专利号:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-9994508-B2 优先权日:2012-12-11 标 题:Versatile and functionalised intermediates for the synthesis of vitamin D and novel vitamin D derivatives 发明人:LOPEZ PEREZ BORJA; SIGUEIRO PONTE RITA; MAESTRO SAAVEDRA MIGUEL A; MOURINO MOSQUERA ANTONIO 权利人:ENDOTHERM GMBH 摘要:Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.
专利号:US-6090810-A 优先权日:1995-09-01 标题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 发明人:KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A 权利人:ALLERGAN SALES INC 摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
专利号:US-8637555-B2 优先权日:2003-10-31 标题:Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof 发明人:SEMPLE GRAEME; SCHRADER THOMAS; SKINNER PHILIP J; COLLETTI STEVEN L; GHARBAOUI TAWFIK; IMBRIGLIO JASON E; JUNG JAE-KYU; LIANG RUI; RAGHAVAN SUBHAREKHA; SCHMIDT DARBY; TATA JAMES R 权利人:SEMPLE GRAEME; SCHRADER THOMAS; SKINNER PHILIP J; COLLETTI STEVEN L; GHARBAOUI TAWFIK; IMBRIGLIO JASON E; JUNG JAE-KYU; LIANG RUI; RAGHAVAN SUBHAREKHA; SCHMIDT DARBY; TATA JAMES R; ARENA PHARM INC; MERCK & CO INC 摘要:The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
专利号:US-5877207-A 优先权日:1996-03-11 标 题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 发明人:KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A 权利人:ALLERGAN SALES INC 摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
专利号:US-2008227851-A1 优先权日:2007-03-12 标题 :Laulimalide and laulimalide analogs 发明人:WENDER PAUL A 权利人:WENDER PAUL A 摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.
参考标题:Convergent Synthesis Of Taxol Skeleton Via Decarbonylative Radical Coupling Reaction 作者:Hiroaki Matoba,Takahiro Watanabe,Masanori Nagatomo,Masayuki Inoue |发布日期:2018.12.7 摘要:The Highly Oxygenated 6/8/6-Membered Abc-Ring 2 Of Taxol Was Assembled In A Convergent Fashion. A Decarbonylative Radical Reaction Between α-Alkoxyacyl Telluride 4 And Cyanocyclohexenone 5 Linked The A- And C-Rings And Stereoselectively Installed The C2- And C3-Tertiary Carbon Centers Of 3. After The C8-Quaternary Stereocenter Was Constructed, The C9-Methyl Ketone And The C11-Vinyl Triflate Of 30 Participated
合成参考文献
摘要:Renzi, P.; Moliterno, M.; Salvio, R.; Bella, M., Science of Synthesis: Applications of Domino Transformations in Organic Synthesis, (2015) 2, 379. 摘要:Svatunek, D.; Houk, K. N., Science of Synthesis, (2021) , 419.