Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-04-17
1997-07-22
Grumbling, Matthew V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142352, 514259, 514311, 514314, 546173, 544115, 544116, 544283, A61K 31505, A61K 3154, C07D41302, C07D40702
Patent
active
056504101
DESCRIPTION:
BRIEF SUMMARY
This is a national stage application filed under 37 CFR 1.371 of international application PCT/JP9500330, filed Mar. 2, 1995.
TECHNICAL FIELD
The present invention relates to an anti-inflammatory agent. Specifically, it relates to an anti-inflammatory agent, particularly an agent for treating arthritis, containing a quinoline or quinazoline derivative or a salt thereof. The present invention also relates to a novel quinoline or quinazoline derivative having anti-inflammatory activity.
BACKGROUND ART
Arthritis is an inflammatory disease of arthroses. Main examples of arthritis are rheumatoid arthritis and its analogous diseases wherein inflammation is observed in arthroses.
In particular, rheumatoid arthritis, also referred to as chronic rheumatism, is polyarthritis chronica whose main lesion is inflammatory changes in synovial membranes of internal layers of articular capsules. Arthritis such as rheumatoid arthritis is progressive and causes articular disorders such as articular deformation, tetany, etc. When an effective treatment is not carried out and the disease worsens, serious physical disorders are often caused.
Hitherto, in treatment of such arthritis, chemotherapy has been carried out using steroids such as adrenal cortical hormones (e.g., cortisone, etc.), etc.; non-steroidal anti-inflammatory agents such as aspirin, piroxicam, indomethacin, etc.; gold preparations such as gold thiomalate, etc.; antirheumatic agents such as chloroquine preparations, D-penicillamine, etc.; antipodagrics such as colchicine, etc.; immunosuppressive agents such as cyclophosphamide, azathioprine, methotrexate, levamisole, etc.
However, drugs using the chemotherapy have problems such as serious side effects, side effects making their long-term use difficult, insufficient efficacy, inefficacy against arthritis which has already produced the symptoms.
Therefore, in clinical treatment of arthritis, drugs having low toxicity and excellent effects in the prophylaxis and treatment of arthritis have been required.
Various quinoline or quinazoline derivatives have been synthesized. Known compounds having an aminomethyl group at the 2 position of the 4-phenylquinoline or 4-phenylquinazoline skeleton are 2-dimethylaminomethyl compounds, 2-morpholinomethyl compounds, etc., described in Synthesis, Vol. 9, p. 718 (1979), and 2-alkylaminomethyl quinoline derivatives, etc., described in Farmaco, Vol. 44, p. 555 (1989). However, none of these literature discloses anti-inflammatory activity of 4-phenylquinoline or 4-phenylquinazoline derivatives.
The main object of the present invention is to provide an anti-inflammatory pharmaceutical composition.
Another object of the present invention is to provide a novel quinoline or quinazoline derivative having anti-inflammatory activity.
These objects as well as other objects and advantages of the present invention will become apparent to those skilled in the art from the following description.
DISCLOSURE OF INVENTION
The present inventors have found that compounds containing at the 2-position of the 4-phenylquinoline or 4-phenylquinazoline skeleton an alkylene group substituted with an optionally substituted amino group have anti-inflammatory activity, particularly antiarthritic activity, and are useful as an agent for inhibiting arthral destruction. Thus, the present invention has been completed.
The present invention provides an anti-inflammatory pharmaceutical composition comprising a compound of the formula (I): ##STR2## wherein.
Y is a nitrogen atom or C--G in which G is an optionally esterified carboxyl group;
R.sup.1 and R.sup.2 are each independently a hydrogen atom, optionally substituted hydrocarbon group or optionally substituted heterocyclic group or R.sup.1 and R.sup.2 are linked together to form a saturated ring;
each of the ring A and ring B may optionally be substituted;
n is an integer of 1 to 4; and
k is 0 or 1; acceptable carrier.
The present invention also provides a compound of the formula (I'): ##STR3## wherein
Y is a nitrogen atom or C--G in which G is an option
REFERENCES:
patent: 3446806 (1969-05-01), Archer et al.
patent: 3509148 (1970-04-01), Bell
patent: 4089953 (1978-05-01), Shenoy
patent: 5352684 (1994-10-01), Zimmermann et al.
patent: 5436247 (1995-07-01), Sohda et al.
F. Gatta et al., "New Synthesis of 3-(Disubstituted-amino)-1,4-benzodiazepin-2-ones", Synthesis, 1979, No. 9, pp. 718-719.
M. Anzini et al., "Synthesis and 5HT-Receptors Affinity of some 4-phenylquinoline Derivatives", IL Farmaco, 1989, 44(6):555-563.
Baba Atsuo
Makino Haruhiko
Sohda Takashi
Grumbling Matthew V.
Takeda Chemical Industries Ltd.
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