CAS: 37441-50-2; 1,2-Thiazinane 1,1-Dioxide

相似化合物

885678-35-3 1801456-92-7 913836-20-1

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📜4-氯丁烷-1-磺酰胺置于sodium Ethanolate体系中,用 乙醇 用作溶剂,化学反应 5.0H,以69%的收率获得1,4-丁烷磺内酰胺
参考文献: 3-(1,1-Dioxotetrahydro-1,2-Thiazin-2-yl) Or 3-(1,1-Doxo-Isothiazolidin-2Yl) Substituted Benzamide Compounds As Asp2 Inhibitors[fr] Composes De Benzamide A Substitution 3-(1,1-Dioxotetrahydro-1,2-Thiazin-2-yl) Ou 3-(1,1-Doxo-Isothiazolidin-2Yl) Utilises Comme Inhibiteurs De L'Enzyme Asp2
标题: 3-(1,1-Dioxotetrahydro-1,2-Thiazin-2-yl) Or 3-(1,1-Doxo-Isothiazolidin-2Yl) Substituted Benzamide Compounds As Asp2 Inhibitors[fr] Composes De Benzamide A Substitution 3-(1,1-Dioxotetrahydro-1,2-Thiazin-2-yl) Ou 3-(1,1-Doxo-Isothiazolidin-2Yl) Utilises Comme Inhibiteurs De L'Enzyme Asp2
摘要:本发明涉及具有a Sp2(β-分泌酶,Bace1或memapsin)抑制活性的化学式(i)的羟基乙烯化合物,其制备过程,含有它们的组合物以及它们在治疗由高β-淀粉样蛋白水平或β-淀粉样蛋白沉积特征的疾病中的应用,特别是阿尔茨海默病,其中r1代表化学式zc的基团.

专利信息

专利号:US-8471010-B2
优先权日:2008-05-13
标题:Synthesis of dihydrothieno[3,2-d]pyrimidine diols
发明人：FRUTOS ROGELIO P; TAMPONE THOMAS G; MULDER JASON ALAN; KRISHNAMURTHY DHILEEPKUMAR; SENANAYAKE CHRIS H
权利人:FRUTOS ROGELIO P; TAMPONE THOMAS G; MULDER JASON ALAN; KRISHNAMURTHY DHILEEPKUMAR; SENANAYAKE CHRIS H; BOEHRINGER INGELHEIM INT
摘要:The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.

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:US-8487108-B2
优先权日:2005-11-14
标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors
发明人：BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T
权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC
摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

专利号:US-8541569-B2
优先权日:2008-09-06
标题:Phosphoramidites for synthetic RNA in the reverse direction, efficient RNA synthesis and convenient introduction of 3'-end ligands, chromophores and modifications of synthetic RNA
发明人：SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P
权利人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P; CHEMGENES CORP
摘要:The present invention provides building blocks and methods for synthesizing very pure RNA in a form that can efficiently be modified at the 3′ end. Reverse RNA monomer phosphoramidites have been developed for RNA synthesis in 5′→3′ direction, leading to very clean oligo synthesis that allows for the introduction of various modifications at the 3′-end cleanly and efficiently. Higher coupling efficiency per step have been observed during automated oligo synthesis with the reverse RNA amidites disclosed herein, resulting in a greater ability to achieve higher purity and produce very long oligonucleotides. The use of the reverse RNA phosphoramidites in the synthetic process of this invention leads to oligonucleotides free of N+1 species.

专利号:US-9994558-B2
优先权日:2013-09-20
标题 :Multicyclic compounds and methods of using same
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).

专利号:US-7186827-B2
优先权日:2003-10-30
标题:Dipeptide synthesis
发明人：BUSACCA CARL ALAN; HADDAD NIZAR; KAPADIA SURESH R; SMITH KEENAN LANA; LORENZ JON CHARLES; SENANAYAKE CHRIS HUGH; WEI XUDONG
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section: