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US 2017/0000753 A1Published application
Kallikrein 7 inhibitors
AssigneeSixera Pharma AB
InventorMarcel LINSCHOTEN
Life of this patent
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Abstract
The present invention relates to methods for inhibiting the activity of human kallikrein 7 (KLK7) (also known as serine protease stratum corneum chymotryptic enzyme, SCCE). The invention further relates to the use of KLK7 inhibitors of Formula I for the treatment and prevention of diseases, more specifically for the treatment and prevention of skin diseases. The invention also provides new compounds demonstrated to be inhibitors of KLK7.
Claims20
A compound according to Formula I
- wherein R1 is selected from aryl, substituted aryl, heteroaryl, and substituted heteroaryl;
- R2 is selected from hydrogen, alkyl, substituted alkyl, aryl, and substituted aryl;
- R3 is selected from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and —C1-C3-alkyl-R5, wherein R5 is selected from cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl;
- R4 is selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, and substituted heteroaryl, and —NH—CO—R6, wherein R6 is selected from aryl and substituted aryl, heteroaryl, and substituted heteroaryl;
- or a pharmaceutical acceptable salt thereof,
- for use in prophylaxis, prevention, or treatment of a skin disease.
3 more elements
A cosmetic or skin care composition comprising at least one compound with the Formula I, or a pharmaceutically acceptable salt thereof, said composition being in a form suitable for topical administration, and selected from the group consisting of a cream, an ointment, a lotion, a liniment, a gel, a paste, a stick, a spray, a shampoo, a soap, a hair conditioner and a powder.
A compound selected from the group consisting of
- [1-methyl-2-[(5-methylisoxazol-3-yl)amino]-2-oxo-ethyl] 2-(4-chlorophenyl) acetate,
- 1-[(5-methylisoxazol-3-yl)carbamoyl]propyl 2-(4-chlorophenyl)acetate,
- [1-methyl-2-[(5-methylisoxazol-3-yl)amino]-2-oxo-ethyl] 2-(4-methoxyphenyl) acetate,
- 1-[(5-methylisoxazol-3-yl)carbamoyl]propyl 2-(4-methoxyphenyl) acetate,
- [1-methyl-2-[(5-methylisoxazol-3-yl)amino]-2-oxo-ethyl] 3-cyclopentylpropanoate,
- [2-(4-methoxyanilino)-1-methyl-2-oxo-ethyl] 2-(4-methoxyphenyl)acetate,
- 1-[(5-methylisoxazol-3-yl)carbamoyl]propyl 3-cyclopentylpropanoate,
- [2-[(5-methylisoxazol-3-yl)amino]-2-oxo-1-phenyl-ethyl] 2-(4-chlorophenyl)acetate,
- [2-[(5-methylisoxazol-3-yl)amino]-2-oxo-1-phenyl-ethyl] 3-cyclopentylpropanoate,
- 1-[(5-methylisoxazol-3-yl)carbamoyl]propyl 2-(4-methoxyphenyl)acetate,
- 1-[(5-methylisoxazol-3-yl)carbamoyl]propyl 2-(1,3-benzodioxol-5-yl)acetate,
- [2-[(5-methylisoxazol-3-yl)amino]-2-oxo-1-phenyl-ethyl] 2-(4-methoxyphenyl) acetate,
- 1-[(5-methylisoxazol-3-yl)carbamoyl]propyl 2-(3,4-dichlorophenyl)acetate,
- 1-[(5-methylisoxazol-3-yl)carbamoyl]propyl 2-(3,4-dimethoxyphenyl)acetate,
- [1-methyl-2-[(5-methylisoxazol-3-yl)amino]-2-oxo-ethyl] 2,2-diphenylacetate,
- [2-[(5-methylisoxazol-3-yl)amino]-2-oxo-1-phenyl-ethyl] 2-benzamido-2-phenyl-acetate,
- [1-methyl-2-[(5-methylisoxazol-3-yl)amino]-2-oxo-ethyl] 2-benzamido-2-phenyl-acetate,
- [2-[(5-methylisoxazol-3-yl)amino]-2-oxo-1-phenyl-ethyl] 2,2-diphenylacetate,
- [2-[(5-methylisoxazol-3-yl)amino]-2-oxo-ethyl] 2-benzamido-2-phenyl-acetate,
- [2-methyl-1-[(5-methyl isoxazol-3-yl)carbamoyl]propyl] 2-(4-chlorophenyl)acetate,
- [2-methyl-1-[(5-methylisoxazol-3-yl)carbamoyl]propyl] 3-cyclopentylpropanoate,
- [2-methyl-1-[(5-methylisoxazol-3-yl)carbamoyl]propyl] 2-benzamido-2-phenyl-acetate,
- [2-methyl-1-[(5-methylisoxazol-3-yl)carbamoyl]propyl] 2,2-diphenylacetate,
- [2-[(5-methylisoxazol-3-yl)amino]-2-oxo-ethyl] 2-(4-chlorophenyl)acetate, and
- [2-methyl-1-[(5-methylisoxazol-3-yl)carbamoyl]propyl] 2-(4-methoxyphenyl)acetate.
