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    • 35. 发明授权
    • 3-(arylalkyl) xanthines
    • 3-(芳烷基)黄嘌呤
    • US06248746B1
    • 2001-06-19
    • US09227057
    • 1999-01-07
    • Mark ChasinDavid J. CavallaPeter Hofer
    • Mark ChasinDavid J. CavallaPeter Hofer
    • A61K3152
    • A61K31/522C07D473/04C07D473/06
    • With the above and other objects in view, the present invention comprises compounds having the general formula (I): wherein: R1 is a C2-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl or cycloalkynyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl or cycloalkynyl is optionally substituted with hydroxy, C1-5 alkoxy, C3-5 cycloalkoxy, halogen, oxo, carbamido, hydroxycarbamido, oximido, C1-5 alkyloximido, C3-5 cycloalkyloximido, C1-5 acyloximido or C3-5 cycloacyloximido; Q is methylene or ethylene; R3 is aryl or heteroaryl wherein said aryl or heteroaryl has one to three substituents selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, cycloalkynyl, C3-5 alkylene, C3-5 cycloalkylene, haloC1-6 alkyl, haloC1-6 cycloalkyl, hydroxy, C1-5 alkoxy, C3-5 cycloalkoxy, C1-2 alkylenedioxy, C1-6 acyl, C3-6 cycloacyl, C1-6 acyloxy, C3-6 cycloacyloxy, halogen, nitro or cyano; R8 is C1-5 alkyl or C3-5 cycloalkyl, optionally substituted by hydroxy, C1-5 alkyloxy, C3-5 cycloalkyloxy, C1-5 acyloxy, C3-5 cycloacyloxy or halogen; and methods of using the compounds of formula I for treatment of patients who can benefit from a modification of PDE IV levels in their bodies.
    • 考虑到上述和其它目的,本发明包括具有通式(I)的化合物:其中:R 1是C 2-8烷基,C 2-8烯基,C 2-8炔基,C 3-8环烷基,C 3-8 环烯基或环炔基,其中所述烷基,烯基,炔基,环烷基,环烯基或环炔基任选被羟基,C 1-5烷氧基,C 3-5环烷氧基,卤素,氧代,氨基甲酰基,羟基氨基甲酰基,肟基,C 1-5烷基酰氧基, 5环烷酰肟基,C1-5酰氧亚氨基或C3-5环亚胺酰脒; Q是亚甲基或亚乙基; R 3是芳基或杂芳基,其中所述芳基或杂芳基具有一至三个选自C 1-6烷基,C 2-6烯基, C2-6炔基,C3-6环烷基,C3-6环烯基,环炔基,C3-5亚烷基,C3-5亚环烷基,卤代C 1-6烷基,卤代C 1-6环烷基,羟基,C 1-5烷氧基,C 3-5环烷氧基,C 1 -2亚烷基二氧基,C1-6酰基,C3-6环酰基,C1-6酰氧基,C3-6环酰氧基,卤素,硝基或氰基; R8是C1-5烷基或C3-5环 任选地被羟基,C 1-5烷氧基,C 3-5烃环氧基,C 1-5酰氧基,C 3-5环芳氧基或卤素取代的烷基;以及使用式I化合物治疗可从PDE修饰中受益的患者的方法 IV级别在他们的身体。
    • 39. 发明授权
    • Apparatus for singularizing stacked portions of books and the like
    • 用于将书籍的堆叠部分单数化的装置等
    • US5026250A
    • 1991-06-25
    • US462810
    • 1990-01-10
    • Peter Hofer
    • Peter Hofer
    • B65H1/30B65G59/06B65H3/24B65H3/56
    • B65G59/068
    • Apparatus for singularizing successive stacks of a series of stacks consisting of superimposed groups of sheets has a transporting unit which advances successive stacks of the series in a horizontal plane against a barrier which intercepts each but the lowermost group of the oncoming stack. An endless conveyor with one or more pushers is provided to advance successive lowermost groups of an intercepted stack through and beyond a clearance between the barrier and a stationary table of the transporting unit. The width of such clearance exceeds the height of a single group but is less than the combined height of two superimposed groups. The width of the clearance and the extent to which the pusher or pushers can extend above the horizontal plane are adjustable. The apparatus further comprises a gate which is pivotable behind an intercepted stack to a position in which it prevents advancement of a fresh stack toward the table and can bias each but the lowermost group of an intercepted stack against the barrier, and a raised position in which the conveyor of the transporting unit is free to deliver a fresh stack toward and into engagement with the barrier. The barrier is adjustable toward and away from the gate.
    • 用于将由叠加的片组组成的一系列堆叠的连续堆叠单个化的装置具有传送单元,该传送单元将水平平面中的串联的连续堆叠抵靠拦截即将到来的堆叠中的每个但最下面的组的屏障。 提供具有一个或多个推动器的环形传送带,用于使所拦截的堆叠的连续最下面的组通过并超过所述屏障和所述传送单元的静止台之间的间隙。 这种间隙的宽度超过单个组的高度,但小于两个重叠组的组合高度。 间隙的宽度以及推动器或推动器可以在水平面上方延伸的程度是可调节的。 该装置还包括一个门,该门可以在被拦截的堆叠之后枢转到一个位置,在该位置,防止一个新的堆栈朝向桌子前进,并且可以将拦截的堆叠的每个而不是最低的一组抵靠着屏障偏置, 输送单元的输送机可自由地向隔板输送一个新的叠层并与该屏障接合。 屏障可以朝向和远离门调节。
    • 40. 发明授权
    • 6-thioxanthines
    • 6-硫代黄嘌呤
    • US4925847A
    • 1990-05-15
    • US78545
    • 1987-07-28
    • Peter Hofer
    • Peter Hofer
    • A61K31/52A61K31/522A61P11/08C07D473/22
    • C07D473/22
    • A 6-thioxanthine of general formula I or a pharmaceutically acceptable salt thereof ##STR1## wherein R.sub.3 is a C.sub.2 to C.sub.6 alkyl, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group and R.sub.8 is a C.sub.1 to C.sub.6 alkyl, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group provided that when R.sub.3 is an ethyl, n-propyl or n-butyl group, R.sub.8 is a C.sub.3 to C.sub.6 alkyl, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group.These 3,8-disubstituted-6-thioxanthines have enhanced bronchodilator activity.
    • 通式I的6-硫代黄嘌呤或其药学上可接受的盐,其中R 3为C 2至C 6烷基,C 3至C 7环烷基或C 4至C 8环烷基烷基,R 8为C 1至C 6烷基, C3至C7环烷基或C4至C8环烷基烷基,条件是当R3为乙基,正丙基或正丁基时,R 8为C 3至C 6烷基,C 3至C 7环烷基或C 4至C 8环烷基烷基 。 这些3,8-二取代-6-硫代黄嘌呤具有增强的支气管扩张剂活性。