专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:WO-2007142258-A1 优先权日:2006-06-06 标 题 :Anthocyanin synthesis regulatory gene, and use thereof 发明人:MANO HIRONORI; SATO KAZUHITO; HIGO HIROMI; MINOBE YUZO 权利人:PLANT GENOME CT CO LTD; MANO HIRONORI; SATO KAZUHITO; HIGO HIROMI; MINOBE YUZO 摘要:A cDNA library is constructed from a tuberous root of each of 'Kokei No.14' (which is a sweet potato cultivar) and 'Ayamurasaki' (which is a new-type sweet potato cultivar containing a large amount of anthocyanin), thereby obtaining cDNA which can be expressed specifically in Ayamurasaki. An analysis is made on the expression of the cDNA, and it is found that the cDNA is strongly expressed only in a tuberous root of Ayamurasaki. The sequencing of the gene is made, and it is found that the gene has an R2R3-MYB domain and encodes a protein comprising 249 amino acid residues. Thus, a gene which regulates the synthesis of anthocyanin in a sweet potato is successfully identified. By using the gene, it becomes possible to produce a plant having an increased anthocyanin content.
专利号:US-10772971-B2 优先权日:2017-06-22 标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates 发明人:GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V 权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC 摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.
专利号:US-7994222-B2 优先权日:2006-09-05 标 题:Monitoring of the inhibition of fatty acid synthesis by iodo-nitrobenzamide compounds 发明人:OSSOVSKAYA VALERIA S; SHERMAN BARRY M 权利人:BIPAR SCIENCES INC 摘要:The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis.
专利号:US-9993570-B2 优先权日:2014-01-05 标题:Radiolabeled tracers for poly (ADP-ribose) polymerase-1 (PARP-1), methods and uses therefor 发明人:MACH ROBERT; CHU WENHUA; ZHOU DONG; MICHEL LOREN; CHEN DELPHINE 权利人:UNIV WASHINGTON 摘要:Disclosed are PARP-1 inhibitors, which can be 18 F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC 50 =6.3 nM). Synthesis of [ 18 F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET imaging using [ 18 F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [ 18 F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging.
专利号:US-9598418-B2 优先权日:2012-12-31 标 题:Substituted phthalazin-1 (2H)-one derivatives as selective inhibitors of poly (ADP-ribose) polymerase-1 发明人:SRIVASTAVA BRIJESH K; DESAI RANJIT C; PATEL PANKAJ R 权利人:CADILA HEALTHCARE LTD 摘要:The present invention relates to novel compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to a process of preparing novel compounds of general formula (I), their stereoisomers, regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
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合成参考文献
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