📜恩前列素中间体置于jones Reagent,Sodium Methylsulfinylcarbanide,二异丁基氢化铝,对甲苯磺酸,溶剂黄146体系中,用 正己烷,二氯甲烷,丙酮,甲苯 作为反应溶剂,化学反应 16.91H,反应生成 硫前列酮 参考文献:N-(Methanesulfonyl)-16-Phenoxyprostaglandin Carboxamides: Tissue-Selective,Uterine Stimulants 标题:N-(Methanesulfonyl)-16-Phenoxyprostaglandin Carboxamides: Tissue-Selective,Uterine Stimulants 摘要:In An Effort To Develop Tissue-Selective Prostaglandin Analogues Resistant To The Metabolic Inactivating Pathways Of The Natural Materials,Hybrid Compounds Modified Both At C-1 With A Sulfonimide Moiety And In The N-Amylcarbinol Side Chain With Substituted Phenoxy Groups Were Synthesized And Evaluated In A Variety Of In Vitro Models. Several Of These Analogues Exhibited Potent,Tissue-Selective,Uterine Stimulant Activity,A Finding Subsequently Confirmed In Clinical Studies With One Member Of This Series,N-(Methanesulfonyl)-16-Phenoxy-Omega-Tetranor-Pge2-Carboxamide (Cp-34089/zk-57671,Sulprostone). DOI:10.1021/jm00143A018
专利号:WO-9614060-A1 优先权日:1994-11-04 标题 :Use of receptor agonists to stimulate superoxide dismutase activity 发明人:MARKLUND STEFAN L; STRAALIN PONTUS 权利人:MARKLUND STEFAN L; STRAALIN PONTUS 摘要:The present invention relates to the use of a substance for the manufacture of a composition for stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells. In particular, the invention relates to the use of a substance for the manufacture of a composition for prophylaxis or treatment of a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical. Further, the invention relates to a method for determining the effect of a substance with respect to stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells and to substances which have been selected by said method. Within the scope of the invention is a method of preventing, diminishing, controlling or inhibiting a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical in a patient who has been established to have a high risk of developing a such disease or disorder, or who has developed a such disease or disorder, the method comprising administering an effective amount of a substance which is capable of stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells.
专利号:US-10100028-B2 优先权日:2013-09-30 标 题:Synthesis routes for prostaglandins and prostaglandin intermediates using metathesis 发明人:YIANNIKOUROS GEORGE PETROS; KALARITIS PANOS; GAMAGE CHAMINDA PRIYAPUSHPA; AREFYEV DENIS VIKTOROVICH 权利人:IRIX PHARMACEUTICALS INC; PATHEON API SERVICES INC 摘要:Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.
专利号:US-5905091-A 优先权日:1996-07-03 标 题 :Enhancement of skin pigmentation by prostaglandins 发明人:FULLER BRYAN B 权利人:UNIV OKLAHOMA 摘要:A composition comprising a carrier and prostaglandin effective in stimulating synthesis of melanin in a human melanocyte thereby enhancing pigmentation of the human skin and optionally comprising a lysosomotropic agent, a phosphodiesterase inhibitor, and/or methylxanthines, and a method of use of the composition. Use of this composition promotes tanning of the human skin and increases photoprotection from ultraviolet radiation.
专利号:US-7772278-B2 优先权日:1999-03-01 标 题:Nitrosated and nitrosylated prostaglandins, compositions and methods of use 发明人:GARVEY DAVID S; GASTON RICKY D; LETTS L GORDON; DE TEJADA INIGO SAENZ; TAM SANG WILLIAM; WORCEL MANUEL 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one vasoactive agent. The invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E 1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. The invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions.
专利号:US-8476471-B2 优先权日:2009-07-13 标 题 :Synthesis of prostanoids 发明人:YIANNIKOUROS GEORGE PETROS; KALARITIS PANOS; GAMAGE CHAMINDA PRIYAPUSHPA; ABERNATHY STEPHANIE BOSSE 权利人:YIANNIKOUROS GEORGE PETROS; KALARITIS PANOS; GAMAGE CHAMINDA PRIYAPUSHPA; ABERNATHY STEPHANIE BOSSE; IRIX PHARMACEUTICALS INC 摘要:The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.
专利号:US-2022160788-A1 优先权日:2019-03-22 标题 :Bifunctional vectors allowing bcl11a silencing and expression of an anti-sickling hbb and uses thereof for gene therapy of b-hemoglobinopathies 发明人:MICCIO ANNARITA; AMENDOLA MARIO; BRUSSON MÉGANE; CAVAZZANA MARINA; MAVILIO FULVIO 权利人:INST NAT SANTE RECH MED; UNIV DEVRY VAL DESSONNE; ASSIST PUBLIQUE HOPITAUX PARIS APHP; UNIV PARIS; FOND IMAGINE 摘要:The #β-hemoglobinopathies #β-thalassemia (BT) and sickle cell disease (SCD) are the most frequent genetic disorders worldwide. These diseases are caused by mutations causing reduced or abnormal synthesis of the β-globin chain of the adult hemoglobin (Hb) tetramer. Here, the inventors intend to improve HSC-based gene therapy for β-thalassemia and SCD by developing an innovative, highly infectious LV vector expressing a potent anti-sickling β-globin transgene and a second biological function either increasing fetal γ-globin expression (for β-thalassemia and SCD). More particularly, the inventors have designed a novel lentivirus (LV), which carry two different functions: βAS3 gene addition and gene silencing. This last strategy allows the re-expression of the fetal γ-globin genes (HBG1 and HBG2) and production of the endogenous fetal hemoglobin (HbF). Elevated levels of HbF and HbAS3 (Hb tetramer containing βAS3-globin) will benefit the β-hemoglobinopathy phenotype by increasing the total amount of β-like globin that will: (i) reduce the alpha precipitates and improve the alpha/non alpha ratio in β-thalassemia, and (ii) reduce the sickling in SCD. This combined strategy will improve the β-hemoglobinopathy phenotype at a lower vector copy number (VCN) per cell compared to a LV expressing the βAS3 alone.
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合成参考文献
参考文献:10.1124/mol.119.115964 摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.