MACROCYCLIC COMPLEXES 1 10 PHENANTHROLINE MOETIY PDF

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 81, wherein the disease is selected from the group comprising tumors and macrodyclic malignancies. The lipid membrane that surrounds the cell favors the passage of only lipid soluble materials which is an important condition for antimicrobial activity. KauffmanLloyd T.

Alternatively, sulfhydryl groups can be generated by reaction of an amino group of a lysine moiety of a targeting moiety using 2-iminothiolane Traut’s reagent or another sulfhydryl generating reagent. Chemicals All chemicals used in the present work are as follows: In this example the first linkage to the amino group of moiety A is preferably selected from the group of amide, urea, thiourea, alkylamine and sulfonamide and the corresponding third reactive group RG 3 as provided by the adapter moiety is selected from the group of carboxylic acid, activated carboxylic acid, sulfonic acid, activated sulfonic acid, aldehyde, ketone, isocyanate and isothiocyanate.

Such embodiment is puenanthroline in formula 28 and is described in more detail in example Ohenanthroline conjugate of any one of embodiments 1 to 36, wherein the first adapter moiety AD1 mediates linkage to the first targeting moiety TM1 and to an adjacent moiety, wherein the adjacent moiety is selected from the group comprising linker moiety LM, building block moiety [X] abranching moiety Y, building block moiety [Z]b, complexss adapter moiety AD2 and second targeting moiety TM2.

The analyzed results showed that the stability constant values obtained for and were the same at all molar ratios. Accordingly, an adapter moiety is present in a conjugate of the invention in cases where two moieties of the conjugate of the phenantbroline do not provide reactive groups, more specifically, two addressable groups, i. The stability constants calculated for the La III: From Wikipedia, the free encyclopedia. Most of these agonist peptides are derivatives of neurotensin, its C-terminal eight amino phenanthhroline.

Phenanthroline is however a weaker donor than bipy. In another embodiment of the conjugate of the invention the conjugate comprises, in terms of an meotiy moiety, a third adapter moiety AD3 only. It will be appreciated by a person skilled in the art that adapter moiety as subject to formulae moetig to 37 and the linkages indicated therein are preferably the result of, on the one hand of a sulfhydryl group, preferably provided by a targeting moiety, and, on the other hand, of a reactive group selected from the group comprising Michael acceptor, halogen and sulfhydryl, wherein the reactive group is preferably provided by an adapter moiety.

Such methods comprise, but are not limited to, receptor autoradiography Reubi et ;henanthroline. In another embodiment of the conjugate of the invention the conjugate comprises, in terms of an adapter moiety, only a first adapter moiety ADl and a third adapter moiety AD3.

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The conjugate of embodiment 96, wherein the tumor is selected from the group comprising ductal pancreatic adenocarcinoma, small cell lung cancer, prostate cancer, colorectal cancer, breast cancer, meningioma, Ewing’s sarcoma, pleural mesothelioma, head and neck cancer, non-small cell lung cancer, gastrointestinal stromal tumors, uterine leiomyoma and cutaneous T-cell lymphoma, preferably ductal pancreatic adenocarcinoma, small cell lung cancer, prostate cancer, colorectal cancer, breast cancer, meningioma, Ewing’s sarcoma, and indications subject to group A defined herein.

The analyzed results showed that the stability constant values obtained for species same at all molar ratios. Preferred embodiments may be taken from the attached dependent claims. In an embodiment and as preferably used herein, a theragnostically active compound is a compound which is suitable for or useful in both the diagnosis and therapy of a disease.

Only for colon phenanthorline or moderate expression under physiological conditions is described. The stability constants for the binary complexes increased as the ionic radii of the metal cations decreased.

View at Google Scholar G. Guanine is a chemically inert oxypurine heteroaromatic molecule.

Bioinorganic Chemistry and Applications

The intermediate 59 was used in many examples. A method for the diagnosis of a disease in a subject, wherein the method comprises administering to the subject a diagnostically effective amount of a compound according to any one of embodiments 1 to In an embodiment and as preferably used herein, Ci-C 5 alkyl means each and individually any of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2- pentyl, 2-methyl-butyl, 3 -methyl -butyl, 3-pentyl, 3-methyl-butyl, 2-methyl-butyl and.

