专利号:US-11926589-B2 优先权日:2019-07-09 标 题 :Process for the synthesis of non-racemic cyclohexenes 发明人:REISMAN SARAH; ROMBOLA MICHAEL; LADD CAROLYN L; MCLAUGHLIN MARTIN JOHN; ZUEND STEPHAN; GOETZ ROLAND 权利人:BASF CORP; CALIFORNIA INST OF TECHN 摘要:This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation M m+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R 10a , R 10b , R 10c , R 10d , R 10a′ , R 10b′ , R 10c′ , R 10d′ , Z and Z′ have the meanings as defined in the description.
专利号:US-5637759-A 优先权日:1992-07-30 标 题 :Metal-ligating amino acid derivatives for MRI and for peptide synthesis 发明人:HEARST JOHN E; RANA TARIQ M; BAN MATT 权利人:UNIV CALIFORNIA 摘要:Novel organic compounds and metal ion-containing amino acid chelates are described which are useful in solid phase synthesis of polypeptides and as magnetic resonance imaging (MRI) enhancing agents. The present invention also relates to a convenient and straightforward method to synthesize a metal-ligating amino acid suitable as MRI enhancing agents or for introducing a strong metal binding site at any chosen position in a peptide. Some compounds are designed to be compatible with N-α-Fmoc peptide synthesis strategy, and can easily be prepared on large scale. Thus, flexible linkers of different lengths and containing various structures can be placed between the α-carbon backbone of peptides and metal binding moieties. These peptides will provide a variety of affinity cleaving reagents which can be directed against protein or nucleic acid targets. Therefore, these molecules can serve as an important tool to study protein folding, protein-protein and protein-nucleic acid interactions.
专利号:US-9777022-B2 优先权日:2012-10-02 标题 :Process for the preparation of macrocyclic polyazacarboxylate ligands and chelates 发明人:MOORE DENNIS A; RAJAGOPALAN RAGHAVAN 权利人:MALLINCKRODT LLC; GUERBET SA 摘要:The present disclosure relates generally to a process for the synthesis of 1,4,7,10-tetraazacyclododecane ligands, chelates, and derivatives thereof. In particular, the present disclosure is directed to a process for the synthesis of 1,4,7,10-tetraaza-1,4,7,10-tetrakis(carboxymethyl)cyclododecane (DOTA) ligands, corresponding DOTA-metal chelates, and various derivatives thereof.
专利号:US-8147805-B2 优先权日:2005-01-05 标题:Conjugates for dual imaging and radiochemotherapy: composition, manufacturing, and applications 发明人:YANG DAVID; YU DONGFANG; CHANDA MITHU; AZHDARINIA ALI; OH CHANGSOK; KIM E EDMUND 权利人:YANG DAVID; YU DONGFANG; CHANDA MITHU; AZHDARINIA ALI; OH CHANGSOK; KIM E EDMUND; UNIV T EXAS SYSTEM BOARD OF REGENTS 摘要:Compositions and methods for dual imaging and for dual chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns compounds comprising the structure X 1 —Y—X 2 , wherein Y comprises two or more carbohydrate residues covalently attached to one another, X 1 and X 2 are diagnostic or therapeutic moieties covalently attached to Y, provided that when Y does not comprise a glucosamine residue, X 1 and X 2 are diagnostic moieties. The present invention also concerns methods of synthesis of these compounds, application of such compounds for dual imaging and treatment of hyperproliferative disease, and kits for preparing a radiolabeled therapeutic or diagnostic compound.
专利号:US-2025051292-A1 优先权日:2021-12-14 标题 :Process for manufacturing a mixture comprising a dimeric macrocycle intermediate of a gadolinium complex 发明人:GAZZETTO SONIA; BOI VALERIA; BANIN ANDREA; BARALE ANDREA 权利人:BRACCO IMAGING SPA 摘要:The present invention relates to a process for the manufacturing of a mixture comprising the intermediate 1-[bis[2-hydroxy-3-[4,7,10-tris[2-(1,1-dimethylethoxy)-2-oxoethyl]-1,4,7,10-tetraazacyclododec-1-yl]propyl]amino]-1-deoxy-D-glucitol. Such intermediate is useful for the synthesis of the dimeric gadolinium complex [μ-[1-[bis[2-(hydroxy-κO)-3-[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN 1 ,κN 4 ,κN 7 ,κN 10 ]propyl]amino]-1-deoxy-D-glucitolate(6-)]]digadolinium complex, which can be employed as a contrast agent in the field of diagnostic imaging, and in particular of Magnetic Resonance Imaging (MRI).
专利号:US-2004022857-A1 优先权日:2002-07-31 标 题 :Synthesis of highly conjugated polymers 发明人:UZGIRIS EGIDIJUS E; MOASSER BAHRAM; FISH KENNETH M; SMITH JOANNE F 摘要:Improved methods for forming substituted polymers having a high degree of conjugation include the steps of activating a steric hindrance molecule under conditions that ensure substantially all the steric hindrance molecules are mono-activated and then reacting with a polymer. An improved method for recovering polypeptides substituted with steric hindrance molecules and having an elongate configuration removes impurities and volatiles without achieving complete dryness of the copolymer.
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