Thienopyridine derivatives and their use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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Details

514291, 540484, 546 83, C07D49314, C07D22300, A61K 31435, A61K 3155

Patent

active

060461896

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention relates to a new thienopyridine derivative useful as an anti-inflammatory drug, especially as a drug for treating arthritis, or a salt thereof. The thienopyridine derivative or a salt thereof also has bone resorption inhibitory activity and is useful as a drug for preventing and treating osteoporosis. In addition, the thienopyridine derivative or a salt thereof is useful, for example, as a drug for preventing and treating immune-related diseases, such as an immunosuppressant.


BACKGROUND OF THE INVENTION

Arthritis, an inflammatory disease of the joint, occurs in various forms such as rheumatoid arthritis and related diseases with joint inflammation.
Rheumatoid arthritis, also called chronic rheumatism, in particular, is a chronic multiple arthritis characterized by inflammatory changes in the synovial membrane of the articular capsule inner layer. Arthritic diseases like rheumatoid arthritis are progressive and cause joint disorders such as deformation and acampsia, often resulting in severe physical disorder due to a lack of effective treatment and subsequent deterioration.
Traditionally, these forms of arthritis have been chemotherapeutically treated with various drugs including steroids and other adrenocortical hormones (e.g., cortisone), non-steroidal anti-inflammatory drugs (e.g., aspirin, piroxicam, indomethacin), gold-containing drugs (e.g., auro-thiomalate), antirheumatic drugs (e.g., chloroquine preparations, D-penicillamine), anti-gout drugs (e.g., colchicine) and immunosuppressors (e.g., cyclophosphamide, azathioprine, methotrexate, levamisole).
However, these drugs have drawbacks such as severe adverse reactions, adverse reactions hampering the drug's long-term use, a lack of efficacy and a failure to be effective against already-occurring arthritis.
Accordingly, there is a need for the development of a drug which exhibits excellent prophylactic/therapeutic action on arthritis with low toxicity in clinical situations.
Heretofore, various compounds have been synthesized as thieno[2,3-b]pyridine derivatives including those described in the Bulletin of the Chemical Society of Japan, Vol. 61, p. 4431 (1988), Chemical and Pharmaceutical Bulletin, Vol. 36, p. 4389 (1988), Phosphorus, Sulfur and Silicon, Vol. 73, p. 127 (1992), Chemical and Pharmaceutical Bulletin, Vol. 40, p. 1376 (1992) and Khim Geterotsikl Soedin, Vol. 1, p. 124 (1987). However, these compounds are limited to the structure in which the substituent at the 6-position in the thieno[2,3-b]pyridine skeleton is a methyl group. Also, no description of anti-inflammatory action, bone resorption inhibitory action or immunosuppressant action is given for these known thienopyridine derivatives.


OBJECTS OF THE INVENTION

One object of the present invention is to provide novel thienopyridine derivatives which have anti-inflammatory activity and useful, for example, as anti-inflammatory drugs, especially as drugs for treating arthritis, as well as which have bone resorption inhibitory activity and immunosuppressant activity and useful as drugs for inhibiting bone resorption and immunosuppressants, or salts thereof.
Another object of the present invention is to provide a pharmaceutical composition useful for treating inflammation, in particular, arthritis, for preventing or treating arthritis, for inhibiting bone resorption and immunosuppressant which comprising the novel thienopyridine derivative or a salt thereof as an effective component.
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.


SUMMARY OF THE INVENTION

The present inventors found that a novel thienopyridine derivative represented by the following formula (A) has antiarthritic activity and serves well as a joint destruction suppressor and also found that the thienopyridine derivative has bone resorption inhibitory activity which functions on a bone directly and serves well as a bone resorption inhibitory drug. In addition, th

REFERENCES:
Journal of Medicinal Chemistry, 1973, vol. 16, No. 3, pp. 214-219.
Journal of Medicinal Chemistry, 1974, vol. 17, No. 6, pp. 624-630.
Khim. Geterotsikl. Soedin., 1987, No. 1, pp. 124-128.
Bulletin of the Chemical Society of Japan, 1988, vol. 61, No. 12, pp. 4431-4433.
Chemical and Pharmaceutical Bulletin, 1992, vol. 40, No. 6, pp. 1376-1382.
Phosphorus, Sulfur, and Silicon and the Related Elements, 1992, vol. 73, pp. 127-135.
Chemical & Pharmaceutical Bulletin, 1988, vol. 36, No. 11, pp. 4389-4402.
Journal fur praktische Chemie, Band 317, 1975, Heft 5, pp. 705-880.

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