专利号:US-9556140-B2 优先权日:2013-01-26 标 题 :Approach for synthesis of catechins 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; RAI KUMAR SANTOSH; TRIPATHI VINAYAK; PATIL ISHWAR RAKESH 权利人:SPHAERA PHARMA PRIVATE LTD 摘要:A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or −) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (−)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.
专利号:WO-9941984-A9 优先权日:1998-02-20 标 题 :INTERACTION BETWEEN THE MEC1-DEPENDENT DNA SYNTHESIS CHECKPOINT AND G1 CYCLIN FUNCTION IN $i(SACCAROMYCES CEREVISIAE) 发明人:VALLEN ELIZABETH A; CROSS FREDERICK R 权利人:HUTCHINSON FRED CANCER RES 摘要:The completion of DNA synthesis in yeast is monitored by a checkpoint that requires MEC1 and RAD53. Overexpression of the S. cerevisiae G1 cyclin CLN1 results in genomic instability and lethality of mec1-1 checkpoint-deficient cells compared to cln1 cln2 mec1-1 cells. Here we show that overexpression of CLN2 or CLB5, but not CLN3, also killed mec1-1 strains. We identified RNR1, which encodes a subunit of ribonucleotide reductase, as a high-copy suppressor of the lethality of mec1-1 GAL1-CLN1. Northern analysis demonstrated that RNR1 expression is reduced by CLN1 or CLN2 overexpression. Since limiting RNR1 expression might decrease dNTP pools, CLN1 or CLN2 may cause lethality in mec1-1 strains by causing initiation of DNA replication with inadequate dNTP pools. In MEC1 strains, a delay of S phase due to the checkpoint would occur, but in mec1-1 strains lethality would result. Consistent with this model, CLN1 overexpression did result in a prolongation of S phase in a MEC1 background. In a cln1 cln2 background, a prolonged period of expression of genes turned on at the G1-S border has been observed. Thus deletion of CLN1 and CLN2 could function similarly to overexpression of RNR1 in suppressing mec1-1 lethality. While Mec1p has been proposed to act in a linear pathway upstream of Rad53p, rad53 lethality was rescued little by deletion of CLN1 and CLN2, suggesting that Rad53p has Mec1-independent activities.
专利号:US-11617804-B2 优先权日:2014-07-18 标题:Hyaluronic acid-based nanoparticles as biosensors for imaging-guided surgery and drug delivery vehicles and methods associated therewith 发明人:MOHS AARON MICHAEL; HILL TANNER KINKADE; KELKAR SNEHA SANJAY; KRIDEL STEVE 权利人:UNIV WAKE FOREST 摘要:The present invention relates to intraoperative fluorescent imaging (IFI) used both pre-clinically using in-vivo models, as well as clinically to map sentinel lymph nodes in breast cancer, skin cancer, GI cancer, lung cancer, prostate cancer and several other cancers. IFI can be used to image solid tumors both non-specifically in hepatobiliary and breast cancers as well as in prostate and ovarian cancer. In one embodiment, two-dimensional resolution to 10 μm 2 is possible with optical imaging, significantly higher than other imaging modalities. n In one embodiment, the present invention relates to a series of self-assembled nanoparticles using HLA (hyaluronic acid) as both a polymeric backbone as well as targeting ligand. In some embodiments, the present invention relates to the synthesis of HLA conjugates, and the effect of variation of the hydrophobic ligand structure and conjugation level on nanoparticle self-assembly, size, ICG loading efficiency, and ICG fluorescence quenching and reactivation.
专利号:JP-2020117531-A 优先权日:2013-01-26 标题 :Novel process for synthesis of catechins
专利号:US-11878963-B2 优先权日:2021-05-10 标 题:Semi synthetic method for dihydroquercetin 发明人:JI JUNQIU; LI XIAOCHANG; LI QIAO; CHEN JUN; LI BING; LIU RURU; ZHAO XIAOHONG 权利人:HEFEI LIFEON PHARMACEUTICAL CO LTD 摘要:The present disclosure provides a semi-synthetic method of dihydroquercetin, belonging to the field of synthesis of organic drugs. The semi-synthetic method includes the following steps: adding quercetin dihydrate to solvent water adjusted to be alkaline with an alkalizing reagent, heating and stirring to dissolve the mixture, and then adding thiourea dioxide under the protection of an inert gas to perform a reduction reaction, to obtain an endpoint reduction reaction solution; diluting the endpoint reduction reaction solution with water and cooling the resultant, and then acidizing, aging, and filtering the resultant to obtain a filtrate and a filter cake; extracting, washing, drying, concentrating, and repeatedly crystallizing the filtrate to obtain dihydroquercetin; and recycling the filter cake after being washed.
专利号:US-8673983-B2 优先权日:2007-12-21 标题:Melanins synthesized chemically or via enzyme catalysis 发明人:HOLMES EARLE W; THOMPSON KENNETH D 权利人:HOLMES EARLE W; THOMPSON KENNETH D; UNIV LOYOLA CHICAGO 摘要:The present invention provides an enzymatic and a chemical synthesis of melanins and novel melanins.
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