CAS: 305-03-3; 4-(4-(Bis(2-Chloroethyl)Amino)Phenyl)Butanoic Acid

上下游产品

4-(4-氨基苯)丁酸甲酯置于盐酸,溶剂黄146,三氯氧磷体系中,用 甲苯 作为反应溶剂,化学反应生成 苯丁酸氮芥
参考文献:Synthesis And Pharmacokinetic Profile Of A Quaternary Ammonium Derivative Of Chlorambucil,A Potential Anticancer Drug For The Chemotherapy Of Chondrosarcoma
标题:Synthesis And Pharmacokinetic Profile Of A Quaternary Ammonium Derivative Of Chlorambucil,A Potential Anticancer Drug For The Chemotherapy Of Chondrosarcoma
摘要:As A Part Of Our Targeting Program Based On The Affinity Of The Quaternary Ammonium Moiety For Cartilage,Our Objective Was To Develop More Selective Anticancer Drugs Towards Chondrosarcoma That Would Concentrate In This Malignant Cartilaginous Tissue And So Improve The Therapeutic Index Through A Reduction Of Side Effects. For This Purpose We Have Synthesized And Labeled With C-14 A Quaternary Ammonium (Qa) Derivative Of Chlorambucil. Biological Studies Performed In Rats Showed That [c-14]-Cqa And [c-14]-Chlorambucil Exhibited Different Pharmacokinetic Profiles. The Blood Elimination Of [c-14]-Cqa Was Faster Than That Of Parent Compound. [c-14]-Cqa Was Principally Excreted By The Fecal Way. However,Until 15 Min After Administration,Levels Of Radioactivity Were Measured In Cartilaginous Tissues Of Rats Given [c-14]-Cqa Which Was Not The Case For The Rats Which Had Received [c-14]-Chlorambucil. Although Rates Of Radioactivity Were Quantified Only During 15 Min,These Results Prove That The Functionalization Of Chlorambucil By A Quaternary Ammonium Group Allows The Molecule To Be Carried Selectively To Cartilaginous Tissues. (C) 2003 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2003.09.006

专利信息

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:WO-2004011474-A1
优先权日:2002-07-31
标题:Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-6653468-B1
优先权日:2002-07-31
标 题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-7816544-B2
优先权日:2004-03-23
标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species
发明人：JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A
权利人:UNIV BOSTON
摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

专利号:US-2010137421-A1
优先权日:2006-11-08
标题 :Small molecule therapeutics, synthesis of analogues and derivatives and methods of use
发明人：THEODORAKIS EMMANUEL; BATOVA AYSE
权利人:THEODORAKIS EMMANUEL; BATOVA AYSE
摘要:Provided herein are compounds that are inducers of apoptosis activators of caspases and pharmaceutically acceptable derivatives thereof. Also provided are methods of synthesis of the compounds and methods for treatment of diseases in which there is uncontrolled cell growth and spread of abnormal cells, such as cancers, by administering the compounds.