Process for treating proliferative skin diseases using certain diamino compounds

Claim 2

A process for treating a non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one diamino compound selected from the groups consisting of the diamines of saturated and unsaturated aliphatic hydrocarbons having 3 to 6 carbon atoms, the diamines of saturated monocarboxylic acids having 4 to 6 carbon atoms and the alkyl esters thereof containing from 1 to 4 carbon atoms, α-methyl ornithine, α-hydrazino ornithine, trans-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine, and N-(5'-phosphopyridoxyl)-ornithine, said compound being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 3

A process in accordance with claim 1 wherein said active component is a diamine of saturated and unsaturated aliphatic hydrocarbons having 3 to 6 carbon atoms.

Claim 4

A process in accordance with claim 1 wherein said active component is a diamine of saturated monocarboxylic acids having 4 to 6 carbon atoms and the alkyl esters thereof containing from 1 to 4 carbon atoms.

Claim 5

A process in accordance with claim 1 wherein said active component is at least one ornithine selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, trans-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine, and N-(5'-phosphopyridoxyl)-ornithine.

Claim 6

A process in accordance with claim 1 wherein said active component is α-methyl ornithine.

Claim 7

A process in accordance with claim 1 wherein said active component is DL-α-difluoromethyl ornithine.

Claim 8

A process for treating a non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one ornithine selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, α-hydrazino-α-methyl ornithine, trans-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine, and N-5'-phosphopyridoxyl)-ornithine, and a minor amount of a glucocorticoid, said compounds being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 9

A process for treating a non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one ornithine selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, α-hydrazino-α-methyl ornithine, trans-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine, and N-5'-phosphopyridoxyl)-ornithine, and a minor amount of a glucocorticoid, said compounds being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 10

A process for treating a non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one ornithine selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, α-hydrazino-α-methyl ornithine, trans-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine and N-(6'-phosphopyridoxyl)-ornithine, in admixture with methylglyoxal bis(guanylhydrazone), said compounds being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 11

A process for treating a non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one ornithine selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, α-hydrazino-α-methyl ornithine, trans-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine and N-(6'-phosphopyridoxyl)-ornithine, in admixture with methylglyoxal bis(guanylhydrazone), said compounds being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 12

A process in accordance with claim 8 wherein said ornithine compound is DLα-difluoromethyl ornithine.

Claim 13

A process for treating non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one ornithine selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, α-hydrazino-α-methyl ornithine, tran-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine and N-(5'-phosphopyridoxyl)-ornithine, in admixture with 1,1'-(methylethanediylidinedinitrilo)-bis-(3-aminoguanidine), said compounds being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 14

A process for treating non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one ornithine selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, α-hydrazino-α-methyl ornithine, tran-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine and N-(5'-phosphopyridoxyl)-ornithine, in admixture with 1,1'-(methylethanediylidinedinitrilo)-bis-(3-aminoguanidine), said compounds being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 15

A process in accordance with claim 10 wherein said ornithine compound is DL-α-difluoromethyl ornithine.

