10 PHENANTHROLINE MOETIY PDF

1,Phenanthroline forms a stable complex with Fe(II) ion called ferroin, which is used as an indicator in Fe(II) salt titrations. Ferroin is also. Structure, properties, spectra, suppliers and links for: phenanthroline, 1,Phenanthroline [ACD/Index Name] [ACD/IUPAC Name]. preferably any one of embodiments 1, 2 and 10, wherein ALK and ALK’ are both propylene, moetiy is typically an antagonist; if under such conditions the second targeting moiety is Tris(4,7-diphenyl- 1,phenanthroline)ruthenium( II).

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These types of linkage are defined by the type of atom arrangements created by the linkage. Finally, the target of the invention if conjugated to an effector provides such effector in an active form despite of the effector being linked to the conjugate.

The conjugate of embodiment 79, wherein the disease is a disease involving a target targeted by the first targeting moiety TM1 or by the scond targeting moiety TM2, preferably the disease is one involving neurotensin receptor, more preferably the disease is a disease involving neurotensin receptor 1.

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 selected from the group of target classes comprising a GPCR, an ion channel, an adhesion molecule, an immunoglobulin superfamily receptor, a receptor tyrosine kinase, a receptor tyrosine phosphatase, a member of the tumor necrosis factor receptor family, an extracellular matrix protin, a transport, a matrix metallo proteinase and CD molecules.

In a further embodiment of the conjugate of the invention the target-binding small molecule is selected from the group comprising a target-binding small molecule fulfilling the rule-of-five Lipinski, J Pharmacol Toxicol Methods,44,Lipinski et al. The conjugate of any one of embodiments 1 to 45, wherein the conjugate comprises a third adapter moiety AD3. In some embodiments, the activated carboxylic acid group is an ester with pentafluorophenol, nitrophenol, benzotriazole, azabenzotriazole, thiophenol or N-hydroxysuccinimide NHS as leaving group.

The conjugate of embodiment 68, wherein the tumor is selected from group A, wherein group A comprises Neoplasms; Neoplasm, benign; Neoplasm, uncertain whether benign or malignant; Neoplasm, malignant; Neoplasm, metastatic; Neoplasm, malignant, uncertain whether primary or metastatic; Tumor cells, benign; Tumor cells, uncertain whether benign or malignant; Tumor cells, malignant; Malignant tumor, small cell type; Malignant tumor, giant cell type; Malignant tumor, fusiform cell type; Epithelial neoplasms; Epithelial tumor, benign; Carcinoma in situ; Carcinoma; Carcinoma, metastatic.

Dermatol, The conjugate of embodiment 31, wherein the building block Z is of general formula. In an embodiment of the conjugate of the invention an adapter moiety realizing the above principles and which mediates the linkage of an amino containing moiety and a amino containing moiety forms linkages to these moieties which are independently selected from the group comprising amide, urea, thiourea, alkylamine and sulfonamide and the corresponding reactive groups as provided by the adapter moiety are independtly selected from the group of carboxylic acid, activated carboxylic acid, sulfonic acid, activated sulfonic acid, aldehyde, ketone, isocyanate and isothiocyanate.

The protein encoded by this gene belongs to the G protein-coupled receptor family that activates a phosphatidylinositol-calcium second messenger system. The preferred type of adapter moieties in one embodiment are dicarboxylic acids, or activated forms thereof.

In connection therewith it is noteworthy that the present inventors found that the conjugate of the invention surprisingly binds to a higher number of binding sites compared to an agonist of comparable binding affinity. Fagan and William A. It is within the present invention that such stability of the further targeting moiety is shown by any embodiment of such further targering moiety.

Orexin AB Antagonists: In an embodiment and as preferably used herein, Ci-C 4 alkyl means each and individually any of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl and tert-butyl. It is imperative that the compound has appropriate in vivo targeting and pharmacokinetic properties. The conjugate of any one of embodiments 1 to 62, wherein the second targeting moiety TM2 is targeting a target different from the target targeted by the first targeting moiety.

  ASTROLOGIE HORAIRE DENIS LABOUR PDF

In an embodiment of the conjugate of the invention the ion channel to which the further targeting moiety of the conjugate of the invention is capable of binding, is selected from the group comprising a voltage-gated ion channel, a ligand-gated ion channel and other ion channels.

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.

Futhermore, these and other problems are solved by the following embodiments. Apart from the central nervous system, NTR1 is highly expressed in a mammalian body and a human body in particular on several neoplastic cells in several tumor indications, whereas the expression of NTR1 in most other tissues of the mammalian and the human body is either not existent or low.

In an embodiment and as preferably used herein, the term “halogen” or “halogenide” means each and individually any of F, CI, Br, I and At. 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 heterogeneously in an indication, preferably in an oncology indication, more preferably in any indication related to oncology.

O-Phenanthroline | C12H8N2 – PubChem

In a preferred embodiment thereof, the adapter moiety forms a thioether linkage with a sulfur atom of the targeting moiety. The conjugate of any one of embodiments topreferably any one of embodiments andwherein Effector is a radioactive metal, wherein preferably the radioactive metal is chelated by Acceptor, wherein Acceptor is a chelator.

