294659-72-6Relevant academic research and scientific papers
Pyridoazepine derivative, pharmaceutical composition and applications thereof
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, (2019/05/16)
The present invention discloses a pyridoazepine derivative, a pharmaceutical composition and applications thereof, wherein the pyridoazepine derivative (I), the isomer, the prodrug, the stable isotopederivative or the pharmaceutically acceptable salt thereof have the following structure. According to the present invention, the pyridoazepine derivative has good regulatory effects on TLR family andrelated signaling pathways, particularly on TLR8, can effectively treat, alleviate and/or prevent various diseases mediated by signaling pathways related to TLR family and TLR, and particularly can effectively treat, alleviate and/or prevent various TLR8 mediated diseases such as cancers, autoimmune diseases, infections, inflammations, transplant rejections, graft versus host diseases and the like. The formula (I) is defined in the specification.
1,6- AND 1,8-NAPHTHYRIDINES
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, (2012/07/28)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
SUBSTITUTED IMIDAZO- AND TRIAZOLOPYRIMIDINES, IMIDAZO- AND PYRAZOLOPYRAZINES AND IMIDAZOTRIAZINES
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, (2011/06/26)
The invention relates to substituted imidazo- and triazolopyrimidines, imidazo- and pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias.
SUBSTITUTED PYRIDINES, AND USE THEREOF AS GSK3 INHIBITORS
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, (2011/08/08)
The invention relates to substituted pyridines and to processes for preparation thereof, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of haematological disorders, preferably of leukopenia and neutropenia
IMIDAZO-, PYRAZOLOPYRAZINES AND IMIDAZOTRIAZINES AND THEIR USE
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Page/Page column 19, (2011/04/14)
The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological di
SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES
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Page/Page column 48, (2010/05/13)
The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia.
TRIAZOLOTRIAZINES AND TRIAZOLOPYRAZINES AND THEIR USE
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Page/Page column 17, (2009/10/21)
The invention relates to substituted triazolotriazines and triazolopyrazines and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular haematologic disorders, preferably of leukopenias and neutropenias.
Synthesis and structure-activity relationships of 7-substituted 3-(2,6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src)
Thompson,Rewcastle,Boushelle,Hartl,Kraker,Lu,Batley,Panek,Hollis Showalter,Denny
, p. 3134 - 3147 (2007/10/03)
7-Substituted 3-(2,6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones are potent inhibitors of protein tyrosine kinases, with some selectivity for c-Src. The compounds were prepared by condensing 4,6-diaminonicotinaldehyde with 2,6-dichlorophenylacetonitrile and selectively converting the 2- and 7-amino groups of the product to hydroxy and fluoro groups, respectively, by prolonged diazotization in 50% aqueous fluoboric acid. N-Methylation, followed by treatment with aliphatic diamines, aromatic amines, or their derived lithium anions, gave the desired compounds. Selected isomeric 1,8-naphthyridin-2(1H)-ones were also prepared in order to evaluate the relative contributions of both ring A aza atoms of the related pyrido[2,3-d]pyrimidin-7(8H)-ones to the inhibitory activity. The compounds were evaluated for their ability to prevent phosphorylation of a model substrate by c-Src, FGF-1 receptor, and PDGF-β receptor enzymes. Overall, there was a high degree of correlation of the activities against the different kinases, with c-Src being generally the most sensitive to structural changes. 1,6-Naphthyridin-2(1H)-one analogues bearing basic aliphatic side chains [7-NH(CH2)(n)NRR, 7-NHPhO(CH2)(n)NRR, or 7-NHPhN(CH2)4NMe] were the most potent against c-Src (IC50s of 10-80 nM), showing good selectivity with respect to PDGFR (10-300-fold) but less with respect to FGFR. The 1,6-naphthyridin-2(1H)-ones showed broadly similar activity to the analogous pyrido[2,3-d]-pyrimidin-7(8H)-ones, whereas the 1,8-naphthyridin-2(1H)-ones were at least 103-fold less potent. These results, indicating that the 3-aza atom in the pyrido[2,3-d]pyrimidin-7(8H)-ones is mandatory, whereas the 1-aza atom is not, support the published binding model for these compounds to c-Src (J. Med. Chem. 1998, 41, 1752), where the 3-aza and 2-NH atoms form a bidentate H-bond donor - acceptor motif that interacts with Met341 and the 1-aza atom is not involved in specific binding interactions.
