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AssigneeTaiho Pharmaceutical Co., Ltd.
InventorsShingo Yano, Tomoyasu Ohno, Kazuo Ogawa, Haruo Yamada, Tetsuhiko Shirasaka, Hiroyuki Kawamura, Shinichi Watanabe
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An oxazolidine derivative represented by the formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are H, optionally halogenated alkyl, optionally halogenated alkoxy, OH, halo, NO.sub.2, amino optionally having acetyl or alkyl, COOH, alkoxycarbonyl, CN, alkanoyl, 2-oxazolyl, or R.sup.1 and R.sup.2 may be combined with each other to represent --(CH.sub.2).sub.p -- or --O(CH.sub.2).sub.q O-- (p is 3-5, q is 1-3) to form a ring, m and n are each 0 or 1, R.sup.4 and R.sup.5 are H or alkyl, X is C or N, Y is CH.sub.2 OH, CHO or COOR.sup.6 (R.sup.6 is alkyl, benzyl or H), A is alkylene, carbonyl or sulfonyl, B is alkylene, E is alkylene which may be substituted with halo or is alkenylene, Z is O or S, except for a compound wherein n is 0, m is 1 and Y is CH.sub.2 OH, and except for a compound wherein n is 0, Y is COOR.sup.6 (R.sup.6 is alkyl), a salt thereof, a process for its preparation, anti-hyperlipidemic composition containing the derivative as an active ingredient and a method for treating hyperlipidemia comprising administering the derivative.
An oxazolidine derivative represented by the formula (I) ##STR110## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different, and each represents a hydrogen atom, a lower straight- or branched-chain alkyl group optionally having one or more halogen atoms, a lower alkoxy group optionally having one or more halogen atoms, a hydroxyl group, a halogen atom, a nitro group, an amino group optionally having one or more acetyl or lower alkyl groups, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a lower alkanoyl group or a 2-oxazolyl group, or R.sup.1 and R.sup.2 may be combined with each other to represent an alkylene chain --(CH.sub.2).sub.p -- or an alkylenedioxy chain --O(CH.sub.2).sub.q O-- wherein p is 3, 4 or 5, q is 1, 2 or 3, thus forming a cyclic structure, m and n are each 0 or 1, R.sup.4 and R.sup.5 are the same or different and each represents a hydrogen atom or a lower alkyl group, X is a carbon atom, Y is a carboxy group, A is a lower alkylene group, a carbonyl group or a sulfonyl group, B is a lower alkylene group, E is a lower alkylene group which may be halogen-substituted or is a lower alkenylene group, Z is an oxygen atom or a sulfur atom, with the proviso that a compound wherein at least two of R.sup.1, R.sup.2 and R.sup.3 represent a nitro group is excluded, and that a compound, wherein at least two of R.sup.1, R.sup.2 and R.sup.3 represent a branched-chain alkyl group and the substitution positions of these branched-chain alkyl groups are adjacent to each other, is excluded;
A method for treating hyperlipidemia comprising administering to a patient in need of such treatment an effective amount of oxazolidine derivative represented by the formula (I) ##STR111## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different, and each represents a hydrogen atom, a lower straight- or branched-chain alkyl group optionally having one or more halogen atoms, a lower alkoxy group optionally having one or more halogen atoms, a hydroxyl group, a halogen atom, a nitro group, an amino group optionally having one or more acetyl or lower alkyl groups, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a lower alkanoyl group or a 2-oxazolyl group, or R.sup.1 and R.sup.2 may be combined with each other to represent an alkylene chain --(CH.sub.2).sub.p -- or an alkylenedioxy chain --O(CH.sub.2).sub.q O-- wherein p is 3, 4 or 5, q is 1, 2 or 3, thus forming a cyclic structure, m and n are each 0 or 1, R.sup.4 and R.sup.5 are the same or different and each represents a hydrogen atom or a lower alkyl group, X is a carbon atom, Y is a hydroxymethyl group, an aldehyde group or a group represented by COOR.sup.6 (R.sup.6 is a lower alkyl group, a benzyl group or a hydrogen atom), A is a lower alkylene group, a carbonyl group or a sulfonyl group, B is a lower alkylene group, E is a lower alkylene group which may be halogen-substituted or is a lower alkenylene group, Z is an oxygen atom or a sulfur atom, with the proviso that when n is O, a compound wherein m is 1 and Y is a hydroxymethyl group is excluded;
Dependencies are inferred from the claim text.