专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-2009247754-A1 优先权日:2008-03-25 标 题:Method of preparing huperzine a and derivatives thereof 发明人:UNDERINER GAIL; GIBSON FRANK; HE LINLI; MEERA HARIHARA SUBRAMANIAN; GNANADEEPAM JESUDOSS MERCY; SAIGANESH RAMANATHAN; TUDHOPE STEPHEN R; AZADI-ARDAKANI MANOUCHEHR 权利人:DEBIOPHARM SA 摘要:The present invention is related to the synthesis of huperzine A. The synthesis includes a variety of process steps that increase productivity, reduce safety concerns, and allow for increasing production of compounds of desired optical isomer. The inventive methods may encompass a single improved reaction step that may be incorporated into a known reaction process for synthesizing huperzine A or a derivative thereof to improve the overall reaction. The inventive methods also encompass complete synthesis methods for preparing huperzine A or a derivative thereof.
专利号:US-8067465-B2 优先权日:2002-01-15 标题:Tricyclic-bis-enone derivatives and methods of use thereof 发明人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO 权利人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO; DARTMOUTH COLLEGE 摘要:Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
专利号:US-6486169-B1 优先权日:2002-02-19 标题:Botanical drug for treatment and prevention of alzhimer's disease 发明人:LIU YAGUANG 摘要:The present invention related to safe botanical drug for treatment and prevention of Alzheimer's disease. Specifically, this invention proves a safe botanical drug, Huperzine (HUE) and Clausenamide (CLE) and their preparation.HUE has the following pharmaceutical functions: inhibiting acetylcholinesterase (CAT), increasing memory, decreasing Alzheimer amyloid protein, increasing RNA and protein synthesis of brain, increasing calcium in brain, decreasing superoxide anion.CLE has the following pharmaceutical functions: increasing memory, decreasing Alzheimer amyloid protein, increasing RNA and protein synthesis of brain, increasing calcium in brain, decreasing superoxide anion, increasing long-term potentiation and increasing dopanmine (DA). It is important that HUE combined with CLE have stronger function as mentioned above.
专利号:US-2002040032-A1 优先权日:2000-07-07 标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system 发明人:GLASKY MICHELLE S; LAHIRI DEBOMOY K; FARLOW MARTIN R 摘要:A method of increasing the synthesis and/or secretion of synaptophysin comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.
参考文献:10.1007/s11274-014-1678-0 摘要:Mao Z, Luo R, Luo H, Tian J, Liu H, Yue Y, Wang M, Peng Y, Zhou L. Separation and purification of bioactive botrallin and TMC-264 by a combination of HSCCC and semi-preparative HPLC from endophytic fungus Hyalodendriella sp. Ponipodef12. World Journal of Microbiology and Biotechnology. 2014 Jun 05;30(9):2533–42. doi: 10.1007/s11274-014-1678-0.