449811-29-4Relevant articles and documents
PROTEIN KINASE INHIBITORS AND USES THEREOF FOR THE TREATMENT OF DISEASES AND CONDITIONS
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, (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.
3,4-dihydropyrido[4,3-d]pyrimidine derivative, and preparation method and use thereof
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Paragraph 0069; 0072; 0090-0093, (2019/10/07)
The invention relates to a 3,4-dihydropyrido[4,3-d]pyrimidine derivative, and a preparation method and a use thereof. The compound is a compound represented by formula I, or a pharmaceutically acceptable salt or stereoisomer or tautomer thereof, and R to R are as defined in the description.
PYRIDO[2,3-D]PYRIMIDIN-7ONES AND RELATED COMPOUNDS AS INHIBITORS OF PROTEIN KINASES
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, (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.
Inhibitors of the fibroblast growth factor receptor
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, (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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, (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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, (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
BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
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, (2014/10/29)
The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
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.
