Bis-(hydroxylakylamino)-anthraquinone inhibitors of protein kinase C
AssigneeSphinx Pharmaceuticals Corporation
InventorsJack B. Jiang, Mary G. Johnson
Life of this patent
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Abstract
The abstract isn’t available for this document.
Claims21
A method of inhibiting protein kinase C which comprises contacting protein kinase C with an inhibitory amount of a substituted anthraquinone having the formula ##STR4## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, or alkylaryl;
- 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).dbd.NR.sub.5, or when m=1, A represents the attachment of the oxygen atom from the adjacent hydroxyl group to form an oxirane ring;
- 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.
A method of inhibiting an oxidative burst in neutrophils which comprises contacting a neutrophil with a substituted anthraquinone having the formula ##STR5## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1-C.sub.10 alkyl, aryl, arylalkyl, or alkylaryl;
- 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).dbd.NR.sub.5, or
- when m=1, A represents the attachment of the oxygen atom from the adjacent hydroxyl group to form an oxirane ring;
- 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 in an amount effective to inhibit said oxidative burst.
A method for treating inflammation which comprises administering to a mammal suffering from inflammation a substituted anthraquinone having the formula ##STR6## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, or alkylaryl;
- n and m are independently 1, 2, or 3;
- A is Halogen, OH, alkoxy, OCO(NR.sup.3 R.sup.4), S--C(NH.sub.2).dbd.NR.sub.5, or when m=1, A represents the attachment of the oxygen atom from the adjacent hydroxyl group to form an oxirane ring;
- 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.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
- in an amount effective to inhibit inflammation.
A method of inhibiting keratinocyte proliferation comprising administering to a keratinocyte a compound having the formula ##STR7## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;
- 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).dbd.NR.sub.5, or when m=1, A represents the attachment of the oxygen atom from the adjacent hydroxyl group to form an oxirane ring;
- 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
- in an amount effective to inhibit proliferation of said keratinocyte.
Dependencies are inferred from the claim text.