449811-28-3Relevant articles and documents
SUBSTITUTED PHENYLPROPENYL PYRIDINE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL APPLICATIONS
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Paragraph 0234-0235, (2021/12/29)
Disclosed are a substituted phenylpropenylpyridine derivative, a preparation method therefor and the use thereof as a PD-1/PD-L1 inhibitor. In particular, disclosed are a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method therefor and the use thereof. The definition of each group in the formula is detailed in the description and claims.
PROTEIN KINASE INHIBITORS AND USES THEREOF FOR THE TREATMENT OF DISEASES AND CONDITIONS
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Paragraph 0087-0089; 0323-0324, (2020/11/30)
Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2) and/or receptor interacting kinase 3 (RIPK3). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 or RIPK3 could provide therapeutic benefit. Compounds that function as RIPK3 inhibitors provide therapeutic benefit in the treatment of inflammatory and degenerative conditions.
PYRIDO[2,3-D]PYRIMIDIN-7ONES AND RELATED COMPOUNDS AS INHIBITORS OF PROTEIN KINASES
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Paragraph 0263-0264; 0021, (2018/12/13)
Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds having the structures below (I) are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.
7-PHENYLETHYLAMINO-4H-PYRIMIDO[4,5-D][1,3]OXAZIN-2-ONE COMPOUNDS AS MUTANT IDH1 AND IDH2 INHIBITORS
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Page/Page column 54, (2018/07/05)
A compound, as defined herein, or pharmaceutical composition containing the compound, for use in treating IDH1 or IDH2 mutant cancer and having the structure: (I).
Inhibitors of the fibroblast growth factor receptor
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Page/Page column 40, (2017/08/01)
Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of FGFR-4.
Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90
Montoir, David,Barillé-Nion, Sophie,Tonnerre, Alain,Juin, Philippe,Duflos, Muriel,Bazin, Marc-Antoine
, p. 17 - 33 (2016/05/24)
Hsp90 is an ATP-dependent chaperone known to be overexpressed in many cancers. This way, Hsp90 is an important target for drug discovery. Novobiocin, an aminocoumarin antibiotic, was reported to inhibit Hsp90 targeting C-terminal domain, and showed anti-proliferative properties, leading to the development of new and more active compounds. Consequently, a new set of novobiocin analogs derived from 1,6-naphthyridin-2(1H)-one scaffold was designed, synthesized and evaluated against two breast cancer cell lines. Subsequently, cell cycle progression and apoptosis were conducted on best candidates, finally Western Blot analysis was performed to measure their ability to induce degradation of Hsp90 client proteins.
INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
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Paragraph 0137; 0138, (2015/07/22)
Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of FGFR-4.
INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
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Page/Page column 53; 54, (2014/02/15)
Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
Differential functionalization of 1,6-naphthyridin-2(1H)-ones through sequential one-pot Suzuki-Miyaura cross-couplings
Montoir, David,Tonnerre, Alain,Duflos, Muriel,Bazin, Marc-Antoine
, p. 1487 - 1495 (2014/03/21)
A practical synthesis of 7-chloro-3-iodo-1-methyl-1,6-naphthyridin-2(1H)- one is described that starts from 2-chloro-4-(methylamino)nicotinaldehyde. The dihalo compound then undergoes sequential, site-selective Suzuki-Miyaura cross-coupling reactions to afford highly functionalized 1,6-naphthyridones in good yields. One-pot, sequential, site-selective Suzuki-Miyaura cross-coupling reactions of 7-chloro-3-iodo-1-methyl-1,6-naphthyridin-2(1H)-one afforded highly functionalized 1,6-naphthyridones in good yields. Copyright
Differential Functionalization of 1,6-Naphthyridin-2(1H)-ones through Sequential One-Pot Suzuki-Miyaura Cross-Couplings
Montoir, David,Tonnerre, Alain,Duflos, Muriel,Bazin, Marc-Antoine
, p. 1487 - 1495 (2015/10/05)
A practical synthesis of 7-chloro-3-iodo-1-methyl-1,6-naphthyridin-2(1H)-one is described that starts from 2-chloro-4-(methylamino)nicotinaldehyde. The dihalo compound then undergoes sequential, site-selective Suzuki-Miyaura cross-coupling reactions to afford highly functionalized 1,6-naphthyridones in good yields.
