CAS: 83602-39-5; (3R,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-Ethyl-33-((1R,2R,E)-1-Hydroxy-2-Methylhex-4-En-1-yl)-6,9,18,24-Tetraisobutyl-3,21-Diisopropyl-1,4,7,10,12,15,19,25,28-Nonamethyl-1,4,7,10,13,16,19,22,25,28,31-Undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29

上下游产品

Cyclosporin A 79217-60-0

7,8-Secocyclosporin-7-Carboxylic Acid置于4-二甲氨基吡啶,1-丙基磷酸酐体系中,用 二氯甲烷,乙酸乙酯 作为反应溶剂,化学反应 30.0H,以67%的收率获得产物环孢菌素 H
参考文献:Expanding The Limits Of Isonitrile-Mediated Amidations: On The Remarkable Stereosubtleties Of Macrolactam Formation From Synthetic Seco-Cyclosporins
标题:Expanding The Limits Of Isonitrile-Mediated Amidations: On The Remarkable Stereosubtleties Of Macrolactam Formation From Synthetic Seco-Cyclosporins
摘要:The Scope Of Isonitrile-Mediated Amide Bond-Forming Reactions Is Further Explored In This Second-Generation Synthetic Approach To Cyclosporine (Cyclosporin A). Both Type I And Type Ii Amidations Are Utilized In This Effort,Allowing Access To Epimeric Cyclosporins A And H From A Single Precursor By Variation Of The Coupling Reagents. This Work Lends Deeper Insight Into The Relative Acylating Ability Of The Formimidate Carboxylate Mixed Anhydride (Fcma) Intermediate,While Shedding Light On The Far-Reaching Impact Of Remote Stereochemical Changes On The Effective Preorganization Of Seco-Cyclosporins.
DOI:10.1021/ja2103372

专利信息

专利号:US-2012253007-A1
优先权日:2011-03-28
标题:Synthesis of Cyclosporin H
发明人：WHITAKER CRAIG; CASPE STEPHANIE
权利人:WHITAKER CRAIG; CASPE STEPHANIE; US GOV SEC NAVY
摘要:A method of preparing purified cyclosporin H includes dissolving cyclosporin A in a first organic solvent and heating the first organic solvent in the presence of an acid catalyst; adding a base to the first organic solvent; recrystallizing cyclosporin H in a second solvent; and purifying the recrystallized cyclosporin H via chromatography to obtain purified cyclosporin H, while excluding recrystallizing the cyclosporin H in the presence of ether. In a further aspect, the method includes, after adding the base and before the recrystallizing, mixing the first organic solvent with a solvent more polar than the first organic solvent, separating the first organic solvent, and drying the first organic solvent. Cyclosporin H prepared as described herein was found to be biologically active, unlike that prepared using a previously-described method.

专利号:US-5214130-A
优先权日:1990-02-27
标题 :Synthesis of novel immunosuppressive cyclosporin analogs with modified amino acids at position-8
发明人：PATCHETT ARTHUR A; TAUB DAVID; GOEGELMAN ROBERT T
权利人:MERCK & CO INC
摘要:New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala]8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.

专利号:US-12201669-B2
优先权日:2021-03-11
标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology
发明人：TSAI LI-HUEI; BLANCHARD JOEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.

专利号:WO-2025079025-A1
优先权日:2023-10-13
标 题 :Ides-rapamycin conjugate in aav gene therapy
发明人：KHAN TAYEBA; KENNISTON JON A; NATARAJAN MADHUSUDAN; PALLISER DEBORAH; LEE HONG MYUNG; RICE ELISE; WATTERS ALEXANDER L; PAPAIOANNOU NIKOLAOS
权利人:TAKEDA PHARMACEUTICALS CO
摘要:The present invention, provides among other things, a conjugate of an IgG degrading protease, e.g., Immunoglobulin G (IgG) degrading enzyme of the S. pyogenes (IdeS) protein or IgG-degrading enzyme/MAC-1 (IdeZ) protein, with an immunosuppressant molecule, e.g., rapamycin, for immunosuppression in applications such as gene therapy. The present disclosure also provides methods of synthesis of conjugates and methods of conjugation (i.e. sortase-mediated conjugation) of payloads to IdeS or IdeZ for use in such applications.

专利号:RO-110144-B1
优先权日:1992-02-13
标题 :New cyclosporins, their method of synthesis and method of treatment and prevention of AIDS