- HEADGROUP LIPID COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
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The application relates to lipids of Formula (A-1) and compositions involving the same. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) include such a lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) further including therapeutic and/ or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
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Paragraph 00411
(2021/04/01)
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- MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.
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Paragraph 0090; 0091
(2019/11/05)
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- Pyrano[3,2-c] julolidin-2-ones: A novel class of fluorescent probes for ratiometric detection and imaging of Hg2+ in live cancer cells
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A novel pyrano[3,2-c]julolidin-2-one based fluorescent molecular rotor PYJO4 has been designed and developed for selective ratiometric detection, quantification and imaging of intracellular Hg2+ in live cells. The probe operates via a Twisted Intramolecular Charge Transfer (TICT) mechanism and exhibits high selectivity and sensitivity up to 1.14 ppb. PYJO4 coated test strips can be used to detect mercury ions in contaminated water.
- Jha, Ajay Kumar,Umar, Shahida,Arya, Rakesh Kumar,Datta, Dipak,Goel, Atul
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p. 4934 - 4940
(2016/07/26)
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- Novel pyranopyrandione compounds or pharmaceutically acceptable salts thereof, process for preparing thereof and pharmaceutical composition comprising the same for treating disease derived from allergic inflammatory response
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The present invention relates to novel pyranopyrandione compounds or pharmaceutically acceptable salts thereof, preparing methods thereof, and pharmaceutical compositions comprising the same for treating diseases resulting from allergic inflammatory respo
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Paragraph 0070-0074
(2017/05/11)
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- Design and synthesis of potent N-phenylpyrimidine derivatives for the treatment of skin cancer
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The development of novel synthetic compounds for the treatment of skin cancer is much needed, as there is a sudden rise in the incidence of skin cancer throughout the world and the available chemotherapy is facing problems of resistance. Hence, present re
- Chaube, Udit J.,Vyas, Vivek K.,Bhatt, Hardik G.
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p. 10285 - 10297
(2016/02/09)
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- New fluoranthene FLUN-550 as a fluorescent probe for selective staining and quantification of intracellular lipid droplets
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A new class of live cell permeant, nontoxic fluoranthene-based fluorescent probe (FLUN-550) having a high Stokes shift in aqueous medium has been discovered. It showed selective staining of lipid droplets (LDs, dynamic cytoplasmic organelles) at a low con
- Goel, Atul,Sharma, Ashutosh,Kathuria, Manoj,Bhattacharjee, Arindam,Verma, Ashwni,Mishra, Prabhat R.,Nazir, Aamir,Mitra, Kalyan
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supporting information
p. 756 - 759
(2014/03/21)
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- A regioselective synthesis of 2,6-diarylpyridines
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A regioselective synthesis of 2,6-diarylpyridines through base (sodium hydroxide in DMSO) catalyzed ring transformation of suitably functionalized 2H-pyran-2-ones with benzamide has been delineated. However, similar reaction of 2H-pyran-2-ones with benzam
- Maurya, Hardesh K.,Vasudev, Prema G.,Gupta, Atul
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p. 12955 - 12962
(2013/08/23)
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- Synthesis and antiviral bioactivities of 2-cyano-3-substitutedamino(phenyl) methylphosphonylacrylates (Acrylamides) containing alkoxyethyl moieties
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An efficient reaction under microwave irradiation has been developed for the synthesis of a series of novel 2-cyano-3-substituted-amino(phenyl) methylphosphonylacrylates (acrylamides) II. The products obtained in shorter reaction time with moderate yields are fully characterized by elemental analysis, IR, 1H, 13C, and 31P NMR spectral data. The role of introducing various substituents and the effect of incorporating a-aminophosphonates with an alkoxyethyl moiety into the parent cyanoacrylate (acrylamide) structure are investigated. Among the studied compounds, both II-17 and II-24 displayed good in vivo curative, protection, and inactivation effects, which were comparable to those of the commercial reference ningnanmycin (inhibitory rates of 58.8, 60.2, 78.9% and 60.0, 58.9, 85.5%, respectively, at 500 mg/L against TMV). To the best of the authors' knowledge, this is the first report on the synthesis and antiviral activity of the title compounds II.
