CAS: 3106-85-2; (S)-2-((S)-2-Acetamido-3-Carboxypropanamido)Pentanedioic Acid

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CAS号10144-33-9 2-Acetamido-4-(... | CAS号56-86-0 L-谷氨酸 | CAS号997-55-7 N-乙酰-L-天门冬氨酸

📜在 Palladium On Activated Charcoal N-甲基吗啉,氢气体系中,用 乙醇,水,溶剂黄146,乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应生成异冬谷酸
参考文献:Piotrovskii,L. B.; Dumpis,M. A.; Poznyakova,L. N.,Journal Of Organic Chemistry Ussr (English Translation),1988,Vol. 24,P. 96-100
标题:Piotrovskii,L. B.; Dumpis,M. A.; Poznyakova,L. N.,Journal Of Organic Chemistry Ussr (English Translation),1988,Vol. 24,P. 96-100

专利信息

专利号:US-2025090698-A1
优先权日:2018-11-27
标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases
发明人：CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT
权利人:INDIAN INSTITUTE OF TECH INDORE
摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-9884132-B2
优先权日:2011-11-30
标题 :Homomultivalent and heteromultivalent inhibitors of prostate specific membrane antigen (PSMA) and uses thereof
发明人：POMPER MARTIN G; RAY SANGEETA; MEASE RONNIE C; SHALLAL HASSAN
权利人:UNIV JOHNS HOPKINS
摘要:The present invention provides bivalent and multivalent ligands with a view to improving the affinity and pharmacokinetic properties of a urea class of PSMA inhibitors. The compounds and their synthesis can be generalized to multivalent compounds of other target antigens. Because they present multiple copies of the pharmacophore, multivalent ligands can bind to receptors with high avidity and affinity, thereby serving as powerful inhibitors. The modular multivalent scaffolds of the present invention, in one or more embodiments, contains a lysine-based (âˆ?, ε-) dialkyne residue for incorporating two or more antigen binding moieties, such as PSMA binding Lys-Glu urea moieties, exploiting click chemistry and one or more additional lysine residues for subsequent modification with an imaging and/or therapeutic nuclides or a cytotoxic ligands for tumor cell killing.

专利号:US-11542234-B2
优先权日:2018-03-16
标题 :2-alkoxy-6-[18F]fluoronicotinoyl substituted lys-c(O)-glu derivatives as efficient probes for imaging of PSMA expressing tissues
发明人：NEUMAIER BERND; ZLATOPOLSKIY BORIS; KRAPF PHILIPP; RICHARZ RAPHAEL; DRZEZGA ALEXANDER
权利人:UNIV KOELN
摘要:6-[18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [18F]DCFPyL, [68Ga]HBED-CC-PSMA, [18F]PSMA-1007 and [Al18F]HBED-CC-PSMA. Unexpectedly, the 6-[18F]fluoro-2-alkoxy and 6-[18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the 18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.

专利号:EP-0450715-B1
优先权日:1990-04-02
标题 :Immunogenic compounds, the process for their synthesis and their use in the preparation of antimalaria vaccines
发明人：PESSI ANTONELLO; BIANCHI ELISABETTA; CORRADIN GIAMPIETRO
权利人:ENIRICERCHE SPA
摘要:A class of immunogenic compounds is described, definable by the formula (I): where: D is L-lysine or branched poly(L-lysine) with a number n of L-lysine amino acid residues (Lys) of a and epsilon amide linkage; n is a whole odd number varying from 1 to 15; A and B, which can be the same or different, are a polypeptide consisting of one or more plasmodial B epitopes covalently bound to one or more peptides with an amino acid sequence corresponding to that of a T epitope such as FNNFTVSFWLRVPKVSASHLEA (TT3) and QYIKANSKFIGITE (TT2), a compound of adjuvant activity, or A-CO or B-CO represent a direct bond or R-A-CO or R-B-CO are a protecting group for the alpha or epsilon -amino group of the L-lysine amino acid residue, with the condition that A and B are not both simultaneously an adjuvant or a direct bond or a protecting group; X is an amino acid residue in which R1 is the side chain of a amino acid residue chosen from L-Asp, L-His, L-Cys, L-Gln, L-Thr, L-Ala, L-Leu, L-Met, L-Phe, L-Glu, L-Arg, L-Tyr, L-Asn, L-Ser, L-Gly, L-Val, L-Ileu, L-Pro and L-Trp, and R2 is OH or NH2; R is hydrogen or an acyl radical; and the corresponding pharmaceutically acceptable salts of acid or basic addition. Compounds of formula (I) are particularly suitable as immunogens for preparing genetically non-restricted antimalaria vaccines, and in diagnostics for determining anti-Plasmodium antibodies in blood, serum and blood spot samples.

专利号:EP-0450715-A1
优先权日:1990-04-02
标 题 :Immunogenic compounds, the process for their synthesis and their use in the preparation of antimalaria vaccines