Sphinx Pharmaceuticals Corporation

Jack B Jiang

Mary George Johnson

Jeffrey B Nichols

The present invention provides compounds having the formula ##STR1## wherein R.sub.1 is alkyl, alkenyl and alkynyl having from 2 to about 20 carbon atoms; R.sub.2, R.sub.3 and R.sub.6 are independently H, phenyl or alkyl having from 1 to about 20 carbon atoms; and R.sub.4 and R.sub.5 are independently H, R.sub.6 imino, or amidino, and pharmaceutically acceptable salts thereof which are useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

1,3-dioxane derivatives having protein kinase C inhibitory activity

##STR1## The present invention provides novel substituted anthraquinones having formula (.alpha.), wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl, or R.sub.1 and R.sub.2 taken together with the adjacent nitrogen atom N form a substituted or unsubstituted cyclic ring which may contain additional heteroatoms; n and m are independently 1, 2, or 3; A is halogen, OH, alkoxy, OCO(NR.sub.3 R.sub.4), S--C(NH.sub.2)=NR.sub.5, or when m=1, comprises an oxirane ring with the adjacent oxygen atom; R.sub.3, R.sub.4, and R.sub.5 are independently H, alkyl, or aryl; X is H, OH, NR.sub.6 R.sub.7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR.sub.8, or CONR.sub.9 R.sub.10 ; and R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are independently H, lower alkyl, or aryl useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

Bis-(hydroxylakylamino)-anthraquinone inhibitors of protein kinase C

The present invention provides novel furocoumarinsufonamide derivatives having the formula ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H or lower alkyl; m, n and p are independently 2, 3, 4, 5 or 6; A is NR.sub.4 (CH.sub.2).sub.P NR.sub.5, NR.sub.6, O or S; R.sub.2 is independently H, lower alkyl or a moiety of the formula ##STR2## useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

Furo-coumarinsulfonamides as protein kinase C inhibitors

The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;

Bis-(hydroxyalkylamino)-anthraquinone inhibitors of protein kinase C

The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, alkyl, aryl, or arylalkyl;

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Chapel Hill, NC, United States of America

Jack B Jiang