专利号:WO-2025088147-A1 优先权日:2023-10-27 标题 :Theranostic psma-targeting ligands for the diagnosis and treatment of psma-expressing cancers and their solid phase synthesis 发明人:Schäfer Martin; BAUDER-WUEST ULRIKE; ROSCHER MAREIKE; REMDE YVONNE; BENEÅ OVÃ?-SCHÄFER MARTINA; BARINKA CYRIL; KUTILOVÃ? ZSÓFIA; MOTLOVÃ? LUCIA 权利人:DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES OEFFENTLICHEN RECHTS 摘要:The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and radiopharmaceuticals for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof. Further the present invention provides synthetic procedures for the synthesis of such PSMA-targeting ligands.
专利号:US-2004266796-A1 优先权日:2003-06-25 标 题:Convergent processes for the synthesis of a GARFT inhibitor containing a methyl substituted thiophene core and intermediates therefor 发明人:DOVALSANTOS ELENA; FLAHIVE ERIK JON; HALDEN BRIAN JOHN; MITCHELL MARK BRYAN; NOTZ WOLFGANG REINHARD LUDWIG; O'NEILL-SLAWECKI STACY ANN; TIAN QINGPING 权利人:AGOURON PHARMA 摘要:The invention relates to processes for the preparation of a GARFT inhibitor containing a methyl substituted thiophene core having the following structure: n n n wherein each of R 1 and R 2 are independently a hydrogen atom or a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; from an intermediate of the formula n n n wherein R 3 is a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; n Pg 1 is an amino protecting group; n R 4 is H; n or Pg 1 can optionally be taken together with R 4 and the nitrogen to which Pg 1 and R 4 are attached to form (i) an imine; or (ii) a fused or bridged bicyclic ring or a spirocyclic ring, wherein said ring is saturated and contains from 5 to 12 carbon atoms in which up to 2 carbon atoms are optionally replaced with a hetero moiety selected from O, S(O) j wherein j is an integer from 0 to 2, and —NR 8 —, provided that two O atoms, two S(O) j moieties, or an O atom and a S(O) j moiety are not attached directly to each other; n R 5 is selected from the group consisting of —C≡C— and —CHâ•?CH—; and n R 8 is independently H or C 1 -C 6 alkyl; n to form the compound of the formula (I) that is optically pure; and to processesfor preparing intermediates thereof.
专利号:US-6916949-B2 优先权日:2001-01-29 标 题 :Methods of chemical systhesis of phenolic nitrogen mustard prodrugs 发明人:SPRINGER CAROLINE JOY; NICULESCU-DUVAZ DAN 权利人:CANCER REC TECH LTD 摘要:This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-{4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl}-L-glutamic acid: wherein: X2 is a halo group, and is -F, -Cl, -Br, or -I; n is an integer from 0 to 4; and, each RA is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic estenfication (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).
专利号:WO-2024169886-A1 优先权日:2023-02-16 标 题 :Psma targeted radioactive drug for integrated diagnosis and treatment, and synthesis and use thereof 发明人:YAN CHENGLONG; YU SHANYOU; FANG PENG; ENG WAI-SI; YANG SI 权利人:NORROY BIOSCIENCE CO LTD 摘要:Provided are a PSMA targeted radioactive drug for integrated diagnosis and treatment, and the synthesis and use thereof. Specifically, the present invention relates to a compound or a pharmaceutically acceptable salt, ester or solvate thereof. The structure of the compound is as represented by formula (I). The compound can be used for diagnosing and/or treating one or more tumors, cancers or cells expressing PSMA.
专利号:WO-02060862-A1 优先权日:2001-01-29 标题:Methods of chemical synthesis of phenolic nitrogen mustard prodrugs
专利号:EP-1355876-B1 优先权日:2001-01-29 标题:Methods of chemical synthesis of phenolic nitrogen mustard prodrugs
[参考文献]: Manolopoulou A, Et Al. Synthesis Of Potent Antagonists Of Substance P By Modifying The Methionyl And Glutaminyl Residues Of Its C-Terminal Hexapeptide And Without Using D-Amino Acids. Int J Pept Protein Res. 1993 Apr;41(4):411-4. [参考文献]: A Manolopoulou, Et Al. Synthesis Of Potent Antagonists Of Substance P By Modifying The Methionyl And Glutaminyl Residues Of Its C-Terminal Hexapeptide And Without Using D-Amino Acids. Int J Pept Protein Res. 1993 Apr;41(4):411-4. [参考文献]: M Antoniou, Et Al. Synthesis And Biological Activity Of Analogues Of The C-Terminal Hexapeptide Of Substance P With Modifications At Glutaminyl And Methioninyl Residues. Structure-Activity Studies. Int J Pept Protein Res. 1992 Nov;40(5):395-400.
合成参考文献
摘要:Neurobehavioral Toxicology and Teratology., 7(275), 1985 []