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    QUINAZOLINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    13.
    发明专利
    QUINAZOLINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 未知

    公开(公告)号：CA2737587C

    公开(公告)日：2016-08-09

    申请号：CA2737587

    申请日：2009-11-04

    Applicant: HOFFMANN LA ROCHE

    Inventor： KNUST HENNER ,  LIMBERG ANJA ,  NETTEKOVEN MATTHIAS ,  RATNI HASANE ,  RIEMER CLAUS ,  VIFIAN WALTER

    IPC: C07D401/04 ,  A61K31/517 ,  A61P25/16 ,  A61P25/18 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

    Abstract: The present invention relates to a compounds of formula I wherein R1 is hydroxy or NR'R"; R' and R" are indepen-dently from each other hydrogen, lower alkyl, cycloalkyl, or may form together with the N-atom to which they are attached a het-eroalkyl ring; R2 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano or S(O)2-Iower alkyl; R3 is lower alkyl, -(CH2)m-aryl, optionally substituted by halogen, or is -(CH2)m-cycloalkyl; R4 and R5 are independently from each other hydrogen or lower alkyl substituted by halogen, or are -(CR2)m-aryl or -(CR2)m-het-eroaryl, wherein the rings may be substituted by one or more substituents, selected from halogen, lower alkyl, lower alkyl substi-tuted by halogen, cyano, hydroxy, NR'R" or by lower alkoxy substituted by halogen, or are -(CR2)m-cycloalkyl, optionally substi-tuted by hydroxy or by aryl, or are a heteroalkyl ring, optionally substituted by =O or -(CR2)m-aryl, or R4 and R5 are together with the N-atom to which they are attached a heterocyclic ring system, optionally substituted by lower alkyl, aryl or halogen-substituted aryl, and R may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; m is 0, 1 or 2; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

    2-OXO-2,3-DIHYDRO-INDOLES FOR THE TREATMENT OF CNS DISORDERS CNS 2--23--
    15.
    发明专利
    2-OXO-2,3-DIHYDRO-INDOLES FOR THE TREATMENT OF CNS DISORDERS CNS 2--23-- 未知

    公开(公告)号：HK1206721A1

    公开(公告)日：2016-01-15

    申请号：HK15107160

    申请日：2015-07-27

    Applicant: HOFFMANN LA ROCHE

    Inventor： BRUNNER DANIELA ,  MALBERG JESSICA ,  SHANKAR BAVANI G G ,  KOLCZEWSKI SABINE ,  LIMBERG ANJA ,  PRINSSEN ERIC ,  RIEMER CLAUS ,  STOLL THEODER

    IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101

    Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein is phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl; is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or halogen; n is 1 or 2; if n is 2, R1 may be the same or not; R2/R2′ are independently from each other lower alkyl, or form together with the carbon atom to which they are attached a C3-6-cycloalkyl ring; R3 is lower alkyl, C3-6-cycloalkyl, CH2—C3-6-cycloalkyl, C3-6-cycloalkyl wherein one ring-carbon atom is replaced by —O—, (CH2)3—O—C3-6-cycloalkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, (CH2)3—S(O)2—C3-6-cycloalkyl or (CH2)2—S(O)2-lower alkyl; R4 is hydrogen, halogen or lower alkyl; m is 1 or 2; if m is 2, R4 may be the same or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.

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