Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-04-22
1995-10-03
Jordan, Kimberly R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514210, 514211, 514212, 514218, 514241, 514242, 514247, 514252, 514255, 514256, 514359, 514383, 514385, 514403, 514409, 514824, A61K 31395, A61K 3155, A61K 3153, A61K 3150, A61K 31495, A61K 31505, A61K 3141, A61K 31415, A61K 3140
Patent
active
054552478
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/US 92/08786 filed Oct. 5, 1992.
This invention relates to a method of treatment of hyperlipidemia in a mammal, including a human, in need thereof which comprises administering to such mammal an effective therefor amount of a substituted azaspirane.
BACKGROUND OF THE INVENTION
Badger et al. U.S. patent application Ser. No. 07/712,325 filed on Jun. 7, 1991, (Badger I) discloses compounds of the formula ##STR1## in which: m is 1 or 2; R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen or straight or branched chain alkyl, provided that the total number of carbon atoms contained by R.sup.1 and R.sup.2 when taken together is 4-10; or R.sup.1 and R.sup.2 together form a cyclic alkyl group containing 3-7 carbon atoms; A is absent or present as C.sub.1 -C.sub.7 alkyl; and R.sup.3 is a heterocyclic or heterobicyclic ring, said heterocyclic or heterobicyclic ring thereby containing up to 10 carbon atoms and from 1-3 heteroatoms of the formula >NR.sup.4, where R.sup.4 is absent or present as hydrogen, or a straight chain alkyl containing 1-3 carbon atoms; or a pharmaceutically acceptable salt, hydrate or solvate thereof.
Badger (I) does not disclose or claim compounds of Formula (I) as antihyperlipidemic agents.
SUMMARY OF THE INVENTION
This invention relates to a method of treatment of hyperlipidemia in a mammal, including a human, in need thereof which comprises administering to such mammal an effective therefor amount of a compound of the formula ##STR2## in which:
m is 1 or 2;
R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen or straight or branched chain alkyl, provided that the total number of carbon atoms contained by R.sup.1 and R.sup.2 when taken together is 4-10; or R.sup.1 and R.sup.2 together form a cyclic alkyl group containing 3-7 carbon atoms;
A is absent or present as C.sub.1 -C.sub.7 alkyl; and
R.sup.3 is a heterocyclic or heterobicyclic ring, said heterocyclic or heterobicyclic ring thereby containing up to 10 carbon atoms and from 1-3 heteroatoms of the formula >NR.sup.4, where R.sup.4 is absent or present as hydrogen, or a straight chain alkyl containing 1-3 carbon atoms;
DETAILED DESCRIPTION OF THE INVENTION
The term "hyperlipidemia" as used in the specification and in the claims is meant the presence of an abnormally high level of lipids in the blood.
The term "antihyperlipidemic" as used herein is meant the lowering of excessive lipid concentrations to desired levels.
Preferred lipids, of which high levels thereof are treated by the presently invented methods, are; cholesterol, triglycerides and low-density lipoproteins.
The preparation of the compounds of Formula (I) and pharmaceutically acceptable salts, hydrates and solvates and formulations thereof is disclosed in U.S. patent application Ser. No. 07/712,325, filed Jun. 7, 1991 the entire disclosure of which is hereby incorporated by reference.
The compounds of this invention are prepared by procedures described here below and illustrated by the examples. Reagents, protecting groups and functionality of the molecule must be consistent with the proposed chemical transformations. Steps in the synthesis must be compatible with the functional groups and the protecting groups.
Formula (I) compounds are prepared as described in Scheme I where R.sup.1, R.sup.2, R.sup.3 and A are as defined in Formula I and the definition of R.sup.3 additionally comprises protecting groups, preferably benzyl protecting groups, which are dissociated to prepare the substituents of R.sup.3 as defined in Formula (I) or are dissociated and further reacted to prepare the substituents of R.sup.3 as defined in Formula (I). ##STR3##
Scheme I depicts formation of Formula (I) compounds. The starting anhydride compounds are known and are synthesized from available precursors using known procedures. According to Scheme I, a solution of an anhydride Compound (a) and a substituted primary amine compound are added to an appropriate organic solvent, preferably xylene or toluene, to fo
REFERENCES:
patent: 4963557 (1990-10-01), Badger et al.
Bugelski Peter J.
Kerns William D.
Dustman Wayne J.
Jordan Kimberly R.
Lentz Edward T.
SmithKline Beecham Corporation
Venetianer Stephen
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