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27 条记录 (耗时 0.021 秒)

    TRIAZOLO-AZEPINE DERIVATIVES
    3.
    发明申请
    TRIAZOLO-AZEPINE DERIVATIVES 有权

    公开(公告)号：US20210395270A1

    公开(公告)日：2021-12-23

    申请号：US16963398

    申请日：2019-01-21

    申请人： Hoffmann-La Roche Inc.

    发明人： Hasane RATNI

    IPC分类号： C07D519/00

    摘要： The present invention relates to a compound of formula (I) wherein Ar is (II) or (II); R is CH3 or OCH3; or a pharmaceutically acceptable acid addition salt or a corresponding enantiomer thereof. The compounds are modulators of γ-secretase (A β42) and may be useful for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

    TRIAZOLO-AZEPINE DERIVATIVES
    4.
    发明申请
    TRIAZOLO-AZEPINE DERIVATIVES 审中-公开

    公开(公告)号：US20200317681A1

    公开(公告)日：2020-10-08

    申请号：US16954996

    申请日：2018-12-17

    申请人： Hoffmann-La Roche Inc.

    发明人： Bjoern BARTELS ,  Xinlan Aloise Ford COOK ,  Hasane RATNI ,  Michael REUTLINGER ,  Walter VIFIAN

    IPC分类号： C07D487/04 ,  A61P25/28

    摘要： The present invention relates to compounds of formula (I), wherein R is hydrogen or halogen, wherein R may be different if n=2 or 3; n is 1, 2 or 3; (II) is a disubstitued bicyclo[1,1,1]pentane or bicyclo[2,2,2]octane as defined below: (III) or (IV); or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

    BRIDGED PIPERIDINE DERIVATIVES
    5.
    发明申请
    BRIDGED PIPERIDINE DERIVATIVES 审中-公开

    公开(公告)号：US20200031831A1

    公开(公告)日：2020-01-30

    申请号：US16337348

    申请日：2017-09-28

    申请人： Hoffmann-La Roche Inc.

    发明人： Bjoern BARTELS ,  Roland JAKOB-ROETNE ,  Anja LIMBERG ,  Werner NEIDHART ,  Hasane RATNI ,  Michael REUTLINGER ,  Jérôme Charles SARIE ,  Greta VASTAKAITE

    IPC分类号： C07D487/04

    摘要： The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; R may be the same or different, if n=2 or 3; n is 1, 2 or 3; m is 1, 2 or 3; Ar is a five or six membered heteroaryl group, selected from (II), (III), (IV) or (V) wherein R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R3 is hydrogen or halogen; -( ) m - is —(CH2)m— or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-in-farct dementia, dementia pugilistica or Down syndrome.

    BICYCLIC HETEROARYL DERIVATIVES
    8.
    发明申请
    BICYCLIC HETEROARYL DERIVATIVES 审中-公开

    公开(公告)号：US20190233427A1

    公开(公告)日：2019-08-01

    申请号：US16339345

    申请日：2017-10-02

    申请人： Hoffmann-La Roche Inc.

    发明人： Bjoern BARTELS ,  Roland JAKOB-ROETNE ,  Anja LIMBERG ,  Werner NEIDHART ,  Hasane RATNI ,  Michael REUTLINGER ,  Greta VASTAKAITE

    IPC分类号： C07D487/04 ,  A61P25/28

    CPC分类号： C07D487/04 ,  A61P25/28

    摘要： The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; and R1 may be different if n is 2 or 3; R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, CN, lower alkoxy or lower alkoxy substituted by halogen; X is CH or N; m is 1, 2 or 3; -( )m is —(CH2)m—; n is 1, 2 or 3; Ar is a five membered heteroaryl group, selected from formula (A), (B), (C), (D), (E) or (F), wherein R3 is hydrogen, methyl or chloro; R4 is hydrogen or methyl; R5 is F, Cl, CHF2 or CF3; or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.