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MACROCYCLIC POLYAZA COMPOUNDS CONTAINING A 5- OR 6-RING RING, METHOD OF PREPARING THEREOF AND PHARMACEUTICAL AGENTS CONTAINING THESE COMPOUNDS

机译:包含五环或六环的大环聚甲醛化合物,其制备方法和包含这些化合物的药物制剂

摘要

Macrocyclic compounds of the general formula I IMAGE in which @is a single or double bond, q is the numbers 0-5, A and B, which are identical or different, are each a straight-chain or branched alkylene group with 2 to 6 carbon atoms, D is a nitrogen, oxygen atom, the group =C=O, =NR2 with R2 being a hydrogen atom or a C1-C6-alkyl group, the group IMAGE with R3 being a hydrogen or halogen atom, a phenyl, a C1-C6-alkyl group which is optionally substituted by one or more phenyl and/or hydroxyl group(s), being the radical OR5 where R5 is a C1-C6-alkyl radical which is optionally substituted by 1 to 3 hydroxyl groups, being the substituent IMAGE where l is the numbers 0 and 1 and R6 and R7 are, independently of one another, hydrogen atoms, the radical R5, phenyl or benzyl radicals which are optionally substituted by 1 to 3 hydroxyl groups, or R6 and R7 are, together with the nitrogen atom, a saturated or unsaturated, 5- or 6-membered ring which optionally contains another nitrogen, oxygen, sulphur atom or a carbonyl group and which is optionally substituted by 1 to 3 radicals R5, or one of the substituents R6 or R7 is the radical IMAGE or being the substituent G where G is a second macrocycle which is bonded via a direct bond, a bis(carbonylamino) group (-NH-CO-CO-NH-) or via a C1-C20-alkylene group which optionally carries at the ends carbonyl ( CO) or carbonylamino (-NH-CO-) groups or oxygen atoms and optionally contains one or more oxygen atom(s), Z-, acyl- or hydroxyacyl-substituted imino groups or one to two C-C double and/or C-C triple bonds, and has the general formula II IMAGE in which D1 has the same meaning as D with the exception that D1 does not contain the substituent G, or is the radical -CH-, =C- or -N- and F1 has the same meaning as F with the exception that F1 does not contain the substituent G, or is the radical -CH-, or =C-, E is a nitrogen, sulphur, oxygen atom, the IMAGE or NR4 group with R4 being a hydroxyl group, being R2 or being an optionally hydroxylated or carboxylated C1-C6-alkyl group, F is (-CHR8-)n or (=CR8)n with n being the numbers 0 or 1 and R8 being R1 or G, R1 is a hydrogen or halogen atom or a C1-C6-alkyl group, Z is a hydrogen atom or the group -CH2COOY with Y being a hydrogen atom and/or a metal ion equivalent of an element of atomic numbers 21-29, 31, 32, 37-39, 42-44, 49 or 57-83, with the proviso that at least two of the substituents Z are the radical -CH2COOY and that the macrocyclic compound of the general formula I does not contain more than one radical G, and the salts thereof with inorganic and/or organic bases, amino acids or amino amides are valuable diagnostic and therapeutic agents.
机译:通式I 的大环化合物,其中@是单键或双键,q是数字0-5,A和B相同或不同,分别为带有2的直链或支链亚烷基碳原子数为6的碳原子,D为氮,氧原子,基团= C = O,= NR 2,R 2为氢原子或C1-C6-烷基,基团,R <3>为氢或卤素原子,苯基,任选被一个或多个苯基和/或羟基取代的C1-C6-烷基,为基团OR <5>,其中R <5>是C 1 -C 6烷基,其任选地被1-3个羟基取代,是取代基,其中l是数字0和1,并且R 6和R 7彼此独立地是,氢原子,可任选地被1-3个羟基取代的基团R 5,苯基或苄基或R 6和R 7与氮原子一起是饱和或不饱和的5-或六元环(可选)在另一个氮,氧,硫原子或羰基中,其任选地被1-3个基团R 5取代,或取代基R 6或R 7中的一个是基团或为取代基G,其中G是第二个大环,它通过直接键,双(羰基氨基)基团(-NH-CO-CO-NH-)或通过C1-C20亚烷基键合,该基团任选在羰基末端带有( (CO)或羰基氨基(-NH-CO-)或氧原子,并任选包含一个或多个氧原子,Z-,酰基-或羟酰基取代的亚氨基或1-2个CC双和/或CC三联键具有通式II ,其中D <1>与D的含义相同,不同之处在于D <1>不包含取代基G,或为基团-CH-,= C-或-N-和F 1与F具有相同的含义,除了F 1不包含取代基G或为基团-CH-或= C-,E为氮,硫,氧原子,或> NR <4>基团以及R <4> b在羟基,R 2或任选地羟基化或羧基化的C 1 -C 6烷基的情况下,F为(-CHR 8-)n或(= CR 8)n,其中n为数字0或1,且R 8为R 1或G,R 1为氢或卤素原子或C 1 -C 6烷基,Z为氢原子或-CH 2 COOY基团,Y为氢原子和/或原子序数为21-29、31、32、37-39、42-44、49或57-83的元素的金属离子当量,但前提是至少两个取代基Z为基团- CH 2 COOY以及通式I的大环化合物不包含一个以上的基团G,以及其与无机和/或有机碱,氨基酸或氨基酰胺形成的盐是有价值的诊断和治疗剂。

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