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    • 61. 发明授权
    • Pyrazine compounds
    • 吡嗪化合物
    • US06599905B2
    • 2003-07-29
    • US09855703
    • 2001-05-16
    • Brian CoxDean David EdneyMichael Simon LoftMalcolm Stuart NobbsGita Punjabhai Shah
    • Brian CoxDean David EdneyMichael Simon LoftMalcolm Stuart NobbsGita Punjabhai Shah
    • A61K314965
    • C07D241/20C07D241/26
    • Compounds of formula (I) where R1 is phenyl substituted by one or more halogen atoms, naphthyl and naphthyl substituted by one or more halogen atoms; R2 is —NH2 and —NHC(═O)Ra; R3 is —NRbRc, —NHC(═O)Ra or hydrogen; R4 is hydrogen, —C1-4 alkyl, —CN, —CH2OH, —CH2ORd, —CH2S(O)xRd and —C1-4 alkyl substituted by one or more halogen atoms in which Ra represents C1-4 alkyl or C3-7cycloalkyl, and Rb and Rc, which may be the same or different, are hydrogen or C1-4 alkyl, or together with the nitrogen atom to which they are attached, form a 6-membered nitrogen containing heterocycle, which heterocycle can be further substituted with one or more C1-4 alkyl; Rd is C1-4 alkyl or C1-4 alkyl substituted by one or more halogen atoms; x is an integer zero, one or two; and salts, solvates and prodrugs thereof, provided that R1 does not represent: when R2 is —NH2, and both R3 and R4 are hydrogen. The compounds are useful as analgesics, anticonvulsants, for treating bipolar disorder and as neuroprotectants.
    • 其中R1是被一个或多个卤素原子取代的苯基,萘基和被一个或多个卤原子取代的萘基的式(I)化合物; R2是-NH2,-NHC(= O)Ra; R3是-NRbRc,-NHC(= O)Ra或氢; R 4是氢,-C 1-4烷基,-CN,-CH 2 OH,-CH 2 OR d,-CH 2 S(O)x R d和被一个或多个卤素原子取代的-C 1-4烷基,其中R a表示C 1-4烷基或C 3-7环烷基 ,Rb和Rc可以相同或不同,为氢或C 1-4烷基,或与它们所连接的氮原子一起形成6元含氮杂环,该杂环可进一步被 一个或多个C 1-4烷基; Rd是被一个或多个卤素原子取代的C 1-4烷基或C 1-4烷基; x是整数零,一或二; 其盐,溶剂合物和前药,条件是R 1不表示:当R 2为-NH 2时,R 3和R 4均为氢。 该化合物可用作止痛剂,抗惊厥药,用于治疗双相性精神障碍和作为神经保护剂。
    • 64. 发明授权
    • Urinary incontinence device
    • 尿失禁装置
    • US06461340B1
    • 2002-10-08
    • US09638255
    • 2000-08-14
    • Jay LenkerRobert RosenbluthBrian CoxGeorge R. Greene
    • Jay LenkerRobert RosenbluthBrian CoxGeorge R. Greene
    • A61F1320
    • A61F13/471A61F2/0009A61F2/0054A61F5/4401A61F5/48A61F13/47209A61F13/82Y10S128/25
    • A device for managing urinary incontinence comprises a resilient body that engages the external genitalia and sealingly occludes the urethral meatus. In female embodiments, the body fits between the labia minora and the floor of the vulval vestibule, occluding the meatus. An adhesive on the body provides a sealing engagement with the meatus. In a first female embodiment, the body has a base with an adhesive layer that seats against the vestibule floor. A pair of flexible, lateral flaps engage the labia minora. A layer of super-absorbent material may be situated between the base and the adhesive layer, and/or a layer of scrim material may be so situated. The body may have a longitudinal ridge with a posterior edge having a finger hole to facilitate installation and removal of the device. In a second female embodiment, the body is substantially tubular, with the adhesive on the exterior surface of the body. In a third female embodiment, the body is an elastomeric bladder, filled with a liquid or gel, that conformingly fits between the labia minora and the vestibule floor so as to occlude the meatus. The exterior surface of the bladder is coated with an adhesive to sealingly occlude the meatus. In male embodiments, the device includes a resilient pad with adhesive on one surface. The pad conforms to and adhesively attaches to the penile glans, with the adhesive sealingly occluding the meatus. Securing tabs may be provided to adhere to the glans or the penile shaft.