22 more elements
A compound selected from the group consisting of
- [2-(4-methoxyanilino)-1-methyl-2-oxo-ethyl] 2-(4-chlorophenyl)acetate,
- 1-[(4-methoxyphenyl)carbamoyl]propyl 2-(4-chlorophenyl)acetate,
- 1-[(4-fluorophenyl)carbamoyl]propyl 2-(4-chlorophenyl)acetate,
- 1-(phenylcarbamoyl)propyl 2-(4-chlorophenyl)acetate,
- [2-(4-methoxyanilino)-1-methyl-2-oxo-ethyl] 3-cyclopentylpropanoate,
- 1-[(4-methoxyphenyl)carbamoyl]propyl 3-cyclopentylpropanoate,
- [2-(4-methoxyanilino)-2-oxo-1-phenyl-ethyl] 2-(4-chlorophenyl)acetate,
- [2-(4-methoxyanilino)-2-oxo-1-phenyl-ethyl] 3-cyclopentylpropanoate,
- 1-[(4-methoxyphenyl)carbamoyl]propyl 2-(4-methoxyphenyl)acetate,
- 1-[(4-fluorophenyl)carbamoyl]propyl 3-cyclopentylpropanoate,
- 1-[(4-fluorophenyl)carbamoyl]propyl 2-(4-methoxyphenyl)acetate,
- (2-anilino-1-methyl-2-oxo-ethyl) 3-cyclopentylpropanoate,
- (2-anilino-2-oxo-1-phenyl-ethyl) 2-(4-chlorophenyl)acetate,
- 1-(phenylcarbamoyl)propyl 2-(4-methoxyphenyl)acetate,
- [2-(4-methoxyanilino)-2-oxo-1-phenyl-ethyl] 2-(4-methoxyphenyl)acetate,
- [2-(benzylamino)-2-oxo-1-phenyl-ethyl] 3-cyclopentylpropanoate,
- [2-(4-methoxyanilino)-2-oxo-ethyl] 2-(4-methoxyphenyl)acetate,
- 1-[(4-methoxyphenyl)carbamoyl]propyl 2,2-diphenylacetate,
- 1-[(4-fluorophenyl)carbamoyl]propyl 2,2-diphenylacetate,
- 1-(phenylcarbamoyl)propyl 2,2-diphenylacetate,
- [2-(4-methoxyanilino)-2-oxo-ethyl] 2-benzamido-2-phenyl-acetate,
- [2-(4-fluoroanilino)-2-oxo-ethyl] 2-benzamido-2-phenyl-acetate,
- (2-anilino-2-oxo-ethyl) 2-benzamido-2-phenyl-acetate,
- 1-[(4-methoxyphenyl)carbamoyl]propyl 2-benzamido-2-phenyl-acetate,
- 1-[(4-fluorophenyl)carbamoyl]propyl 2-benzamido-2-phenyl-acetate,
- (2-anilino-1-methyl-2-oxo-ethyl) 2-benzamido-2-phenyl-acetate,
- [2-(4-methoxyanilino)-1-methyl-2-oxo-ethyl] 2-benzamido-2-phenyl-acetate,
- (2-anilino-2-oxo-1-phenyl-ethyl) 2-benzamido-2-phenyl-acetate,
- [2-(4-methoxyanilino)-2-oxo-1-phenyl-ethyl] 2,2-diphenylacetate,
- [2-(benzylamino)-1-methyl-2-oxo-ethyl] 2-benzamido-2-phenyl-acetate,
- [2-methyl-1-(phenylcarbamoyl)propyl] 2-(4-chlorophenyl)acetate,
- [1-[(4-methoxyphenyl)carbamoyl]-2-methyl-propyl] 2-(4-chlorophenyl)acetate,
- [2-methyl-1-(phenylcarbamoyl)propyl] 2-benzamido-2-phenyl-acetate,
- [2-methyl-1-(phenylcarbamoyl)propyl] 2-(4-methoxyphenyl)acetate,
- [1-[(4-methoxyphenyl)carbamoyl]-2-methyl-propyl] 2-benzamido-2-phenyl-acetate, and
- [1-[(4-fluorophenyl)carbamoyl]-2-methyl-propyl] 2-benzamido-2-phenyl-acetate.
33 more elements
Dependencies are inferred from the claim text.