专利号:US-7230101-B1 优先权日:2002-08-28 标 题:Synthesis of methotrexate-containing heterodimeric molecules 发明人:MURTHI KRISHNA K; SMITH CHASE C 权利人:GPC BIOTECH INC 摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:
专利号:WO-9943409-A1 优先权日:1998-02-27 标 题:Hplc fractionation of complex chemical mixtures 发明人:COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN 权利人:ISIS PHARMACEUTICALS INC; COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN 摘要:The rapid deconvolution of complex chemical mixtures, such as combinatorial libraries prepared via solution-phase simultaneous addition of functionalities is demonstrated using HPLC. Libraries containing 25-216 members were screened for biological activity and active libraries are fractionated into discreet pools using preferred reversed-phase HPLC. The entire process can be completed from a single synthesis of 15-50 mg, without the need for fixed positions, serial synthesis, or tagging.
专利号:US-5763625-A 优先权日:1995-04-25 标 题:Synthesis and use of β-lapachone analogs 发明人:BOOTHMAN DAVID A; FRYDMAN BENJAMIN J; WITIAK DONALD T 权利人:WISCONSIN ALUMNI RES FOUND 摘要:3-Substituted-β-lapachone analogs and their use either alone or to augment chemotherapy or radiotherapy to induce programmed neoplastic cell death without exhibiting toxicity to surrounding normal cells are disclosed. In particular, 3-allyl-β-lapachones, 3-alkyl-β-lapachones and 3-halo-β-lapachones were found to be Topoisomerase (Topo I) inhibitors. When these analogs are used alone there is a reversible single-strand break in the DNA of neoplastic cells causing apoptosis and cell death in some cells. However, when these analogs are combined with chemotherapy or X-irradiation, an irreversible Topo I-mediated break is achieved. A new and more efficient chemical synthesis of the compounds is also disclosed.
专利号:US-2025009786-A1 优先权日:2021-09-30 标 题 :Automated synthesis of polymeric dual drugs 发明人:MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL 权利人:SONY GROUP CORP 摘要:Compounds useful as biologically active compounds with or without fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, M1, M2, M3, l, m, n, p, and q are as defined herein. Additional compound, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.
专利号:US-2022395555-A1 优先权日:2020-06-11 标题:Derivatives of antibiotics 发明人:FARBER BORIS; FARBER SOF'YA; MARTYNOV ARTUR VIKTOROVICH 权利人:FARBER BORIS; FARBER SOFYA; MARTYNOV ARTUR VIKTOROVICH 摘要:Field of application: The invention relates to chemistry, pharmacy and cosmetology, allows to synthesize of supramolecular structure on base antibiotics derivatives for use in pharmacy, cosmetology and pharmacy. n The essence of the invention: a new derivatives of antibiotics based on supramolecular structures and a method for their preparation, characterized in that the supramolecular structures are obtained by combinatorial synthesis of an antibiotic from one source molecule with two or more groups available in the reaction for covalent modification, at least with two different modifiers simultaneously, this creates a mixture of modified derivatives of the original molecule, with a maximum variety of derivatives with forming new supramolecular structure, and as biologically active substances to create pharmaceutical compositions use such supramolecular structure without separation into individual components, and in the reaction a combinatorial mixture of modified derivatives of the original molecule is formed antibiotic, the maximum number of combinations. n Technical result: modified combinatorial derivatives of antibiotics with antimicrobial and antifungal activity against multiresistant and pan drug resistance strains of microorganisms and fungi. Means have a wide spectrum of action, and the supramolecular and combinatorial structure of their tens and hundreds of derivatives eliminates the resistance of microorganisms.
专利号:US-9890126-B2 优先权日:2012-04-24 标 题:Synthesis of novel inhibitors of isoprenoid biosynthesis (ISPF) 发明人:HAGEN TIMOTHY J; ZHANG ZHENG; LAZOWSKI ZACHARY; CLARE MICHAEL; BEGLEY DARREN W 权利人:UNIV NORTHERN ILLINOIS BOARD OF TRUSTEES; BERYLLIUM DISCOVERY CORP 摘要:Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.
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