专利号:US-5424432-A 优先权日:1994-05-26 标题:Process for the preparation of imidazolutidine 发明人:FREDENBURGH LAURA E; LARSEN ROBERT D; LIU JI; REAMER ROBERT A; SENANAYAKE CHRIS H; VERHOEVEN THOMAS R 权利人:MERCK & CO INC 摘要:This invention relates to a method for the preparation of a compound of formula I: I a key intermediate in the synthesis of a series of Angiotensin II receptor antagonists. The invention also relates to a selective reagent for conducting the Hofmann rearrangement, particularly in the formation of a pyridinoimidazolone, which is a percursor to the formation of an imidazopyfidine of formula I. This invention also relates to a method for the preparation of imidazolutidine, a key intermediate in the synthesis of 3-(2'-(N-benzoyl)sulfonamidobiphen-4-yl)-methyl-5,7 -dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridine, using pyridinoimidazolone, an unreactive urea.
专利号:US-7977371-B2 优先权日:2007-02-26 标题 :Pyrrole derivative having ureido group and aminocarbonyl group as substituents 发明人:KAWASHIMA KENJI; ENOMOTO HIROSHI; ISHIZAKA NORIKO; YAMAMOTO MINORU; KUDOU KAZUHIRO; MURAI MASAAKI; INABA TAKAAKI; OKAMOTO KAZUYOSHI 权利人:SANTEN PHARMACEUTICAL CO LTD 摘要:Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; R 1 represents a halogen atom, a hydrogen atom, a lower alkyl group or the like; R 2 represents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group, a lower alkynyl group which may have a substituent, a lower cycloalkyl group, an aryl group, a hydroxy group, a lower alkoxy group which may have a substituent or the like; and n represents 0, 1, 2, 3 or the like.