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-2023271983-A1 优先权日:2020-07-29 标题 :Functionalized isonitriles and products, preparation and uses thereof 发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA 权利人:UNIV SANTIAGO COMPOSTELA 摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
专利号:WO-2025030095-A1 优先权日:2023-08-03 标 题 :Methods of synthesis 发明人:DERSTINE BRENDEN PAUL; TUCKER JOHN LLOYD 权利人:NEUROCRINE BIOSCIENCES INC 摘要:This present disclosure relates to processes for preparing a compound of Formula (A) which is useful as an intermediate in the preparation of mAChR agonist compounds; and compositions comprising the compound of Formula (A).
专利号:US-9550795-B2 优先权日:2011-08-31 标 题:Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 发明人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS 权利人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS; 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:WO-2012172449-A1 优先权日:2011-06-13 标题:Lactams as beta secretase inhibitors 发明人:BRODNEY MICHAEL AARON 权利人:PFIZER; BRODNEY MICHAEL AARON 摘要:Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compound of formula I is useful as beta secretase inhibitor for use in the treatment of Alzheimer's and other neurodegenerative and/or neurological disorders.
专利号:US-2016229847-A1 优先权日:2013-10-04 标 题:Novel bicyclic pyridinones as gamma-secretase modulators 发明人:PETTERSSON MARTIN YOUNGJIN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; JOHNSON DOUGLAS SCOTT; KAUFFMAN GREGORY WAYNE; O'DONNELL CHRISTOPHER WILLIAM; PATEL NANDINI CHATURBHAI; STEPAN ANTONIA FRIEDERIKE; STIFF CORY MICHAEL; SUBRAMANYAM CHAKRAPANI; TRAN TUAN PHONG; 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 II as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
1: Barbe AG. Long-term Use of the Sialogogue Medications Pilocarpine and Cevimeline Can Reduce Xerostomia Symptoms and Increase Salivary Flow in Head and Neck Cancer Survivors After Radiotherapy. J Evid Based Dent Pract. 2017 Sep;17(3):268-270. doi: 10.1016/j.jebdp.2017.06.013. Epub 2017 Jul 3. doi: 10.1016/j.autneu.2017.05.010. Epub 2017 May 30.
合成参考文献
摘要:Physicians Desk Reference. 58th ed. Thomson PDR. Montvale, NJ 2004., p. 1183 摘要:Thomson.Micromedex. Drug Information for the Health Care Professional. 24th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2004., p. 792 摘要:Cowl, C.T. Physician's Handbook 10th edition. Lippincott Williams & Wilkins, Philadelphia, PA. 2003, p. 294 参考文献:10.1016/s0049-0172(99)80001-8 摘要:Anaya JM, Talal N. Sjögren's syndrome comes of age. Semin Arthritis Rheum. 1999 Jun;28(6):355–9. doi: 10.1016/s0049-0172(99)80001-8.