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Title:
【発明の名称】1,4,7,10―テトラアザシクロドデカン誘導体,その製法及び該化合物を含有するNMR診断,レントゲン診断,超音波診断及び放射線診断並びに放射線治療のための剤
Document Type and Number:
Japanese Patent JPH0753720
Kind Code:
B2
Abstract:
Compounds of the general formula I in which Y is a nitrogen or phosphorus atom, A<1> and A<2> are identical or different and are each a straight-chain or branched alkylene group having 2 to 6 carbon atoms, U<1>, U<2>, U<3>, U<4> are identical or different and are each a direct bond or a straight-chain or branched alkylene group having 1 to 6 carbon atoms, D<1>, D<2>, D<3>, D<4> are identical or different and are each an oxygen or sulphur atom, an alkylene group having 1 to 6 carbon atoms or a group N-R<7> where R<7> has the meaning of a hydrogen atom, a straight-chain or branched alkylene chain having 1 to 4 carbon atoms, which carries a COOR<1> group at the end, in which R<1> represents a hydrogen atom or a metal ion equivalent, D<5> has the meaning given for D<1>, D<2>, D<3> and D<4> and the group where R<5> has the meaning of a hydrogen atom or of a straight-chain or branched, saturated or unsaturated C1-C20-alkylene group which may contain imino, phenyleneoxy, phenyleneimino, amide, ester groups, oxygen, sulphur and/or nitrogen atoms and may be substituted by hydroxyl, mercapto, imino and/or amino groups and has either a functional group or bound via this group a macromolecule B at the end, s and t are integers from 0 to 5, R<2> is hydrogen, a linear or branched, saturated or unsaturated, alkyl, acyl or acylalkyl group of 1 to 16 carbon atoms which is unsubstituted or substitute by one or more hydroxyl or lower alkoxy groups, or is -CH2-X-V where X has the meaning of carbonyl, of a straight-chain or branched alkylene group having 0 to 10 carbon atoms, which is unsubstituted or substituted by one or more hydroxyl or lower alkoxy groups, or of a straight &tilde& chain or branched alkylene group having 2 to 23 carbon atoms which is interrupted by oxygen atoms, V has the meaning or -COOR<6> in which R<3> and R<4>, independently of one another, are hydrogen, a linear o branched alkyl group having 1 to 16 carbon atoms which is unsubstituted or substituted by one or more hydroxyl or lower alkoxy groups, or R<3> and R<4> together with the nitrogen atom represent a saturated 5- or 6-membered ring which may contain a further hetero atom and R<6> represents hydrogen or a saturated, unsaturated, straight-chain or branched or cyclic hydrocarbon radical having up to 16 carbon atoms or represents an aryl or aralkyl group, or R<2> or R<3> denotes a second macrocycle of the formula I' which is bound via an alkylene chain (K) containing 2 to 20 carbon atoms, which, if desired carries carbonyl groups at the ends and, if desired, is interrupted by one or more oxygen atoms or R<1>-carboxymethylimino groups or substituted by one or more hydroxyl, lower alkoxy or carboxy-lower alkyl groups, which macrocycle can have a structure which is different from that of the parent structure, or R<2> denotes B or CH2-COB, with the proviso that if Rz represents B or CH2-COB, R<5> denotes a hydrogen atom, that at least two COORi groups are present in the molecule and that two hetero atoms of the macrocycle are each bound to at least two carbon atoms via an alkylene group and functional groups present in the molecule are, if desired conjugated with macromolecules and, if desired free carboxyl groups have been converted with organic or inorganic bases or amino acids and basic groups with inorganic or organic acids to the salts.

Inventors:
Heinz Grease
Bernd Rade Uchel
Ulrich Speck
Hans-Joachim Vwainmann
Application Number:
JP18679487A
Publication Date:
June 07, 1995
Filing Date:
July 28, 1987
Export Citation:
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Assignee:
Schie-Ring Actien Gezershaft
International Classes:
A61K49/00; A61K49/04; A61K49/06; A61K51/00; C07B59/00; C07D257/02; C07D273/00; C07F5/00; C07F9/547; C07F9/645; C07F9/6524; C07F9/6561; C07F9/6568; C07F9/6578; C07F9/6584; C07F11/00; C07F13/00; C07F15/00; C07F15/02; C07F15/04; C07F15/06; (IPC1-7): C07D257/02; A61K49/00; A61K49/04; A61K51/00; C07B59/00; C07F5/00; C07F9/6524; C07F13/00; C07F15/00
Domestic Patent References:
JP59139390A
JP62190175A
JP63502659A
Other References:
【文献】国際公開86/2352(WO,A)
Attorney, Agent or Firm:
Toshio Yano (1 outside)