少一个表面,用于从所述批量接收计数量的药丸的载荷,所述相对端部中的一个还限定用于卸载所述计数量的喷口 在药丸容器中的药丸,具有下表面的盖构件,所述盖构件安装在基座构件上并且可在两个极限位置之间移动,即,第一位置,其中盖构件的下表面远离 基部构件的上表面和槽构件的凹部的表面; 第二位置,其中盖构件的下表面靠近并且在基部构件的上表面和槽构件的凹部的表面之上,从而形成空腔; 设置在所述托盘和/或所述盖构件中的至少一个端口,并且适于与所述空腔流体连通并与可远程控制的真空装置的进气口连接; 应当理解,当盖处于第二位置并且对所述至少一个端口施加真空时,在所述表面之间建立空气流以夹带可能存在于所述表面上的真空装置颗粒以清洁所述表面。 使用上述药丸计数装置的清洁方法。