24015-98-3Relevant academic research and scientific papers
FUSED HETEROCYCLIC DERIVATIVES, THEIR PREPARATION METHODS THEREOF AND MEDICAL USES THEREOF
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Paragraph 0246; 0252; 0369-0372, (2019/07/03)
The present invention relates to fused heterocyclic derivatives, processes for their preparation and their use in medicine. Specifically, the present invention relates to a novel derivative represented by the formula (I′), or its pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the derivative or its pharmaceutically acceptable salt thereof, and the method for preparing the derivative and its pharmaceutically acceptable salt thereof. The present invention also relates to the use of the derivative and its pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the derivative and its pharmaceutically acceptable salt thereof in the preparation of medicines, in particularly as IDO inhibitor medicines, for treating and/or preventing cancers. Wherein each substituent of the formula (I′) is the same as defined in the specification.
Method for synthesizing 6-bromomethyl-3-methoxy-2-nitropyridine
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Paragraph 0016; 0017; 0018; 0020, (2018/11/03)
The invention discloses a method for synthesizing 6-bromomethyl-3-methoxy-2-nitropyridine. The method comprises the synthesizing steps: firstly, mixing 6-methyl-3-hydroxyl-2-nitropyridine, magnesium iodide and water, dropwise adding dimethyl sulfate, carrying out a reaction for 24 hours with heating, carrying out extraction with ethyl acetate, and boiling off the ethyl acetate, so as to obtain 6-methyl-3-methoxyl-2-nitropyridine; and adding carbon tetrachloride and sodium bromide, carrying out stirring for dissolving, dropwise adding hydrogen peroxide, carrying out a reaction with heating, boiling off the carbon tetrachloride, adding 200ml of water, carrying out extraction with ethyl acetate, boiling off the ethyl acetate so as to obtain crude 6-bromomethyl-3-methoxyl-2-nitropyridine, carrying out column chromatography separation, and carrying out recrystallization with acetonitrile water, thereby obtaining the 6-bromomethyl-3-methoxy-2-nitropyridine. According to the method, the yieldis 75%.
Discovery of (E)-3-((styrylsulfonyl)methyl)pyridine and (E)-2-((styrylsulfonyl)methyl)pyridine derivatives as anticancer agents: Synthesis, structure-activity relationships, and biological activities
Lu, Tiangong,Goh, Aik Wye,Yu, Mingfeng,Adams, Julian,Lam, Frankie,Teo, Theodosia,Li, Peng,Noll, Ben,Zhong, Longjin,Diab, Sarah,Chahrour, Osama,Hu, Anran,Abbas, Abdullahi Y.,Liu, Xiangrui,Huang, Shiliang,Sumby, Christopher J.,Milne, Robert,Midgley, Carol,Wang, Shudong
, p. 2275 - 2291 (2014/04/17)
ON01910.Na is a highly effective anticancer agent that induces mitotic arrest and apoptosis. Clinical studies with ON01910 in cancer patients have shown efficacy along with an impressive safety profile. While ON01910 is highly active against cancer cells,
Phosphodiesterase inhibitors. Part 3: Design, synthesis and structure-activity relationships of dual PDE3/4-inhibitory fused bicyclic heteroaromatic-dihydropyridazinones with anti-inflammatory and bronchodilatory activity
Ochiai, Koji,Takita, Satoshi,Eiraku, Tomohiko,Kojima, Akihiko,Iwase, Kazuhiko,Kishi, Tetsuya,Fukuchi, Kazunori,Yasue, Tokutaro,Adams, David R.,Allcock, Robert W.,Jiang, Zhong,Kohno, Yasushi
experimental part, p. 1644 - 1658 (2012/04/23)
(-)-6-(7-Methoxy-2-trifluoromethylpyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4, 5-dihydro-3-(2H)-pyridazinone (KCA-1490) is a dual PDE3/4 inhibitor that exhibits potent combined bronchodilatory and anti-inflammatory activity. A survey of potential bicyclic heteroaromatic replacement subunits for the pyrazolo[1,5-a]pyridine core of KCA-1490 has identified the 4-methoxy-2- (trifluoromethyl)benzo[d]thiazol-7-yl and 8-methoxy-2-(trifluoromethyl)quinolin- 5-yl analogues as dual PDE3/4-inhibitory compounds that potently suppress histamine-induced bronchoconstriction and exhibit anti-inflammatory activity in vivo.
COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS
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Page/Page column 47, (2012/01/13)
.A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilising or immobilisable derivative thereof; wherein: any one or two of X·,, X2 and X3 is a N atom and the remaining two or one of X1, X2 and
PYRIDAZINONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT
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Page/Page column 71, (2010/04/25)
It is to provide a novel pyridazinone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1 represents H or C1-6 alkyl, each of R2 and R3 represents H, X, C1-6 alkoxy, Z represents O or S, and A represents AA or BB, wherein AA represents: and BB represents: wherein R4 represents H or C1-6 alkyl, and each of R5 and R6 represents C1-6 alkyl.
Discovery and optimization of antibacterial AccC inhibitors
Cheng, Cliff C.,Shipps Jr., Gerald W.,Yang, Zhiwei,Sun, Binyuan,Kawahata, Noriyuki,Soucy, Kyle A.,Soriano, Aileen,Orth, Peter,Xiao, Li,Mann, Paul,Black, Todd
scheme or table, p. 6507 - 6514 (2010/05/17)
The biotin carboxylase (AccC) is part of the multi-component bacterial acetyl coenzyme-A carboxylase (ACCase) and is essential for pathogen survival. We describe herein the affinity optimization of an initial hit to give 2-(2-chlorobenzylamino)-1-(cyclohe
TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES
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Page/Page column 22-23, (2008/12/08)
The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH2, CH2-CH2, CH2-NH, or NH; R1 is halogen, or R1 is alkyl, alkenyl
Amino-pyridines as inhibitors of beta-secretase
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Page/Page column 23-24, (2008/06/13)
The present invention provides an amino-pyridine compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
