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    NOVEL ELATONIN LIGANDS HAVING ANTIDEPRESSANT ACTIVITY AS WELL AS SLEEP INDUCING PROPERTIES
    1.
    发明公开
    NOVEL ELATONIN LIGANDS HAVING ANTIDEPRESSANT ACTIVITY AS WELL AS SLEEP INDUCING PROPERTIES 有权
    新Elatoninliganden具有抗抑郁活性和睡眠功能

    公开(公告)号：EP1973868A1

    公开(公告)日：2008-10-01

    申请号：EP07701686.3

    申请日：2007-01-12

    申请人： McGill University ,  Universita Degli Studi Di Parma ,  UNIVERSITA' DEGLI STUDI DI MILANO ,  Universita Degli Studi Di Urbino

    发明人： GOBBI, Gabriella ,  MOR, Marco ,  RIVARA, Silvia ,  FRASCHINI, Franco ,  TARZIA, Giorgio ,  BEDINI, Annalida ,  SPADONI, Gilberto ,  LUCINI, Valeria

    IPC分类号： C07C237/04 ,  A61P25/00 ,  A61P25/24

    CPC分类号： C07C233/43 ,  C07C233/36

    摘要： Novel melatonin ligands of Formula (I) or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8;Y is selected from the group consisting of hydrogen, aryl, heteroaryl, CrC6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, -OCF3, CF3, C1-C8 alkyl, C1C8 alkyloxy, C1C8 alkylthio, halogen and -Z-(CH2)P-A; R1 is selected from the group consisting of C1C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1C4 alkyl, hydroxy-substituted C3-C6 cycloalkyl, and NHR5, wherein R5 is C1C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1C4 alkyl, C1C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1C4 alkyl, C1C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an -0-(CH2)v bridge representing with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring system; R4 is selected from the group consisting of hydrogen, C1C4 alkyl, C1C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R6 is selected from the group consisting of hydrogen and C1C6 alkyl; R7 is selected from the group consisting of hydrogen, C1C4 alkyl, C1C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; and R8 is selected from the group consisting of hydrogen and C1C4 alkyl.

    PERIPHERALLY RESTRICTED FAAH INHIBITORS
    6.
    发明公开
    PERIPHERALLY RESTRICTED FAAH INHIBITORS 有权
    与降低外周FAAH抑制剂

    公开(公告)号：EP2598477A2

    公开(公告)日：2013-06-05

    申请号：EP11812991.5

    申请日：2011-07-22

    申请人： The Regents of the University of California ,  Università Degli Studi Di Urbino "Carlo Bo" ,  Universita Degli Studi di Parma

    发明人： PIOMELLI, Daniele ,  CLAPPER, Jason, R. ,  MORENO-SANZ, Guillermo ,  DURANTI, Andrea ,  TONTINI, Andrea ,  MOR, Marco ,  TARZIA, Giorgio

    IPC分类号： C07C271/56 ,  A61K31/27 ,  A61P29/00 ,  A61P37/00

    CPC分类号： C07C271/56 ,  C07C2601/14

    摘要： Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R
    1 is a polar group. In some embodiments, R
    1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R
    2 and R
    3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R
    4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R
    5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R
    6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.