June 17, 2013

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The following patent record is from the CAplusSM database.

CAPLUS COPYRIGHT 2013 ACS

Patent Number: WO 2013054108
Title: Preparation of Mono-fluoro spiro compounds as beta-secretase inhibitors for treating amyloid beta related pathologies
Inventor(s): Minidis, Anna; Rahm, Fredrik; Viklund, Jenny
Patent Assignee(s): AstraZeneca AB, Swed.; AstraZeneca UK Limited
Source: PCT Int. Appl., 90 pp. CODEN: PIXXD2
Language: English

Abstract:
Beta-secretase inhibitors of formula I (wherein A is -O-, -CH2-, -CH2CH2-, -OCH2-, -CH2O-, or -CF2-; n = 0-1; R1 is H, C1-6 alkyl or C0-6-alkylC3-6cycloalkyl; R2 is (un)substituted C0-6-alkylaryl, (un)substituted C0-6-alkylheteroaryl, etc.; R3 is H; R4 is H; R5 and R6 are independently H, (un)substituted heterocyclyl, (un)substituted aryl, etc., or together form part of a ring; and R9 is one or more substituents selected from H, F, OH, CH3, Cl or OCH3), pharmaceutical compns. comprising them and therapeutic methods using them for the treatment and/or prevention of Abeta-related pathologies are claimed.  Such pathologies include Down's syndrome, beta-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders assocd. with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's Disease, memory loss, attention deficit symptoms assocd. with Alzheimer's disease, neurodegeneration assocd. with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia assocd. with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.  Synthetic procedures for prepg. I are exemplified.  Example compd. II was prepd. by Suzuki coupling of the corresponding 6'-bromo spiro intermediate (mixt. of isomers) and 5-(prop-1-ynyl)pyridin-3-ylboronic acid.  In a TR-FRET assay using the sol. part of the human beta-secretase, II had an IC50 of 18 nM.

Please note:  Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention. The actual title of the patent is Mono-fluoro beta-secretase inhibitors.

 View the full-text here.

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