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27 条记录 (耗时 0.017 秒)

    NOVEL ELATONIN LIGANDS HAVING ANTIDEPRESSANT ACTIVITY AS WELL AS SLEEP INDUCING PROPERTIES
    6.
    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.

    MODULATION OF ANXIETY THROUGH BLOCKADE OF ANANDAMIDE HYDROLYSIS
    7.
    发明公开
    MODULATION OF ANXIETY THROUGH BLOCKADE OF ANANDAMIDE HYDROLYSIS 有权
    焦虑状态由BLOCKADE大麻素水解调制

    公开(公告)号：EP1558591A2

    公开(公告)日：2005-08-03

    申请号：EP03773201.3

    申请日：2003-10-07

    申请人： The Regents of the University of California ,  Universita Degli Studi di Urbino ,  Universita Degli Studi di Parma

    发明人： PIOMELLI, Daniele ,  DURANTI, Andrea ,  TONTINI, Andrea ,  MOR, Marco ,  TARZIA, Georgio

    IPC分类号： C07D271/00 ,  A61K31/21

    CPC分类号： C07C311/29 ,  C07C271/56 ,  C07C275/54 ,  C07C2601/14 ,  C07D209/08 ,  C07D211/06 ,  C07D215/06 ,  C07D307/79 ,  C07D487/04

    摘要： Fatty acid amide hydrolase inhibitors of the Formula (I) are provided, wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that, if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula (I) and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

    PERIPHERALLY RESTRICTED FAAH INHIBITORS
    10.
    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.