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    MALONAMIDES AS OREXIN ANTAGONISTS
    71.
    发明专利
    MALONAMIDES AS OREXIN ANTAGONISTS 未知

    公开(公告)号：CA2679985A1

    公开(公告)日：2008-09-18

    申请号：CA2679985

    申请日：2008-03-05

    Applicant: HOFFMANN LA ROCHE

    Inventor： ROGERS-EVANS MARK ,  KNUST HENNER ,  NETTEKOVEN MATTHIAS ,  ROCHE OLIVIER ,  MALHERBE PARICHEHR ,  PINARD EMMANUEL ,  GOBBI LUCA

    IPC: C07C233/08 ,  A61K31/167 ,  C07C233/15 ,  C07C233/22

    Abstract: The present invention relates to compounds of formula wherein Ar1 and Ar2 are independently from each other unsubstituted or substituted aryl or hete roaryl; R1/R2 are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, -(CH2)o-O-lower alkyl, -(CH2)o-N-(lower alkyl )2, (CH2 )p-cycloalkyl, (CH2)p-heterocycloalkyl, (CH2)p-aryl, (CH2)p-heteroa ryl, which rings may be substituted by R, or R1 and R2 may form together wit h the N-atom to which they are attached a heterocyclic ring, optionally with further ring-heteroatoms selected from N, O or S, which ring may be substit uted by R; R is halogen, lower alkyl, lower alkyl substituted by halogen, lo wer alkoxy or lower alkoxy substituted by halogen; R3 is hydrogen or lower a lkyl; n is O, 1, 2, 3 or 4; o is 1, 2 or 3; P is 0, 1 or 2; or to pharmaceut ically suitable acid addition salts, optically pure enantiomers, racemates o r diastereomeric mixtures thereof. It has been found that the compounds of f ormula I are orexin receptor antagonists and the related compounds may be us eful in the treatment of disorders, in which orexin pathways are involved li ke sleep disorders.

    DIAZACARBAZOLE DERIVATIVES AS TAU-PET-LIGANDS
    78.
    发明专利
    DIAZACARBAZOLE DERIVATIVES AS TAU-PET-LIGANDS 未知

    公开(公告)号：MY190196A

    公开(公告)日：2022-04-04

    申请号：MYPI2016000604

    申请日：2014-10-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： GOBBI LUCA ,  KNUST HENNER ,  KOERNER MATTHIAS ,  MURI DIETER

    IPC: C07D471/04 ,  A61K31/44 ,  A61P25/28

    Abstract: The present invention relates to a compound of general formula wherein R is hydrogen or tritium; F is fluoro or 18fluoro; or to a pharmaceutically acceptable acid addition salt. Compounds cif formula I include 2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3 ',4'-d]pyrrole, H-2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3',4'-d]pyrrole and [ 18F]-2-( 6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3 ',4'-d]pyrrole. The compounds may be used for binding and imaging tau aggregates and related beta-sheet aggregates including besides others beta-amyloid aggregates or alpha-synuclein aggregates. (No suitable figure)

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