专利号:US-9708317-B2 优先权日:2013-11-25 标 题 :Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-B]pyrazin-3-one derivatives 发明人:ZAMBON ALFONSO; NICULESCU-DUVAZ DAN; CHUBB RICHARD; SPRINGER CAROLINE JOY 权利人:CANCER RES TECH LTD; INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE); OXY SCIENT LTD; THE INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL 摘要:The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
专利号:WO-2025061707-A1 优先权日:2023-09-19 标题:Synthesis of sulfoximines containing a benzimidazole moiety 发明人:SMITS HELMARS; DUMEUNIER RAPHAEL; PERROTTA DANIELE 权利人:SYNGENTA CROP PROTECTION AG 摘要:A process for the preparation of enantiomerically enriched sulfoximines of formula (I) is provided, wherein R1, R2, S*, R3, R4, X and X2 are as defined in the description.
专利号:WO-2024233563-A1 优先权日:2023-05-09 标 题:6,6-fused bicyclic amides and compositions for use as 15-prostaglandin dehydrogenase modulators 发明人:GREENMAN KEVIN LLOYD; WANG HUI-LING; WEIRES NICHOLAS ANTHONY; ALLEN JOHN G; AMEGADZIE ALBERT K; BOURBEAU MATTHEW P; LI KEXUE 权利人:AMGEN INC 摘要:The present disclosure provides novel 15-hydroxy-prostaglandin dehydrogenase inhibitors, pharmaceutical compositions comprising such compounds, and methods of using such compounds and compositions in treating 15-hydroxy-prostaglandin dehydrogenase-mediated disease. Also provided are methods of making such compounds and intermediates thereof. The compounds have a structure of Formula (I): or a pharmaceutically acceptable salt thereof; wherein is Formula (i) or Formula (ii) Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:US-2011021532-A1 优先权日:2008-04-22 标题 :Novel substituted heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:POWELL DAVID; LEBRUN MARIE-EVE; BHAT SATHESH; RAMTOHUL YEEMAN K 权利人:MERCK FROSST CANADA LTD 摘要:Substituted heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis. Formula (I).
专利号:RU-2193036-C2 优先权日:1997-02-25 标 题:Derivatives of imidazo[1,2-a]pyridine, methods of their synthesis, pharmaceutical preparation based on thereof, method of inhibition of gastric acid secretion, method of treatment of gastroenteric inflammatory diseases and method of treatment of states with helicobacter pylori infection
参考文献:10.1107/s1600536811017077 摘要:Dahmani S, Kandri Rodi Y, Luis SV, Essassi el M, El Ammari L. Ethyl 8-amino-6-bromoimidazo[1,2-a]pyridine-2-carb-oxy-late. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1390.