Flynn, Daniel L. et al. published their patent in 2012 |CAS: 1012882-90-4

The Article related to preparation heterocyclic urea derivative kinase inhibitor treatment hyperproliferative disease, Aliphatic Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.HPLC of Formula: 1012882-90-4

On September 6, 2012, Flynn, Daniel L.; Kaufman, Michael D. published a patent.HPLC of Formula: 1012882-90-4 The title of the patent was Preparation of heterocyclic urea derivatives as kinase inhibitors useful for the treatment of hyperproliferative and other diseases. And the patent contained the following:

Compounds of the present invention (I, wherein E1 is substituted phenyl; A is substituted pyrazolyl and imidazolyl; X2 is a direct bond, wherein E1 is directly linked to the NH group; X3 is -O-; Z6 is independently and individually selected from H, C1-6 alkyl, branched C3-7 alkyl, hydroxy, etc.; t = 1-3), alone and in combination with other active agents, find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to for example malignant melanomas, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof. More generally the invention relates to a method of treating mammalian disease with I wherein the disease etiol. or progression is at least partially mediated by the kinase activity of c-ABL kinase, BCR-ABL kinase, FLT-3 kinase, TIE-2 kinase, TRK-A kinase, TRK-B kinase, TRK-C kinase, VEGFR-2 kinases, c-MET kinase, PDGFR-alpha kinase, PDGFR-beta kinase, HER-1 kinase, HER-2 kinase, HER-3 kinase, HER-4 kinase, FGFR kinases, c-KIT kinase, RET kinase, c-FMS kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs of any of the foregoing. Synthetic procedures for preparing I are exemplified. Thus, e.g., II was prepared by coupling of 2,2,2-trichloroethyl 3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-ylcarbamate (preparation given) with 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide (preparation given). Assays were described for evaluating binding of I to various kinases, e.g., II demonstrated an IC50 value of 4 nM in the p-Abl kinase assay. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).HPLC of Formula: 1012882-90-4

The Article related to preparation heterocyclic urea derivative kinase inhibitor treatment hyperproliferative disease, Aliphatic Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.HPLC of Formula: 1012882-90-4

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com