CAS: 10023-07-1; Frenolicin

专利信息

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-7101684-B2
优先权日:1995-07-06
标 题:Modified modular polyketide synthase
发明人：KHOSLA CHAITAN; PIEPER REMBERT; LUO GUANGLIN; CANE DAVID
权利人:UNIV BROWN RES FOUND
摘要:Modular polyketide synthases modified so as not to incorporate natural starter units can be used for clean synthesis of novel polyketides.

专利号:US-6080555-A
优先权日:1995-07-06
标题 :Synthesis of polyketides from diketides

专利号:US-6927286-B1
优先权日:1999-01-06
标 题 :Bleomycin gene cluster components and their uses
发明人：SHEN BEN; DU LIANGCHENG; SANCHEZ CESAR; CHEN MEI; EDWARDS DANIEL J
权利人:UNIV CALIFORNIA
摘要:This invention provides detailed sequence analysis and characterization of the gene cluster responsible for the synthesis of bleomycin in Streptomyces verticillus . The bleomycin gene cluster provides the first hybrid polyketide synthase/nonribosomal peptide synthetase pathway and elucidation of the various modules and enzymatic domains characterizing the pathway provides convenient synthetic routes for bleomycins, bleomycin analogs, and various other polyketides.

专利号:US-7595175-B2
优先权日:2000-08-14
标题 :Polyketides and their synthesis
发明人：PETKOVIC HRVOJE; KENDREW STEVEN GARY; LEADLAY PETER FRANCIS
权利人:BIOTICA TECH LTD
摘要:Biosyntheses of compounds whereof at least portions are polyketides produced by means of polyketide synthase (PKS) enzyme complexes are carried out after specific alterations have been made within the acyltransferase (AT) domains of the PKSs. Particular motifs in or near the substrate binding pocket are disclosed, such that alterations therein affect substrate specificity.

专利号:WO-9702358-A1
优先权日:1995-07-06
标题 :Cell-free synthesis of polyketides