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    2.
    发明专利
    未知

    公开(公告)号：DE60227657D1

    公开(公告)日：2008-08-28

    申请号：DE60227657

    申请日：2002-05-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： CAI HAI-YING ,  DILLON MICHAEL PATRICK ,  GALLEY GUIDO ,  GOERGLER ANNICK ,  KOLCZEWSKI SABINE ,  MUSZYNSKI-BARSY DAWN MARIE

    IPC: C07D498/10 ,  A61K31/535 ,  A61K31/537 ,  A61P1/08 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00

    Abstract: The invention relates to compounds of the general formulawherein(R1)n is independently from from each other halogen, lower alkyl or lower alkoxy;R2 is hydrogen, lower alkyl, lower halogen-alkyl, -(CH2)m-OH, -(CH2)m-NR2, -(CH2)mO-lower alkyl, -(CH2)m-C(O)-NR2, or is -(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, -(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl;R is hydrogen or lower alkyl and may be the same or different in case of R2;n is 0, 1, or 2;m is 0, 1, 2, 3 or 4;and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.

    3.
    发明专利
    未知

    公开(公告)号：BR0209604A

    公开(公告)日：2004-03-23

    申请号：BR0209604

    申请日：2002-05-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： CAI HAI-YING ,  DILLON MICHAEL PATRICK ,  GALLEY GUIDO ,  GOERGLER ANNICK ,  KOLCZEWSKI SABINE ,  MUSZYNSKI-BARSY DAWN MARIE

    IPC: A61K31/535 ,  A61K31/537 ,  A61P1/08 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D498/10

    Abstract: The invention relates to compounds of the general formulawherein(R1)n is independently from from each other halogen, lower alkyl or lower alkoxy;R2 is hydrogen, lower alkyl, lower halogen-alkyl, -(CH2)m-OH, -(CH2)m-NR2, -(CH2)mO-lower alkyl, -(CH2)m-C(O)-NR2, or is -(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, -(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl;R is hydrogen or lower alkyl and may be the same or different in case of R2;n is 0, 1, or 2;m is 0, 1, 2, 3 or 4;and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.

    1-OXA-3,9-DIAZA-ESPIRO[5.5]UNDECAN-2-ONAS
    5.
    发明专利
    1-OXA-3,9-DIAZA-ESPIRO[5.5]UNDECAN-2-ONAS 未知

    公开(公告)号：AR033631A1

    公开(公告)日：2003-12-26

    申请号：ARP020101705

    申请日：2002-05-10

    Applicant: HOFFMANN LA ROCHE

    Inventor： CAI HAI-YING ,  DILLON MICHAEL PATRICK ,  GALLEY GUIDO ,  GOERGLER ANNICK ,  KOLCZEWSKI SABINE ,  MUSZYNSKI DAWN MARIE

    IPC: A61K31/535 ,  A61K31/537 ,  A61P1/08 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D498/10 ,  A61P19/02 ,  A61P11/06

    Abstract: Compuestos de la formula general en la cual: (R1)n es independientemente entre sí, halogeno alquilo inferior o alcoxi inferior; R2 es hidrogeno, alquilo inferior, halogeno-alquilo inferior, -(CH2)m-OH, -(CH2)m-NR2, -(CH2)mO-alquilo inferior, -(CH2)m- C(O)-NR2, o es -(CH2)m-heteroarilo de seis miembros, opcionalmente substituido por uno o más alcoxi inferior, -(CH2)m heterociclilo no aromático de 5 o 6 miembros, opcionalmente substituido por hidroxi o alquilo inferior, R es hidrogeno o alquilo inferior y puede ser igual o diferente en caso de R2; n es 0, 1 o 2 m es 0, 1, 2, 3 o 4; y a sales de adicion ácidas farmacéuticamente aceptables de los mismos. Estos compuestos presentan una buena afinidad por el receptor de NK-1, y por lo tanto, son adecuados para el tratamiento de enfermedades relacionadas con dicho receptor. Otros objetos de la presente son: Medicamentos, usos y Procedimiento para preparar los compuestos.

    6.
    发明专利
    未知

    公开(公告)号：DK1390372T3

    公开(公告)日：2008-09-15

    申请号：DK02742943

    申请日：2002-05-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： CAI HAI-YING ,  DILLON MICHAEL PATRICK ,  GALLEY GUIDO ,  GOERGLER ANNICK ,  KOLCZEWSKI SABINE ,  MUSZYNSKI-BARSY DAWN MARIE

    IPC: C07D498/10 ,  A61K31/535 ,  A61K31/537 ,  A61P1/08 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00

    Abstract: The invention relates to compounds of the general formulawherein(R1)n is independently from from each other halogen, lower alkyl or lower alkoxy;R2 is hydrogen, lower alkyl, lower halogen-alkyl, -(CH2)m-OH, -(CH2)m-NR2, -(CH2)mO-lower alkyl, -(CH2)m-C(O)-NR2, or is -(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, -(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl;R is hydrogen or lower alkyl and may be the same or different in case of R2;n is 0, 1, or 2;m is 0, 1, 2, 3 or 4;and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.

    7.
    发明专利
    未知

    公开(公告)号：AT401333T

    公开(公告)日：2008-08-15

    申请号：AT02742943

    申请日：2002-05-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： CAI HAI-YING ,  DILLON MICHAEL ,  GALLEY GUIDO ,  GOERGLER ANNICK ,  KOLCZEWSKI SABINE ,  MUSZYNSKI-BARSY DAWN

    IPC: C07D498/10 ,  A61K31/535 ,  A61K31/537 ,  A61P1/08 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00

    Abstract: The invention relates to compounds of the general formulawherein(R1)n is independently from from each other halogen, lower alkyl or lower alkoxy;R2 is hydrogen, lower alkyl, lower halogen-alkyl, -(CH2)m-OH, -(CH2)m-NR2, -(CH2)mO-lower alkyl, -(CH2)m-C(O)-NR2, or is -(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, -(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl;R is hydrogen or lower alkyl and may be the same or different in case of R2;n is 0, 1, or 2;m is 0, 1, 2, 3 or 4;and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.

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