1196153-28-2Relevant articles and documents
COMPOUNDS AND THEIR USES AS SPLEEN TYROSINE KINASE INHIBITORS
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Paragraph 0102, (2021/12/28)
Provided are compounds of Formula (I) which can be used as Syk inhibitors and potently as therapeutic agents against diseases mediated by Syk.
Macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one and pharmaceutical composition and application thereof
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Paragraph 0384; 0385; 0386, (2018/10/19)
The present invention relates to a macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one as shown in the formula (I) and/or a pharmaceutically acceptable salt thereof, and a composition of a compound of the formula (I) and/or a pharmaceutically acceptable salt thereof, a preparation method thereof, application thereof as a Wee1 inhibitor and application thereof as a sensitizer for cancer chemotherapy or radiotherapy. The macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one can effectively inhibit Wee1 and related signaling pathways, and has good cancer treatment and/or relieving effect.The formula is shown in the description.
SYK INHIBITORS
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Paragraph 3321-3323, (2016/10/07)
The present disclosure a Syk compound inhibitors, including state cancer and inflammation and various disease States thereof in the treatment of relates to the use of. In one aspect a particular embodiment, . given by formula I which is marked as a chemical structure of compound. In formula said, X 1, X 2, X 3, R 2, R 3, R 4, R 5, and Y has described herein is. The present disclosure of a formula I compounds or a pharmaceutically acceptable salt of pharmaceutical compositions including, mediated by Syk and to treat conditions a employing these compounds and compositions further provides a method. (by machine translation)
Structure activity relationship of pyridoxazinone substituted RHS analogs of oxabicyclooctane-linked 1,5-naphthyridinyl novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-6)
Singh, Sheo B.,Kaelin, David E.,Wu, Jin,Miesel, Lynn,Tan, Christopher M.,Meinke, Peter T.,Olsen, David B.,Lagrutta, Armando,Wei, Changqing,Liao, Yonggang,Peng, Xuanjia,Wang, Xiu,Fukuda, Hideyuki,Kishii, Ryuta,Takei, Masaya,Yajima, Masanobu,Shibue, Taku,Shibata, Takeshi,Ohata, Kohei,Nishimura, Akinori,Fukuda, Yasumichi
, p. 3636 - 3643 (2015/08/06)
Abstract Oxabicyclooctane linked 1,5-naphthyridinyl-pyridoxazinones are novel broad-spectrum bacterial topoisomerase inhibitors (NBTIs) targeting bacterial DNA gyrase and topoisomerase IV at a site different than quinolones. Due to lack of cross-resistance to known antibiotics they present excellent opportunity to combat drug-resistant bacteria. A structure activity relationship of the pyridoxazinone moiety is described in this Letter. Chemical synthesis and activities of NBTIs with substitutions at C-3, C-4 and C-7 of the pyridoxazinone moiety with halogens, alkyl groups and methoxy group has been described. In addition, substitutions of the linker NH proton and its transformation into amide analogs of AM-8085 and AM-8191 have been reported. Fluoro, chloro, and methyl groups at C-3 of the pyridoxazinone moiety retained the potency and spectrum. In addition, a C-3 fluoro analog showed 4-fold better oral efficacy (ED50 3.9 mg/kg) as compared to the parent AM-8085 in a murine bacteremia model of infection of Staphylococcus aureus. Even modest polarity (e.g., methoxy) is not tolerated at C-3 of the pyridoxazinone unit. The basicity and NH group of the linker is important for the activity when CH2 is at the linker position-8. However, amides (with linker position-8 ketone) with a position-7 NH or N-methyl group retained potency and spectrum suggesting that neither basicity nor hydrogen-donor properties of the linker amide NH is essential for the activity. This would suggest likely an altered binding mode of the linker position-7,8 amide containing compounds. The amides showed highly improved hERG (functional IC50 >30 μM) profile.
Rational design and synthesis of novel Syk-kinase inhibitors
Zeifman, Alexey A.,Titov, Ilya Yu.,Svitanko, Igor V.,Rakitina, Tatiana V.,Lipkin, Aleksey V.,Stroylov, Viktor S.,Stroganov, Oleg V.,Novikov, Fedor N.,Chilov, Ghermes G.
scheme or table, p. 73 - 74 (2012/07/03)
Molecular modeling and subsequent synthesis of novel Syk-kinase inhibitors, 7H-pyrrolo[2,3-d]pyrimidine and 1,3,5-triazine derivatives, have been carried out. The best of the obtained compounds demonstrated to inhibit Syk-kinase activity at IC50/sub
BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
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Page/Page column 100, (2011/06/16)
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.