- Yang, Jia-Qiang,Song, Bao-An,Bhadury, Pinaki S.,Chen, Zhuo,Yang, Song,Xue-Jian, Cai,Hu, De-Yu,Xue, Wei
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experimental part
p. 2730 - 2735
(2011/07/31)
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- Donor-acceptor 9-uncapped fluorenes and fluorenones as stable blue light emitters
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The "green emission defect" (GED) produced by fluorenones has significantly retarded the commercial scope of fluorene-based B-OLEDs. In this paper, for the first time, it is demonstrated that the "green light" emitting fluorenones 7 can be converted to "b
- Goel, Atul,Chaurasia, Sumit,Dixit, Manish,Kumar, Vijay,Prakash, Sattey,Jena, Bijayalaxmi,Verma, Jai K.,Jain, Mayank,Anand,Manoharan, S. Sundar
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supporting information; experimental part
p. 1289 - 1292
(2009/08/08)
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- Synthesis and antiviral activities of cyanoacrylate derivatives containing an α-aminophosphonate moiety
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Target compounds 8 were obtained by the reaction of alkyl 2-cyano-3,3-dimethylthioacrylate or cyarylamide (7a-7e) and α- aminobenzylphosphonate (5a-5e) under reflux condition using ethanol as solvent. Their structures were clearly verified by spectroscopic data (IR and 1H, 13C, and 31P NMR) and elemental analysis. These compounds were shown to be antivirally active in the bioassay. It was found that title compounds 8d and 8e had the same inactivation effect against tobacco mosaic virus (EC50 = 55.5 and 55.3 μg/mL) as the commercial product ningnanmycin (EC50 = 50.9 μg/mL). To the best of our knowledge, this is the first report on the synthesis and antiviral activity of cyanoacrylate derivatives containing an α-aminophosphonate moiety.
- Long, Ning,Cai, Xue-Jian,Song, Bao-An,Yang, Song,Chen, Zhuo,Bhadury, Pinaki S.,Hu, De-Yu,Jin, Lin-Hong,Xue, Wei
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scheme or table
p. 5242 - 5246
(2010/04/06)
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- Synthesis, antiviral and antifungal bioactivity of 2-cyano-acrylate derivatives containing phosphonyl moieties
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Alkyl 2-cyano-3-methylthio-3-phosphonylacrylates were synthesized by the reaction of alkyl 2-cyano-3,3-dimethylthioacrylates with dialkyl phosphites. The structures of the new compounds were characterized by elemental analyses, IR, 1H-, 13
- Lv, Yin-Pu,Wang, Xian-You,Song, Bao-An,Yang, Song,Yan, Kai,Xu, Guang-Fang,Bhadury, Pinaki S.,Liu, Fang,Jin, Lin-Hong,Hu, De-Yu
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p. 965 - 978
(2008/02/07)
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- Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors
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N,N′-Disubstituted ketene aminals are good bioisosteres of thiourea functional groups. We report the design and synthesis of a novel class of ketene aminal-based lactam derivatives as potent and orally active FXa inhibitors.
- Shi, Yan,Zhang, Jing,Stein, Philip D.,Shi, Mengxiao,O'Connor, Stephen P.,Bisaha, Sharon N.,Li, Chi,Atwal, Karnail S.,Bisacchi, Gregory S.,Sitkoff, Doree,Pudzianowski, Andrew T.,Liu, Eddie C.,Hartl, Karen S.,Seiler, Steven M.,Youssef, Sonia,Steinbacher, Thomas E.,Schumacher, William A.,Rendina, Alan R.,Bozarth, Jeffrey M.,Peterson, Tara L.,Zhang, Ge,Zahler, Robert
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p. 5453 - 5458
(2007/10/03)
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- 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof
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Novel 6-heterocyclyl-pyrazolo[3,4-d]pyrimidin-4-ones, useful in treating cardiovascular disease, are prepared by reacting a 5-amino-1H-pyrazole-4-carboxamide with heterocyclylcarboxaldehyde or by reacting a 5-amino-1H-pyrazole-4-carbonitrile with a heterocyclylcarboxamidine, followed by diazotization and hydrolysis of the resulting 4-amino-6-heterocyclyl-pyrazolo[3,4-d]pyrimidine.
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- Synthesis, Reactions, and Tautomerism of Ketene N,S-Acetals with Benzothiazoline Ring
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Ketene dithioacetals 2 react with 2-aminothiophenol to afford the corresponding substituted 2(3H)-methylenebenzothiazoles 3.Some compounds 3 react with α,β-unsaturated esters to give 1H-pyridobenzothiazole derivatives 4 and 5 by an electrophilic addition and cyclocondensation sequence.
- Huang, Zhi-Tang,Shi, Xian
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p. 541 - 547
(2007/10/02)
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- 4H-quinolizin-4-one compounds useful for the treatment of allergic bronchial asthma, allergic rhinitis atropic dermatitis and the like
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This invention provides novel 4H-quinolizin-4-one compounds which exhibit a selective inhibitory activity against IgE-antibody formation, and have utility for treatment of diseases associated with IgE formation in mammals, such as allergic bronchial asthma, allergic rhinitis, atopic dermatitis, hypersensitiveness, and the like.
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