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29 条记录 (耗时 0.037 秒)

    Bridged piperidine derivatives
    1.
    发明授权
    Bridged piperidine derivatives 有权

    公开(公告)号：US10604517B2

    公开(公告)日：2020-03-31

    申请号：US15913087

    申请日：2018-03-06

    申请人： Hoffmann-La Roche Inc.

    发明人： Karlheinz Baumann ,  Guido Galley ,  Roland Jakob-Roetne ,  Anja Limberg ,  Werner Neidhart ,  Rosa Maria Rodriguez Sarmiento ,  Björn Bartels ,  Hasane Ratni

    IPC分类号： C07D417/14 ,  C07D519/00 ,  A61P25/28 ,  C07D413/14

    摘要： The present invention relates to compounds of formula hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S-lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or two neighboring carbon atoms may form on phenyl an additional ring containing —O—CH2—O—; n is 1 to 5; R2 is hydrogen or lower alkyl substituted by halogen; R3 is hydrogen or lower alkyl substituted by halogen; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers or optical isomers or stereoisomers 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
    2.
    发明授权
    Bridged piperidine derivatives 有权

    公开(公告)号：US10562903B2

    公开(公告)日：2020-02-18

    申请号：US16004145

    申请日：2018-06-08

    申请人： Hoffmann-La Roche Inc.

    发明人： Bjoern Bartels ,  Hasane Ratni ,  Karlheinz Baumann ,  Guido Galley ,  Georg Jaeschke ,  Roland Jakob-Roetne ,  Anja Limberg ,  Werner Neidhart ,  Rosa Maria Rodriguez-Sarmiento

    IPC分类号： C07D487/04 ,  C07D471/04 ,  A61P25/28

    摘要： The present invention relates to a compound of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, or lower alkoxy; R2 is lower alkyl substituted by halogen, —CH2—C3-6-cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C3-6-cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n=2, R1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or 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
    4.
    发明申请
    BRIDGED PIPERIDINE DERIVATIVES 审中-公开

    公开(公告)号：US20180237432A1

    公开(公告)日：2018-08-23

    申请号：US15913087

    申请日：2018-03-06

    申请人： Hoffmann-La Roche Inc.

    发明人： Karlheinz Baumann ,  Guido Galley ,  Roland Jakob-Roetne ,  Anja Limberg ,  Werner Neidhart ,  Rosa Maria Rodriguez Sarmiento ,  Björn Bartels ,  Hasane Ratni

    IPC分类号： C07D417/14 ,  C07D413/14 ,  A61P25/28

    CPC分类号： C07D417/14 ,  A61P25/28 ,  C07D413/14 ,  C07D519/00

    摘要： The present invention relates to compounds of formula hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S-lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or two neighboring carbon atoms may form on phenyl an additional ring containing —O—CH2—O—; n is 1 to 5; R2 is hydrogen or lower alkyl substituted by halogen; R3 is hydrogen or lower alkyl substituted by halogen; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers or optical isomers or stereoisomers 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.

    ARYL-QUINOLINE DERIVATIVES
    9.
    发明申请
    ARYL-QUINOLINE DERIVATIVES 有权
    芳基喹啉衍生物

    公开(公告)号：US20130116234A1

    公开(公告)日：2013-05-09

    申请号：US13666202

    申请日：2012-11-01

    申请人： Hoffmann-La Roche Inc.

    发明人： Simona M. Ceccarelli ,  Aurelia Conte ,  Holger Kuehne ,  Bernd Kuhn ,  Werner Neidhart ,  Ulrike Obst Sander ,  Markus Rudolph

    IPC分类号： A61K31/4709 ,  A61K31/47 ,  C07D413/14 ,  C07D401/14 ,  C07D215/54 ,  C07D401/04 ,  A61K31/5377 ,  C07D413/04

    CPC分类号： C07D491/048 ,  C07D215/00 ,  C07D215/02 ,  C07D215/227 ,  C07D215/54 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14

    摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.

    摘要翻译： 本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和n如本文所述，包括该化合物的组合物和使用该化合物的方法。 本发明化合物可用作脂肪酸结合蛋白（FABP）4和/或5抑制剂，可用于治疗或预防脂肪营养不良，2型糖尿病，血脂异常，动脉粥样硬化，涉及炎症，脂肪变性和/或纤维化的肝脏疾病 ，如非酒精性脂肪性肝病，特别是非酒精性脂肪性肝炎，代谢综合征，肥胖，慢性炎性和自身免疫性炎性疾病。

    Bicyclic heteroaryl derivatives
    10.
    发明授权
    Bicyclic heteroaryl derivatives 有权

    公开(公告)号：US10941147B2

    公开(公告)日：2021-03-09

    申请号：US16346623

    申请日：2017-10-30

    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, 1-1 or 1-2 wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, or lower alkoxy substituted by halogen; R1 may be different if n=2 or 3 n is 1, 2 or 3 Ar is a six membered heteroaryl group, selected from wherein R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R3 is hydrogen or halogen; or to a pharmaceutically active acid addition salt 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.