RU2006145639A - APPLICATION OF PYRAZOLINE DERIVATIVES FOR THE PRODUCTION OF A MEDICINE FOR THE PREVENTION AND / OR TREATMENT OF DISEASES ASSOCIATED WITH CELL PROLIFERATION - Google Patents

Claims (3)

1. The use of a pyrazoline derivative of the general formula (I)

where R ₁ represents a hydrogen atom, methyl, fluoromethyl, difluoromethyl, trifluoromethyl, carboxyl group, lower alkyl carboxylate group with 1-4 carbon atoms, carboxamide group or cyano group, R ₂ represents a hydrogen atom or a methyl group, R ₃ , R ₄ , R ₇ and R ₈ , identical or different, represent a hydrogen, chlorine, fluorine atom, a methyl, trifluoromethyl group or a methoxy group, R ₅ represents a hydrogen atom, chlorine, fluorine, methyl, trifluoromethyl group, methoxy, trifluoromethoxy, methylsulfonyl, amino-sulfonyl or acetylaminosulfonyl group, R ₆ represents an aminosulfonyl or acetylaminosulfonyl group, with the proviso that one of the substituents R ₅ or R ₆ represents a methylsulfonyl, aminosulfonyl or acetylaminosulfonyl group, and provided that when R ₁ represents a methyl group, R ₂ represents a hydrogen atom or a methyl group, R ₃ and R ₈ , identical or different, represent a hydrogen, chlorine, fluorine atom, a methyl or trifluoromethyl group, R ₄ represents a hydrogen atom, fluorine, methyl, trifluoromethyl group or methoxy group, R ₅ represents a fluorine atom, a trifluoromethyl group, a trifluoromethoxy, methylsulfonyl, aminosulfonyl or acetylaminosulfonyl group, R ₆ represents an aminosulfonyl or acetylaminosulfonyl group, with the proviso that one of the substituents R ₅ or R ₆ represents a methylsulfonyl, aminosulfonyl or acetylaminosulfonyl group, and R ₇ represents a hydrogen atom, chlorine, fluorine, methyl, trifluoromethyl group or methoxy group; or one of its physiologically acceptable salts, for the manufacture of a medicament for the prevention or treatment of diseases associated with cell proliferation, in particular for the prevention or treatment of precancerous or neoplastic processes, tumor angiogenesis, cachexia and processes associated with tumor necrosis factor (TNF), and, in general, processes in which may have a beneficial effect on the inhibition of expression of the gene responsible for the synthesis of cyclooxygenase-2 (COX-2) in mammals, including humans. 2. The use according to claim 1 of a compound of general formula (I) selected from the group including: [1] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-methylphenyl) -3-trifluoromethyl-1H-pyrazole, [2] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5-methyl-5-phenyl-3-trifluoromethyl-1H-pyrazole, [3] 1- (4-aminosulfonylphenyl) -5- (2,4-difluorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [5] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5-phenyl-3-trifluoromethyl-1H-pyrazole, [8] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-fluorophenyl) -3-trifluoromethyl-1H-pyrazole, [11] 1- (4-aminosulfonylphenyl) -5- (3,4-difluorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [13] 1- (4-aminosulfonylphenyl) -5- (2,4-dichlorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [14] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2-methylphenyl) -3-trifluoromethyl-1H-pyrazole, [15] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (3-methylphenyl) -3-trifluoromethyl-1H-pyrazole, [16] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2-fluorophenyl) -3-trifluoromethyl-1H-pyrazole, [18] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (3-fluorophenyl) -3-trifluoromethyl-1H-pyrazole, [20] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-methoxyphenyl) -3-trifluoromethyl-1H-pyrazole, [21] 1- (4-aminosulfonylphenyl) -5- (3-chloro-4-fluorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [22] 1- (4-aminosulfonylphenyl) -4,5-dihydro-3-trifluoromethyl-5- (4-trifluoromethoxyphenyl) -1H-pyrazole, [23] 1- (4-aminosulfonylphenyl) -5- (2,3-difluorophenide) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [24] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2,4-dimethylphenyl) -3-trifluoromethyl-1H-pyrazole, [26] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-fluorophenyl) -3-methyl-1H-pyrazole, [28] 1- (4-aminosulfonylphenyl) -4,5-dihydro-3-methyl-5- (4-methylphenyl) -1H-pyrazole, [30] 