Claims
- 1. A naphthalene derivative having the formula and a pharmacologically acceptable salt thereof: ##STR161## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or an acyl group;
- R.sup.2 independently represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a cycloalkyl group, a cycloalkylalkyl group, a hydroxyl group, an aryl group which may be substituted, an arylalkyl group whose aryl group may be substituted, a heteroaryl group, or a heteroarylalkyl group;
- R.sup.3 and R.sup.4 are the same or different and represent a lower alkyl group, a lower alkenyl group, an aryl group which may have a substituent, an arylalkyl group whose aryl group may be substituted, an arylalkenyl group whose aryl group may be substituted, a cycloalkyl group, an alkoxyalkyl group, a heteroaryl group, a heteroarylalkyl group, a carboxyl group or R.sup.3 is a hydrogen atom, a carboxyalkyl group, an aminoalkyl group, or a cyano group; provided R.sup.3 is other than hydrogen when R.sup.4 is lower alkyl;
- R.sup.5 represents a group of the formula, --OR.sup.7, (wherein R.sup.7 represents a hydrogen atom or a lower alkyl group), or a group of the formula, ##STR162## (wherein R.sup.8 and R.sup.9 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sup.8 and R.sup.9 can form, along with the nitrogen atom bonded with R.sup.8 and R.sup.9, a ring which may contain an oxygen atom);
- R.sup.6 independently represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, an amino group, an arylalkyl group, or an aryl group; and
- m is 0 or an integer of from 1 to 2, and n is 0 or an integer of from 1 to 4.
- 2. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1 and R6 is a lower alkyl attached to the 5-position of the naphthalne ring.
- 3. The naphthalene derivative and the salt as claimed in claim 1, in which m is 1 and R2 is a lower alkoxy attached to the 3-position of the naphthalene ring.
- 4. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1, R6 is a lower alkyl attached to the 5-position of the naphthalene ring, m is 1 and R2 is a lower alkoxy attached to the 3-position of the naphthalene ring.
- 5. The naphthalene derivative and the salt as claimed in claim 1, in which R3 is hydrogen and R4 is a lower alkyl.
- 6. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1, R6 is a lower alkyl attached to the 5-position of the naphthalene ring, m is 1 and R2 is a lower alkoxy attached to the 3-position of the naphthalene ring, R3 is hydrogen and R4 is a lower alkyl.
- 7. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1, R6 is ethyl attached to the 5-position of the naphthalene ring.
- 8. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1, R6 is ethyl attached to the 5-position of the naphthalene ring, m is 1 and R2 is methoxy attached to the 3-position of the naphthalene ring.
- 9. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1, R6 is ethyl attached to the 5-position of the naphthalene ring, m is 1 and R2 is methoxy attached to the 3-position of the naphthalene ring, R3 is hydrogen and R4 is a lower alkyl.
- 10. The naphthalene derivative and the salt as claimed in claim 1, in which R1 is hydrogen, a lower alkyl or an acyl.
- 11. The naphthalene derivative and the salt as claimed in claim 1, in which R1 is an acyl.
- 12. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1, R6 is a lower alkyl attached to the 5-position of the naphthalene ring, m is 1, R2 is a lower alkoxy attached to the 3-position of the naphthalene ring, R3 is hydrogen, R4 is a lower alkyl and R1 is hydrogen.
- 13. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1, R6 is a lower alkyl attached to the 5-position of the naphthalene ring, m is 1, R2 is a lower alkoxy attached to the 3-position of the naphthalene ring, R3 is hydrogen, R4 is a lower alkyl and R1 is an acyl.
- 14. The naphthalene derivative and the salt as claimed in claim 1, in which n is 1, R6 is a lower alkyl attached to the 5-position of the naphthalene ring, m is 1, R2 is a lower alkoxy attached to the 3-position of the naphthalene ring, R3 is hydrogen, R4 is a lower alkyl and R1 is acetyl.
- 15. The naphthalene derivative and the salt as claimed in claim 1, in which the naphthalene ring has one or more lower alkyl at the 5-, 7- and 8-positions.
- 16. A pharmaceutical composition which comprises a therapeutically effective amount of the naphthalene derivative defined in claim 1 or a pharmacologically acceptable salt thereof and a pharmacologically acceptable carrier.
- 17. The composition as claimed in claim 16, which is to treat a disease for which an inhibitory action on the production of IL-1 is effective.
- 18. A method for treating a desease for which an inhibitory action on the production of IL-1 is effective, which comprises administering to a human being suffering from the disease a therapeutically effective amount of the naphthalene derivative defined in claim 1 or a pharmacologically acceptable salt thereof.
- 19. The method as claimed in claim 18, in which the disease is an autoimmune disease.
- 20. The method as claimed in claim 18, in which the disease is chronic articular rheumatism, systematic lupus erythromatodes, systematic scleroderm, Bechet's disease, periarteritis nodosa, ulcerative colitis, chronic active hepatitis or glomerulonephritis.
- 21. The method as claimed in claim 18, in which the disease is an intractable disease based on the morbid states of inflammatory symptoms.
- 22. The method as claimed in claim 18, in which the disease is arthritis deformans, gout, atherosclerosis, psoriasis, atopic dermatitis, lung diseses accompanied by granuloma or an encephalites.
Priority Claims (1)
Number |
Date |
Country |
Kind |
63-331621 |
Dec 1988 |
JPX |
|
Parent Case Info
This is a division of application Ser. No. 07/451,468, filed Dec. 15, 1989 now U.S. Pat. No. 5,134,111.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5134111 |
Okita |
Jul 1992 |
|
Non-Patent Literature Citations (8)
Entry |
CA74(11):53331t (1971). |
CA105(25):226086f (1986). |
CA88(5):37483c (1977). |
CA68(13):59350w 1967. |
CA93(25):239314n 1980. |
CA93(25):239314n 1980 (different structures). |
CA102(23):203862e 1985. |
CA106(23):196242e 1986. |
Divisions (1)
|
Number |
Date |
Country |
Parent |
451468 |
Dec 1989 |
|