51674-77-2Relevant academic research and scientific papers
Syntheses of Some Azolopyridopyrimidines
Petric, Andrej,Tisler, M.,Stanovnik, Branko
, p. 615 - 624 (1983)
Syntheses of isomeric azolopyridopyrimidines are described.As starting material the corresponding pyridopyrimidines were used.It could be established that in many cases a transformation of a functional group with the purpose to form an annelated five-membered ring proceeded with ring opening at the pyrimidine part.Subsequent ring closure with one carbon synthons gave then the desired tricyclic heterocycles. - Keywords: Cyclization with C-N and N-N bond formation; Tricyclic heterocyclic compounds
ION CHANNEL INHIBITOR COMPOUNDS FOR CANCER TREATMENT
-
Paragraph 0221; 0222, (2021/01/25)
The present invention concerns a compound of following general formula (I): where: either R is an R1 group and R′ is an -A1-Cy1 group, or R is an -A1-Cy1 group and R′ is an R1 group, R1 particularly being H or (C1-C6)alkyl group;A1 being an —NH— radical or —NH—CH2— radical;Cy1 particularly being a phenyl group,A is a fused (hetero)aromatic ring having 5 to 7 atoms, for use for treating cancer.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
-
Paragraph 00648, (2013/03/26)
Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
-
Page/Page column 79, (2012/05/21)
Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinase function of the epidermal growth factor receptor
Rewcastle, Gordon W.,Palmer, Brian D.,Thompson, Andrew M.,Bridges, Alexander J.,Cody, Donna R.,Zhou, Hairong,Fry, David W.,McMichael, Amy,Denny, William A.
, p. 1823 - 1835 (2007/10/03)
Following the discovery of the very high inhibitory ability of the 4-[(3-bromophenyl)amino]-quinazolines against the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (e.g., 3, IC50 0.029 nM), four series of related pyrido[d]pyrimidines bearing electron-donating groups at the 6- or 7-positions have been synthesized and evaluated. The compounds were prepared by nucleophilic substitution of the corresponding 6- and 7-fluoro analogues. While members of all series showed potent inhibitory activity against isolated EGFR, there were important differences between the different isomeric pyrido[d]pyrimidines and the parent quinazolines. Overall, the [3,4-d] and [4,3-d] series were the most potent, followed by the [3,2-d] compounds, with the [2,3-d] analogues being least active. Whereas in the parent quinazoline series the addition of steric bulk to a 6- or 7-NH2 substituent (i.e., NHMe and NMe2 groups) dramatically decreased potency, no such trend was discernable in the [3,2-d] series. Furthermore, in the 7-substituted pyrido[4,3-d]- and 6-substituted pyrido[3,4-d]pyrimidine series, and to a limited extent in the 7-substituted pyrido[2,3-d] series, such substitution increased potency dramatically, to the extent that the 7-(methylamino)pyrido[4,3-d]pyrimidine (5f) (IC50 0.13 nM) and 6-(methylamino)pyrido[3,4-d]pyrimidine (7f) (IC50 0.008 nM) constitute important new leads. Selected compounds were evaluated for their ability to inhibit EGFR autophosphorylation in A431 cells, and a positive quantitative correlation was found between this activity and inhibitory activity against the isolated enzyme.
Ring-Opening Reactions of Triazolo- and Tetrazolo-Pyridopyrimidines or Quinazolines with some Carbon Nucleophiles
Petric, Andrej,Tisler, Miha,Stanovnik, Branko
, p. 1309 - 1320 (2007/10/02)
Syntheses of some new pyridotriazolo- and pyridotetrazolopyrimidines are described.These tricyclic systems and tetrazoloquinazoline react with some carbon nucleophiles, generated from compounds with reactive methylene groups, exclusively at position 2 of
