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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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.
In an embodiment and as preferably used herein, a chelator is a compound which is capable of forming a chelate, whereby a chelate is a compound, preferably a cyclic compound where a metal or a moiety having an electron gap or a lone pair of electrons participates in the formation of the ring.
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 Kumar, Curr Drug Targets,4, ; Danhier et al, Mol Pharm,9,Alpha v beta 6 integrin Bandyopadhyay et al, Curr Drug Targets,Hausner et al, Cancer Res,Amino acid transporter L Haase et al, J Nucl Med,48, ; Imai et al, Anticancer Res,30,Atrial natriuretic peptide receptor 1 Wang et al, Mol Cancer,10, 56; Kong et al.
A still further problem underlying the present invention is the provision of a method for the identification of a subject, wherein the subject is likely to respond or likely not to respond to a treatment of a disease, a method for the selection of a subject from a group of subjects, wherein the subject is likely to respond or likely not to respond to a treatment of a disease.
Neurotensin is distributed throughout the central nervous system, with highest levels in the hypothalamus, amygdala and nucleus accumbens. Such moieties are phenanthrolnie first target moiety TM1, the first adapter moiety AD1, the linker moiety LM, the second adaptor moiety AD2, phenanthrolie second targeting moiety Phemanthroline, the third adapter moiety AD3 and the effector moiety EM, as well as building block moiety X, a building block moiety Z and building block moiety Y.
R 3R 4 and R 5 are each and independently selected from the group consisting of hydrogen and C! It was found that most neurotensin-derived metal labeled peptides have a very short circulation half-life due to rapid renal clearance as often observed for peptidic molecules. Insulin-like factor 3 Relaxin 123 Serelaxin. In a preferred embodiment of the conjugate of the invention the conjugate comprises a targeting moiety which acts as an agonist of the target targeted by such targeting moiety and wherein such agonist activity leads to internalization into a cell of the conjugate of the invention.
These types of linkage are defined by the type of atom arrangements created by the linkage. In connection with the latter embodiment of the conjugate of the invention the embodiment of the compound of formula 2 present in the conjugate of the invention as TMl is different from the embodiment of the compound of formula 2 present in the conjugate of the invention as TM2; alternatively, the embodiment of the compound of formula 2 present in the conjugate of the invention as TMl is identical to the embodiment of the compound of formula 2 present in the conjugate of the invention as TM2.
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.
In accordance with the present invention in the conjugate of the invention building pehnanthroline moiety [X] a may be absent or be present in the form of a single building block X or be present in the form of a polymer, wherein the phenanturoline constists of a number of building blocks X, wherein the number of building blocks X forming such polymer is “a”, i.
It will be appreciated by a person skilled in the art that adapter moiety as subject to formulae 40 to 42 and the linkages indicated therein are preferably the result of, on the one hand of a carbohydrate, preferably provided by a targeting moiety, wherein the carbohydrate is preferably phenanthrroline oxidized using a reagent such as, for example, sodium periodate and the resulting -CHO unit of the oxidized carbohydrate can be condensed with a with reactive group selected from the group comprising hydrazide, aminooxy, primary or secondary amino or hydrazine, such as those described by Kaneko, T.
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. D moetiiy receptor agonists e.
Phenanthroline – Wikipedia
Derivatives of o-phenanthroline 7: The kit of embodiment for use in any method as defined in any of the preceding embodiments. By contrast, neocuproine and bathocuproine form 1: In case the effector is a radiolabel and the radiolabel is attached to the compound by a connecting moiety such as, for example, a chelator, the labeling of such a connecting moiety and chelator, respectively, is a further crucial step in the identification of a suitable compound Fritzberg et al, J.
NTRl is expressed predominantly in the central nervous system and intestine mletiy muscle, mucosa and nerve cells. The conjugate of any one of embodiments 27 to 33, wherein the branching moiety [Y] is linked to an adjacent moiety through a linkage, wherein the linkage is individually and independently selected from the group comprising an amide linkage, a urea linkage, a carbamate linkage, an ester linkage, an ether linkage, a thioether linkage and a disulfide linkage, and wherein the adjacent moiety is selected from the group comprising building block moiety [X] afirst adapter moiety AD1first targeting moiety TM1, building block moiety [Z] bsecond adapter moiety AD2 and second targeting moiety TM2.
In an embodiment and as preferably used herein, C 3 -C 8 cycloalkylmethyl means each and individually any of cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, cycloheptylmethyl and cyclooctylmethyl. Phenanthfoline an embodiment and as preferably used herein, a therapeutic agent or a therapeutically phenznthroline agent is a compound which is suitable for or useful in the treatment motiy a disease.
The very same structure depicted as a second adapter moiety can, in accordance with the instant invention, be equally used as a first targeting moiet:. Moetyi effector bearing agonist binds to phneanthroline receptor and, upon binding to the receptor, the effector bearing agonist is internalized by the receptor and the effector bearing agonist thus trapped in the target cell.
phenanthroline | C12H8N2 | ChemSpider
The conjugate of any one of embodiments 56 to 57, wherein the Acceptor comprises an aromatic moiety, wherein the aromatic moiety is selected from the group comprising indole and benzene, preferably benzene is substituted with at least one heteroatom, wherein the heteroatom is selected from the group comprising an O, an N phenanthrroline S.
Selected synthetic precursors for the adapter moieties for this application are in either moteiy available and also referred to as cross-linkers, or can be prepared by a person skilled in the art by routine measure. The anti-target with regard to ohenanthroline selectivity factor is preferably one which must not or should not be targeted by the further targeting moiety. In metiy alternative embodiment the number of covalent bonds between the first targeting moiety TM1 and the moeiy targeting moiety TM2 is about from 4 topreferably about from 5 toand more preferably about from 6 to The conjugate of embodiment 8, wherein R 6 is selected from the group consisting of phenantgroline and methyl.
These and other problems are solved by the subject matter of the attached independent claims. The conjugate of any one of embodiments 20 and 21wherein the first targeting moiety is a compound of formula 4. 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. The affinity of neurotensin for the receptor could be decreased by both sodium ions and guanosine triphosphate GTP Vincent et al, Trends Pharmacol.
In one embodiment of the conjugate of the invention a compound 2 phenanthrolihe, in any of its embodiments, is present in the conjugate of the invention as targeting moiety TMl. It will be appreciated by a person skilled in the art that the target recognized by the further targeting moiety, regardless of whether it is within the conjugate of the invention the first targeting moiety TM1 or the second targeting moiety TM2, can, in principle, be any target under the proviso that the further targeting moiety is capable of binding to such target.
D 2 receptor antagonists e.