where Pyr means the group of formulas or where R1 - phenyl substituted with definite substituents; R1a - benzyl-group possibly substituted with Hal; RIV - H, Hal. (C1-C6)-alkyl; RV - phenyl-group substituted with definite substituents, or RV - naphthyl, pyridine or styrene substituted with (C1-C4)-alkyl, or RIV and RV taken together mean the group -2Ph-(CH2)i where phenyl-group substitutes pyrazole at 5 position and group (CH2)i where i = 1-3 substitutes pyrazole at position 4; R-H1(C1-C4)-alkyl; Z - -OH1(C1-C6)-alkoxy, amino; X and X1 - H or one of these is H and another is (C1-C6)-alkyl, (C3-C6)-cycloalkyl-(C1-C4)-alkyl, acetamido-(C1-C4)-alkylthiomethyl, guanidino-(C1-C4)-alkyl, carboxy-(C1-C4)-alkyl, nitroguanidino-(C1-C4)-alkyl, (C3-C7)-cycloalkyl, phenyl-(C1-C4)-alkyl possibly substituted with Hal, OH; heteroaryl-(C1-C4)-alkyl where heteroaryl - imidazolyl or indolyl, or X is H and X1 and R taken together form with nitrogen atoms the cycle of the formula (II) where m = 1-2, or indolinyl cycle, or 4,5,6,7-tetrahydro-[2,3-c]-thienopyridine cycle, or X and X1 where each means (C1-C4)-alkyl-(C3-C6)-cycloalkyl or phenyl, or X and X1 together with carbon atom form (C3-C12)-cycloalkylidene group that is substituted if necessary with (C1-C3)-alkyl, adamantylene, quinuclidinylidene, 4-piperidinylidene group which is possibly substituted with N-benzyl, tetrahydronaphthylidene, 4-tetrahydropyranyliedene, dihydro-2,3(4H)-4-benzothiopyranylidene, or dihydro-(4H)-4-benzopyranylidene group, or the group of the formulas a () and b (), or their salts with acids or bases and pharmaceutical composition based on the indicated compounds. ???EFFECT: improved method of synthesis."/>
AMIDOPYRAZOLE DERIVATIVES OR THEIR SALTS WITH ORGANIC OR MINERAL ACIDS OR WITH ORGANIC OR INORGANIC BASES AND PHARMACEUTICAL COMPOSITION SHOWING INHIBITING ACTIVITY WITH RELATION TO NEUROTENSINE
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AMIDOPYRAZOLE DERIVATIVES OR THEIR SALTS WITH ORGANIC OR MINERAL ACIDS OR WITH ORGANIC OR INORGANIC BASES AND PHARMACEUTICAL COMPOSITION SHOWING INHIBITING ACTIVITY WITH RELATION TO NEUROTENSINE
AMIDOPYRAZOLE DERIVATIVES OR THEIR SALTS WITH ORGANIC OR MINERAL ACIDS OR WITH ORGANIC OR INORGANIC BASES AND PHARMACEUTICAL COMPOSITION SHOWING INHIBITING ACTIVITY WITH RELATION TO NEUROTENSINE
FIELD: organic chemistry, pharmacy. SUBSTANCE: products: derivatives of amidopyrazole of the general formula (I) where Pyr means the group of formulas or where R1 - phenyl substituted with definite substituents; R1a - benzyl-group possibly substituted with Hal; RIV - H, Hal. (C1-C6)-alkyl; RV - phenyl-group substituted with definite substituents, or RV - naphthyl, pyridine or styrene substituted with (C1-C4)-alkyl, or RIV and RV taken together mean the group -2Ph-(CH2)i where phenyl-group substitutes pyrazole at 5 position and group (CH2)i where i = 1-3 substitutes pyrazole at position 4; R-H1(C1-C4)-alkyl; Z - -OH1(C1-C6)-alkoxy, amino; X and X1 - H or one of these is H and another is (C1-C6)-alkyl, (C3-C6)-cycloalkyl-(C1-C4)-alkyl, acetamido-(C1-C4)-alkylthiomethyl, guanidino-(C1-C4)-alkyl, carboxy-(C1-C4)-alkyl, nitroguanidino-(C1-C4)-alkyl, (C3-C7)-cycloalkyl, phenyl-(C1-C4)-alkyl possibly substituted with Hal, OH; heteroaryl-(C1-C4)-alkyl where heteroaryl - imidazolyl or indolyl, or X is H and X1 and R taken together form with nitrogen atoms the cycle of the formula (II) where m = 1-2, or indolinyl cycle, or 4,5,6,7-tetrahydro-[2,3-c]-thienopyridine cycle, or X and X1 where each means (C1-C4)-alkyl-(C3-C6)-cycloalkyl or phenyl, or X and X1 together with carbon atom form (C3-C12)-cycloalkylidene group that is substituted if necessary with (C1-C3)-alkyl, adamantylene, quinuclidinylidene, 4-piperidinylidene group which is possibly substituted with N-benzyl, tetrahydronaphthylidene, 4-tetrahydropyranyliedene, dihydro-2,3(4H)-4-benzothiopyranylidene, or dihydro-(4H)-4-benzopyranylidene group, or the group of the formulas a () and b (), or their salts with acids or bases and pharmaceutical composition based on the indicated compounds. ???EFFECT: improved method of synthesis.
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