Compositions and methods for reparation and prevention of fibrotic lesions
First Claim
1. A method for the reparation of, and prophylaxis against, fibrotic lesional tissue in a mammal, comprising administering internally to said mammal a pharmaceutical composition having one or more compounds selected from the group consisting of N-substituted 2-(1H) pyridones and N-substituted 3-(1H) pyridones as active anti-fibrotic ingredient(s), said composition being administered to said mammal at a rate of from about 5 mg per kilogram of body weight per day to about 300 mg per kilogram of body weight per day, said group excluding 5-methyl-1-phenyl-2-(1H) pyridone, but including, exclusively, 5-Methyl-1-(3-nitrophenyl-2)-(1H) pyridone, 5-Methyl-1-(4'"'"'-methoxyphenyl)-2-(1H) pyridone, 5-Methyl-1-p-tolyl-2-(1H) pyridone, 5-Methyl-1-(3'"'"'-trifluoromethylphenyl)-2-(1H)-pyridone, 1-(4'"'"'Chlorophenyl)-5-Methyl-2)-(1H) pyridone, 5-Methyl-1-(2'"'"'-naphthyl)-2-(1H) pyridone, 5-Methyl-1-(1'"'"'naphthyl)-2-(1H) pyridone, 3-Methyl-1-phenyl-2-(1H) pyridone, 6-Methyl-1-phenyl-2-(1H) pyridone, 3,6-Dimethyl-1-phenyl-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-Thienyl)-2-(1H) pyridone, 1-(2'"'"'-Furyl)-5-Methyl-2-(1H) pyridone, 5-Methyl-1-(5'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(4'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(3'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(4'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-thiazolyl)-2-(1H) pyridone, 1-(2'"'"'-Imidazolyl)-5-Methyl-2-(1H) pyridone, 5-Ethyl-1-phenyl-2-(1H) pyridone, 1-Phenyl-2-(1H) pyridone, 1-(4'"'"'-Nitrophenyl)-2-(1H) pyridone, 1,3-Diphenyl-2-(1H) pyridone, 1-Phenyl-3-(4'"'"'-chlorophenyl)-2-(1H) pyridone, 1,3-Diphenyl-5-methyl-2-(1H) pyridone, 3-(4'"'"'-Chlorophenyl)-5-Methyl-1-phenyl-2-(1H) pyridone, 5-Methyl-3-phenyl-1-(2'"'"'-thienyl)-2-(1H) pyridone, 5-Methyl-1-phenyl-3-(1H) pyridone, 5-Methyl-1-(4'"'"'-methoxyphenyl)-3-(1H) pyridone, 5-Methyl-1-p-tolyl-3-(1H) pyridone, 1-(4'"'"'-Chlorophenyl)-5-methyl-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-naphthyl)-3-(1H) pyridone, 4-Methyl-1-phenyl-3-(1H) pyridone, 6-Methyl-1-phenyl-3-(1H) pyridone, 5-Methyl-1(2'"'"'-Thienyl)-3-(1H) pyridone, 1-(2'"'"'-Furyl)-5-methyl-3-(1H) pyridone, 5-Methyl-1-(5'"'"'-quinolyl)-3-(1H) pyridone, 5-Methyl-1-(3'"'"'-pyridyl)-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-pyridyl)-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-quinolyl)-3-(1H) pyridone, 5-Ethyl-1-phenyl-3-(1H) pyridone, and 1-Phenyl-3-(1H) pyridone.
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Abstract
In a preferred embodiment, drugs having pharmacological properties which are useful in the medicinal therapy of fibrotic disease for the reparation and prevention of fibrotic lesional tissues, such drugs including as the active ingredient one or more N-substituted 2-(1H) pyridone(s). The composition of this invention is novel as an anti-fibrotic drug, namely, as an agent for treating fibrosis. Any existing compounds have not been shown to be effective for the reparation and prevention of fibrotic lesions.
