CAS: 389139-89-3; (4S,4As,5Ar,12As)-4,7-Bis(Dimethylamino)-3,10,12,12A-Tetrahydroxy-9-((Neopentylamino)Methyl)-1,11-Dioxo-1,4,4A,5,5A,6,11,12A-Octahydrotetracene-2-Carboxamide
该化合物是一种合成四环衍生物,具有广泛频谱抗菌活动,主要用于治疗急性细菌皮肤和皮肤结构感染以及社区获得的细菌肺炎; 百环虫功能,抑制细菌蛋白合成,具体针对30S 脊髓膜炎亚元素,这扰乱了细菌生长和繁殖所必需的转化过程; 其特点是,在存在某些抗药性机制的情况下,该化合物具有稳定性,它对其他四环菌产生影响,使其能有效防治一系列克格伦和格拉姆阴性细菌,包括一些抗药性菌株; 百环虫是静脉注射或口腔注射的,其药用动力基因基因学功能可以方便地施用剂量疗法; 此外,该化合物具有有利的安全性特征,具有常见的副作用,包括胃肠扰动; 百虫环虫的发育代表了抗生治疗的重大进步,特别是在抗生素抗药性上升的情况下. 它独特的化学结构和行动机制将它与传统的四环细菌区别,在临床感染管理中提供重要选择.
- 英文名称(4S,4As,5Ar,12As)-4,7-Bis(Dimethylamino)-3,10,12,12A-Tetrahydroxy-9-((Neopentylamino)Methyl)-1,11-Dioxo-1,4,4A,5,5A,6,11,12A-Octahydrotetracene-2-Carboxamide
- IUPAC名称(4S,4aS,5aR,12aS)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-9-((neopentylamino)methyl)-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
- CAS编号389139-89-3
- MFCD编号:MFCD19443723
- EINECS号:863-367-3
- FDA UNII编号:090IP5RV8F
- 分子式:C29H40N4O7分子量:556.66
- 产品CID: 1401274
- 同类组份化合物CAS389139-89-3 (free base)1196800-40-4 (mesylate)1075240-43-5 (tosylate)1196800-39-1 (HCl)
- 产品分类原料药 → 抗生素类药物
- 相似结构搜索
- InChIKey: JEECQCWWSTZDCK-IQZGDKDPSA-N
- JEECQCWWSTZDCK-IQZGDKDPSA-N
- 计算化学: 氢键受体数10.0氢键供体数6.0可旋转键数7.0
物理性质
MSDS等安全信息
合成工艺路线路线简述
- 1075240-41-3 = 389139-89-3 + 1075240-42-4
反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water; 24 H,17 °C
标题:Synthesis Development Of An Aminomethylcycline Antibiotic Via An Electronically Tuned Acyliminium Friedel-Crafts Reaction
作者:Chung,John Y. L.; Hartner,Frederick W.; Cvetovich,Raymond J.
参考文献:Tetrahedron Letters 日期:2008 卷标:49(42) 页码:6095-6100
专利信息
专利号:US-2023357135-A1
优先权日:2020-06-11
标 题:Crystalline forms of omadacycline, methods of synthesis thereof and methods of use thereof
发明人：WARCHOL TADEUSZ; JOHNSTON SEAN M
权利人:PARATEK PHARM INNC
摘要:The present invention provides omadacycline crystalline freebase and methods of synthesis thereof. The present invention also provides pharmaceutical compositions comprising omadacycline crystalline freebase and methods of use thereof for treating bacterial infections. The present invention also provides methods of purifying crude omadacycline freebase that comprise crystallization to produce crystalline omadacycline freebase. The omadacycline crystalline freebase may also be used to prepare salts of omadacycline, e.g., a tosylate salt.
专利号:PT-117254-B
优先权日:2021-05-26
标题 :METHOD FOR SYNTHESIS OF 9-AMINOMETHYL TETRACYCLINE COMPOUNDS
专利号:US-9295731-B2
优先权日:2013-04-01
标题 :Cleavable drug conjugates, compositions thereof and methods of use
发明人：NGUYEN MARK QUANG
权利人:NGUYEN MARK QUANG
摘要:Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.
专利号:JP-2010532759-A
优先权日:2007-07-06
标 题 :Method for the synthesis of substituted tetracycline compounds
专利号:US-11980627-B2
优先权日:2019-06-14
标 题 :Triple pharmaceutical composition for proteinaceous infection
发明人：ATIBA JOSHUA O
权利人:ATIBA JOSHUA O
摘要:There are disclosed therapies and preventions of prion protein complex infections. The transcription of the amyloid precursor protein gene and PrP gene and the RNA transcript are the rate-limiting steps and are most susceptible for blockage and control of the process of amyloid protein formation and PrP sc formation. Thus, therapies and prevention regimes for prion protein complex infections interrupt this process at the level of DNA transcription to RNA, RNA transport to the mitochondrion for protein synthesis and deposition in the cerebral cortex neurons.
专利号:EP-4165016-A1
优先权日:2020-06-11
标题:Crystalline forms of omadacycline, methods of synthesis thereof and methods of use thereof
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
: Kovacs SJ, Ting L, Praestgaard J, Sunkara G, Sun H, Stein DS, Tanaka SK, Villano S. An Open-Label Study of the Impact of Hepatic Impairment on the Pharmacokinetics and Safety of Single Oral and Intravenous Doses of Omadacycline. Antimicrob Agents Chemother. 2020 Aug24:AAC.01650-20. doi: 10.1128/AAC.01650-20. Epub ahead of print. 584(7821):338-341. doi: 10.1038/d41586-020-02418-x. 98(3):115129. doi: 10.1016/j.diagmicrobio.2020.115129. Epub ahead of print. 2006–. Omadacycline. 2020 Jul 20. 2020 Jan–. 20(1):189. doi: 10.1186/s12866-020-01869-6.
8: Iregui A, Landman D, Quale J. Activity of Omadacycline and Other Tetracyclines Against Contemporary Gram-Negative Pathogens from New York City Hospitals. Microb Drug Resist. 2020 Jun 22. doi: 10.1089/mdr.2019.0423. Epub ahead of print. 64(9):e00499-20. doi: 10.1128/AAC.00499-20.
10: Begum K, Bassères E, Miranda J, Lancaster C, Gonzales-Luna AJ, Carlson TJ, Rashid T, Eyre DW, Wilcox MH, Alam MJ, Garey KW. In Vitro Activity of Omadacycline, a New Tetracycline Analog, and Comparators against Clostridioides difficile. Antimicrob Agents Chemother. 2020 Jul 22;64(8):e00522-20. doi: 10.1128/AAC.00522-20. 75(8):2160-2163. doi: 10.1093/jac/dkaa138.
合成参考文献
参考文献:10.1007/s40265-022-01676-5
摘要:Chou A, Welch E, Hunter A, Trautner BW. Antimicrobial Treatment Options for Difficult-to-Treat Resistant Gram-Negative Bacteria Causing Cystitis, Pyelonephritis, and Prostatitis: A Narrative Review. Drugs. 2022 Mar 14;82(4):407–38. doi: 10.1007/s40265-022-01676-5.
📝 需求与反馈
尽可能描述清楚需求与问题信息
