专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-9981949-B2 优先权日:2008-12-01 标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:OYSTER POINT PHARMA INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
专利号:US-8604191-B2 优先权日:2008-12-01 标 题:Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3YLVINYL)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT; TARGACEPT INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-yl)pyrimidine, novel salt forms, and novel polymorphic forms of these salts.
专利号:US-10035796-B2 优先权日:2014-08-14 标题:Crystalline forms of a BACE inhibitor, compositions, and their use 发明人:KAZAKEVICH IRINA; TRZASKA SCOTT; FENG TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.
专利号:WO-2024127343-A1 优先权日:2022-12-16 标 题 :Inhibitors of ectonucleotide pyrophosphatase / phosphodiesterase 1 (enpp-1) 发明人:RAMANARAYANAN GANAPATHY BHOTLA VENKATA; SARAVANAN PERUMAL; SARAVANAN VADIVELU; NAGARAJ KULKARNI 权利人:SRAVATHI AI TECH PRIVATE LIMITED 摘要:The present invention discloses a novel type of highly potent ENPP-1 inhibitors for the treatment of various diseases particularly, cancer. The compounds of the invention have tail, core, and zinc binding portions (ZBP), where the key feature includes positioning of a sulfoximine-type moiety and an amino nitrogen atom specified as G 1 or G 2 fragment in a saturated cyclic ring in the core part. Synthesis of compounds of formula (1), pharmaceutical compositions and use thereof are also disclosed.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
1: Soares JC, Perfetto JG, Antonio BB, Oliveira MG. Effects of the M1 Muscarinic Antagonist Dicyclomine on Emotional Memory Retrieval. Behav Neurosci. 2015 Nov 30. [Epub ahead of print] doi: 10.1128/AAC.00796-15. Epub 2015 Aug 10. 3: Shah DA, Rana JP, Chhalotiya UK, Baldania SL, Bhatt KK. Development and validation of a liquid chromatographic method for estimation of dicyclomine hydrochloride, mefenamic Acid and paracetamol in tablets. Indian J Pharm Sci. 2014 Nov-Dec;76(6):529-34. 4: Das S, Mondal S, Datta A, Bandyopadhyay S. A rare case of dicyclomine abuse. J Young Pharm. 2013 Sep;5(3):106-7. doi: 10.1016/j.jyp.2013.08.004. Epub 2013 Sep 13.
合成参考文献
摘要:Kiso to Rinsho. Clinical Report., 8(1954), 1974 摘要:Farmaco. Scienza e Tecnica., 7(448), 1952 摘要:British Medical Journal., 288(901), 1984 参考文献:10.2165/00044011-199713020-00004 摘要:Rohde H, Bihr AM, Schwantes U, Eisebitt R, Meurer J, Fischer M, Topfmeier P. Effect of Trospium Chloride on Duodenal Motility during Upper Gastrointestinal Endoscopy: A Randomised, Double-Blind, Placebo-Controlled Trial. Clin Drug Investig. 1997;13(2):85–9. doi: 10.2165/00044011-199713020-00004. 参考文献:10.1186/1477-7517-9-40 摘要:Suohu K, Humtsoe C, Saggurti N, Sabarwal S, Mahapatra B, Kermode M. Understanding the association between injecting and sexual risk behaviors of injecting drug users in Manipur and Nagaland, India. Harm Reduction Journal. 2012 Dec 18;9(1):40. doi: 10.1186/1477-7517-9-40.