75 Citations
12 Claims
- 1. A method for the reparation of, and prophylaxis against, fibrotic lesional tissue in a mammal, comprising administering internally to said mammal a pharmaceutical composition having one or more compounds selected from the group consisting of N-substituted 2-(1H) pyridones and N-substituted 3-(1H) pyridones as active anti-fibrotic ingredient(s), said composition being administered to said mammal at a rate of from about 5 mg per kilogram of body weight per day to about 300 mg per kilogram of body weight per day, said group excluding 5-methyl-1-phenyl-2-(1H) pyridone, but including, exclusively, 5-Methyl-1-(3-nitrophenyl-2)-(1H) pyridone, 5-Methyl-1-(4'"'"'-methoxyphenyl)-2-(1H) pyridone, 5-Methyl-1-p-tolyl-2-(1H) pyridone, 5-Methyl-1-(3'"'"'-trifluoromethylphenyl)-2-(1H)-pyridone, 1-(4'"'"'Chlorophenyl)-5-Methyl-2)-(1H) pyridone, 5-Methyl-1-(2'"'"'-naphthyl)-2-(1H) pyridone, 5-Methyl-1-(1'"'"'naphthyl)-2-(1H) pyridone, 3-Methyl-1-phenyl-2-(1H) pyridone, 6-Methyl-1-phenyl-2-(1H) pyridone, 3,6-Dimethyl-1-phenyl-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-Thienyl)-2-(1H) pyridone, 1-(2'"'"'-Furyl)-5-Methyl-2-(1H) pyridone, 5-Methyl-1-(5'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(4'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(3'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(4'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-thiazolyl)-2-(1H) pyridone, 1-(2'"'"'-Imidazolyl)-5-Methyl-2-(1H) pyridone, 5-Ethyl-1-phenyl-2-(1H) pyridone, 1-Phenyl-2-(1H) pyridone, 1-(4'"'"'-Nitrophenyl)-2-(1H) pyridone, 1,3-Diphenyl-2-(1H) pyridone, 1-Phenyl-3-(4'"'"'-chlorophenyl)-2-(1H) pyridone, 1,3-Diphenyl-5-methyl-2-(1H) pyridone, 3-(4'"'"'-Chlorophenyl)-5-Methyl-1-phenyl-2-(1H) pyridone, 5-Methyl-3-phenyl-1-(2'"'"'-thienyl)-2-(1H) pyridone, 5-Methyl-1-phenyl-3-(1H) pyridone, 5-Methyl-1-(4'"'"'-methoxyphenyl)-3-(1H) pyridone, 5-Methyl-1-p-tolyl-3-(1H) pyridone, 1-(4'"'"'-Chlorophenyl)-5-methyl-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-naphthyl)-3-(1H) pyridone, 4-Methyl-1-phenyl-3-(1H) pyridone, 6-Methyl-1-phenyl-3-(1H) pyridone, 5-Methyl-1(2'"'"'-Thienyl)-3-(1H) pyridone, 1-(2'"'"'-Furyl)-5-methyl-3-(1H) pyridone, 5-Methyl-1-(5'"'"'-quinolyl)-3-(1H) pyridone, 5-Methyl-1-(3'"'"'-pyridyl)-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-pyridyl)-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-quinolyl)-3-(1H) pyridone, 5-Ethyl-1-phenyl-3-(1H) pyridone, and 1-Phenyl-3-(1H) pyridone.
- 8. A method for the reparation of, and prophylaxis against, fibrotic lesional tissue in a mammal, comprising administering topically to said mammal a pharmaceutical composition containing one or more compounds selected from the group consisting of N-substituted 2-(1H) pyridones and N-substituted 3-(1H) pyridones as active anti-fibrotic ingredient(s) in an amount of from about 1% to about 20%, said group excluding 5-methyl-1-phenyl-2-(1H) pyridone, but including, exclusively, 5-Methyl-1-(3-nitrophenyl-2)-(1H) pyridone, 5-Methyl-1-(4'"'"'-methoxyphenyl)-2-(1H) pyridone, 5-Methyl-1-p-tolyl-2-(1H) pyridone, 5-Methyl-1-(3'"'"'-trifluoromethylphenyl)-2-(1H)-pyridone, 1-(4'"'"'Chlorophenyl)-5-Methyl-2)-(1H) pyridone, 5-Methyl-1-(2'"'"'-naphthyl)-2-(1H) pyridone, 5-Methyl-1-(1'"'"'naphthyl)-2-(1H) pyridone, 3-Methyl-1-phenyl-2-(1H) pyridone, 6-Methyl-1-phenyl-2-(1H) pyridone, 3,6-Dimethyl-1-phenyl-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-Thienyl)-2-(1H) pyridone, 1-(2'"'"'-Furyl)-5-Methyl-2-(1H) pyridone, 5-Methyl-1-(5'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(4'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(3'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-pyridyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(4'"'"'-quinolyl)-2-(1H) pyridone, 5-Methyl-1-(2'"'"'-thiazolyl)-2-(1H) pyridone, 1-(2'"'"'-Imidazolyl)-5-Methyl-2-(1H) pyridone, 5-Ethyl-1-phenyl-2-(1H) pyridone, 1-Phenyl-2-(1H) pyridone, 1-(4'"'"'-Nitrophenyl)-2-(1H) pyridone, 1,3-Diphenyl-2-(1H) pyridone, 1-Phenyl-3-(4'"'"'-chlorophenyl)-2-(1H) pyridone, 1,3-Diphenyl-5-methyl-2-(1H) pyridone, 3-(4'"'"'-Chlorophenyl)-5-Methyl-1-phenyl-2-(1H) pyridone, 5-Methyl-3-phenyl-1-(2'"'"'-thienyl)-2-(1H) pyridone, 5-Methyl-1-phenyl-3-(1H) pyridone, 5-Methyl-1-(4'"'"'-methoxyphenyl)-3-(1H) pyridone, 5-Methyl-1-p-tolyl-3-(1H) pyridone, 1-(4'"'"'-Chlorophenyl)-5-methyl-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-naphthyl)-3-(1H) pyridone, 4-Methyl-1-phenyl-3-(1H) pyridone, 6-Methyl-1-phenyl-3-(1H) pyridone, 5-Methyl-1(2'"'"'-Thienyl)-3-(1H) pyridone, 1-(2'"'"'-Furyl)-5-methyl-3-(1H) pyridone, 5-Methyl-1-(5'"'"'-quinolyl)-3-(1H) pyridone, 5-Methyl-1-(3'"'"'-pyridyl)-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-pyridyl)-3-(1H) pyridone, 5-Methyl-1-(2'"'"'-quinolyl)-3-(1H) pyridone, 5-Ethyl-1-phenyl-3-(1H) pyridone, and 1-Phenyl-3-(1H) pyridone.
Specification