185039-46-7

Usage

Chemical Properties

Off-White Solid

InChI:InChI=1/C15H11Cl2N3OS/c1-20-13-8(7-18-15(19-13)22-2)6-9(14(20)21)12-10(16)4-3-5-11(12)17/h3-7H,1-2H3

Upstream product

• 90793-64-9 ethyl 2-(2,6-dichlorophenyl)acetate 
• 185040-32-8 4-methylamino-2-methylthiopyrimidine-5-carboxaldehyde 
• 54551-83-6 methyl 2-(2,6-dichlorophenyl)acetate 
• 185039-29-6 6-(2,6-Dichlorophenyl)-8-methyl-2-methylsulfanyl-8H-pyrido[2,3-d]-pyrimidin-7-ylideneamine 
• 76360-82-2 4-methylamino-2-methylsulfanyl-pyrimidine-5-carboxylic acid ethyl ester 
• 17759-30-7 (4-methylamino-2-methylsulfanyl-pyrimidin-5-yl)-methanol 
• 5909-24-0 4-chloro-2-methanesulfanylpyrimidine-5-carboxylic acid ethyl ester 
• 3215-64-3 2,6-dichlorophenylacetonitrile 
• 185039-37-6 N-[6-(2,6-dichlorophenyl)-8-methyl-2-methylsulfanyl-8H-pyrido[2,3-d]pyrimidin-7-ylidene]-acetamide 

Downstream Products

• 185039-89-8 PD-166285 
• 185039-34-3 6-(2,6-dichlorophenyl)-2-hydroxy-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one 
• 212391-57-6 SKI DV₂ 47 
• 185039-73-0 6-(2,6-Dichlorophenyl)-2-(4-methoxyphenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one 
• 212391-58-7 2-[4-(2-Amino-ethoxy)-phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one 
• 185039-70-7 6-[6-(2,6-Dichlorophenyl)-8-methyl-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidin-2-ylamino]-hexanoic acid, tert-butyl ester 

Relevant academic research and scientific papers

Design of pyrido[2,3-d]pyrimidin-7-one inhibitors of receptor interacting protein kinase-2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling

Receptor interacting protein kinase-2 (RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain (NOD) cell signaling, a pathway implicated in numerous chronic inflammatory conditions. Herein, a pyrido[

PYRIDO[2,3-D]PYRIMIDIN-7ONES AND RELATED COMPOUNDS AS INHIBITORS OF PROTEIN KINASES

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.

Part 3: Notch-sparing γ-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones

In search for novel lead compounds as γ-secretase inhibitors, analogs of aminopyrido[2,3-d]pyrimidin-7-ones (I) were synthesized and evaluated for inhibitory effects on amyloid-β-peptide production and cleavage of the Notch1 receptor mediated by γ-secretase. Selected pyridopyrimidines, such as 1, 8, 9,10, 11 and 16 are γ-secretase inhibitors that did not have an effect on Notch1 receptor processing.

New effective inhibitors of the Abelson kinase

The effects of substituents on the aryl ring were studied by the preparation and testing of several PD173955 analogs. Inserting a single carbon atom into the C-N bond in the aniline subunit (PDC) reduced the kinase inhibition by a factor of 200. Despite its decreased affinity for Abl compared with PD173955, PDC exhibits a Ki very similar to that reported for Imatinib. Increased water solubility is also gained by replacing the thiomethyl group with an amino or glycyl moiety. For both PD173955 and PDC, the analogs with amino groups in place of the methylthio group are 10 times more inhibitory than the parent molecules. Two molecules were identified with Kis about three orders of magnitude lower than reported for Imatinib.

A facile, KF/Al2O3 mediated method for the preparation of functionalized pyrido[2,3-d]pyrimidin-7(8H)-ones

A series of functionalized pyrido[2,3-d]pyrimidin-7(8H)-ones were prepared by a KF/Al2O3 mediated condensation of 4-(alkylamino)-2-(methylthio)pyrimidine-5-carbaldehydes and phenyl acetic acid ester derivatives.

Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d] pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1

A series of 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones were synthesized and evaluated for their inhibitory properties against the non-receptor kinase c-Src and the G2/M checkpoint kinase Wee1. Overall, the compounds were 10-100-fold more potent i

PYRIDOPYRIMIDINE KINASE INHIBITORS

The present invention provides compounds of formula (0): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (0) and provides methods of treat

2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. Structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity

While engaged in therapeutic intervention against a number of proliferative diseases, we have discovered the 2-aminopyrido[2,3- d]pyrimidin-7(8H)-ones as a novel class of potent, broadly active tyrosine kinase (TK) inhibitors. An efficient route was devel