224309-64-2Relevant academic research and scientific papers
LIPID NANOPARTICLE COMPOSITION
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Paragraph 00477, (2021/10/15)
Provided herein are lipids that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination.
Material for adsorbing hexamethyldisiloxane
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Paragraph 0012, (2019/10/01)
TiO2 as a photocatalytic material having excellent performance has the most practical prospects in the field of organic waste gas treatment. Hexamethyldisiloxane is a commonly used solvent with high volatility. When TiO2 photocatalytic treatment is perfor
Design, synthesis, and biological evaluation of radioiodinated benzo[d]imidazole-quinoline derivatives for platelet-derived growth factor receptor β (PDGFRβ) imaging
Effendi, Nurmaya,Mishiro, Kenji,Takarada, Takeshi,Yamada, Daisuke,Nishii, Ryuichi,Shiba, Kazuhiro,Kinuya, Seigo,Odani, Akira,Ogawa, Kazuma
, p. 383 - 393 (2019/01/04)
Several malignant tumors and fibrotic diseases are associated with PDGFRβ overexpression and excessive signaling, making this receptor attractive for molecular targeting and imaging approaches. A series of benzo[d]imidazole-quinoline derivatives were designed and synthesized to develop radioiodinated compounds as PDGFRβ-specific imaging probes. The structure activity relationship (SAR) evaluation of the designed compounds was performed. Among them, 2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]-8-(piperazin-1-yl)quinoline (5a) and 4-{2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl}morpholine (5d) exhibited a relatively high PDGFRβ-TK inhibitory potency, whereas iodinated 5a derivative 5-iodo-2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]-8-(piperazin-1-yl)quinoline (8) exhibited a superior inhibitory potency as PDGFRβ inhibitor than iodinated 5d derivative 4-{5-iodo-2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl}morpholine (11). Furthermore, [125I]8 and [125I]11 were synthesized and evaluated for PDGFRβ radioligand ability, both in vitro and in vivo. Cellular uptake experiments showed that [125I]8 had a higher uptake in BxPC3-luc cells as PDGFRβ-positive cells than [125I]11. Incubation of [125I]8 after pretreatment of PDGFRβ ligands significantly reduced the uptake of [125I]8. In biodistribution experiments using tumor-bearing mice, [125I]8 accumulation in the tumor 1 h postinjection was higher than that of the benzo[d]imidazol-quinoline derivative [125I]IIQP, used in our previous research. These results indicate that [125I]8 could be a promising PDGFRβ imaging agent. Although its clinical application requires further structural modifications, the results obtained in this research may be useful for the development of PDGFRβ-specific radioligands.
POLYCYCLIC COMPOUNDS AS INHIBITORS OF BRUTON'S TYROSINE KINASE
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Page/Page column 103; 123, (2017/07/06)
The present disclosure is directed to compounds of Formula (I) as Bruton's kinase inhibitors and their preparation, as well as compositions comprising compounds of Formula (I).
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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Paragraph 00217; 00218, (2015/02/25)
The present invention relates to compounds of formula I: in which n, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a pro
THERAPEUTICALLY ACTIVE COMPOUNDS AND USE THEREOF
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Page/Page column 64; 65, (2015/02/19)
Provided are therapeutically active compounds and the use in manufacture of medicaments for treating a cancer characterized by the presence of a mutant allele of IDH1.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column 64, (2015/02/19)
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column, (2015/03/31)
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column, (2015/02/19)
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
Synthesis and structure-activity relationship studies on novel 8-amino-3-[2-(4-fluorophenoxy)ethyl]-1,3-diazaspiro[4.5]decane-2,4-dione derivatives as anticonvulsant agents
Madaiah,Prashanth,Revanasiddappa,Veeresh
, p. 2633 - 2644 (2013/07/26)
A series of novel 8-amino-3-[2-(4-fluorophenoxy)ethyl]-1,3-diazaspiro[4.5] decane-2,4-dione derivatives 7-36 was synthesized and their pharmacological activity was determined with the objective to better understand their structure-activity relationship for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) test and their neurotoxic effects were determined by rotarod test. Majority of the compounds were active in MES tests. Compounds 24, 27, and 34 showed a significant and protective effect on seizure, when compared with standard drug phenytoin. The compounds having amide bond showed moderate protective effect on MES induced seizures compared to sulfonamide.
