On May 26, 2000, Kubo, Keiji; Hori, Akira; Kusaka, Masami published a patent.Category: esters-buliding-blocks The title of the patent was Benzimidazole derivatives as neovascularization inhibitors and pharmaceutical compositions containing them. And the patent contained the following:
Neovascularization inhibitors contain the derivatives I [ring A = (un)substituted phenyl; ring B = (un)substituted cyclyl; R4, R6 = (1) H, (ii) C1-6 alkyl which may have substituents selected from mono- or di(C1-6 alkyl)amino, 5-7-membered cyclic amino, CO2H, or C2-7 alkoxycarbonyl, (iii) C2-6 alkenyl, (iv) C3-7 cycloalkyl, (v) C7-13 aralkyl which may have 1-5 substituents selected from halo, C1-6 alkoxy, C1-6 alkyl, mono- or di(C1-6 alkyl)amino, (vi) C2-7 alkoxycarbonyl; R5 = (i) H, (ii) halo, (iii) C1-6 alkyl which may have substituents selected from mono- or di(C1-6 alkyl)amino and halo, (iv) C1-6 alkoxy, (v) C2-7 alkoxycarbonyl, (vi) mono- or di(C1-6 alkyl)amino, (vii) carbamoyl which may be substituted with C1-6 alkyl or C7-13 aralkyl; X = (i) direct bond, (ii) C1-6 alkylene, (iii) C2-6 alkenylene, (iv) C1-6 alkylene-aminocarbonyl, (v) C1-6 alkylene-oxycarbonylamino; Y = CO, SO2, NHCO, C1-6 alkylenecarbonyl, C2-6 alkenylenecarbonyl, C1-6 alkylene] or their pharmaceutically acceptable salts. Also claimed are pharmaceutical compositions containing I or their salts for treatment of neoplasm, inflammatory diseases, diabetic retinopathy, etc. IC50 of 2-(4-methoxyphenyl)-5-[3-methoxy-4-(4-pyridyl)methoxybenzoyl]aminobenzimidazole (preparation given) against recombinant VEGF-induced proliferation of HUVEC was 0.012 μM. The experimental process involved the reaction of tert-Butyl 2-(4-nitrophenyl)acetate(cas: 29704-38-9).Category: esters-buliding-blocks
The Article related to benzimidazole derivative preparation neovascularization inhibitor, angiogenesis inhibitor benzimidazole derivative preparation, Pharmacology: Effects Of Cardiovascular, Hematologic, and Renal Drugs and other aspects.Category: esters-buliding-blocks
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