专利号:US-5874433-A 优先权日:1993-11-29 标题 :Blocking utilization of tetrahydrobiopterin to block induction of nitric oxide synthesis 发明人:GROSS STEVEN S 权利人:CORNELL RES FOUNDATION INC 摘要:Inhibitor of the use of tetrahydrobiopterin as a cofactor for nitric oxide synthase, e.g., substituted 4-phenyl(hydropyridines) such as 1-methyl-4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine or, 4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine) or tetrahydropterin analog which does not replace tetrahydrobiopterin as a substrate for nitric oxide synthase such as (6R,S)-6,7-dimethyl-tetrahydropterin or (6R,S)-tetrahydrofolic acid or 2,4-diamino-, 2,6-diamino, or 4,6-diamino mono- or disubstituted pyrimidines or the corresponding pyrimidine-3-oxides such as 2,4-diamino-6-(diethylamino)pyrimidine, 2,4-diamino-6-piperidino-pyrimidine-3-oxide, 2,4-diamino-6-hydroxypyrimidine, 4,6-diamino-2-hydroxypyrimidine or 2,5-diamino-4,6-dihydroxypyrimidine is administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylaxis or treatment of cytokine- or endotoxin-induced hypotension (e.g., septic shock). The latter two types are advantageously administered with nitric oxide synthase inhibitors (concurrent therapy) or to potentiate the effect of α 1 -adrenergic agonists in the prophylaxis or treatment of induced hypotension.
专利号:WO-2021078995-A1 优先权日:2019-10-25 标 题 :Selective polypeptide synthesis stalling assay and compound 发明人:STROUS GERARDUS JACOBUS ANTONIUS MARIA; MOL JAN ADRIANUS; VAN DER VELDEN LIEKE MARIE; KLUMPERMAN JUDITH; MAAS PETRUS EMMANUEL MARIE; PIET DENNIS PATRICK; DE KLERK-SPRENKELS NANDA ELISABETH; TIJHUIS JOHANN HEINRICH; VIÉTOR HENDRIK ENGELBERTUS; MAURICE MADELON MARIA; VAN DER KRIFT FELIX 权利人:UMC UTRECHT HOLDING BV; UNIV UTRECHT HOLDING BV; BIMINI BIOTECH B V 摘要:The invention relates to compounds, in particular pyrimidine-2,4-diamines, analogues and salts thereof and pharmaceutical compositions comprising pyrimidine-2,4-diamines analogues and salts thereof for use in the treatment and prevention of a disease, in particular a growth hormone receptor-dependent condition. The invention also relates to methods of using these compounds and compositions to treat physiological disorders related to the amount or activity of growth hormone. In a particular embodiment, the invention relates to a compound according to formula 1 for use in the treatment or prevention of a disease in a subject.
专利号:US-8372971-B2 优先权日:2004-08-25 标 题:Heterocyclic compounds and methods of use 发明人:WRASIDLO WOLFGANG; DNEPROVSKAIA ELENA 权利人:TARGEGEN INC; WRASIDLO WOLFGANG; DNEPROVSKAIA ELENA 摘要:Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
专利号:WO-9514468-A1 优先权日:1993-11-29 标题:Blocking utilization of tetrahydrobiopterin to block induction of nitric oxide synthesis
专利号:EP-0730451-A4 优先权日:1993-11-29 标题 :INHIBITION OF THE USE OF TETRAHYDROBIOPTERIN TO BLOCK THE INDUCTION OF NITRIC OXIDE SYNTHESIS
专利号:EP-0730451-A1 优先权日:1993-11-29 标题 :Blocking utilization of tetrahydrobiopterin to block induction of nitric oxide synthesis
参考标题:Lewis Acid-Catalyzed Synthesis Of 4-Aminopyrimidines: A Scalable Industrial Process 作者:Ulla Létinois,Jan Schütz,Ralph Härter,Rinke Stoll,Florian Huffschmidt,Werner Bonrath,Reinhard Karge |发布日期:2013.3.15 摘要:Pyrimidine Synthesis Starting From Acrylonitrile Has Been Known Since The 1960S. The New Lewis Acid-Catalyzed Condensation Reaction Allows The Synthesis Of 4-Aminopyrimidines Starting From The Easily Accessible Chemical Acrylonitrile Without The Need For Carcinogenic Chemicals And Costly Derivatization In Up To 90% Yield. The Method Is Versatile And Applicable For Industrial-Scale Synthesis Of Biologically
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 323. 摘要:J. C. Gage. J. Chem. Soc. 1949, 469. 摘要:B. Roth and J.Z. Strelitz. J. Org. Chem. 34, 821 (1969).