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    ISOQUINOLINE DERIVATIVES AS PERK INHIBITORS
    6.
    发明申请
    ISOQUINOLINE DERIVATIVES AS PERK INHIBITORS 审中-公开

    公开(公告)号：US20190241573A1

    公开(公告)日：2019-08-08

    申请号：US16318408

    申请日：2017-07-18

    申请人： GlaxoSmithKline Intellectual Property Development Limited

    发明人： Jeffrey Michael AXTEN ,  Raghava Reddy KETHIRI ,  Rajendra KRISTAM ,  Chandregowda VENKATESHAPPA

    IPC分类号： C07D487/04 ,  C07D471/04 ,  A61P35/00 ,  A61P25/28 ,  A61P27/06

    CPC分类号： C07D487/04 ,  A61K31/4725 ,  A61K31/519 ,  A61K45/06 ,  A61P25/28 ,  A61P27/02 ,  A61P27/06 ,  A61P35/00 ,  C07D471/04

    摘要： The invention is directed to substituted isoquinoline derivatives and uses thereof. Specifically, the invention is directed to compounds according to Formula I and the use of compounds of Formula (I) in treating disease states: wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined herein.The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, Parkinson disease, diabetes, metabolic syndrome, metabolic disorders, Huntington's disease, Creutzfeldt-Jakob Disease, fatal familial insomnia, Gerstmann-Sträussler-Scheinker syndrome, and related prion diseases, amyotrophic lateral sclerosis, progressive supranuclear palsy, myocardial infarction, cardiovascular disease, inflammation, organ fibrosis, chronic and acute diseases of the liver, fatty liver disease, liver steatosis, liver fibrosis, chronic and acute diseases of the lung, lung fibrosis, chronic and acute diseases of the kidney, kidney fibrosis, chronic traumatic encephalopathy (CTE), neurodegeneration, dementias, frontotemporal dementias, tauopathies, Pick's disease, Neimann-Pick's disease, amyloidosis, cognitive impairment, ather osclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

    BICYCLIC HETEROARYL DERIVATIVES
    9.
    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.