CAS: 382180-17-8; N1-Hydroxy-N8-(Pyridin-3-yl)Octanediamide

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CAS号405096-07-3 8-oxo-8-(3-pyri... | CAS号3946-32-5 辛二酸单甲酯

8-Oxo-8-(3-Pyridinylamino)-octanoic Acid Methyl Ester置于氢氧化钾,盐酸羟胺体系中,用 甲醇 作为反应溶剂,以47%的收率获得产物n-羟基-N'-3-吡啶基辛二酰胺
参考文献:人组蛋白脱乙酰基酶的抑制剂:直链异羟肟酸酯的合成以及酶和细胞活性.
标题:人组蛋白脱乙酰基酶的抑制剂:直链异羟肟酸酯的合成以及酶和细胞活性.
摘要:组蛋白脱乙酰基酶(hdac)的抑制剂已显示出可诱导人肿瘤细胞系的终末分化,并在体内具有抗肿瘤作用.我们准备了辛二酰苯胺异羟肟酸(saha)和曲古抑菌素a的类似物,并已在人类hdac酶抑制试验,P21(waf1)(p21)启动子试验和单层生长抑制试验中对其进行了评估.发现一种化合物4-(二甲基氨基)-N-[7-(羟基氨基)-7-氧庚基]-苯甲酰胺可不同地影响一组八个人类肿瘤细胞系的生长.
DOI:10.1021/jm015568C

专利信息

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

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-2025064840-A1
优先权日:2021-12-16
标 题 :Drug delivery systems based on endoperoxides useful in diagnosis and therapy, and methods thereof
发明人：SILVA MAGALHAES DIOGO; MOREIRA RUI; LOPES FRANCISCA; RODRIGUES CECILIA; MARQUES VANDA
权利人:FACULDADE DE FARMACIA DA UNIV DE LISBOA
摘要:The present invention relates to novel drug delivery systems based on endoperoxide moieties such as 1,2,4,5-tetraoxanes, namely compounds of formula I, appropriately modified to release active pharmaceutical ingredients (API) in the presence of higher levels of Fe (II), in a subject, whereinIron metabolism dysregulation occurs in diseases such as malaria and cancer. Therefore, the present invention also relates to biomarkers comprising said compounds of formula I.Another aspect, the present invention relates to a process of synthesis of compounds of formula I and respective intermediaries.Further, the present invention also relates to a process for labelling, detection, and identification of tumours in a tissue sample.The present invention is thus applicable to the medical and pharmacological areas, in related to particular the ones cancer detection and treatment, and malaria treatment.

专利号:US-2024262839-A1
优先权日:2020-10-13
标 题 :Scalable anion capture macrocycles
发明人：FLOOD AMAR HUGH; DOBSCHA JAMES ROBERT
权利人:FLOOD AMAR HUGH; DOBSCHA JAMES ROBERT; UNIV INDIANA RES & TECH CORP
摘要:The present disclosure concerns scalable single-pot synthesis, anion binding features, liquid-liquid extraction of salts of the triazolophane macrocycle of Formula (I): n n n n n n n n n n wherein the substituents R are independently selected from the group consisting of a linear and branched alkyl, a linear and branched alkyl substituted with an ionizable functional group such as an amine or carboxylic acid, a linear and branched alkoxy (R=—OR), an alkyl comprising —O(CH 2 CH 2 O) n CH 3 , where n is 1-20, an amide —CO—NR 1 R 2 , where R 1 is any alkyl, organic substituent, R 2 is any alkyl, organic substituent, wherein R 1 and R 2 may be identical or different, —OCO—R, wherein R is any alkyl, organic substituent, an aromatic ring and their substituted analogues, any length and sequence of natural and unnatural amino acids that make up a peptide chain, and —C≡C—R where R is any alkyl, organic substituent.