Abstract: Ether and amide derivatives are disclosed, which are represented by the following formula (I) and its pharmaceutical acceptable salt, and which are useful for the treatment of diabetes.
R1—A—R2 (I)
wherein
(with the provisos that (i) when A is —O—, then n is 2 or 3 (ii) when
then
n is 1 or 2. R3 is OH—, CH3SO2NH—, CF3SO2NH—, CH3SO2NHCH2—, CF3SO2NHCH2—, HOOC—, CH3OOC—,
HOOC—CH2SO2NH—, CF3—CH2SO2NH—,
R8—NHSO2—,
R8—NHSO2—CH2—, HOOC—CH2—O—, HSO3N═CH—, or R9—SO2NHCO—;
R4 is H, OH, O-alkyl or O—CH2OCH3;
R5 is H, halogen atom, —CH2COOH or OH;
R6 and R7 are hydrogen, t-butyl or pyrolidyl;
R8 is hydrogen or lower alkyl;
R9 is alkyl or thienyl;
R10 is lower alkyl)
or a pharmaceutically acceptable salt.
Abstract: A method for preparation of a cycloheptimidazole compound having formula (5),
wherein: R4 is a lower alkyl group, comprising reacting a compound of formula (1),
with an alkylamidine hydrochloride.
Abstract: The present invention relates to compounds of formula (1).
wherein: R1 is hydrogen atom or lower alkyl group, X is bromine atom or chlorine atom; and which are useful for the preparation of the cycloheptanoides such as cycloheptimidazole derivatives. The compound having formula (1) is obtained in a single pot by the reaction of a trialkylsilylether compound with a dihalocarbene which, in turn, is prepared from the reaction of chloroform or bromoform in the presence of base.
Abstract: New therapeutic agents of isoquinuclidine derivatives are represented by the following formula or its hydrochloride salts. ##STR1## (wherein R.sub.1 is hydrogen, carboxyl group, ethoxycarbonyl group, 4-(ethoxycarbonyl)phenyl group, 4-(carboxy)phenyl group, 2-(carboxy)-thiophene-5-yl group, quinoline-5-yl group, 4-(quinoline-5-yl)phenyl group or 4-(3-oxo-2-azabicyclo[2.2.2]octane-2-yl)-phenyl group; R.sub.2 is hydrogen or allyl group; Both X.sub.1 and X.sub.2 are hydrogen and X.sub.1 and X.sub.2 may form an oxo group; m stands for an integer of 0 to 2.) These compounds, have excellent inhibitory activities against squalene synthase, and are useful as a treatment agent for hypercholesterolemia.