- NANOMATERIALS
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Lipid nanoparticle compositions for delivery of nucleic acids are described. In various embodiments the lipid nanoparticle contains an ionizable lipid of the Formula (I). Methods of using such lipid nanoparticle compositions to achieve targeted delivery of therapeutic cargo without the need for a targeting ligand are also provided.
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Paragraph 0320; 0321; 0322
(2021/07/17)
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- NANOMATERIALS
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Lipid nanoparticle compositions for delivery of nucleic acids are described. The lipid nanoparticle may contain a conformationally constrained ionizable lipid as part of the composition. These compositions may allow for delivery of cargo without the need for a targeting ligand.
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Paragraph 0436-0438
(2021/06/11)
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- FLAME RETARDANT ITACONIC ACID-BASED COMPOUNDS
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A flame retardant itaconic acid-based compound, a process for forming a flame retardant polymer, and an article of manufacture comprising a material that contains a flame retardant itaconic acid-based polymer are disclosed. The flame retardant itaconic acid-based compound has variable moieties, which include methylene bridge groups, carbonyl groups, vinyl groups, functionalized groups, phenyl-substituted flame retardant groups, and/or functionalized flame retardant groups. The process for forming the flame retardant polymer includes forming a phosphorus-based flame retardant molecule, forming an itaconic acid derivative, chemically reacting the phosphorus-based flame retardant molecule and the itaconic acid derivative to form a flame retardant itaconic acid-based compound, and incorporating the itaconic acid-based flame retardant compound into a polymer to form the flame retardant polymer.
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Paragraph 0053
(2019/04/25)
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- Insecticide dinotefuran intermediate 3 - hydroxy methyl tetrahydrofuran synthetic method
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The invention discloses a synthetic method of pesticide dinotefuran intermediate 3-hydroxymethyl tetrahydrofuran, and the synthetic method is as follows: reacting compound succinic acid dialkyl ester with formic acid alkyl ester in the presence of a strong alkali to obtain a compound III, then obtaining a compound II by a reduction reaction, finally, in the presence of an acid catalyst, obtaining a compound shown as formula I by a dehydration cyclization reaction, and R or R ' respectively independently represents C1-5 alkyl. The synthetic method is low in raw material cost, simple in reaction operation, less in pollution, high in yield of each step, 99% in the yield of the reducing step, and suitable for industrial production.
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Paragraph 0029; 0048; 0049
(2018/04/01)
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- Method for synthesizing 3-tetrahydrofurfuryl alcohol
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The invention relates to a method for synthesizing 3-tetrahydrofurfuryl alcohol. According to the technical scheme, 2-bromoethanol and diethyl malonate serve as starting materials, under the alkaline condition, 2-hydroxyethyl-diethyl malonate is generated through a reaction, hydrolysis is conducted on the 2-hydroxyethyl-diethyl malonate to generate 2-hydroxyethyl-malonate, catalyzing and high-pressure hydrotreatment are conducted on the 2-hydroxyethyl-malonate to generate 2-hydroxymethyl-1,4-butanediol, and dehydration cyclization is conducted on the 2-hydroxyethyl-1,4-butanediol to generate the 3-tetrahydrofurfuryl alcohol. According to the method for synthesizing the 3-tetrahydrofurfuryl alcohol, the yield can reach over 85 percent, the purity can reach above 95 percent, the reaction condition is mild, the cost is low, operation is easy, and the method has the advantage of being suitable for industrial production.
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Paragraph 0007; 0022
(2017/01/17)
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- A 3-hydroxy methyl tetrahydrofuran method for the synthesis of
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The invention discloses a synthetic method for 3-hydroxylmethal tetrahydrofuran. The synthetic method comprises the following steps: with 2-chloroethanol and diethyl malonate as raw materials, reacting under the action of alkaline in the presence of an organic solvent or in absence of a solvent to obtain an intermediate 2-ethoxy-diethyl succinate; then, reducing the intermediate 2-ethoxy-diethyl succinate by virtue of metal borohydride to obtain 2-hydroxymethyl-1,4-butanediol; and finally, producing 3-hydroxylmethal tetrahydrofuran under the action of a dehydrating agent. According to the synthetic method, the usage amount of the reducing agent metal borohydride is remarkably lowered, and yield of a byproduct sodium metaborate is reduced at the same time. The invention provides the synthetic method for the drug intermediate 3-hydroxylmethal tetrahydrofuran.