1- (4-aminosulfonylphenyl) -4,5-dihydro-3-methyl-5- (4-trifluoromethylphenyl) -1H-pyrazole, [31] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5-phenyl-1H-pyrazole, [34] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-methylphenyl) -1H-pyrazole-3-carboxylic acid, [35] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5-phenyl-1H-pyrazole-3-carboxylic acid, [37] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-methylphenyl) -1H-pyrazole-3-methylcarboxylate, [38] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5-phenyl-1H-pyrazole-3-methylcarboxylate, [40] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5-phenyl-1H-pyrazole-3-carboxamide, [41] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-methylphenyl) -1H-pyrazole-3-carboxamide, [44] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (3,4-dimethylphenyl) -3-trifluoromethyl-1H-pyrazole, [45] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (3-methyl-4-methoxyphenyl) -3-trifluoromethyl-1H-pyrazole, [46] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (3-fluoro-4-methoxyphenyl) -3-trifluoromethyl-1H-pyrazole, [47] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2-fluoro-4-methoxyphenyl) -3-trifluoromethyl-1H-pyrazole, [48] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2,4-dimethoxyphenyl) -3-trifluoromethyl-1H-pyrazole, [49] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-fluoro-2-methoxyphenyl) -3-trifluoromethyl-1H-pyrazole, [50] 1- (4-aminosulfonylphenyl) -3-difluoromethyl-4,5-dihydro-5- (2,4-dimethylphenyl) -1H-pyrazole, [51] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2,3,4-trifluorophenyl) -3-trifluoromethyl-1H-pyrazole, [52] 1- (4-aminosulfonylphenyl) -5- (2-chloro-4-fluorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [53] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2-fluoro-4-trifluoromethylphenyl) -3-trifluoromethyl-1H-pyrazole, [54] 1- (4-aminosulfonylphenyl) -5- [2,4- (bistrifluoromethyl) phenyl] -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [55] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2-methyl-3-fluorophenyl) -3-trifluoromethyl-1H-pyrazole, [56] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2-methyl-3-methoxyphenyl) -3-trifluoromethyl-1H-pyrazole, [57] 1- (4-aminosulfonylphenyl) -5- (2,4-difluorophenyl) -3-difluoromethyl-4,5-dihydro-1H-pyrazole, [58] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-fluoro-2-trifluoromethylphenyl) -3-trifluoromethyl-1H-pyrazole, [60] 1- (4-aminosulfonylphenyl) -5- (2-chlorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [61] 1- (4-aminosulfonylphenyl) -5- (4-chloro-2-fluorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [62] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (4-fluoro-2-methylphenyl) -3-trifluoromethyl-1H-pyrazole, [63] 1- (4-aminosulfonylphenyl) -4,5-dihydro-5- (2-fluoro-4-methylphenyl) -3-trifluoromethyl-1H-pyrazole, [64] 1- (4-acetylaminosulfonylphenyl) -5- (2,4-difluorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [79] (+) - 1- (4-aminosulfonylphenyl) -5- (2,4-difluorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, [80] (-) - 1- (4-aminosulfonylphenyl) -5- (2,4-difluorophenyl) -4,5-dihydro-3-trifluoromethyl-1H-pyrazole, or one of its physiologically acceptable salts, for the manufacture of a medicament for the prevention or treatment of diseases associated with cell proliferation, in particular for the prevention or treatment of precancerous or neoplastic processes, tumor angiogenesis, cachexia and processes associated with tumor necrosis factor (TNF), and, in general, processes in which may have a beneficial effect on the inhibition of expression of the gene responsible for the synthesis of cyclooxygenase-2 (COX-2) in mammals, including humans. 3. The use according to claim 1 of a compound of general formula (I) or one of its physiologically acceptable salts, together with another product commonly used in the treatment of neoplasia, for the manufacture of a medicament for the prevention or treatment of diseases associated with cell proliferation, in particular for prevention or treatment of precancerous or neoplastic processes, tumor angiogenesis, cachexia and processes associated with tumor necrosis factor (TNF), and, in general, processes in which inhibition can have a beneficial effect expression of the gene responsible for the synthesis of cyclooxygenase-2 (COX-2) in mammals, including humans.