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    INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES
    2.
    发明专利
    INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES 未知

    公开(公告)号：CA2915536C

    公开(公告)日：2021-10-19

    申请号：CA2915536

    申请日：2014-06-16

    Applicant: HOFFMANN LA ROCHE

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

    IPC: C07D405/14 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61P25/00 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07H19/044

    Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar is a heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o-O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o-S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH2)o-S(O)2-lower alkyl, lower alkyl substituted by halogen or CH2CH(OH)CF3; R3 is halogen or lower alkyl; X is CH or N; X1 is CH or N; n is 1 or 2; o is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line is a bond 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 The compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

    2-oxo-2,3-dihidro-indoles para el tratamiento de trastornos del SNC
    3.
    发明专利
    2-oxo-2,3-dihidro-indoles para el tratamiento de trastornos del SNC 未知

    公开(公告)号：ES2590531T3

    公开(公告)日：2016-11-22

    申请号：ES13759241

    申请日：2013-09-10

    Applicant: HOFFMANN LA ROCHE

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

    IPC: C07D403/12 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/437 ,  A61K31/44 ,  A61K31/506 ,  A61P25/00 ,  C07D209/34 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04

    Abstract: Un compuesto de fórmula**Fórmula** en la que:**Fórmula** es fenilo o un grupo heteroarilo, seleccionado de piridinilo, pirimidinilo, imidazolilo, isoxazolilo o pirazolilo;**Fórmula** es fenilo o piridinilo, en el que el átomo de N del grupo piridinilo puede estar en todas las posiciones libres; R1 es hidrógeno, alquilo C1-7, alquilo C1-7 sustituido con halógeno, alcoxi C1-7 o halógeno; n es 1 o 2; si n es 2, R1 puede ser el mismo o no; R2/R2' son independientemente entre sí alquilo C1-7 o forman junto con el átomo de carbono al que están unidos un anillo cicloalquilo C3-6; R3 es alquilo C1-7, cicloalquilo C3-6, CH2-cicloalquilo C3-6, cicloalquilo C3-6 en el que un átomo de carbono del anillo se reemplaza por -O-, (CH2)3-O-cicloalquilo C3-6, alquilo C1-7 sustituido con hidroxi, alquilo C1-7 sustituido con halógeno, (CH2)3-S(O)2-cicloalquilo C3-6 o (CH2)2-S(O)2-alquilo C1-7; R4 es hidrógeno, halógeno o alquilo C1-7; m es 1 o 2; si m es 2, R4 puede ser el mismo o no; así como con las sales farmacéuticamente aceptables de los mismos, con una mezcla racémica o con los enantiómeros correspondientes y/o isómeros ópticos y/o estereoisómeros de los mismos.

    2-OXO-2,3-DIHYDRO-INDOLES FOR THE TREATMENT OF CNS DISORDERS
    4.
    发明专利
    2-OXO-2,3-DIHYDRO-INDOLES FOR THE TREATMENT OF CNS DISORDERS 未知

    公开(公告)号：SG11201501923WA

    公开(公告)日：2015-04-29

    申请号：SG11201501923W

    申请日：2013-09-10

    Applicant: HOFFMANN LA ROCHE

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

    IPC: C07D403/12 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/437 ,  A61K31/44 ,  A61K31/506 ,  A61P25/00 ,  C07D209/34 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04

    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.

    2-OXO-2,3-DIHYDRO-INDOLES FOR THE TREATMENT OF CNS DISORDERS CNS 2--23--
    6.
    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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