专利号:US-12201669-B2 优先权日:2021-03-11 标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology 发明人:TSAI LI-HUEI; BLANCHARD JOEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.
专利号:US-9073935-B2 优先权日:2011-11-11 标 题:Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; HOPKINS COREY R; MELANCON BRUCE J; POSLUSNEY MICHAEL S 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-2016200733-A1 优先权日:2013-08-23 标 题 :Substituted thieno[2,3-b]pyridine-2-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; POSLUSNEY MICHAEL S; MELANCON BRUCE J 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted thieno[2,3-b]pyridine-2-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9868746-B2 优先权日:2012-02-23 标题:Substituted 5-aminothieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; TARR JAMES C; SALOVICH JAMES M; POSLUSNEY MICHAEL S 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-9708278-B2 优先权日:2013-11-27 标 题 :Substituted 4-benzyl-3,4-dihydro-2H-benzo[B][1,4]oxazine-2-carboxamide analogs as positive allosteric modulators of muscarinic acetycholine receptor M1 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; STAUFFER SHAUN R; PANARESE JOSEPH D 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to N-substituted 3,4-dihydro-benzo[£][1,4]oxazine-2-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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