专利号:US-8487094-B2 优先权日:2008-07-25 标题 :Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 发明人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA 权利人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA; BOEHRINGER INGELHEIM INT 摘要:Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).
专利号:WO-2023203374-A1 优先权日:2022-04-20 标 题 :[1,2]selenazolo[2,3-a]pyridin-8-ium inhibitors of pyruvate kinase isoform m2 发明人:ARSENJANS PAVELS; DIMITRIJEVS PAVELS; MAKRECKA-KUKA MARINA 权利人:LATVIAN INST ORGANIC SYNTHESIS 摘要:The present invention relates to a novel isoselenazolopyridinium salts as anticancer agents by inhibiting pyruvate kinase isoform M2 (PKM2) activity, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of various diseases and disorders by administration of such substances.
专利号:US-9919064-B2 优先权日:2012-08-10 标 题 :Compositions, methods, and systems for the synthesis and use of imaging agents 发明人:CESATI RICHARD R; RADEKE HEIKE S; PANDEY SURESH K; PUROHIT AJAY; ROBINSON SIMON P 权利人:LANTHEUS MEDICAL IMAGING INC 摘要:The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.
专利号:US-2010004245-A1 优先权日:2006-10-20 标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K 权利人:MERCK FROSST CANADA LTD 摘要:Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. 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; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
专利号:WO-2009017671-A1 优先权日:2007-07-26 标题 :Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
专利号:US-2010256363-A1 优先权日:2007-07-26 标题 :SYNTHESIS OF INHIBITORS OF 11ß-HYDROXYSTEROID DEHYDROGENASE TYPE 1