    • 用于管理尿失禁的装置包括与外生殖器接合并密封地封闭尿道口的弹性体。 在女性实施例中,身体适合于阴唇小阴唇和外阴前庭的地板之间,阻塞肠道。 身体上的粘合剂提供与口腔的密封接合。 在第一女性实施例中,身体具有基部,其具有抵靠前庭地板的粘合剂层。 一对柔软的外侧襟翼与小阴唇接触。 一层超吸收材料可以位于基底和粘合剂层之间,和/或一层稀松布材料可以如此定位。 主体可以具有纵向脊,其后边缘具有指孔,以便于装置的安装和拆卸。 在第二女性实施例中,身体基本上是管状的,其中粘合剂在身体的外表面上。 在第三女性实施例中,身体是充满液体或凝胶的弹性囊,其适配于阴唇小室和前庭地板之间,从而封闭肠道。 膀胱的外表面涂有粘合剂以密封地堵塞肠道。 在男性实施例中,该装置包括在一个表面上具有粘合剂的弹性垫。 垫片符合并粘附到阴茎龟头,粘合剂密封地封闭肠管。 可以提供固定突片以粘附到龟头或阴茎轴。
    • 66. 发明授权
    • New organic compounds having opioid properties
    • 具有阿片样物质性质的新型有机化合物
    • US4996223A
    • 1991-02-26
    • US295037
    • 1989-02-09
    • John M. H. ReesBrian RobinsonBrian Cox
    • John M. H. ReesBrian RobinsonBrian Cox
    • C07D487/08
    • C07D487/08
    • New echiboline derivatives with opioid properties which are 6-hydroxy-9-methyl-echiboline derivatives having, in the 10-position, a hydrocarbon substituent of up to 4 carbon atoms--preferably a group R.CH.sub.2 -- (wherein R represents a hydrogen atom or a hydrocarbon group of up to 3 carbons) and especially a methyl, cyclopropyl-methyl or allyl group.These are made by dealkylating corresponding 6-alkoxy-9-methyl-10-substituted echibolines, thereby converting the 6-alkoxy group to a 6-hydroxy group, especially using boron tribromide as dealkylating reagent.Specific examples are 6-hydroxy-9,10-dimethyl-echiboline, 6-hydroxy-9-methyl-10-allyl-echiboline and 6-hydroxy-9-methyl-10-cyclopropylmethyl-echiboline.The compounds may be in free base or salt form, and be incorporated as active ingredient into pharmaceutical compositions.Also, the corresponding 6-alkoxy-9-methyl-10-substituted echiboline derivatives as useful novel intermediates, which may be made from a 6-alkoxy-9-methyl-echiboline by (A) reaction with a reagent which introduces the desired substituent into 10-position or (B) acylating to introduce the substituent R--CO-- into the 10-position and reducing the acyl group to RCH.sub.2 --.
    • PCT No.PCT / GB87 / 00457 Sec。 371日期1989年2月9日第 102(e)日期1989年2月9日PCT Filted 1987年6月30日PCT公布。 出版物WO88 / 00193 日期:1988年1月14日。具有阿片样物质性质的新的异链鸟苷衍生物是6-位羟基-9-甲基 - 异链鸟苷衍生物,其在10位具有至多4个碳原子的烃取代基 - 优选基团R.CH 2 - (其中R表示氢原子或最多3个碳的烃基),特别是甲基,环丙基 - 甲基或烯丙基。 这些是通过使相应的6-烷氧基-9-甲基-10-取代的echiboline脱烷基化,从而将6-烷氧基转化成6-羟基,特别是使用三溴化硼作为脱烷基试剂。 具体实例是6-羟基-9,10-二甲基 - 异链鸟嘌呤,6-羟基-9-甲基-10-烯丙基 - 异链鸟嘌呤和6-羟基-9-甲基-10-环丙基甲基 - 异链鸟嘌呤。 化合物可以是游离碱或盐形式,并且作为活性成分掺入药物组合物中。 另外,作为有用的新型中间体,可以使用6-烷氧基-9-甲基 - 异链鸟嘌呤衍生物作为有用的新的中间体,通过(A)与导入所需取代基的试剂反应来制备相应的6-烷氧基-9-甲基-10-取代的异鸟胆啉衍生物 进入10位或(B)酰化以将取代基R-CO-引入10位并将酰基还原成RCH 2 - 。
    • 69. 发明授权
    • Lawn logos
    • 草坪标志
    • US08220386B2
    • 2012-07-17
    • US12872965
    • 2010-08-31
    • Riley C. FieldsBrian CoxDaniel Lee Bizzell
    • Riley C. FieldsBrian CoxDaniel Lee Bizzell
    • B05C17/06
    • B44D2/007A01G2/00B44D2/002G09F19/228
    • A combination for creating artwork such as a sports logo on a lawn includes a lawn stencil having one or more openings configured to facilitate creation of a portion of the artwork. The combination further includes a container of spray paint and elongate members each having an elongate shaft with proximal and distal portions. The distal portion of each elongate shaft is pointed and includes a shape for accommodating insertion of the distal portion into the lawn. A container holds the lawn stencil, the container of paint, and the plurality of elongate members. The lawn stencil further comprises a connecting member that extends across a said opening of the lawn stencil for maintaining structural integrity of the lawn stencil and for distributing tension in the lawn stencil when the lawn stencil is laid upon the ground with the plurality of elongate members extending through the lawn stencil into the lawn.
    • 用于在草坪上创建诸如运动标志的艺术作品的组合包括具有一个或多个开口的草坪模板,其被配置为有助于创建艺术品的一部分。 该组合还包括喷雾剂容器和细长构件,每个细长构件具有带有近端部分和远端部分的细长轴。 每个细长轴的远端部分是尖的,并且包括用于容纳将远端部分插入到草坪中的形状。 容器保持草坪模板,油漆容器和多个细长构件。 草坪模板还包括连接构件,该连接构件延伸穿过草坪模板的所述开口,用于维持草坪模板的结构完整性,并且当草坪模板放置在地面上时分布张力,多个细长构件延伸 通过草坪模板进入草坪。