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.
专利号:US-6664282-B2 优先权日:1999-09-17 标 题:Synthesis of [3,5,7]-1H-imidazo [1,5-a]imidazol-2 (3H)- one compounds 发明人:ELABDELLAOUI HASSAN M; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:Individual substituted [3,5,7]-1H-imidazo[1,5-a]imidazol-2(3H)-one compounds and their pharmaceutically-acceptable salts are disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
专利号:US-9085605-B2 优先权日:2010-05-27 标 题:Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate 发明人:LIU GANG; ZHAO NAN; MA YAO 权利人:LIU GANG; ZHAO NAN; MA YAO; SHENZHEN SALUBRIS PHARM CO LTD 摘要:The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.
专利号:US-5856107-A 优先权日:1997-02-04 标 题 :Combinatorial libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene derivatives, methods of making the libraries and compounds therein 发明人:OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene compounds. The present invention further provides methods of preparing the libraries and the individual compounds made by the combinatorial synthesis.
专利号:WO-9834113-A1 优先权日:1997-02-04 标题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein 发明人:OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; HOUGHTEN RICHARD A; BLONDELLE SYLVIE E; SCHONER CHRISTA C 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.
专利号:US-6359144-B1 优先权日:1997-02-04 标 题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein 发明人:OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; BLONDELLE SYLVIE E; SCHONER CHRISTA C; HOUGHTEN RICHARD A 权利人:LION BIOSCIENCE AG 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.
[参考文献]: Cui Y, Et Al. Inhibition Kinetics And Molecular Simulation Of P-Substituted Cinnamic Acid Derivatives On Tyrosinase. Int J Biol Macromol. 2017 Feb;95:1289-1297. [参考文献]: Kátia Aparecida De Siqueira, Et Al. Isolation Of 4-Chlorocinnamic Acid From Streptomyces Griseocarneus R132, And Its Inhibition Activity Against Sweet Pepper Postharvest Anthracnose. Biocontrol Science And Technology. Volume 32, 2022-Issue 6 [参考文献]: Silva Rhn, Et Al. Antimicrobial Activity Of 4-Chlorocinnamic Acid Derivatives. Biomed Res Int. 2019 Apr 23;2019:3941242.
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