15029-40-0Relevant articles and documents
CONTACT LENS DISPLAYING IMPROVED VISION ATTRIBUTES
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Page/Page column 54, (2021/03/05)
Described are contact lenses that contain high energy visible (HEV) light absorbing compounds and their use for improving one or more vision attributes.
MULTIFOCAL CONTACT LENS DISPLAYING IMPROVED VISION ATTRIBUTES
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Page/Page column 54, (2021/03/05)
Described are multifocal contact lenses that contain high energy visible (HEV) light absorbing compounds and their use for improving one or more vision attributes.
POLYMERIZABLE FUSED TRICYCLIC COMPOUNDS AS ABSORBERS OF UV AND VISIBLE LIGHT
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Page/Page column 55; 56, (2021/01/23)
Described are polymerizable fused tricyclic compounds of formula I: wherein R1, R2, R3, m, n, t, and rings B, C, and D are as defined herein. The compounds absorb various wavelengths of ultraviolet and/or visible light (such as high energy visible light) and are suitable for incorporation in a variety of products, such as biomedical devices and ophthalmic devices.
Structure-activity relationship of spop inhibitors against kidney cancer
Dong, Ze,Wang, Zhen,Guo, Zhong-Qiang,Gong, Shouzhe,Zhang, Tao,Liu, Jiang,Luo, Cheng,Jiang, Hualiang,Yang, Cai-Guang
, p. 4849 - 4866 (2020/06/08)
Speckle-type POZ protein (SPOP) is overexpressed in the nucleus and misallocated in the cytoplasm in almost all the clear-cell renal cell carcinomas (ccRCCs), which leads to kidney tumorigenesis. Previously, we elucidated that the oncogenic SPOP-signaling pathway in ccRCC could be suppressed by 6b that inhibits SPOP-mediated protein interactions. Herein, we have established a structure-activity relationship for 6b analogues as SPOP inhibitors. Compound 6lc suppresses the viability and inhibits the colony formation of ccRCC cell lines driven by cytoplasmic SPOP, superior to 6b. Compound 6lc binds to the SPOP protein in vitro and disrupts SPOP binding to phosphatase-and-tensin homologue (PTEN) in HEK293T cells, which causes the observable phenomena: a decline in the ubiquitination of PTEN, elevated levels of both PTEN and dual-specificity phosphatase 7, and decreased levels of phosphorylated AKT and ERK when ccRCC cell lines are exposed to 6lc in a dose-response manner. Taken together, compound 6lc is a potent candidate against kidney tumorigenesis.
POLYMERIZABLE ABSORBERS OF UV AND HIGH ENERGY VISIBLE LIGHT
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Page/Page column 68-69, (2019/09/18)
Described are polymerizable high energy light absorbing compounds. The compounds absorb various wavelengths of ultraviolet and/or high energy visible light and are suitable for incorporation in various products, such as biomedical devices and ophthalmic devices, such as hydrogel contact lens. The monomers have general formula I below, wherein X is O, S, NR, SO, or S02; Y is a linking group; Pg is a polymerizable group; EWG is an electron withdrawing group.
FTO INHIBITORS
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Paragraph 0221; 0222; 0223, (2017/01/31)
The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
KINASE INHIBITORS
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Paragraph 0393; 0394, (2013/03/26)
Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.
A class of 5-nitro-2-furancarboxylamides with potent trypanocidal activity against Trypanosoma brucei in vitro
Zhou, Linna,Stewart, Gavin,Rideau, Emeline,Westwood, Nicholas J.,Smith, Terry K.
supporting information, p. 796 - 806 (2013/03/28)
Recently, the World Health Organization approved the nifurtimox- eflornithine combination therapy for the treatment of human African trypanosomiasis, renewing interest in nitroheterocycle therapies for this and associated diseases. In this study, we have synthesized a series of novel 5-nitro-2-furancarboxylamides that show potent trypanocidal activity, ~1000-fold more potent than nifurtimox against in vitro Trypanosoma brucei with very low cytotoxicity against human HeLa cells. More importantly, the most potent analogue showed very limited cross-resistance to nifurtimox-resistant cells and vice versa. This implies that our novel, relatively easy to synthesize and therefore cheap, 5-nitro-2-furancarboxylamides are targeting a different, but still essential, biochemical process to those targeted by nifurtimox or its metabolites in the parasites. The significant increase in potency (smaller dose probably required) has the potential for greatly reducing unwanted side effects and also reducing the likelihood of drug resistance. Collectively, these findings have important implications for the future therapeutic treatment of African sleeping sickness.
Cyanoacetamides (IV): Versatile one-pot route to 2-quinoline-3-carboxamides
Wang, Kan,Herdtweck, Eberhardt,Doemling, Alexander
scheme or table, p. 316 - 322 (2012/06/18)
Cyanoacetic acid derivatives are the starting materials for a plethora of multicomponent reaction (MCR) scaffolds. Herein, we describe scope of a valuable general protocol for the synthesis of arrays of 2-aminoquinoline-3-carboxamides from cyanoacetamides and 2-aminobenzaldehydes or heterocyclic derivatives via a Friedlaender reaction variation. In many cases, the reactions involve a very convenient work up by simple precipitation and filtration. More than 40 new products are described. We foresee our protocol and the resulting derivatives becoming very valuable to greatly expanding the scaffold space of cyanoacetamide derivatives.
Synthesis of new 8-formyl-4-methyl-7-hydroxy coumarin derivatives
Manidhar,Rao, K. Uma Maheswara,Reddy, N. Bakthavatchala,Sundar, Ch. Syama,Reddy, C. Suresh
, p. 459 - 463 (2012/11/07)
8-Formyl-4-Methyl-7-Hydroxy Coumarin Derivatives were synthesized via Penchem condensation followed by Duffs reaction. Treatment of this with N,N-di substituted cyano acetamides in the presence of piperdine afforded New 8- Formyl-4-Methyl-7-Hydroxy Coumarin Derivatives (7a-o). Their structures were characterized by IR, 1H and 13C NMR and Mass spectral and elemental analysis data.