The Article related to thienopyridine preparation pharmaceutical composition, thienopyrimidine preparation vegf hgf receptor signaling inhibitor, thieno pyridine preparation vegf hgf receptor signaling inhibitor, pyridine thieno preparation treatment proliferative disease, pyrimidine thieno preparation treatment proliferative disease and other aspects.Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene
On May 18, 2007, Saavedra, Oscar Mario; Claridge, Stephen William; Zhan, Lijie; Raeppel, Franck; Vaisburg, Arkadii; Raeppel, Stephane; Deziel, Robert; Mannion, Michael; Zhou, Nancy Z.; Isakovic, Ljubomir published a patent.Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene The title of the patent was Thienopyridine and thienopyrimidine derivatives and their preparation, pharmaceutical compositions, and use as inhibitors of VEGF receptor and HGF receptor signaling for treatment of proliferative diseases. And the patent contained the following:
The invention relates to the inhibition of vascular endothelial growth factor (VEGF) receptor signaling and hepatocyte growth factor (HGF) receptor signaling. The invention provides compounds of formula I and methods for inhibiting VEGF receptor signaling and HGF receptor signaling for treatment of proliferative diseases. Compounds of formula I, wherein T is (un)substituted (hetero)aryl(alkyl), cycloalkyl or heterocyclyl; W is O, S, NH, or NMe; Z is O, S, or NH; X and X1 are independently H, (un)substituted C1-6 alkyl, halo, CN, or NO2; or X and X1 together may form C3-7 cycloalkyl; R1, R2, R3, R4 are independently H, halo, trihalomethyl, CN, NO2, NH2 and derivatives, OH and derivatives, CO2H and derivatives, COH and derivatives, (un)substituted C1-4 alkoxy, (un)substituted C1-4 alkylthio, (un)substituted C1-6 alkyl, (un)substituted C2-4 alkenyl, or (un)substituted C2-6 alkynyl; R5 is H, CN, (un)substituted (CH2)2-5 (hetero)aryl, (un)substituted C1-6 alkyl, (un)substituted C2-6 alkenyl, C2-6 alkynyl, CH2(CH2)0-4T2, (un)substituted C1-4 alkylcarbonyl, (un)saturated 3- to 7-membered carboxycyclic or heterocyclic group; where T2 is OH, OMe, OEt, NH2, NHMe, or NMe2; Q is CH2, O, S, NH, N(C1-6 alkyl), N(alkyl)aryl, NOMe, NCH2OMe, or NBn; D is C-E or N; L is N or CR where R is H, halo, CN, (un)substituted C1-6 alkyl, (un)substituted C2-4 alkenyl, or (un)substituted C2-6 alkynyl; E is E1, E2 or E3 wherein E1 is H, halo, NO2, azido, (un)substituted C1-6 alkyl, C3-10 cycloalkyl, etc.; E2 is (un)substituted alkynes; E3 is (un)substituted heterocyclyl(ene); and the pharmaceutically acceptable salts and complexes thereof are claimed in this invention. Example compound II was prepared by chlorination of thieno[3,2-b]pyridine-7-ol followed by carboxylation and the resulting lithium carboxylate was converted into the corresponding acid chloride, which reacted with dimethylamine to give compound III; compound III underwent coupling with 2-fluoro-4-nitrophenol, and the resulting 7-(2-fluoro-4-nitrophenoxy)-N,N-dimethylthienopyridinecarboamide was reduced to give the corresponding arylamine, which was reacted with phenylacetyl isocyanate to give example compound II. Addnl. 329 examples were prepared in this invention. The example compounds were tested for their in vitro HGF receptor and VEGF receptor signaling inhibition and solid tumor growth inhibition. The invention compounds showed inhibitory activity and was reported to have IC50 values less than 50 nM, ≥50 but <250 nM, ≥250 but <500 nM, ≥ 500 nM, or no activity in various assays. Example compound II showed and IC50 of >50 nM for inhibition of VEGF receptors, and this compound also showed tumor growth inhibition (TGI) against several types of tumors. Example compound II had greater than 100% TGI against U87MG, which indicated tumor shrinkage. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene
The Article related to thienopyridine preparation pharmaceutical composition, thienopyrimidine preparation vegf hgf receptor signaling inhibitor, thieno pyridine preparation vegf hgf receptor signaling inhibitor, pyridine thieno preparation treatment proliferative disease, pyrimidine thieno preparation treatment proliferative disease and other aspects.Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com