Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1997-10-07
1999-01-19
Krass, Frederick
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
5147721, 514788, 424 7801, 424 7814, 424 7816, 424 7836, 424 7837, 525390, 525391, 525397, A61K 31785, C08G 6548
Patent
active
058614370
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to poly(phenylene ether) resins which have the effect of lowering the level of cholesterol and are useful as medicaments.
BACKGROUND ART
It is already known that a certain anion exchange resin has the effect of lowering the level of cholesterol in blood and therefore is applicable as a cholesterol reducing agent (U.S. Pat. Nos. 3,499,960 and 3,780,171, U. K. Patent No. 929,391, a published Japanese Patent Application (Kokai) No. Sho 53-10386). The mechanism by which the level of cholesterol in blood is lowered by taking the anion exchange resin is considered as follows. Namely, the anion exchange resin adsorbs and fixes bile acids in the intestinal tract to prevent the reabsorption of the bile acids, and in the liver conversion from cholesterol, which is in an equilibrium relation with bile acids, to bile acids is stimulated by this action, and consequently, the cholesterol in blood is reduced.
Cholestyramine, a typical anion exchange resin which is used as a cholesterol reducing agent, has been employed as an agent for the treatment of hypercholesterolemia extensively and clinically. However, cholestyramine has the disadvantage that it must be taken in high doses (from 8 to 16 g per day except for excipients) to obtain effective action clinically. Furthermore, cholestyramine is chemical-structurally unstable and eliminates amines easily because it has quaternary ammonium groups at the benzyl position. Accordingly, cholestyramine has a bad smell typical to an aliphatic amine and is difficult to use by itself. Therefore, cholestyramine must be used together with a deodorant or a fragrance, or must be used after coating on the surface to reduce the bad smell. In consequence, there remains a problem that it is obliged to increase the amount of the dosage owing to use of an additive.
DISCLOSURE OF INVENTION
The present invention relates to a poly(phenylene ether) resin composed of structural units represented by the general formula: ##STR4## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each represents an alkyl group having from 1 to 12 carbon atoms, a cycloalkyl group having from 3 to 15 carbon atoms, a cycloalkylalkyl group having from 4 to 15 carbon atoms, an aralkyl group having from 9 to 15 carbon atoms or a hydrogen atom with the proviso that two or more of R.sup.1, R.sup.2 and R.sup.3 do not represent a hydrogen atom at the same time, or one of R.sup.1, R.sup.2 and R.sup.3 represents an alkyl group having from 1 to 12 carbon atoms or a hydrogen atom while the others are adjacent to each other and together form a saturated ring together with the nitrogen atom binding to them, which may have one or more additional hetero atoms, or R.sup.1, R.sup.2 and R.sup.3 are adjacent to each other and together form an aromatic ring together with the nitrogen atom binding to them, which may have one or more additional hetero atoms; A represents an alkyl group having from 1 to 3 carbon atoms; p is an integer of from 3 to 5; and Y.sup.- represents a pharmaceutically acceptable acid residue and/or structural units represented by the general formula: ##STR5## wherein R.sup.4, R.sup.5 and R.sup.6 are the same or different and each represents an alkyl group having from 1 to 12 carbon atoms, a cycloalkyl group having from 3 to 15 carbon atoms, a cycloalkylalkyl group having from 4 to 15 carbon atoms, an aralkyl group having from 9 to 15 carbon atoms or a hydrogen atom with the proviso that two or more of R.sup.4, R.sup.5 and R.sup.6 do not represent a hydrogen atom at the same time, or one of R.sup.4, R.sup.5 and R.sup.6 represents an alkyl group having from 1 to 12 carbon atoms or a hydrogen atom while the others are adjacent to each other and together form a saturated ring together with the nitrogen atom binding to them, which may have one or more additional hetero atoms, or R.sup.4, R.sup.5 and R.sup.6 are adjacent to each other and together form an aromatic ring together with the nitrogen atom binding to them, which may have one or more additional
REFERENCES:
patent: 3780171 (1973-12-01), Irmscher et al.
patent: 4863998 (1989-09-01), Yeager
Harada Hiromu
Hotei Yukihiko
Hujikura Hideki
Ichihara Mitsuhiro
Kamata Koji
Kissei Pharmaceutical Company, Ltd.
Krass Frederick
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