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Paragraph 0020
(2017/03/08)
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- Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents
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NAmPRTase (PBEF/Visfatin) plays a pivotal role in the salvage pathway of NAD+ biosynthesis. NAmPRTase has been an attractive target for anti-cancer agents that induce apoptosis of tumor cells via a declining plasma NAD+ level. In this report, a series of structural analogs of FK866 (1), a known NAmPRTase inhibitor, was synthesized and tested for inhibitory activities against the proliferation of cancer cells and human NAmPRTase. Among them, compound 7 showed similar anti-cancer and enzyme inhibitory activities to compound 1. Further investigation of compound 7 with X-ray analysis revealed a co-crystal structure in complex with human NAmPRTase, suggesting that Asp219 in the active site of the enzyme could contribute to an additional interaction with the pyrrole nitrogen of compound 7.
- You, Hyun,Youn, Hyung-Seop,Im, Isak,Bae, Man-Ho,Lee, Sang-Kook,Ko, Hyojin,Eom, Soo Hyun,Kim, Yong-Chul
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experimental part
p. 1153 - 1164
(2011/04/17)
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- Novel isopentenyladenosine analogues: Synthesis, characterization, and evaluation of antiproliferative activity on bladder carcinoma cells
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Isopentenyladenosine (iPA), a member of the cytokinin family of plant hormones, exerts a marked antiproliferative activity on some leukemic and epithelial cancer cell lines. To characterize the molecular moieties required for the in vitro antitumor activity of the molecule and to obtain cytostatic iPA derivatives potentially useful as chemotherapeutic agents, N9-acyclic analogues have been synthesized using regioselective Mitsunobu reaction and characterized by elemental analyses, 1H and 13C NMR. These compounds were analyzed for their activity on human bladder cancer cell lines. In this study, we report that iPA inhibited the proliferation but not the migration of human bladder cancer cells, while the newly synthesized analogues revealed no significant cytostatic activity apart from the compound with a saturated double bond of the isopentenyl chain. These results indicate that the integrity of the ribose ring is required for the cytostatic activity of iPA.
- Ottria, Roberta,Casati, Silvana,Maier, Jeanette A. M.,Mariotti, Massimo,Ciuffreda, Pierangela
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experimental part
p. 736 - 751
(2010/09/04)
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- PREVENTION AND TREATMENT OF CANCER AND OTHER DISEASES
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Nucleoside chemical compounds, which interact with specific structures of deoxyribonucleic acid (DNA) or ribonucleic acid (RNA) are disclosed. The compounds interfere with the activities of telomerase and reverse transcriptase, and are useful as antivirals, antibacterials and anticancer agents. Methods of treating or preventing cancers in patients involving administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases (RTs) expressed in cells of the patients are also disclosed. Method of using nucleoside analogs and other inhibitors of RTs in conjunction with DNA damaging agents such as genotoxic agents or radiation or photodynamic therapy or combinations these for the treatment of various cancers are also disclosed.
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Page/Page column 68
(2008/06/13)
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- DUTPASE INHIBITORS
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Deoxyuridine derivatives of the formula (I) where R1 is H or various substituents; D is -NHCO-, -CONH-, -0-, -C(=O)-, -CH=CH, -CΞC-, -NR5-; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is -O-, -S-, -CHR10-, -C(=O)-; J is -CH2-, or when G is CHR10 may also be -O- or -NH-; R10 is H, F, -CH3, -CH2NH2, -CH2OH; -OH R11 is H, F, -CH3, -CH2 NH2, -CH2OH, CH(OH)CH3, CH(NH3)CH3; or R10 and R11 together define an olefinic bond, or together form a -CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.
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Page/Page column 40
(2008/06/13)
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- An Improved Total Synthesis of PET HSV-tk Gene Reporter Probe 9-(4-[ 18F]Fluoro-3-hydroxymethylbutyl)guanine ([18F]FHBG)
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An improved total synthesis of [18F]FHBG starting from triethyl-1,1,2-ethanetricarboxylate and 2-amino-6-chloropurine is reported. [18F]FHBG was prepared by nucleophilic substitution of the appropriate precursor with [18F]KF/Kryptofix 2.2.2 followed by a quick deprotection reaction and purification with a simplified Silica Sep-Pak solid-phase extraction (SPE) method in 20-25% radiochemical yield.
