CAS: 64-85-7; (8S,9S,10R,13S,14S,17S)-17-(2-Hydroxyacetyl)-10,13-Dimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-Tetradecahydro-3H-Cyclopenta[a]Phenanthren-3-One

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黄体酮置于cytochrome P450 46A35 Mutant体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应生成 去氧皮质酮
参考文献:细胞色素 P450 挖掘用于蟾蜍二烯内酯多样化
标题:细胞色素 P450 挖掘用于蟾蜍二烯内酯多样化
摘要:蟾蜍二烯内酯是一类在 C17 处具有独特 α-吡喃酮环的类固醇,主要由蟾蜍产生,由 100 多种直系同源物组成.它们具有强效的强心和抗肿瘤活性,是中药蟾酥和华蟾素的活性成分.直接从蟾蜍中提取成本高昂,化学合成也很困难,限制了具有多种修饰和痕量含量的活性蟾蜍二烯内酯的获取.在这项工作中,基于转录组和基因组分析,使用基于酵母的筛选平台,我们从蟾蜍中获得了八种细胞色素p450(cyp)酶,它们在不同位点催化蟾蜍灵和resibufogenin的羟基化.此外,据报道,一种真菌 Cyp 酶 Sth10 被发现在蟾蜍灵和resibufogenin的多个位点修饰中发挥作用.共生产并鉴定了15种蟾蜍二烯内酯,其中6种为首次发现.所有化合物均能有效抑制肿瘤细胞的增殖,特别是19-羟基-蟾毒灵(2)和1β-羟基-蟾毒灵(3),它们是由cyp46A35催化蟾毒灵羟基化产生的. Cyp46A35的催化效率提
DOI:10.1021/acschembio.4C00089

专利信息

专利号:WO-9101724-A1
优先权日:1989-07-27
标题 :Renal-selective prodrugs for the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:EP-1360308-B1
优先权日:2001-01-25
标题 :Concatemers of differentially expressed multiple genes
发明人：GOLDSMITH NEIL; SORENSEN ALEXANDRA M P SANTANA; NIELSEN SOREN V S; NAESBY MICHAEL
权利人:EVOLVA LTD
摘要:In the present invention are disclosed concatemers of concatenated expression cassettes and vectors that enable the synthesis of such concatemers. The concatemer comprises in the 5' ->3' direction a cassette of nucleotide sequence of the general formula [rs2-SP-PR-X-TR-SP-rs1]n wherein rs1 and rs2 together denote a functional restriction site, SP individually denotes a spacer of at least two nucleotide bases, PR denotes a promoter, capable of functioning in a cell, X denotes an expressible nucleotide sequence, TR denotes a terminator, and SP individually denotes a spacer of at least two nucleotide bases, and n >/= 2, and wherein at least a first cassette is different from a second cassette. The main purpose of these concatemers is the controllable and co-ordinated expression of large numbers of heterologous genes in a single host. Furthermore, the invention relates to a concatemer of cassettes of nucleotide sequences and a method for preparing the concatemers. In a further aspect, the invention relates to transgenic host cells comprising at least one concatemer according to the invention, as well as to a method for preparing the transgenic host cells. Finally, the invention relates to a vector comprising a cassette of nucleotides, a method for preparing said vector, a nucleotide library comprising at least two primary vectors each comprising a cassette of nucleotides, a method for preparing the library.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:WO-2024147726-A1
优先权日:2023-01-05
标 题:Synthesis of desoxycorticosterone pivalate
发明人：RENTERIA GÓMEZ MARVIN; AGUILAR BRIONES RAÚL; DE LA ROSA BARRALES ARTURO
权利人:INTERQUIM S A DE C V
摘要:The invention provides a process for synthesising desoxycorticosterone pivalate (DCP), which comprises the following steps: brominating the 21-position of pregnenolone with copper bromide; substituting the 21-bromo pregnenolone with potassium pivalate; and transforming the 3-hydroxy group of the pregnenolone into ketone and purifying the DCP obtained, wherein the purity and total yield of the DCP are greater than those achieved using methods described in the prior art.