This includes stabilization of different oxidation states and modulation of the solvophilicity and electrophilic and nucleophilic properties of the metal ion [ 4 — 6 ]. The solutions were adjusted to an ionic strength of 0. In an embodiment and as preferably used herein, a therapeutically active compound is a compound which is suitable for or useful in the treatment of a disease. The conjugate of embodimentwherein the tumor is selected from the group comprising ductal pancreatic adenocarcinoma, small cell lung cancer, prostate cancer, colorectal cancer, breast cancer, meningioma, E wing’s sarcoma, pleural mesothelioma, head and neck cancer, non-small cell lung cancer, gastrointestinal stromal tumors, uterine leiomyoma and cutaneous T-cell lymphoma, preferably ductal pancreatic adenocarcinoma, small cell lung cancer, prostate cancer, colorectal cancer, breast cancer, meningioma, Ewing’s sarcoma, and indications subject to group A as defined herein.

The conjugate of embodiment 40, wherein the linkage is individually and independently selected from the group comprising an amide linkage, a sulfonamide linkage, a urea linkage, a thioether linkage, an ether linkage, a carbamate linkage, an amine linkage, a triazole linkage, an oxime linkage, a hydrazone linkage, a disulfide linkage, a pyrazine linkage and a dihydropyrazine linkage.

The conjugate of any one of embodiments 1 to 59, wherein one of the first targeting moiety TM1 and the second targeting moiety TM2 is selected from the group comprising an antibody, an antigen-binding antibody fragment, a camelid heavy chain IgG hcIgGa cartilaginous fish IgNAR antibody, a protein scaffold, a target-binding peptide, a peptide nucleic acid PNAa target-binding polypeptide or protein, a target binding nucleic acid molecule, a carbohydrate, a lipid and a target-binding small molecule.

In one embodiment of the conjugate of the invention a compound 2in any of its embodiments, is present in the conjugate of the invention as targeting moiety TMl.

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 5 beta lAlpha 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, A-type amino acid transporter, Avidin, Bcr-Abl tyrosine kinase, Bombesin receptor, Bombesin receptor subtype-3, CA antigen, CA In an embodiment thereof NTR is not expressed by a cell involved in said indication and more preferably not expressed by a diseased cell involved in said indication.

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It is within the present invention that a target to which the further targeting moiety of the conjugate of the invention is capable of binding, is a target that is expressed in an indication, preferably in an oncology indication, more preferably in any indication related to oncology, where NTR is expressed at a low density.

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

A composition, preferably a pharmaceutical composition, wherein the composition comprises a compound according to any one of embodiments 1 to 78 and a pharmaceutically acceptable excipient. The method of embodimentwherein the conjugate comprises a diagnostically active agent, whereby the agent is preferably a radionuclide. The rationale behind this understanding in the art is that an effective in vivo diagnosis and therapy, particular in case such diagnosis and therapy makes use of a radiolabel such as a radionuclide attached to a compound having an affinity to phenamthroline target molecule such as a receptor, requires that such compound shows good internalization properties leading to a 100 in vivo accumulation and retention of the compound and thus of the effector in the tissue and cells, respectively, expressing the target molecule.

The Royal Society of Chemistry. Reddish-brown homogeneous solution was obtained. A slight positive pressure of purified nitrogen was maintained in the titration cell in order to exclude oxygen and carbon dioxide from the reaction solutions.

Phenanthroline – Wikipedia

Because of this, the other moieties attached to the compound of formula 2 in the conjugate of the invention can vary in a broad manner as is further supported by the example part.

The conjugate of embodiment 8, wherein R 6 is selected from the group consisting of hydrogen and methyl.

The conjugate of any one of embodiments 1, 2, 3, 4, 5, 6 and 7, preferably any one of embodiments 1 and 2, wherein R3, R4 and R5 are each and independently selected from the group consisting of hydrogen and methyl under the proviso that one of R3, R4 and R5 is of the following formula 3. In a further embodiment of the conjugate of the invention an adapter moiety is one of.

Species distribution curves of the Y III ion and a Phen system as a function of —log [ ] for a solution initially containing 1.

It will be appreciated by a person skilled in the art that phenanthrokine various moieties of the conjugate of the invention are complexe to or connected with each other by a linkage.

In light of these surprising characteristics it is possible that, without wishing to be bound by any theory, because of the two targeting moieties more patients can be positively diagnosed and treated, respectively, within an indication. Depending on the characteristics of the first targeting moiety of the conjugate of the invention in.