CAS: 404951-53-7; Dacinostat

上下游产品

(2E)-3-[4-([(2-Hydroxyethyl)-[2-(1H-Indol-3-yl)Ethyl]Amino]Methyl)Phenyl]-2-Propenoic Acid Methyl Ester 619324-72-0
N-Hydroxy-3-[4-({[2-(Tert-Butyldimethylsilanyloxy)-Ethyl]-[2-(1H-Indol-3-yl)-Ethyl]-Amino}-Methyl)-Phenyl]-(2E)-2-Propenamide 404951-57-1
(2E)-3-[4-[[[2-(1H-Indol-3-yl)Ethyl]Amino]Methyl]Phenyl]-2-Propenoic Acid Methyl Ester 404951-55-9
色胺 Tryptamine 61-54-1

(2E)-3-[4-[[[2-(1H-Indol-3-yl)Ethyl]Amino]Methyl]Phenyl]-2-Propenoic Acid Methyl Ester置于sodium Hydroxide,羟胺,Potassium Carbonate体系中,用 甲醇,乙腈 作为反应溶剂,化学反应 18.0H,反应生成 达西司特
参考文献:N-Hydroxy-3-Phenyl-2-Propenamides As Novel Inhibitors Of Human Histone Deacetylase With In Vivo Antitumor Activity: Discovery Of (2E)-N-Hydroxy-3-[4-[[(2-Hydroxyethyl)[2-(1H-Indol-3-yl)Ethyl]Amino]Methyl]Phenyl]-2-Propenamide (Nvp-Laq824)
标题:N-Hydroxy-3-Phenyl-2-Propenamides As Novel Inhibitors Of Human Histone Deacetylase With In Vivo Antitumor Activity: Discovery Of (2E)-N-Hydroxy-3-[4-[[(2-Hydroxyethyl)[2-(1H-Indol-3-yl)Ethyl]Amino]Methyl]Phenyl]-2-Propenamide (Nvp-Laq824)
摘要:A Series Of N-Hydroxy-3-Phenyl-2-Propenamides Were Prepared As Novel Inhibitors Of Human Histone Deacetylase (Hdac). These Compounds Were Potent Enzyme Inhibitors,Having Ic(50)S < 400 Nm In A Partially Purified Enzyme Assay. However,Potency In Cell Growth Inhibition Assays Ranged Over 2 Orders Of Magnitude In Two Human Carcinoma Cell Lines. Selected Compounds Having Cellular Ic50 < 750 Nm Were Tested For Maximum Tolerated Dose (Mtd) And For Efficacy In The Hct116 Human Colon Tumor Xenograft Assay. Four Compounds Having An Mtd 100 Mg/kg Were Selected For Dose-Response Studies In The Hct116 Xenograft Model. One Compound,9 (Nvp-Laq824),Had Significant Dose-Related Activity In The Hct116 Colon And A549 Lung Tumor Models,High Mtd,And Low Gross Toxicity. On The Basis,In Part,Of These Properties,9 Has Entered Human Clinical Trials In 2002.
DOI:10.1021/jm030235W

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

专利号:US-9365532-B1
优先权日:2011-02-14
标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines
发明人：ISAACMAN STEVEN
权利人:ISAACMAN STEVEN; NANOMETICS LLC
摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.

专利号:US-2019031650-A1
优先权日:2016-01-29
标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies
发明人：HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN
权利人:UNIV YALE
摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.