Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-07-26
1996-12-10
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142242, 5142268, 5142282, 5142245, 544101, 544 52, 544 54, 544 586, 544 14, C07D49806, C07D51304, A61K 31535, A61K 3154
Patent
active
055831354
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This relates to new heterotricyclic derivatives and pharmaceutically acceptable salts thereof which are useful as a medicament.
BACKGROUND ART
Some heterotricyclic derivatives have been known as described, for example, in U.S. Pat. No. 4,547,511.
DISCLOSURE OF INVENTION
This invention relates to new heterotricyclic derivatives. More particularly, this invention relates to new heterotricyclic derivatives and pharmaceutically acceptable salts thereof which have pharmacological activities, processes for preparation thereof, a pharmaceutical composition comprising the same and a use of the same.
Accordingly, one object of this invention is to provide the new and useful heterotricyclic derivatives and pharmaceutically acceptable salts thereof which possess a strong immunomodulating activity (e.g. an inhibitory activity on the production of an autoantibody, etc.), anti-inflammatory activity and anti-cancer activity.
Another object of this invention is to provide processes for preparation of the heterotricyclic derivatives and salts thereof.
A further object of this invention is to provide a pharmaceutical composition comprising said heterotricyclic derivatives or a pharmaceutically acceptable salt thereof.
Still further object of this invention is to provide a use of said heterotricyclic derivatives or a pharmaceutically acceptable salt thereof as a medicament for the treatment and/or prevention of inflammatory conditions, various pains, collagen diseases, auto-immune diseases, various immunity diseases, cancer and the like in human being and animals.
The object heterotricyclic derivatives of the present invention are novel and can be represented by the following general formula (I): ##STR3## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino, formula: ##STR4## (in which n is 0, 1 or 2).
The object compound (I) of the present invention can be prepared by the following processes. ##STR5## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.8 and --Z-- are each as defined above, --COR.sup.6 is amidated carboxy,
Suitable pharmaceutically acceptable salts of the object compound (I) are conventional non-toxic salts and may include e.g. a salt with a base or an acid addition salt such as a salt with an inorganic base, for example, an alkali metal salt (e.g. sodium salt, potassium salt, etc.), an alkaline earth metal salt (e.g. calcium salt, magnesium salt, etc.), an ammonium salt; a salt with an organic base, for example, an organic amine salt (e.g. triethylamine salt, pyridine salt, picoline salt, ethanolamine salt, triethanolamine salt, dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt, etc.); an inorganic acid addition salt (e.g. hydrochloride, hydrobromide, sulfate, phosphate, etc.); an organic carboxylic or sulfonic acid addition salt (e.g. formate, acetate, trifluoroacetate, maleate, tartrate, methanesulfonate, benzenesulfonate, toluenesulfonate, etc.); a salt with a basic or acidic amino acid (e.g. arginine, aspartic acid, glutamic acid, etc.).
In the above and subsequent descriptions of the present specification, suitable example and illustration of the various definitions which the present invention intends to include within the scope thereof are explained in detail as follows.
The term "lower" is used to intend a group having 1 to 6, preferably 1 to 4, carbon atom (s), unless otherwise provided.
The term "higher" is used to intend a group having 7 to 20 carbon atoms, unless otherwise provided.
Suitable "lower alkyl" and "lower alkyl moiety" in the terms "lower alkylthio" "ower alkylsulfinyl" and "lower alkylsulfonyl" may include straight or branched one such as methyl, ethyl, propyl, isopropyl, butyl, t-butyl, pentyl, hexyl, and the like, in which more preferable example may be C.sub.1 -C.sub.4 alkyl.
Suitable "lower alkoxy" may include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, t-butoxy, pentyloxy, t -pentyloxy, hexyloxy and the like, in which more preferable example may be C.sub.1 -C.sub.4 alkoxy.
Suit
REFERENCES:
patent: 4547511 (1985-10-01), Eriksoo et al.
Klippel, J. H. et al. Internal Medicine, Stein, J. H. et al. ed. (Mosby, St. Louis), pp. 2422-2423 (1994).
Llach, F. et al. Internal Medicine, Stein, J. H. et al. ed. (Mosby, St. Louis), pp. 2609-2614 (1994).
Albert, S. et al. Internal Medicine, Stein, J. H. et al. ed. (Mosby, St. Louis), pp. 2765-2773 (1994).
Nordlund, J. J. et al. Internal Medicine, Stein, J. H. et al. ed. (Mosby, St. Louis), pp. 919-921 (1994).
Katritzky, A. R., et al. Handbook of Heterocyclic Chemistry (Pergamon Press, Oxford), pp. 148, 151, 167, 174, 195, 298, 307, 317, and 318 (1985).
Gilchrist, T. L. Heterocyclic Chemistry (Longman Scientific & Technical, Essex, England), pp. 302, 346, 347 (1992).
Gilchrist, T. L. Aromatic and Heteroaromatic Chemistry, vol. 4, edited by Bird, C. W. et al. (Chemical Society, London) p. 363 (1976).
Gilchrist, T. L. Aromatic and Heteroaromatic Chemistry , vol. 2, edited by Bird, C. W. et al. (Chemical Society, London) pp. 373, 375, and 379 (1974).
Martin, L. et al. Internal Medicine (Mosby, St. Louis) edited by Stein, J. H., p. 2349 (1994).
Salmon, S. E. et al. Basic & Clinical Pharmacology, edited by Katzung, B. G. (Appleton & Lange, Norwalk) p. 824 (1995).
Matsuo Masaaki
Nakamura Katsuya
Spears Glen W.
Tsuji Kiyoshi
Fujisawa Pharmaceutical Co. Ltd.
Shah Mukund J.
Wong King Lit
LandOfFree
Heterotricyclic derivatives, process for their preparation and p does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Heterotricyclic derivatives, process for their preparation and p, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Heterotricyclic derivatives, process for their preparation and p will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-424385