专利号:US-2010035799-A1 优先权日:2002-07-24 标 题:Method for the synthesis of anthracycline-peptide conjugates 发明人:FERNANDEZ ANNE-MARIE; DUBOIS VINCENT 权利人:UNIV CATHOLIQUE LOUVAIN; DIATOS SA 摘要:The present invention relates to a method for the preparation of a compound of formula (I) or pharmaceutically acceptable salts thereof and intermediates thereof, comprising the steps of: n n n n n n n n n n n n a) halogenating a compound of formula (II), resulting in compound of formula (IIa), n n n n n n n n n n n n n n n n b) reacting a compound of formula (IIa) at its 14 position with the thiol moiety of a peptide of formula (III), optionally in the presence of a suitable linker, to obtain said compound of formula (I), n n n n n n n n n n n n n n n n wherein R 1 represents OH, NH 2 or NH-peptide; R 2 represents H or —CO-peptide; R 3 represents OCH 3 , OH or H; R 4 represents H, or COCF 3 ; R 5 represents OH, O-tetrahydropyranyl or H; R 6 represents OH or H; R 7 represents H, OH, OCO(CH 2 ) 3 CH 3 or OCOCH(OC 2 H 5 ) 2 ; R 8 represents OH or H; R 9 represents OH or H; R 10 represents a halogen and L is an optional suitable linker arm.
专利号:US-2006183886-A1 优先权日:1995-11-22 标题:Ligands to enhance cellular uptake of biomolecules 发明人:TSO PAUL O; DUFF ROBERT; ZHOU YUANZHONG; DEAMOND SCOTT; ROBY CLINTON 权利人:CELL WORKS THERAPEUTICS INC A 摘要:The present invention relates to the design and synthesis of homogeneous A-L-P constructs, which contain a hepatic ligand to direct an oligomer or “payloadâ€? to a hepatocyte intracellularly via a receptor-mediated, ligand-directed pathway.
专利号:US-2008267981-A1 优先权日:2004-06-30 标题:Compositions and Methods for Delivery of Antitumor Agents 发明人:JANDA KIM D; WIRSCHING PETER; BOGER DALE L 权利人:SCRIPPS RESEARCH INST 摘要:Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.
专利号:US-2008207523-A1 优先权日:2006-09-08 标题 :Compounds as aptamer-dimers and their uses in diagnosis and therapy 发明人:FRIEBE MATTHIAS; STEPHENS ANDREW; SRINIVASAN ANANTH; HECHT MAREN 权利人:FRIEBE MATTHIAS; STEPHENS ANDREW; SRINIVASAN ANANTH; HECHT MAREN 摘要:The object of the present invention is solved by compositions of peptide linkers and their use for synthesis and annealing of aptamer oligonucleotides in form of dimers. The present invention in particularly provides said compositions for the use as a diagnostic and/or therapeutic agent. n In another preferred embodiment the present invention relates to a kit for preparing a radiopharmaceutical preparation, said kit comprising a vial comprising a quantity of the compound according to the invention. n A further preferred embodiment of the present invention relates to methods of producing said compounds, comprising synthesis of said compound in an automated peptide synthesizer. n In another preferred embodiment the present invention concerns the use of said compounds according to the present invention for the manufacture of a medicament, preferably for diagnosis or therapy of proliferative diseases. n In a further preferred embodiment the present invention concerns methods for treating or diagnosing patients administering or utilizing the compounds according to the present invention.
专利号:US-6221602-B1 优先权日:1998-11-10 标题:Functionalized nanocrystals and their use in labeling for strand synthesis or sequence determination 发明人:BARBERA-GUILLEM EMILIO; NELSON M BUD; CASTRO STEPHANIE L 权利人:BIO PIXELS LTD 摘要:Provided are compositions comprising functionalized nanocrystal-labeled nucleobases that are produced by operably linking a nucleobase to a functionalized nanocrystal via reactive functionalities. Also provided are kits comprising a plurality of species of functionalized nanocrystal-labeled nucleobases. The functionalized nanocrystal-labeled nucleobases may be added to a strand synthesis reaction under suitable conditions to be incorporated into one or more strands synthesized in the reaction.
专利号:WO-0028089-A1 优先权日:1998-11-10 标 题:Functionalized nanocrystals and their use in labeling for strand synthesis or sequence determination 发明人:BARBERA-GUILLEM EMILIO; NELSON M BUD; CASTRO STEPHANIE 权利人:BIOCRYSTAL LTD 摘要:Provided are compositions comprising functionalized nanocrystal-labeled nucleobases that are produced by operably linking a nucleobase to a functionalized nanocrystal via reactive functionalities. Also provided are kits comprising a plurality of species of functionalized nanocrystal-labeled nucleobases. The functionalized nanocrystal-labeled nucleobases may be added to a strand synthesis reaction under suitable conditions to be incorporated into one or more strands synthesized in the reaction.
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