These and other problems are solved by the subject matter of the attached independent claims. For instance, the linking of a moiety comprising a primary or secondary amino with a moiety comprising a carboxylic acid leads to a linkage named amide which is also referred to as amide linkage, -CO-N- -N-CO. AA-COOH is an amino acid selected from the group consisting of 2-amino adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3. In a preferred embodiment of the conjugate of the invention R8 of the adapter moiety is – CH 2 -CH 2 -0 r -CH 2 – with r being an integer from 1, 2, 3, 4, 5, 6, 7, 8, 9 and 10, preferably r is 2.

In an embodiment of the conjugate of the invention an adapter moiety realizing the above principles and which mediates the linkage of an amino containing moiety and a carboxylic acid containing moiety forms linkages to these moieties wherein the first linkage to the amino group is selected from the group comprising amide, urea, thiourea, alkylamine and sulfonamide and the corresponding reactive group as provided by the adapter moiety is independently selected from the group of carboxylic acid, activated carboxylic acid, sulfonic acid, activated sulfonic acid, aldehyde, ketone, isocyanate and isothiocyanate.

Such linkage is typically indicated in the formulae of the conjugate of the invention such as formulae 1 or in embodiments I to VII of the conjugate of the invention or in embodiments VIII to XV of the linker moiety by. Inserted into a conjugate of the invention an adaptor moiety as preferably used in the conjugate of the invention is one which is indicated in the following formulae, whereby it is understood that to the extent the adapter moiety is represented in the formulae as being inserted between linking moiety LM and targeting moiety TM2 thus being a second adapter moiety, this is made for purpose of illustration only and the adapter moiety as such is the structure contained in square brackets.

It is understood by a person skilled in the art that several different technical and mechanistical alternatives exist to realize a specific type of linkage, for instance an amide bond. Most preferably, the linkage is a covalent bond or a coordinate bond. Biol,28, ; Garcia-Garayoa et al, J.

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Theoretically, a high affinity of the compound as such, i. If, for example, the targeting moiety is a protein, such as an pheanthroline or antibody fragment, the preferred reactive groups for forming a linkage with another moiety and an adapter moiety in particular, are sulfhydryl groups and amino groups.

Preferably the terms conjugate of the invention and compound of the invention are used interchangeably. The conjugate of any one of embodiments 1 to 72, wherein the conjugate interacts with a neurotensin receptor, wherein the neurotensin receptor is preferably selected from the group comprising neurotensin receptor 1 NTR1 and neurotensin receptor 2 NTR2.

Neurotensin is distributed throughout the central nervous system, with highest levels in the hypothalamus, amygdala and nucleus accumbens. R 1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting of 2-amino adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3. The conjugate of any one of embodiments 2 to 71, wherein the Effector is a diagnostically active nuclide or a therapeutically active nuclide, wherein the diagnostically active nuclide and the therapeutically active radionuclide is individually and independently selected from the group comprising m In, 99m Tc, 67 Ga, 52 Fe, 68 Ga, 72 As, m In, 97 Ru, Pb, 62 Cu, “Cu, 51 Cr, 52m Mn, Gd, 64 Cu, 89 Zr, and ,77 Lu, phenznthroline Re, 90 Y, 67 Cu, 68 Ga, 69 Er.

Phenanthroline

It is also involved in regulation of dopamine pathways. The conjugate of embodiment 34, wherein the branching moiety [Y] is of a structure as described in any one of embodiment 28 to 33 for building block moiety [X] a and building block moiety [Z]b. In an embodiment and as preferably used herein, a diagnostic moetij or a diagnostically active agent is a compound which is suitable for or useful in the diagnosis of a disease. Insulin-like factor 3 Relaxin 123 Serelaxin. The conjugate according to any one of embodiments 1 and 2, wherein.

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

The 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, second adapter moiety AD2 and second targeting moiety TM2.

The conjugate of any one of embodiments 27 to 30, wherein building block moiety [Z] b is linked to an adjacent moiety through a linkage, wherein the linkage is individually and independently selected from the group comprising an amide moetiiy, a urea linkage, a carbamate linkage, an ester linkage, an ether linkage, a thioether linkage and a disulfide linkage, metiy wherein the adjacent moiety is selected from the group comprising branching moiety [Y], building block moiety [X] afirst adapter moiety AD1, first targeting moiety TM1, second adapter moiety AD2 and second ometiy moiety TM2.

Additionally, phenanthrooline is thus possible to diagnose and treat, respectively, tumors expressing a target with low density, such as, for example copies of the target or less per tumor cell while said tumors express a second target with high density, such as, for example, more than copies of the second target per tumor cell.

Effector is selected from the group comprising a diagnostically active agent and a therapeutically active agent. As well-known from molecular-pharmacologic investigations efficient internalization is usually provided predominantly by agonists Bodei et ah, J.

In an embodiment and as preferably used herein, C 3 -C 8 heterocyclo refers to a C 3 – C heterocycle group defined above wherein one of the carbocycles group hydrogen atoms is replaced with a bond.