Squaric acid derivatives
    35.
    发明授权
    Squaric acid derivatives 失效
    方酸衍生物

    公开(公告)号:US06740654B2

    公开(公告)日:2004-05-25

    申请号:US09899488

    申请日:2001-07-05

    IPC分类号: C07D23514

    CPC分类号: C07D495/04 C07D235/30

    摘要: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain  in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述式(1)的方酸衍生物:其中Het是任选取代的双环稠环杂芳族基团; L 2是共价键或-O - , - S - , - C(O) - , -C(S) - , - S(O) - , - S(O)2,-N(R 8) - 或-C(R 8)(R 8a) - ; Ar 2 >是任选取代的芳族或杂芳族基团; Alk是一种链霉素,其中R是羧酸(-CO 2 H)或其衍生物或生物试剂; R 1是氢原子或C 1-6烷基; L 1, 是共价键或连接原子或基团; Alk 1是任选取代的脂族链; n是0或整数1; R 2是氢原子或任选取代的杂脂肪族,脂环族,杂脂族,多环烷基, 除2,6-二氮杂萘-1-基,异喹啉-1-基,2,7-萘啶-1-基或喹唑啉-4-基之外的杂多环脂族,芳族或杂芳族基;以及盐,溶剂合物,水合物和 N-氧化物。化合物能够抑制整联蛋白与其配体的结合 并且可用于预防和治疗免疫或炎性疾病或涉及细胞不适当生长或迁移的病症。

    Switching device for optionally passing a flow of medium through a first or second treatment member
    36.
    发明授权
    Switching device for optionally passing a flow of medium through a first or second treatment member 有权
    用于可选地使介质流通过第一或第二处理构件的开关装置

    公开(公告)号:US06668860B1

    公开(公告)日:2003-12-30

    申请号:US10110688

    申请日:2002-08-27

    IPC分类号: F16K3514

    摘要: A switching device for optionally passing a flow of medium, such as a highly pressurized gas, through a first or second treatment member (2, 3), in which the medium is subjected to a treatment, such as filtration, heating, cooling or the like, comprises a medium inlet, a medium outlet and two distribution valves (1, 5), of which the valve bodies, which are provided with passages, are attached to a common rotation pin (10). For safety's sake, safety valves (12, 13, 14, 15) are arranged in the connections between distribution valves arranged at the inlet and at the oulet and the two treatment members.

    摘要翻译: 一种切换装置,用于任选地使诸如高压气体的介质流通过第一或第二处理构件(2,3),其中介质经过诸如过滤,加热,冷却或 包括介质入口,介质出口和两个分配阀(1,5),其中设置有通道的阀体附接到公共旋转销(10)。 为了安全起见,安全阀(12,13,14,15)被布置在布置在入口处和在底部和两个处理构件之间的分配阀之间的连接处。

    3-Substituted isoquinolin-1-yl derivatives
    38.
    发明授权
    3-Substituted isoquinolin-1-yl derivatives 失效
    3-取代的异喹啉-1-基衍生物

    公开(公告)号:US06403608B1

    公开(公告)日:2002-06-11

    申请号:US09867060

    申请日:2001-05-29

    IPC分类号: C07D21708

    摘要: 3-Substituted isoquinoline containing squaric acids of formula (1) are described: wherein Ar1 is a 3-substituted isoquinolin-1-yl group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted aromatic or heteroaromatic chain; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disordes or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述了含有式(1)的方酸的3-取代的异喹啉:其中Ar1是3-取代的异喹啉-1-基; L2是共价键或连接原子或基团; Ar2是任选取代的芳族或杂芳族链; Alk是其中R是羧酸(-CO 2 H)或其衍生物或生物试剂的链霉素; R 1是氢原子或C 1-6烷基; L 1是共价键或连接原子或基团; Alk1是任选取代的脂族 链; n为零或整数1; R 2为氢原子或任选取代的杂脂族,脂环族,杂环脂族,多环芳族,杂多环脂族,芳族或杂芳族基团;及其盐,溶剂合物,水合物和N-氧化物。 能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎症性紊乱或紊乱。

    Method and apparatus for frequency modulation synthesis
    40.
    发明授权
    Method and apparatus for frequency modulation synthesis 失效
    用于频率调制合成的方法和装置

    公开(公告)号:US6011448A

    公开(公告)日:2000-01-04

    申请号:US949574

    申请日:1997-10-14

    摘要: A method for frequency modulation synthesis and apparatus for performing the method. The method uses additions rather than multiplies and therefore saves the space and cost of multipliers in circuit implementations. The method saves further resources by using the coordinate rotation digital computer (CORDIC) algorithm to acquire sine values as opposed to an extensive sine look-up table. The method can be implemented with either a dedicated digital circuit or a programmed special purpose processor such as a digital signal processor. The hardware for implementing the method is normally integrated onto a semiconductor device.

    摘要翻译: 一种用于频率调制合成的方法和用于执行该方法的装置。 该方法使用加法而不是乘法,从而节省乘法器在电路实现中的空间和成本。 该方法通过使用坐标旋转数字计算机(CORDIC)算法来获得正弦值而不是广泛的正弦查找表来节省更多的资源。 该方法可以使用专用数字电路或诸如数字信号处理器的编程专用处理器来实现。 用于实现该方法的硬件通常集成在半导体器件上。