专利号:US-9018371-B2 优先权日:2007-03-07 标 题 :Adenosine derivatives, method for the synthesis thereof, and the pharmaceutical compositions for the prevention and treatment of the inflammatory diseases containing the same as an active ingredient 发明人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH 权利人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH; FM THERAPEUTICS CO LTD; US OF AMERICA AS REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES THE OFFICE OF TECHNO 摘要:Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A 3 adenosine receptors and act as A 3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.
专利号:US-2024368164-A1 优先权日:2021-04-28 标 题 :Purine nucleosides, their intermediates, and methods of preparation thereof 发明人:RAVI RAMA SURESH; JACOBSON KENNETH A; POE RUSSELL BIRCH 权利人:ASTROCYLE PHARMACEUTICALS INC; US HEALTH 摘要:The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.
专利号:US-2023286975-A1 优先权日:2020-07-07 标题:Improved method for the production of lysergic acid diethylamide (lsd) and novel derivatives thereof 发明人:GRILL MATTHIAS 权利人:COMPASS PATHFINDER LTD 摘要:The present invention provides an improved method for the production of lysergic acid diethylamide (LSD) for GMP purposes. Furthermore, the present invention provides novel LSD derivatives of formula I as well as their synthesis and purification. Due to the affinity of the presented substances for the 5-HT 2A receptor, the invention may find application in numerous forms of therapy, such as against depression or drug addiction.
专利号:US-2007105821-A1 优先权日:2005-02-25 标 题 :Methods for the synthesis of unsymmetrical cycloalkyl substituted xanthines
专利号:WO-9636631-A1 优先权日:1995-05-19 标题:Multiply-substituted fullerenes and methods for their preparation and characterization 发明人:MURPHY RANDALL B; WILSON STEPHEN R; LU QUING 权利人:SPHERE BIOSYSTEMS INC 摘要:The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the Cn fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by 3He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.
专利号:US-2023271983-A1 优先权日:2020-07-29 标题 :Functionalized isonitriles and products, preparation and uses thereof 发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA 权利人:UNIV SANTIAGO COMPOSTELA 摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
参考标题:Ring Opening Reactions: Synthesis Of Aicar Analogs As Potential Antimetabolite Agents 作者:S. Costanzi,C. Lambertucci,F. R. Portino,R. Volpini,S. Vittori,G. Cristalli |发布日期:2005.4.1 摘要:Adenosine, We Planned The Synthesis Of The Corresponding Derivatives Of The 5′-N-Ethylcarboxamidoadenosine (Neca). For This Purpose, We Designed The Synthesis Of 2-Mercapto-Neca To Be Pursued By Means Of An "Opening-Closure" Method. We Obtained The Open Aicar Analog; However, Ring Closure Efforts Failed To Give The Desired Compound. The Newly Synthesized Aicar Derivative Could Potentially Be Endowed With Antiviral
合成参考文献
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