Macrocylic compounds

Details Macrocylic compounds Macrocylic compounds

C - Chemistry, Metallurgy

07

D

167/35, 167/46,

C07D 257/02 (2006.01) A61K 49/00 (2006.01) A61K 49/06 (2006.01) C07D 273/00 (2006.01) C07F 5/00 (2006.01) C07F 13/00 (2006.01)

Patent

CA 1341176

1,4,7,10-Tetraazacyclododecanes of general Formula II (see formula II) wherein: each R1, independently of each other, is hydrogen or metal ion equivalent of a complexible metal; R2 is a linear or branched, saturated or unsaturated hydrocarbyl, acyl or acyl-alkylene group each of 1-16 carbon atoms substituted by from 1 to 10 hydroxy or lower alkoxy groups, -CH2-X-V wherein X is carbonyl, alkylene of 0-10 carbon atoms, optionally substituted by hydroxy and/or lower alkoxy, or alkylene of 5-23 carbon atoms interrupted by oxygen atoms, V is (see formula III) or -COOR6, wherein R3 and R4, independently of each other, each is hydrogen, alkyl of 1-16 carbon atoms, or alkyl of 1-16 C-atoms substituted by hydroxy and/or lower alkoxy, or R3 and R4 together with the connecting nitrogen atom form a five- or six-membered saturated ring which can also contain an additional hetero N, S or O atom, and 2/2 R6 is aliphatic hydrocarbyl of up to 16 carbon atoms, C6-10-aryl or C6-10-ar-C1-4-alkyl, or R2 or R3 represent a second macrocycle of Formula II', (see formula II') which is of a structure the same as or different from that of the basic skeleton of Formula II, linked by way of an alkylene chain containing 2-20 carbon atoms which optionally carries carbonyl groups at its ends and/or optionally is interrupted by oxygen or R1-carboxymethylimino and/or optionally is substituted by hydroxy, lower alkoxy or carboxy-lower alkyl, or R2 is B or CH2-COB, wherein B is a biomolecule or synthetic polymer that accumulates to an especially great extent in the organ or organ part to be investigated or in a tumor; are valuable complex-forming compounds and complexes for diagnostics and therapy. They are useful, e.g., in NMR and X-ray diagnostics.

543027

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