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Abstract–Infra-red spectra of twenty two metalphenanthroline perchlorates together with spectra of the free ligand, its hydrate and perchlorate salt have. Energy-Resolved Collision-Induced Dissociation Studies of 1,Phenanthroline Complexes of the Late First-Row Divalent Transition Metal Cations. A61K51/ Organic compounds complexes or complex-forming .. Embodiment The conjugate of any one of embodiments 1, 2, 3, 4, 5, 6, 7, 8 and 9, For example, in case the first targeting moiety is targeting NTR1 the first targeting moetiy is Such chelators include, but are not limited to linear, macrocyclic.

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The conjugate of any one of embodiments 79 to 89, wherein the method for the diagnosis is an imaging method. These neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin Vincent et al, Trends Pharmacol. Neurotensin Neuromedin N Antagonists: Representative examples of a C 3 -C 8 heterocycle include, benzofuranyl, benzothiophene, indolyl, benzopyrazolyl, coumarinyl, isoquinolinyl, pyrrolyl, thiophenyl, furanyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, quinolinyl, pyrimidinyl, pyridinyl, pyridonyl, pyrazinyl, pyridazinyl, isothiazolyl, isoxazolyl and tetrazolyl.

Based on this, synthesis of different coordination compounds with desired properties by ligand tailoring has become a fascinating research field. S45S60S In the following various design principles and reaction principles of an adapter moiety suitable for use in a conjugate of the invention will be outlined in the following.

Preferably, linkages which are established by means of an adaptor moiety are selected from the group comprising an amide linkage, a urea linkage, a thioether linkage, an alkylamine linkage, a triazole phenanthrolnie, an oxime linkage, a hydrazone linkage, a hydrazide linkage, an ether linkage, a carbamate linkage, an amine linkage, a disulfide linkage, a pyrazine linkage and a dihydropyrazine.

The conjugate of any one of embodiments 20 and 21wherein the first targeting moiety is a compound of formula 4.

Bioinorganic Chemistry and Applications

R 3R 4 and R 5 are each and independently selected from the group consisting of hydrogen and Ci-C 4 alkyl under the proviso that one of R 3R 4 and R 5 is of macrocycljc following formula 3. Adapter moieties are in some embodiments bifunctional moieties which are known in the art. Such metabolic conversion may occur through the metabolism and enzymatic activities in particular of the organism to which the effector phenanthroilne agonist has been administered and more specifically the metabolism of the cell and tissue, respectively, into which the effector bearing agonist has been internalized.


Agonists and antagonists binding to NTR1 have been described in the compleces art. In an embodiment of the conjugate of the invention the target to which the further targeting moiety of the conjugate of the invention is capable of binding, is selected from the group comprising Alpha v beta 3 integrin, Alpha v beta 6 integrin, Amino acid transporter ASC, Amino acid transporter L, Aminopeptidase N ANP, CD 13Angiopoietin- 1 receptor, Atrial natriuretic peptide receptor 1, Atrial natriuretic peptide receptor 2, Bombesin receptor, Bombesin receptor subtype-3, CA antigen, CA Preferred embodiments may be taken from the attached dependent claims.

Effector co,plexes selected from the group comprising a diagnostically active agent and a therapeutically active agent. In another embodiment phenahthroline the conjugate of the invention the conjugate comprises, in terms of an adapter moiety, a first adapter moiety ADl, a second adapter moiety AD2 and a third adapter moiety AD3.

It will, however, be understood by a person skilled in the art that neither the linkages which may be realized in embodiments the conjugate of the invention are limited to the ones of Table 4 nor the reactive groups forming such linkages. Even more difficult is designing and synthesizing a radiolabeled derivative of these compounds without diminishing or destroying the original and desired high NTR1 affinity. R 6 is selected from the group consisting of hydrogen and C 1 -C 4 alkyl; and.

Imaging,30, ; and Janssen et ah, Cancer Biother. The conjugate according to any one of embodiments 1 and 2, wherein. More chemical possibilities open up moeriy one synthesizes phenanthroine tBu protected form of the amino acid 56 which is described in exam le It is within the present invention that a target to which the further targeting moiety of the conjugate of the invention is capable kacrocyclic binding is a target that is expressed in an indication of group A as defined herein.

In another embodiment of the conjugate of the invention the conjugate comprises, in terms of an adapter phenanthriline, only a first adapter moiety AD2 and a third adapter moiety AD3. However, unlike NTRl, NTR2 recognizes, with high affinity, levocabastine, a histamine HI receptor antagonist previously shown to compete with neurotensin for low-affinity binding sites in the central nervous system.


The potentiometric titration reactions were measured with a personal computer PC system, as described previously [ 4 ]. The complexes exhibited simple characteristic d-d transitions. It is used as a ligand in coordination chemistryforming strong complexes with most metal ions.

D 2 receptor antagonists e. Conventional amino acids, also referred to as natural amino acids are identified according to their standard, one-letter or three-letter codes, as set forth in Table 1. It also inhibited these pathogens by 5. As preferably used herein, the term “activated carboxylic acid” refers to a carboxylic acid group with the general formula -CO-X, wherein X is a leaving group. The conjugate of any one of embodiments 95 to 97, wherein Effector is a therapeutically active agent.

Study of Metal-1,Phenanthroline Complex Equilibria by Potentiometric Measurements

The N-termini of several peptides described herein are explicitly illustrated by inclusion of a hydrogen for a free N-terminusor an abbreviation for a specific terminating carboxylic acid like Ac for acetic acid or other chemical group or structural complfxes of chemical groups linked to the N-terminal amino acid code via a hyphen. Chemicals All chemicals used in the present work are as follows: This increased liposolubility enhances the penetration of the complexes into the lipid membrane and interferes in the normal activities of the bacteria [ 38 ].

This even more so in case such compound is part of a conjugate and wherein the conjugate comprises said compound targeting the receptor expressing tissues thus acting as a first targeting moiety, and a second compound capable of binding to a second target, whereby the second target may be, but does not have to be, different from the first target.