Claims
- 1. A compound of formula (I): ##STR39## in which: X represents halogen,
- n represents 0, 1, or 2,
- B represents ##STR40## in which: R.sub.3 represents hydrogen, optionally substituted aryl, optionally substituted arylalkyl or optionally substituted heteroaryl,
- A represents either:
- * the radical ##STR41## in which x represents 0 or 1, Alk represents a saturated bivalent hydrocarbon radical having 3 to 6 carbon atoms inclusive in a straight or branched chain, and Z represents a radical selected from the group consisting of:
- a) nitrile and, carboxy or alkoxycarbonyl only when x=1,
- b) the radical ##STR42## in which: T.sub.1, T.sub.2 and T.sub.3, which may be identical or different, are selected from linear or branched alkyl radicals having 1 to 5 carbon atoms inclusive, optionally substituted aryl radical, and an optionally substituted arylalkyl radical,
- Q represents halogen, or a residue of an organic acid,
- c) the radical ##STR43## in which each of m and p, independently of the other, represents 1 or 2, z represents 0 to (m+2) inclusive and R represents alkyl having 1 to 5 carbon atoms inclusive in a straight or branched chain, aryl, or arylalkyl, each of which is optionally substituted,
- d) the radical ##STR44## in which R.sub.4 represents hydrogen, carboxy, alkoxycarbonyl, or optionally substituted aminocarbonyl,
- e) the radical ##STR45## in which each of W and W', independently of the other, represents H.sub.2, O or S, t represents 0 or 1, r represents 1 or 2, g represents 0 to (r+2) inclusive and R is as defined above,
- f) the radical ##STR46## in which W, W' and r are as defined above and each of R.sub.a and R'.sub.a, independently of the other, represents hydrogen, alkyl having 1 to 5 carbon atoms inclusive in a straight or branched chain, optionally substituted aryl, or optionally substituted arylalkyl,
- g) the radical ##STR47## in which E represents O, S or the group N--H, each of s and u, independently of the other, represents 1 or 2 and R is as defined above,
- * or the radical ##STR48## in which v represents 1 to 4 inclusive, R.sub.a and x are as defined above and each of R.sub.b and R'.sub.b, independently of the other, represents alkyl having 1 to 5 carbon atoms inclusive in a straight or branched chain, optionally substituted aryl, or optionally substituted arylalkyl,
- or the radical ##STR49## in which x, Alk, T.sub.1 and T.sub.2 are as defined above, or the radical ##STR50## in which x is as defined above and R.sub.5 represents a hydrocarbon radical having 5 to 20 carbon atoms inclusive in a straight or branched chain and including at least one unsaturation in the form of a double bond: ##STR51## it being understood that, unless otherwise specified, "aryl radical" represents a radical chosen from phenyl and naphtyl, "arylalkyl radical" represents a radical chosen from phenyl and naphthyl bound to an alkyl radical containing from 1 to 4 carbon atoms inclusive and "heteroaryl radical" represents a radical chosen from pyridyl, pyrrolyl, pyrazinyl, pyridazinyl, pyrimidazinyl, quinolyl and indolyl,
- it being also understood that, unless otherwise specified, the expression "optionally substituted" means that the alkyl, aryl, arylalkyl or heteroaryl group may be substituted by one or more substituents chosen from halogen, hydroxy, nitro, cyano, alkyl, alkoxy, acyl, haloalkyl, amino, alkylamino and dialkylamino, and their possible stereoisomers, epimers, N-oxides and addition salts with a pharmaceutically, acceptable acid or base.
- 2. A method for treating a mammal afflicted with a condition requiring inhibitors of cytokines, resulting from pain, the rejection of a transplanted organ, inflammatory disorders and disorders capable of inducing septic shock, comprising the step of administering to said mammal an amount of a compound of claim 1 which is effective for alleviation of said condition.
- 3. A pharmaceutical composition useful in inhibiting cytokines which contains as active ingredient an effective amount of a compound according to claim 1, in combination with one or more pharmaceutically, acceptable inert, non-toxic excipients or vehicles.
- 4. A compound of claim 1 which is N-(3-dimethylammonio-1-propyl)-N-(3-pyridiniomethyl-2-amino-5-chlorobenzothiazolium trichloride.
- 5. A compound of claim 1 which is 2-(3-dimethylammoniopropylamino)-5-chlorobenzothiazolium dichloride.
- 6. A compound of claim 1 which is bis-(5-chlorobenzothiazol-2-yl)-3-dimethylaminopropyl)ammonium chloride.
Priority Claims (1)
Number |
Date |
Country |
Kind |
92 06353 |
May 1992 |
FRX |
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Parent Case Info
The present application is a division of our prior-filed application Ser. No. 08/226,633, filed Apr. 12, 1994, now U.S. Pat. No. 5,550,143, which in turn is itself a division of Ser. No. 08/066,524, filed May 24, 1993, now abandoned.
US Referenced Citations (7)
Foreign Referenced Citations (1)
Number |
Date |
Country |
48-78166 |
Oct 1973 |
JPX |
Non-Patent Literature Citations (2)
Entry |
Chemical Abstracts 51, 12101 (b), (c) 1957 (Fujii). |
Fujii Chem Ab, 51, 12101 f (1957) Not Applied. |
Divisions (2)
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Number |
Date |
Country |
Parent |
226633 |
Apr 1994 |
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Parent |
66524 |
May 1993 |
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