专利号:US-7723082-B2 优先权日:2002-06-21 标题 :Polynucleotides and polypeptides coded by said polynucleotides involved in the synthesis of diketopiperazine derivatives 发明人:GONDRY MURIEL; GENET ROGER; LAUTRU SYLVIE; PERNODET JEAN-LUC 权利人:COMMISSARIAT ENERGIE ATOMIQUE; CENTRE NAT RECH SCIENT 摘要:The invention concerns novel isolated natural or synthetic polynucleotides and polypeptides coded by said polynucleotides, involved in the synthesis of diketopiperazine derivatives, vectors comprising said polynucleotides, micro-organisms transformed with said polynucleotides, uses of said polynucleotides and said polypeptides, as well as methods for the synthesis of diketopiperazine derivatives, including cyclodipeptides and diketopiperazine derivatives 3- and 6-substituted by α,β-unsaturated amino acid side chains.
专利号:US-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
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:WO-9600391-A1 优先权日:1994-06-23 标题:Methods for the synthesis of diketopiperazines 发明人:CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN 权利人:AFFYMAX TECH NV; CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN 摘要:Libraries of diverse diketopiperazines bound to a support and methods for synthesizing diketopiperazines on a solid support are described. These libraries have utility in the area of drug design as they can be screened against biological substances to identify compounds which have desirable biological activity.
专利号:US-2009011476-A1 优先权日:2005-08-19 标 题 :Gene cluster and method for the biosynthesis of terrequinone a 发明人:HOFFMEISTER DIRK; KELLER NANCY P 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides a novel gene cluster containing five genes (tdiA-E) involved in indole alkaloid synthesis. Disruption of tdiB, encoding an enzyme with prenyltransferase activity, transferring dimethylallylpyrophosphate to C-2 of an indole structure, eliminated the production of the antitumor compound terrequinone A, a metabolite not known from A. nidulans . The invention further provides a method for expressing terrequinone A in a host cell and isolating purified terrequinone A therefrom.
专利号:US-2006051837-A1 优先权日:2002-06-21 标 题 :Polynucleotides and polypeptides coded by said polynucleotides involved in the synthesis of diketopiperazine derivatives
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