2-溴-2',4'-二氯苯乙酮置于n,N-Diethylaniline Borane,碳酸氢钠,三乙胺,(S)-2-甲基-Cbs-恶唑硼烷体系中,用 四氢呋喃,水,二甲基亚砜,乙酸乙酯,甲苯 用作溶剂,化学反应 9.0H,反应生成卢立康唑 参考文献: Compounds Of R-(-)-(E)-[4-(2,4-Dichlorophenyl)-1,3-Dithiolan-2-Ylidene]-1-Imidazolylacetonitrile-Ha (Luliconazole-Ha) As Antifungals[fr] Composés De R-(-)-(E)-[4-(2,4-Dichlorophényl)-1,3-Dithiolan-2-Ylidène]-1-Imidazolylacétonitrile-Ha (Luliconazole-Ha) à Titre D'Antifongiques 标题: Compounds Of R-(-)-(E)-[4-(2,4-Dichlorophenyl)-1,3-Dithiolan-2-Ylidene]-1-Imidazolylacetonitrile-Ha (Luliconazole-Ha) As Antifungals[fr] Composés De R-(-)-(E)-[4-(2,4-Dichlorophényl)-1,3-Dithiolan-2-Ylidène]-1-Imidazolylacétonitrile-Ha (Luliconazole-Ha) à Titre D'Antifongiques 摘要:本发明涉及化合物r-(-)-(e)-[4-(2,4-二氯苯基)-1,3-二硫杂环戊烯-2-基]-1-咪唑乙腈ha,其中ha是一种酸;以及它们的制备过程.本发明还涉及使用化合物r-(-)-(e)-[4-(2,4-二氯苯基)-1,3-二硫杂环戊烯-2-基]-1-咪唑乙腈ha高产率和纯度制造luliconazole和其药学上可接受的盐或共晶体.本发明还针对该化合物r-(-)-(e)-[4-(2,4-二氯苯基)-1,3-二硫杂环戊烯-2-基]-1-咪唑乙腈ha在治疗真菌感染方面的应用.
专利号:US-2024336559-A1 优先权日:2021-10-06 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
专利号:US-10443047-B2 优先权日:2014-05-01 标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase 发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E 权利人:NOVOGY INC 摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.
专利号:US-12325678-B2 优先权日:2017-06-16 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; DEL POETA MAURIZIO; LAZZARINI CRISTINA; HARANAHALLI KRUPANANDAN; SUN YI 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n nand use of the compound for inhibiting the growth of or killing.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:US-11858880-B2 优先权日:2017-06-16 标题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
专利号:US-11944609-B1 优先权日:2023-06-16 标题:Antifungal ionic liquid and Amphotericin B combination 发明人:RATHER SAMI-ULLAH; WANI MOHMMAD YOUNUS; BAMUFLEH HISHAM S; ALHUMADE HESHAM; SAEED USMAN; TAIMOOR AQEEL AHMAD; ALALAYAH WALID M; RATHER IRFAN AHMAD 权利人:KING ABDULAZIZ UNIVERISTY; UNIV KING ABDULAZIZ 摘要:Provided herein are ionic liquids that can be used as antifungal agents alone or in combination with Amphotericin B. Also disclosed are methods of synthesis of the ionic liquids and inhibiting fungal growth and methods of treating fungal infections using the disclosed compounds. The disclosure provides antifungal agents that potentiate the antifungal activity of Amphotericin B, a commonly used antifungal drug that could be used alone or in combination. This combination will help control and combat the infections caused by drug resistant Candida. auris in immunocompromised patients.
1: Luliconazole cream (Luzu) for tinea infections. Med Lett Drugs Ther. 2014 Jun 23;56(1445):50-1. Epub 2014 Apr 7. doi: 10.1111/myc.12168. Epub 2014 Mar 12. doi: 10.1128/AAC.02370-12. Epub 2013 Apr 1. 8: Jerajani H, Janaki C, Kumar S, Phiske M. Comparative assessment of the efficacy and safety of sertaconazole (2%) cream versus terbinafine cream (1%) versus luliconazole (1%) cream in patients with dermatophytoses: a pilot study. Indian J Dermatol. 2013 Jan;58(1):34-8. doi: 10.4103/0019-5154.105284. 9: Koga H, Nanjoh Y, Kaneda H, Yamaguchi H, Tsuboi R. Short-term therapy with luliconazole, a novel topical antifungal imidazole, in guinea pig models of tinea corporis and tinea pedis. Antimicrob Agents Chemother. 2012 Jun;56(6):3138-43. doi: 10.1128/AAC.05255-11. Epub 2012 Mar 5.
合成参考文献
参考文献:10.1007/s11046-020-00481-6 摘要:Chen YH, Chi MJ, Sun PL, Yu PH, Liu CH, Cano-Lira JF, Li WT. Histopathology, Molecular Identification and Antifungal Susceptibility Testing of Nannizziopsis arthrosporioides from a Captive Cuban Rock Iguana (Cyclura nubila). Mycopathologia. 2020 Dec;185(6):1005–12. doi: 10.1007/s11046-020-00481-6.