SCREENING ASSAY FOR IDENTIFYING HUMAN PURINORECEPTOR LIGANDS
    3.
    发明申请
    SCREENING ASSAY FOR IDENTIFYING HUMAN PURINORECEPTOR LIGANDS 审中-公开
    用于识别人体感应器配置的筛选测定

    公开(公告)号:WO9955901A3

    公开(公告)日:2000-04-20

    申请号:PCT/US9908923

    申请日:1999-04-23

    Applicant: ABBOTT LAB

    CPC classification number: C07K14/705 G01N33/566 G01N2500/00

    Abstract: A method of screening candidate compounds for their ability to modulate expression of human purinoreceptors is provided. The method relates to the use of stably transfected cell lines that express human or other mammalian purinoreceptors to identify purinoreceptor ligands, and to determine the amount of a receptor agonist or antagonist in a test sample.

    Abstract translation: 提供了筛选候选化合物调节人类嘌呤受体表达能力的方法。 该方法涉及使用稳定转染的细胞系,其表达人或其他哺乳动物嘌呤受体以鉴定嘌呤受体配体,并确定测试样品中受体激动剂或拮抗剂的量。

    4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS

    公开(公告)号:CA2697382A1

    公开(公告)日:2009-03-05

    申请号:CA2697382

    申请日:2008-08-26

    Abstract: 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). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1- C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula -X-W, where X is a single bond, C1-C4-alkylene or C1-C4-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; R9 is a group of the formula -Y-Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m-R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-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.

    NUEVAS BENCESULFONAMIDAS COMO BLOQUEADORES DE CANALES DE CALCIO

    公开(公告)号:CO6400194A2

    公开(公告)日:2012-03-15

    申请号:CO11097206

    申请日:2011-08-02

    Applicant: ABBOTT LAB

    Abstract: Inhibidores de canales de calcio que comprenden compuestos de fórmula (I), de fórmula (II), de fórmula (III) o de fórmula (IV),donde L1 es C(O) o S(O)2; uno de R1 y R2 es X, y el otro de R1 y R2 es Y; X es (i) o (ii); Y es -NRcAr1, -NRcAr2-Ar1, -NRcCH(Ar1)2, entre otros: R3, R4, R5 y R6 son en forma independiente entre sí hidrógeno, alcoxi, alquilo, o halógeno; R7 es -S(O)2Ar3, -C(O)Ar3, -S(O)2(CRaRb)pAr3, -C(O)(CRaRb)pAr3, entre otros y Rc es hidrógeno o alquilo. Además, la presente solicitud relaciona composiciones que comprenden dichos compuestos o sales farmacéuticamente aceptables de éstos, en combinación con uno o más vehículos farmacéuticamente aceptables y métodos para tratar afecciones y trastornos relacionados con los canales de calcio. Más particularmente, un método para tratar el dolor en un sujeto que lo necesita.

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