Cyclic anthranilic acid derivatives and process of preparing the

Details Cyclic anthranilic acid derivatives and process of preparing the Cyclic anthranilic acid derivatives and process of preparing the

1991-04-25

1993-09-07

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514211, 514213, 514431, 514456, 540468, 540476, 540552, 540593, C07D51300, A61K 3155, A61K 3138, A61K 31335

Patent

active

052429121

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE TECHNIQUE

The present invention concerns novel cyclic anthranilic acid derivatives, their acid addition salts or alkali salts which have immuno-modulating action and strong inducing ability of suppressor T-cell as well as curing effect to rheumatic arthritis, preparing process thereof, and antirheumatic drug and immunodisease curing drug containing them as an active ingredient.


BACKGROUND OF THE TECHNIQUE

Chronic diseases related to immune responses include rheumatoid arthritis and other autoimmune diseases (systemic lupus erychematosus, psoriatic arthritis, atopic dermatitis, ankylosing spondylitis). These diseases are considered to be caused by bacteria, virus or autoantigens or by an aberration in cytokine regulation of T cells. Especially, patients with rheumatoid arthritis demonstrate various immune abnormalities including reduced functions of suppressor T cells and hyperactivity of B cells.
Non-steroidal antiinflammatory drugs are widely used as first choice drugs in the therapy of rheumatoid arthritis and other diseases due to immunological disorders. While these drugs offer symptomatic relief for patients with these diseases, they fail to alter the underlying immunological dysfunction or the overall course of the disease process. Furthermore, serious side effects from prolonged use of these drugs also have been well documented.
On the other hand, second choice antirheumatic drugs, such as gold salt and D-penicillamine have little acute antiinflammatory effects, but they appear to slow or halt the tissue destruction and more especially the progression of articular damage. They also have immunomodulatory effects. However, it is necessary to improve the safety and other aspects of these drugs, because of the higher incidence of side effects that have been observed in 40-50% of the patients treated with these drugs.
Metabolic bone diseases as generic term include osteoporosis, osteomalacia and ostetic fibrous. In patients with the diseases, there are morbid changes in weight, constitution and structure of bone as a result of the failure of the systemic bone formation and resorption process. This is caused by abnormalities in the somatological regulatory system due to various hormones or vitamins and by congenital or acquired abnormalities of the functions of the osteocytes. It is also associated with abnormal calcium and phosphorus metabolism. Vitamin D, calcium, calcitonin and phosphorus are used as therapeutic drugs, but their effectiveness has not been clearly proven and development of a superior drug has been strongly desired.


DISCLOSURE OF INVENTION

As the result of earnest investigations on the development of antirheumatism agent, the inventors of the present invention have found that the novel cyclic anthranilic acid derivatives, their acid addition salts or alkali salts represented by a general formula [I] of a category different from the known drugs have immuno-modulating action and strong inducing ability of suppressor T-cell, and further have excellent curing effect to rheumatic arthritis and high safety condition.
Furthermore, the inventors of the present invention have found that the compounds of the present invention have inhibitory action against destruction of bone, which has led to the completion of the present invention. ##STR2## wherein R.sup.1, R.sup.2 or R.sup.3, being same or different each other, denotes hydrogen atom, halogen atom, lower alkyl group of carbon number 1-3, lower alkoxy group of carbon number 1-3, amino group, nitro group, hydroxyl group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which can be substituted, ethynyl group which may be substituted, lower alkanoylamino group of carbon number 1-3, benzoylamino group which may be substituted, lower alkylsulfonylamino group of carbon number 1-3 or phenylsulfonylamino group which can be substituted respectively, R.sup.4 or R.sup.5, being same or different, denote

REFERENCES:
patent: 3794646 (1974-02-01), Welstead, Jr. et al.
patent: 3941806 (1976-03-01), Welstead, Jr. et al.
patent: 4935511 (1990-06-01), Youssofyeh et al.
Meyers et al. J. Org. Chem. (1981) vol. 46 pp. 783-788.

Affiliated with

Also associated with

Rating

Cyclic anthranilic acid derivatives and process of preparing the does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Cyclic anthranilic acid derivatives and process of preparing the, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cyclic anthranilic acid derivatives and process of preparing the will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-487922