Heterocyclic urea derivatives as inhibitors of DNA gyrase and topoisomerase IV / or

摘要

Pharmaceutical ingredients containing these substances, used as drugs, and in the treatment of bacterial infections. Item 1: a compound characterized by a salt acceptable in formula (1) or medicine, wherein ring a is combined with a carbon atom, which is represented by o *;R1 is selected from C1-6, alquenio c2-6, c2-6, c2-6 or C3-6 plasma tar; in this case, R1 can be replaced by one or more R7 carbon; R2 can be selected from C1-6 hydrogen or tar; in this case, C1-6 tar can be replaced by one or more groups independent of halogenation and cyanogen, 1. Hydroxyl group, nitro group and amino group; or R1 and R2, together with the nitro group attached to them, form an isomer in which one or more carbon atoms can replace one or more R8;If the isomer contains a residual n-o-s, one oxo group can be selected to replace the nitration, and one or two oxo groups can be selected to replace the sulfur; if the isomer contains a residual NH group, one group selected from R9 can be selected to replace the nitration; R3 is C1-6 tar or c3-14 carbocyclo; in this case, tar or carbohydrate may choose to replace one or more carbon atoms with one or more carbon atoms; R5 is - Oh, one C1-6, one n - (C1-6 tar) amine, or N, N - (C1-6 tar) 2amine, where alcox C1-6,1. N - (C1-6 tar) amino or N, N - (C1-6 tar) 2amine can be replaced by one or more R14 independently selected on one or more carbon atoms; R6 should be selected from hydrogen, C1-10 tar, c3-4-l - and non cyclic-l-groups;In this case, R6 is replaced by one or more R16 on one or more carbon atoms, and in the case that the isomer contains one or more other substances, the nitration can be replaced by one oxo group, and the sulfur can be replaced by one or two oxo groups; If there is a residue - NH - in the isomer, it can be replaced by a group of selected R17; provided that one R5 or R6 should be replaced by phosphine or R24 should not be h; L is directly linked or C1-6 tar; R7, R8 and R10 are carbon substitutes, The selected substance is independent of halide, nitro group, cyanogen group, hydrogen group and amino group,carboxy, carbamoyl, mercapto, sulfamoyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, C1-6alkanoyl, C1-6alkoxy, N- (C1-6alkyl) amino, N, N - (C1-6alkyl) 2amino, C1-6alkanoylamino, N- (C1-6alkyl) carbamoyl, N, N- (C1-6alkyl) 2carbamoyl, C1-6Salkyl (O) a- where a is 0, 1 or 2, C 1-6 alkoxycarbonyl, C 1-6 alkoxycarbonylamino, N- (C 1-6 alkyl) sulfamoyl, N, N- (C 1-6 alkyl) 2sulfamoyl, C 1-6 alkylsulfonylamino, C 3-6 carbocyclyl and heterocyclyl; wherein R7, R8, and R10, independently of one another, may be optionally substituted on one or more carbons by one or more R19;In this case, if isopropene contains a residual - NH - this nitrate - this substance can be replaced by a selected group of R20; if isopropene contains a residual - n-o-s - this substance can be replaced by an oxo group, and this sulfur can be replaced by one or two oxo groups; R14 and R16. They are carbon substitutes, in each case, selected independently of halogen, nitrate, cyanogen, hydrogen, ammonia, carboxi, carbamoilo, mercato, sulfuric acid, C1-6, alquenilo c2-6, C1-6, acoxi C1-6, alkane C1-6, alkane 1-6oxi. N - (C1-6 tar) amine, N, N - (C1-6 tar) 2amine, alkane-6amine,N- (C1-6 alkyl) carbamoyl. N, N- (C1-6 alkyl) 2carbamoyl, C1-6S alkyl (O) a- where a is 0, 1 or 2, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonylamino, N- (C1-6 alkyl) sulfamoyl, N, N- (C 1-6 alkyl) 