Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-10-26
2000-07-04
Huang, Evelyn Mei
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514241, 514242, 514254, 514256, 5142352, 514311, 544128, 544179, 544182, 544238, 544333, 544336, 546167, 546177, A61K 314709, C07D40104, C07D40114, A61P 2900, A61P 3708
Patent
active
060839597
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to new heterocyclic compounds and pharmaceutically acceptable salts thereof.
More particularly, it relates to new heterocyclic compounds and pharmaceutically acceptable salts thereof which have activities as bradykinin antagonists, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like, in human being or animals.
One object of this invention is to provide new and useful heterocyclic compounds and pharmaceutically acceptable salts thereof which possess activities as bradykinin antagonists.
Another object of this invention is to provide processes for the preparation of said compounds and salts thereof.
A further object of this invention is to provide a pharmaceutical composition comprising, as an active ingredient, said heterocyclic compounds and pharmaceutically acceptable salts thereof.
Still further object of this invention is to provide a therapeutical method for the prevention and/or the treatment of bradykinin or its analogues mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like, using said heterocyclic compounds and pharmaceutically acceptable salts thereof.
BACKGROUND ART
Some heterocyclic compounds have been known as described, for example, in EP-A-224,086, EP-A-261,539, Chemical Abstracts 90:34849g (1979), or Chemical Abstracts 97:18948c (1982). However, it is not known that said compounds have activities as bradykinin antagonists.
Heterocyclic compounds having activities as bradykinin antagonists have been known as described in EP-A-596,406, EP-A-622,361, WO 96/13485 and WO 97/11069.
DISCLOSURE OF THE INVENTION
The object heterocyclic compounds of this invention are new and can be represented by the following general formula [I]: ##STR2## wherein R.sup.1 is lower alkyl, group consisting of lower alkyl and acyl, and hydrogen or lower alkyl.
The object compound [I] or its salt can be prepared by processes as illustrated in the following reaction schemes. ##STR3## wherein above.
In the above and subsequent description of the present specification, suitable examples of the various definitions to be included within the scope of the invention are explained in detail in the following.
The term "lower" is intended to mean a group having 1 to 6 carbon atom(s), unless otherwise provided.
In this respect, the term "lower" in lower alkenyl moieties in the various definitions is intended to mean a group having 2 to 6 carbon atoms.
Further, the term "lower" in ar(lower)alkenoyl moiety, heterocyclic(lower)alkenoyl moiety and pyridyl(lower)alkenoyl moiety in the various definitions is intended to mean a group having 3 to 6 carbon atoms.
Suitable "lower alkyl" and lower alkyl moiety such as in the term "lower alkylcarbamoyl", etc., may be straight or branched one such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl or the like, in which preferable one is C.sub.1 -C.sub.4 alkyl such as methyl, ethyl, propyl, isobutyl or tert-butyl.
Suitable "halogen" may be fluorine, chlorine, bromine and iodine.
Suitable "acyl" and acyl moiety in the term "acylamino" may be substituted or unsubstituted alkanoyl such as alkanoyl [e.g. formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, pivaloyl, hexanoyl, heptanoyl, 3,3-dimethylbutyryl, etc.], halo(lower)alkanoyl [e.g. chloroacetyl, trifluoroacetyl, bromoacetyl, bromobutyryl, heptafluorobutyryl, etc.], hydroxy(lower)alkanoyl [e.g. glycoloyl, lactoyl, 3-hydroxypropionyl, glyceroyl, etc.], lower alkylsulfonyloxy(lower)alkanoyl [e.g. mesyloxyacetyl, ethylsulfonyloxyacetyl, mesyloxypropionyl, etc.], lower alkoxy(lower)alkanoyl [e.g. methoxyacetyl, ethoxyacetyl, methoxypropionyl, ethoxypropionyl, propoxypropionyl, methoxybutyryl, etc.], lower alkylthio(lower)alkanoyl [e.g. methylthioacetyl, ethylthioacetyl, m
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Abe Yoshito
Inoue Takayuki
Kayakiri Hiroshi
Oku Teruo
Satoh Shigeki
Fujisawa Pharmaceutical Co. Ltd.
Huang Evelyn Mei
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