📜1-N-Boc-4-(2-叔丁氧基-2-氧代乙基)哌嗪置于盐酸体系中,用 甲醇,水 用作溶剂,化学反应 12.0H,以350 Mg的收率获得2-(哌嗪-1-基)-乙酸水合物 参考文献: Novel Tetrahydropyridopyrimidines For The Treatment And Prophylaxis Of Hbv Infection[fr] Nouvelles Tétrahydropyridopyrimidines Pour Le Traitement Et La Prophylaxie D'Une Infection Par Le Vhb 标题: Novel Tetrahydropyridopyrimidines For The Treatment And Prophylaxis Of Hbv Infection[fr] Nouvelles Tétrahydropyridopyrimidines Pour Le Traitement Et La Prophylaxie D'Une Infection Par Le Vhb 摘要:本发明提供了具有一般式(i)的新化合物,其中r1至r4,A,W,Q和y如本文所述,包括这些化合物的组合物和使用这些化合物的方法.
专利号:WO-0061545-A1 优先权日:1999-04-14 标题 :Methods for solid phase combinatorial synthesis of integrin inhibitors 发明人:GOPALSAMY ARIAMALA; YANG HUI YU 权利人:AMERICAN HOME PROD 摘要:Compounds of the formula (I) are useful in the treatment of various disorders including, but not limited to, cancer (tumor metathesis, tumorgenesis/tumor growth), angiogenesis (as in cancer, diabetic retinopathy, rheumatoid arthritis), restenosis (following balloon angioplasty or stent implantation), inflammation (as in rheumatoid arthritis, psoriasis), bone diseases (osteopenia induced by bone metastases, immobilization and glucocortocoid treatment, periodontal disease, hyperparathyroidism and rheumatoid arthritis), and as antiviral agents. Novel method of making compounds of formula (I) are also provided.
专利号:US-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
专利号:US-6528275-B1 优先权日:1996-04-24 标题:Substrates and inhibitors of proteolytic enzymes 发明人:QUIBELL MARTIN; JOHNSON TONY; HART TERANCE 权利人:MEDIVIR UK LTD 摘要:The present invention relates to the field of compounds which are substrates or inhibitors of proteolytic enzymes and to apparatus and methods for identifying substrates or inhibitors for proteolytic enzymes. We have devised a combinatorial method for the rapid indentification of binding motifs which will greatly expedite the synthesis of inhibitors of a variety of proteolytic enzymes such as aspartyl proteases, serine proteases, metallo proteases and cysteinyl proteases.
专利号:US-11225655-B2 优先权日:2010-04-16 标题:Bi-functional complexes and methods for making and using such complexes 发明人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK 权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS 摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.
专利号:US-11702652-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries
专利号:US-2009264300-A1 优先权日:2005-12-01 标题 :Enzymatic encoding methods for efficient synthesis of large libraries
参考文献:10.1177/1087057116635503 摘要:Voter AF, Manthei KA, Keck JL. A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. J Biomol Screen. 2016 Jul;21(6):626–33.