2sulfamoyl, C 1-6 alkyl sulfonylamino, C 3-6 carbocyclyl, heterocyclyl and phosphonoxy; wherein R14 and R16 independently of one another can optionally be substituted on one or more carbons by one or more R21; and wherein if said heterocyclyl contains a -NH- moiety, said nitrogen may optionally be replaced by a group selected from R22;If there is a residue = n-o-s in the isomer, one oxo group can be selected to replace the nitrogen, and one or two oxo groups can be selected to replace the sulfur; in each case, screening should be carried out on the basis of not considering C1-6, C1-6, c1-6sulfur. Alcoxc1-6 carbonilo, carbamoilo, N - (C1-6 tar) carbamoilo, N, N - (C1-6 tar) carbamoilo, bencilo, bencilo, benciloxicoboni, benzoilo and fenilsulfonie; wherein R9, R17, R20 and R22 are independent of each other,they can optionally be substituted on carbon by one or more R23; and R19, R21 and R23, in each case, are independently selected from halo, nitro, cyano, hydroxy, trifluoromethoxy, trifluoromethyl, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1-6 alkyl, C1-6 alkoxy, acetyl, acetoxy , methylamino, ethylamino, dimethylamino, diethylamino, N-methyl-N-ethylamino, acetylamino, N-methylcarbamoyl, N-ethylcarbamoyl, N, N-dimethylcarbamoyl, N, N-diethylcarbamoyl, N-methyl-N-ethylcarbamoyl, methylthio, ethylthio , methylsulfinyl, ethylsulfinyl, mesyl, ethylsulfonyl, methoxycarbonyl, ethoxycarbonyl, N-methylsulfamoyl, N-ethylsulfamoyl, N, N-dimethylsulfamoyl,N N- diethyl sulfur or N- methyl-n-ethylsulfonyl; R24 is selected from a group of substances composed of hydrogen, halogen, nitro, cyanogen, hydrogen group, aminobenzene, Mercato, isopropene, C1-6, Alquenilo C2-6, asphalt C2-6, alcox C1-6, N- (C1-6 asphalt) amino, N- (C1-6- asphalt) 2amine and LC1-6sulfanilo; 24 can be replaced in one group Or more than one R25; in the case of one residue (NH) contained in the isomer, the nitroglycerin can be replaced by C1-6 tar; R25 is a carbon substitute, in each case, it is selected independently of halogenation, nitration, cyanogen, hydroxy, aminobenzene, carboxi, carbamoilo, mercato, sulamoilo, C1-6 tar,Alquenilo c2-6, c12-6, alcoxi C1-6, alkane C1-6, alkane 1-6ox. 1 - (1 - (1) 1 - (1 -) 3. Propylene, carbohydrate C3-6 or isopropene; R25 One or more R26 can be selected to replace one or more carbon; if the isocyclohexane contains one residual NH, one selected R27 can be selected to replace it;and wherein if said heterocyclyl contains a = N- or -S- moiety, said nitrogen can optionally be substituted by an oxo group and said sulfur can optionally be substituted by one or two oxo groups; R26 and R28, in each case, are independently selected from halo, nitro, cyano, hydroxy, trifluoromethoxy, trifluoromethyl, amino, carboxy, carbamoyl, mercapto. Sulfamoyl, C1-6alkyl, C1-6alkoxy, acetyl, acetoxy, methylamino, ethylamino, dimethylamino, diethylamino, N-methyl-N-ethylamino, acetylamino, N-methylcarbamoyl, N-ethylcarbamoyl, N, N-diethylcarbamoyl, N-methyl-N-ethylcarbamoyl, methylthio, ethylthio, methylsulfinyl, ethylsulfinyl, mesyl, ethylsulfonyl,methoxycarbonyl, ethoxycarbonyl, N-methylsulfamoyl, N-ethylsulfamoyl, N, N-dimethylsulfamoyl, N, N-diethylsulfamoyl, or N-methyl-N-ethylsulfamoyl; and R27, in each occurrence, is independently selected from C1-6alkyl, C3-6alkyl, C1-6alkanoyl, C1-6alkyl sulfonyl, C1-6alkoxycarbonyl, carbamoyl, N- (C1-6alkyl) carbamoyl, N, N - (C1-6 alkyl) 2carbamoyl, benzyl, benzyloxycarbonyl, benzoyl and phenylsulfonyl, where R27 can optionally be substituted on carbon by one or more R28.