Patent ES-2172461-A1 (ES)
Title: Novel gd(iii) ligands with bi- and bis-azolic structures
Inventor: BALLESTEROS GARCIA PALOMA
IPC: A61K49/00
Filed: 2001-01-25
Abstract: The invention relates to 1) a compound having general formula A, wherein radicals R>1<, R>2<, R>3< and R>4< have the values that are universally known in the organic chemistry formulation, and which can be used in the preparation of chelates that are used as contrast agents in imaging diagnosis 2) the compound in claim 1, wherein X in formula A is (CH>2<)>n< 3) the compound in claim 2, wherein n is 0 4) the compound in claim 2, wherein n is 1 5) the compound in claim 1, wherein X in formula A is CH>2<OCH>2< 6) the compound in claim 1, wherein X in formula A is CH>2<NHCH>2< 7) a method for obtaining the general formula A compound from claim 1, which is characterised in that a biazole is made to react with 1,2-dibromoethane in the presence of BTBA and sodium hydroxide in order to obtain the corresponding alkyl derivative, which is subsequently made to react with methyl iminodiacetate, thereby synthesising the corresponding methyl derivative which in turn reacts with sodium hydroxide in the presence of water, in order to produce the desired sodium salt 8) a method for obtaining the general formula A compound from claim 1, which is characterised in that two 1-chloroethyl-3,5-dimethylprazol molecules are made to react with paraformaldehyde in an acid medium and the reaction mixture is subsequently heated in the presence of chlorohydric acid in order to obtain the corresponding bispyrazole which, in turn, is made to react with methyl iminodiacetate in order to obtain the corresponding intermediary methyl compound, whose hydrolysis in a basic medium produces the desired sodium salt 9) the complexes of the compounds in claim 1 with transition metals and lanthanides 10) the complexes in claim 9, wherein the metal to be chelated is gadolinium 11) the complexes in claim 9, wherein the metal to be chelated is dysprosium 12) the clinical use in imaging diagnosis of the compounds in claim 1 and the corresponding complexes thereof.The invention relates to 1) a compound having general formula A, wherein radicals R1, R2, R3 and R4 have the values that are universally known in the organic chemistry formulation, and which can be used in the preparation of chelates that are used as contrast agents in imaging diagnosis 2) the compound in claim 1, wherein X in formula A is (CH2)n 3) the compound in claim 2, wherein n is 0 4) the compound in claim 2, wherein n is 1 5) the compound in claim 1, wherein X in formula A is CH2OCH2 6) the compound in claim 1, wherein X in formula A is CH2NHCH2 7) a method for obtaining the general formula A compound from claim 1, which is characterised in that a biazole is made to react with 1,2-dibromoethane in the presence of BTBA and sodium hydroxide in order to obtain the corresponding alkyl derivative, which is subsequently made to react with methyl iminodiacetate, thereby synthesising the corresponding methyl derivative which in turn reacts with sodium hydroxide in the presence of water, in order to produce the desired sodium salt 8) a method for obtaining the general formula A compound from claim 1, which is characterised in that two 1-chloroethyl-3,5-dimethylprazol molecules are made to react with paraformaldehyde in an acid medium and the reaction mixture is subsequently heated in the presence of chlorohydric acid in order to obtain the corresponding bispyrazole which, in turn, is made to react with methyl iminodiacetate in order to obtain the corresponding intermediary methyl compound, whose hydrolysis in a basic medium produces the desired sodium salt 9) the complexes of the compounds in claim 1 with transition metals and lanthanides 10) the complexes in claim 9, wherein the metal to be chelated is gadolinium 11) the complexes in claim 9, wherein the metal to be chelated is dysprosium 12) the clinical use in imaging diagnosis of the compounds in claim 1 and the corresponding complexes thereof.