Kinase modulators for the treatment of cancer

摘要

Compounds of the substituted pyrazole class as treatments for cancer are reported. A method of treating cancer in which a compound that inhibits the activity of receptor kinases. Said method is effective and can be provided in addition to standard therapies, notably chemotherapy using cytotoxic drugs and other forms of immune therapy including therapeutic vaccines.

主权项

1. A compound according to Formula 1 wherein: R1=is phenyl substituted with 0 to 3 substituents selected from alkyl of 1 to 5 carbons, halogen, nitrile, alkoxy, nitro; A=N; R2 and R3 are independently selected from either no atom in the case of A=O, and hydrogen, methyl, ethyl, isopropyl, sec-butyl
isobutyltert-butyl2-(3-methyl)butylcyclopropylcyclobutylcyclopentylcyclohexylmethylcyclohexylmethylcyclopentylhydroxycyclohexylhydroxycyclopentylbenzyl1-phenylethyl(4-hydroxy)cyclohexyl1-(1-phenyl)propyl1-(1,2,3,4-tetrahydro)naphthyl1-(2-phenyl)propyl1-(1-methyl-3-phenyl)propyl1,2-diphenylethyl1,3-diphenyl-2-propyl(4-tert-butyl)benzyl4-fluorobenzyl2-(2-para-xylyl)ethyl(1-naphthyl)methyl(2-thiophenyl)methyl2-(2-thiophenyl)ethyl(2-benzo[b]thiophenyl)methyl(2-furyl)methyl[(5-methyl)furan-2-yl]-methyl(2-pyridyl)methyl(3-pyridyl)methyl(4-pyridyl)methyl; R4=carboxyl, carboxymetyhl, carboxyethyl, nitrile, amido, phenyl with 0 to 3 substituents selected from, Cl, Br, I, F, CF3, OCF3; or R3=R4 and is selected from carbonyl, —(C═O)—NR10—(C═O)—, wherein R10 is selected from H, methyl, ethyl; R8=H; R9=methyl, ethyl, isopropyl, sec-butyl
isobutyltert-butyl2-(3-methyl)butylcyclopropylcyclobutylcyclopentylcyclohexylmethylcyclohexylmethylcyclopentylhydroxycyclohexylhydroxycyclopentylbenzyl1-phenylethyl(4-hydroxy)cyclohexyl1-(1-phenyl)propyl1-(1,2,3,4-tetrahydro)naphthyl1-(2-phenyl)propyl1-(1-methyl-3-phenyl)propyl1,2-diphenylethyl1,3-diphenyl-2-propyl(4-tert-butyl)benzyl4-fluorobenzyl2-(2-para-xylyl)ethyl(1-naphthyl)methyl(2-thiophenyl)methyl2-(2-thiophenyl)ethyl(2-benzo[b]thiopheneyl)methyl(2-furyl)methyl[(5-methyl)furan-2-yl]-methyl(2-pyridyl)methyl(3-pyridyl)methyl(4-pyridyl)methyl.