Claim 16

A process for treating a non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one of the compounds selected from the groups consisting of (I) A compound of the formula ##STR6## wherein R 1 is H or methyl; R 2 is H or phenyl; R 3 is propyl, isopropyl or phenyl; R 4 is H, bromine, methylthio, or benzylthio; X is oxygen or methylene; (II) a compound of the formula ##STR7## wherein R 1 and R 2 are hydrogen or hydroxyl; Y is hydrogen, or alkali metal; Z is hydrogen, benzylthio, thiol, halogen, alkylthio wherein alkyl is from 1 to 8 carbon atoms, inclusive, and hydroxy; R 4 is hydrogen, ##STR8## wherein R 5 is phenyl, benzyl or alkyl of 1 to 8 carbon atoms; (III) a compound of the formula ##STR9## wherein R 1 is --CONH 2 , --C(NH)NH 2 , --C(NH)NHOH, --CN, or --COOCH 3 ; R 1 and R 2 are hydrogen or hydroxy; Y is hydrogen or alkali metal; (IV) a compound selected from the group consisting of compounds characterized by the formula ##STR10## wherein R is halogen, hydrogen, lower alkyl and lower alkoxy; R 2 , R 3 and R 4 taken independently of each other are hydrogen, lower alkoxy or hydroxy-lower alkoxy and provided that R 2 , R 3 and R 4 taken independently of each other represent at least one oxygenated substituent; or R, R 2 , R 3 and R 4 taken as an adjacent pair is methylenedioxy and the optical antipodes thereof, and (V) Prostaglandin compounds of the D-type (PGD) selected from the group consisting of PGE 1 , PGE 2 , PGE 3 or the alkyl ester thereof containing from 1 to 8 carbon atoms inclusive, or 13, 14-dihydro PGE 1 or the alkyl esters thereof containing from 1 to 8 carbon atoms inclusive, and PGD 2 and the alkyl esters thereof containing from 1 to 8 carbon atoms inclusive, and at least one ornithine compound selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, α-hydrazino-α-methyl ornithine, trans-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine and N-(5'-phosphopyridoxyl)-ornithine, said compounds being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 17

A process for treating a non-malignant proliferative skin disease which comprises administering to the afflicted human or animal, a composition containing as an active component at least one of the compounds selected from the groups consisting of (I) A compound of the formula ##STR6## wherein R 1 is H or methyl; R 2 is H or phenyl; R 3 is propyl, isopropyl or phenyl; R 4 is H, bromine, methylthio, or benzylthio; X is oxygen or methylene; (II) a compound of the formula ##STR7## wherein R 1 and R 2 are hydrogen or hydroxyl; Y is hydrogen, or alkali metal; Z is hydrogen, benzylthio, thiol, halogen, alkylthio wherein alkyl is from 1 to 8 carbon atoms, inclusive, and hydroxy; R 4 is hydrogen, ##STR8## wherein R 5 is phenyl, benzyl or alkyl of 1 to 8 carbon atoms; (III) a compound of the formula ##STR9## wherein R 1 is --CONH 2 , --C(NH)NH 2 , --C(NH)NHOH, --CN, or --COOCH 3 ; R 1 and R 2 are hydrogen or hydroxy; Y is hydrogen or alkali metal; (IV) a compound selected from the group consisting of compounds characterized by the formula ##STR10## wherein R is halogen, hydrogen, lower alkyl and lower alkoxy; R 2 , R 3 and R 4 taken independently of each other are hydrogen, lower alkoxy or hydroxy-lower alkoxy and provided that R 2 , R 3 and R 4 taken independently of each other represent at least one oxygenated substituent; or R, R 2 , R 3 and R 4 taken as an adjacent pair is methylenedioxy and the optical antipodes thereof, and (V) Prostaglandin compounds of the D-type (PGD) selected from the group consisting of PGE 1 , PGE 2 , PGE 3 or the alkyl ester thereof containing from 1 to 8 carbon atoms inclusive, or 13, 14-dihydro PGE 1 or the alkyl esters thereof containing from 1 to 8 carbon atoms inclusive, and PGD 2 and the alkyl esters thereof containing from 1 to 8 carbon atoms inclusive, and at least one ornithine compound selected from the group consisting of ornithine, α-methyl ornithine, α-hydrazino ornithine, α-hydrazino-α-methyl ornithine, trans-3-dehydro-D,L-ornithine, DL-α-difluoromethyl ornithine and N-(5'-phosphopyridoxyl)-ornithine, said compounds being in association with a pharmaceutical carrier wherein the concentration of said active component is effective to alleviate a proliferative skin disease.

Claim 18

A process in accordance with claim 12 wherein said composition includes methyl glyoxal bis-(guanyl hydrazone).

Claim 19

A process in accordance with claim 12 wherein said composition includes 1,1'-(methylethanediylidinedinitrilo)-bis-(3-aminoguanidine).