- Zheng, Qi-Huang,Wang, Ji-Quan,Liu, Xuan,Fei, Xiangshu,Mock, Bruce H.,Glick-Wilson, Barbara E.,Sullivan, Michael L.,Raikwar, Sudhanshu P.,Gardner, Thomas A.,Kao, Chinghai,Hutchins, Gary D.
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p. 689 - 704
(2007/10/03)
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- Selective and Practical Synthesis of Penciclovir
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A selective and practical method has been developed for the synthesis of penciclovir (1) in gram quantities involving a highly N9 selective alykylation of 2-amino-6-chloropurine (9) with 2-(2-phenyl-1,3-dioxane-5-yl)ethanol (12) as a key step.
- Toyokuni, Tatsushi,Walsh, Joseph C.,Namavari, Mohammad,Shinde, Shirin S.,Moore, Jennifer R.,Barrio, Jorge R.,Satyamurthy, Nagichettiar
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p. 3897 - 3905
(2007/10/03)
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- Novel radiosynthesis of PET HSV-tk gene reporter probes [ 18F]FHPG and [18F]FHBG employing dual Sep-Pak SPE techniques
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Positron emission tomography (PET) herpes simplex virus thymidine kinase (HSV-tk) gene reporter probes 9-[(3-[18F]fluoro-1-hydroxy-2-propoxy) methyl]guanine ([18F]FHPG) and 9-(4-[18F]fluoro-3- hydroxymethylbutyl)guanine ([18F]FHBG) were prepared by nucleophilic substitution of the appropriate tosylated precursors with [18F]KF/ Kryptofix 2.2.2 followed by a quick deprotection reaction and purification with a simplified dual Silica Sep-Pak solid-phase extraction (SPE) method in 15-30% radiochemical yield.
- Wang, Ji-Quan,Zheng, Qi-Huang,Fei, Xiangshu,Mock, Bruce H.,Hutchins, Gary D.
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p. 3933 - 3938
(2007/10/03)
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- A mild and rapid regeneration of alcohols from their allylic ethers by chlorotrimethylsilane/sodium iodide
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A new extremely facile and efficient cleavage of allyl ethers is developed employing chlorotrimethylsilane/sodium iodide.
- Kamal,Laxman,Venugopal Rao
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p. 371 - 372
(2007/10/03)
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- Synthesis and Antiviral Activity of 9-purines
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Alkylation of 2-amino-6-chloropurine with 5-(2-bromoethyl)-2,2-dimethyl-1,3-dioxane (5) provided 2-amino-6-chloro-9-purine (6) in high yield.This aminochloropurine 6 readily converted to the antiviral acyclonucleoside 9-guanine (1) and to its 6-chloro (10), 6-thio (11), 6-alkoxy (12-17), 6-amino (20), and 6-deoxy (21) purine analogues.The guanine derivative 1 was converted to its xanthine analogue 9.Similarly, alkylation of 6-chloropurine with 5 provided a route to 8, the hypoxanthine analogue of 1.Of these 9-substituted purines, the guanine derivative 1 showed the highest activity against herpes simplex virus types 1 and 2 in cell cultures, and in some tests it was more active than acyclovir, with no evidence of toxicity for the cells.A series of monoesters (30-33) and diesters (24-27, 29) of 1 were prepared, and some of these also showed antiherpes virus activity in cell cultures, the most active ester being the dihexanoate 27.
- Harnden, Michael R.,Jarvest, Richard L.,Bacon, Teresa H.,Boyd, Malcolm R.
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p. 1636 - 1642
(2007/10/02)
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- AN IMPROVED SYNTHESIS OF THE ANTIVIRAL ACYCLONUCLEOSIDE 9-(4-HYDROXY-3-HYDROXYMETHYLBUT-1-YL)GUANINE
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Alkylation of 2-amino-6-chloropurine with 5-(2-bromoethyl)-2,2-dimethyl-1,3-dioxan (7) and subsequent acid hydrolysis provides an improved procedure for synthesis of the antiviral acyclonucleoside 9-(4-hydroxy-3-hydroxymethylbut-1-yl)guanine (3).
- Harnden, M.R.,Jarvest, R.L.
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p. 4265 - 4268
(2007/10/02)
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