专利号:US-6818633-B2 优先权日:2001-06-29 标题:Antiviral compounds and methods for synthesis and therapy 发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-2010055750-A1 优先权日:2008-09-03 标 题:Polyester synthesis 发明人:WOSNICK JORDAN H 权利人:XEROX CORP 摘要:The present disclosure provides for enzymatic polymerization to produce polyester resins suitable for use in manufacturing toners. In embodiments, crystalline copolymers, which are polyesters, may be synthesized from lactones, cyclic anhydrides, cyclic carbonates, and combinations thereof. These crystalline copolymers, in turn, may be utilized in the synthesis of toner particles.
专利号:US-11466046-B2 优先权日:2014-10-08 标题 :14-membered ketolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.
专利号:US-10022366-B2 优先权日:2013-04-23 标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery 发明人:STINCHCOMB AUDRA L; GHOSH PRIYANKA 权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND 摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
参考标题:A New Trifluoromethylating Agent: Synthesis Of Polychlorinated (Trifluoromethyl)Benzenes And 1,3-Bis(Trifluoromethyl)Benzenes And Conversion Into Their Trichloromethyl Counterparts And Molecular Structure Of Highly Strained Polychloro-M-Xylenes 作者:J. Castaner,J. Riera,J. Carilla,A. Robert,E. Molins,C. Miravitlles |发布日期:1991.1 摘要:Mixtures Of Ccl3F And Alcl3 Replace Cf3 For H In Polychlorobenzenes. Thus, By Treatment Of A Solution Of The Suitable Polychlorobenzene In Ccl3F With Alcl3, The Following Compounds Can Be Prepared: Pentachloro- (2), 2,3,4,5-Tetrachloro- (5), 2,3,4,6-Tetrachloro- (8), 2,3,5,6-Tetrachloro- (11), 2,3,4-Trichloro- (14), 2,4,5-Trichloro- (17), And 2,4,6-Trichloro-1-(Trifluoromethyl)Benzene (20), As Well As 4,5,6-Trichloro- (31) And 2,4,6-Trichloro-1,3-Bis(Trifluoromethyl)Benzene (32). The Reaction Of The Above-Mentioned Trifluoromethylated Compounds With Alcl3 In Cs2 Yields Their Trichloromethyl Counterparts: 3, 6, 9, 12, 15, 18, 21, 34, And 36. The Chlorination Of 32 Or 36 By Means Of Silberrad'S Reagent (So2Cl2, Alcl3, And S2Cl2) Affords Perchloro-M-Xylene (38), A New Highly Strained Chlorocarbon Whose Synthesis Was Attempted Repeatedly In The Past. 9, 15, 17, And 21, When Treated With Oleum And Then With Water, Are Converted Into 2,3,4,6-Tetrachloro- (22), 2,3,4-Trichloro- (23), 2,4,5-Trichloro- (24), And 2,4,6-Trichlorobenzoic Acid (25), Respectively; Under Similar Treatment, 34, 36, And 38 Give 4,5,6-Trichloro- (33), 2,4,5-Trichloro- (35), And Tetrachloroisophthalic Acid (39), Respectively. The Formation Of The (Trifluoromethyl)Benzenes Is Discussed, And In This Connection It Has Been Found That Ccl3F Solutions Of 3 And 18 In The The Presence Of Alcl3 Give Back 2 And 17, Respectively. Molecular Structures Of Highly Strained M-Xylenes 36 And 38, As Well As That Of The Much Less Strained 34, Ascertained By X-Ray Analysis, Are Reported And Commented. Ir, Uv, And Nmr Spectral Data Of The Compounds Synthesized Are Presented. The Interesting Uv Spectrum Of 21 Is Discussed.