专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-8557979-B2 优先权日:2004-06-10 标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation 发明人:CHOI WOO-BAEG; KOWALIK EWA 权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
专利号:US-6264962-B1 优先权日:1997-12-19 标 题:Use of cinnamic acid or of at least one of its derivatives in a cosmetic composition 发明人:BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE 权利人:OREAL 摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids. n The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.
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-10933051-B2 优先权日:2017-06-09 标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections 发明人:CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN 权利人:FOB SYNTHESIS INC 摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
1: Saarikoski T, Saari TI, Hagelberg NM, Backman JT, Neuvonen PJ, Scheinin M, Olkkola KT, Laine K. Effects of terbinafine and itraconazole on the pharmacokinetics of orally administered tramadol. Eur J Clin Pharmacol. 2015 Mar;71(3):321-7. doi: 10.1007/s00228-014-1799-2. Epub 2015 Jan 6. doi: 10.4103/0378-6323.158634. doi: 10.1007/s13318-014-0205-x. Epub 2014 Jun 4. doi: 10.1111/j.1468-3083.2012.04584.x. Epub 2012 May 28. Review. doi: 10.1007/s11096-014-9969-y. Epub 2014 Jul 2. Review. doi: 10.4103/0253-7613.169574. 7: Alipour M, Mozafari NA. Terbinafine susceptibility and genotypic heterogeneity in clinical isolates of Trichophyton mentagrophytes by random amplified polymorphic DNA (RAPD). J Mycol Med. 2015 Mar;25(1):e1-9. doi: 10.1016/j.mycmed.2014.09.001. Epub 2015 Jan 30. doi: 10.1007/s00105-016-3853-8. Review. German. doi: 10.1007/s40261-014-0171-8. 10: Dolton MJ, Perera V, Pont LG, McLachlan AJ. Terbinafine in combination with other antifungal agents for treatment of resistant or refractory mycoses: investigating optimal dosing regimens using a physiologically based pharmacokinetic model. Antimicrob Agents Chemother. 2014;58(1):48-54. doi: 10.1128/AAC.02006-13. Epub 2013 Oct 14.
合成参考文献
参考文献:10.1159/000089024 摘要:Farhi D, Viguier M, Cosnes A, Reygagne P, Dubertret L, Revuz J, Roujeau JC, Bachelez H. Terbinafine-induced subacute cutaneous lupus erythematosus. Dermatology. 2006;212(1):59–65. doi: 10.1159/000089024. 参考文献:10.1097/01.mlg.0000181462.08683.0c 摘要:Doty RL, Haxel BR. Objective assessment of terbinafine-induced taste loss. Laryngoscope. 2005 Nov;115(11):2035–7. doi: 10.1097/01.mlg.0000181462.08683.0c. 参考文献:10.1136/emj.2009.088211d 摘要:Grayson A, Mackenzie L. Best Evidence Topic report. BET 4. What best scratches the itch Emerg Med J. 2010 Feb;27(2):145–6. doi: 10.1136/emj.2009.088211d. 参考文献:10.1016/j.jaad.2009.04.062 摘要:Piraccini BM, Sisti A, Tosti A. Long-term follow-up of toenail onychomycosis caused by dermatophytes after successful treatment with systemic antifungal agents. Journal of the American Academy of Dermatology. 2010 Mar;62(3):411–4. doi: 10.1016/j.jaad.2009.04.062. 参考文献:10.1016/j.jaad.2009.09.001 摘要:Daniel CR, Jellinek NJ. Commentary: The illusory tinea unguium cure. Journal of the American Academy of Dermatology. 2010 Mar;62(3):415–7. doi: 10.1016/j.jaad.2009.09.001.