NOVEL 4-((CYCLOALKYL OR CYCLOALKENYL SUBSTITUTED) 1MINO, ALKYLAMINO OR ALKENYLAMINO) BENZOIC ACIDS, SALTS AND DERIVATIVES

The invention provides novel amino-substituted phenyl and heteroaryl compounds which show pharmaceutically useful properties, particularly as hypolipidemic and anti-atherosclerotic agents, and processes for the preparation of the novel compounds. The novel compounds have the formula: Q is wherein Y...

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1. Verfasser: ROBERT GORDON SHEPHERD
Format: Patent
Sprache:eng
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Zusammenfassung:The invention provides novel amino-substituted phenyl and heteroaryl compounds which show pharmaceutically useful properties, particularly as hypolipidemic and anti-atherosclerotic agents, and processes for the preparation of the novel compounds. The novel compounds have the formula: Q is wherein Y is loweralkyl, loweralkoxy, hydroxy, nitro, acycloxy or halo, and m is an integer of from 0 to 4 inclusive, or a 5- or 6-membered heteroaryl ring containing 1 or more nitrogen, sulfur or oxygen atoms and which may be optionally substituted with one fluorine atom; R is hydrogen or a group convertible in vivo thereinto; Z is: a) -@-J wherein J is selected from the group consisting of hydroxy, loweralkoxy, loweralkoxyloweralkyloxy, diloweralkylaminoloweralkoxy, hydrogen, loweralkyl, (mono- or polyhydroxy)loweralkoxy, (mono- or polycarboxy)loweralkoxy, (mono- or polycarboxy)hydroxyloweralkoxy, allyloxy, 2,3-epoxypropoxy, substituted or unsubstituted(phenoxy, benzyloxy and 3-pyridyloxy), pyridylmethoxy, tetrahydropyranyloxy, (mono- or polyhydroxyl)loweralkylamino, (mono- or polycarboxy)loweralkylamino, (mono- or polycarboalkoxy)loweralkylamino, allylamino, propargylamino, 2-sulfoethylamino, (substituted or unsubstituted aroyl)amino, loweralkanoylamino, loweralkanesulfonylamino, (substituted or unsubstituted arene)sulfonylamino, loweralkanoylhydrazino, hydroxylamino, polymethyleneimino, (4-carboxy- or 4-carboethoxy)thiazolidino, and loweralkyl bearing one or more carboxy, carboloweralkoxy, carbamoyl, acyl, sulfinyl or sulfonyl groups, or b) -B-@-OK wherein B is a saturated or unsaturated loweralkylene group and K is selected from the group consisting of hydrogen, loweralky, loweralkyl, loweralkoxyethyl, diloweralkyl aminoethyl, (mono- or polyhydroxy)loweralkyl, (mono- or polycarboxy)loweralkyl, (mono- or polycarboxy)hydroxyloweralkyl, allyl, 2,3-epoxypropyl, substituted or unsubstituted (phenyl, benzyl or 3-pyridyl) or pyridylmethyl and tetrahydropyranyl; and wherein Q, Y, m and X are defined as follows: Formula I-A) Q is i