Topical application of spiperone or derivatives thereof for treatment of pathological conditions associated with immune responses

A method for the treatment of a cutaneous, ocular, or mucosal pathology associated with an immune response in a human or other mammal comprises topical application of an effective amount of a compound selected from the group consisting of a quaternary salt of spiperone and a quaternary salt of a spiperone derivative of the formula:

• ##STR5## wherein R.sub.1 =H;
• alkyl, Y--CH.sub.2 (CH.sub.2).sub.n -- or Ar.sub.1,
• R.sub.2 =H or C.sub.1 to C.sub.20 alkyl;
• R.sub.3 =H;
• alkyl, CN(CH.sub.2).sub.2 --;
• X--(CH.sub.2).sub.n --;
• X--(CH.sub.2).sub.n CO--;
• NH.sub.2 C(NH)NHC(NH)(aryl)(CH.sub.2).sub.n --;
• or X-(aryl)-(CH.sub.2).sub.n --;
• R.sub.4 =H, C.sub.6 H.sub.5 CH(CH.sub.2 CH.sub.3)CH.sub.2 --, C.sub.6 H.sub.5 CH(CH.sub.3)(CH.sub.2).sub.2 --, C.sub.6 H.sub.5 CH.sub.2 CH(CH.sub.3)CH.sub.2 --, C.sub.6 H.sub.5 CH.sub.2 CH.sub.2 CH(CH.sub.3)--, C.sub.6 H.sub.5 CH(CH.sub.3)(CH.sub.2).sub.3 --, (2, 3, or 4)-(alkyl)-C.sub.6 H.sub.4 CH(CH.sub.3)(CH.sub.2).sub.3 --, (2, 3, or 4)-(alkyloxy)-C.sub.6 H.sub.4 CH(CH.sub.3)(CH.sub.2).sub.3, C.sub.6 H.sub.5 CH(OCH.sub.3)(CH.sub.2).sub.2 --, ##STR6## C.sub.6 H.sub.5 CO(CH.sub.2).sub.3, C.sub.6 H.sub.5 CO(CH.sub.2).sub.4 --, (2, 3, or 4)-(alkyl)-C.sub.6 H.sub.4 CO(CH.sub.2).sub.3 --, (2, 3, or 4)-(alkyl-oxy)-C.sub.6 H.sub.4 CO(CH.sub.2).sub.3 --, (2, 3, or 4)-X--C.sub.6 H.sub.4 -alkyl-, (2, 3, or 4)-X--C.sub.6 H.sub.4 CO(CH.sub.2).sub.n --, 2-thienyl-CO-(CH.sub.2).sub.3 --, ##STR7## (2, 3, or 4)-X--C.sub.6 H.sub.4 C(CH.sub.3)CH(CH.sub.2).sub.2 --, where the conformation about the double bond is cis or trans,
• (2, 3, or 4)-X--C.sub.6 H.sub.4 C(CH.sub.3)CHCH.sub.2 --, where the conformation about the double bond is cis or trans,
• (2, 3, or 4)-X--C.sub.6 H.sub.4 COCH.dbd.CHCH.sub.2 --, Y--CH.sub.2 (CH.sub.2).sub.n --, Ar.sub.1 --(CH.sub.2).sub.n --, C.sub.1 to C.sub.20 alkyl, X--(CH.sub.2).sub.n CO--, or X--(CH.sub.2).sub.n --;
• n=1 to 6;
• p is 1 to 20;
• X=is independently F, Cl, Br, I, OCH.sub.3, SO.sub.3.sup.-, NH.sub.2, H, --OH, --COOH, --COOR, wherein R is alkyl or benzyl, --SO.sub.3 H, --CN, --NHSO.sub.3 H, --NO.sub.2, or --SO.sub.2 NH.sub.2 ;
• Y=H, F, Cl, Br, I, --SO.sub.3, --PO.sub.4.sup.=, --OH, --SH, --SCH.sub.3, --CH.sub.3 SO.sub.2.sup.-, --NH.sub.2, or --CO.sub.2.sup.- ;
• and
• Ar.sub.1 is, independently, aryl, (2, 3, or 4-X--C.sub.6 H.sub.4 --), (2, 3, or 4)-(CH.sub.2 X)C.sub.6 H.sub.4 --, (2, 3, or 4)-(CX.sub.3)C.sub.6 H.sub.4 --, (2, 3, or 4)-(CHX.sub.2)C.sub.6 H.sub.4 --, 2-thienyl, or (2, 3, or 4)-X--C.sub.6 H.sub.4 CH.sub.2 --;
• or its pharmaceutically acceptable salt optionally in a pharmaceutical carrier.