Abstract: The synthesis of tamoxifen derivatives, most particularly halo, halo alkyl, hydroxy, and amino tamoxifen derivatives is disclosed. The native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule. Particular tamoxifen derivatives of the invention include chloro, bromo, iodo, fluoro, amino and DTPA tamoxifen derivatives, and corresponding lower alkyl halogenated forms. The halogenated tamoxifen derivatives possess superior binding affinities for estrogen receptor rich tissues, such as uterine tissue and breast tissue, relative to unsubstituted native tamoxifen. Radiolabeled forms of the tamoxifen derivatives may be used as highly specific imaging agents for estrogen receptor rich tissues. The fluoro and bromo tamoxifen derivatives are particularly useful for imaging estrogen receptors by PET whereas the iodinated tamoxifens are particularly useful in imaging estrogen receptors by SPECT.

Abstract: Compounds of general Formula I ##STR1## wherein Z.sup.1 and Z.sup.2 in each case independently mean the residue--(CH.sub.2).sub.m --(C.sub.6 H.sub.4).sub.q --(O).sub.k --(CH.sub.2).sub.n --(C.sub.6 H.sub.4).sub.l --(O).sub.r --R,whereinm and n means the numbers 0-20,k, l, q and r means the numbers 0 and 1, andR means a hydrogen atom, an optionally OR.sup.1 -substituted C.sub.1 -C.sub.6 -alkyl residue, or a CH.sub.2 COOR.sup.1 group with R.sup.1 meaning it hydrogen atom, a C.sub.1 -C.sub.6 -alkyl residue, or a benzyl group,X means a hydrogen atom and/or a metal ion equivalent of an element of atomic number 21-29, 42, 44 or 57-83,with the provisos that at least two the substituents X stand for a metal ion equivalent; that one of the substituents Z.sup.1 and Z.sup.2 stands for a hydrogen and the other is not H; that--if n and l each mean the number 0--k and r do not simultaneously mean the number 1; that --(O).sub.r --R is not --OH; and that Z.sup.1 and Z.sup.2 are not --CH.sub.2 --C.sub.6 H.sub.4 --O--CH.sub.

Abstract: A biocompatible graft co-polymer adduct including a polymeric carrier, a protective chain linked to the polymeric carrier, a reporter group linked to the carrier or to the carrier and the protective chain, and a reversibly linked Pt(II) compound. The invention also relates to a method of treating a disease in a patient, particularly cancer, by administering to the patient a therapeutically effective amount of the adduct, and may include scanning the patient using an imaging technique which can provide a visible image of the distribution of the adduct.

Abstract: A compound is provided of formula I: ##STR1## wherein n is 4-16, Det is an organic group comprising a radioisotope or capable of chelating a radioisotope, and Z.sup.- is one equivalent of a biologically acceptable anion, which compounds are useful to radiolabel cellular membranes, as of hematopoietic cells.

Abstract: A metalorganic complex of the formula:MA.sub.y Xwherein:M is a y-valent metal;A is a monodentate or multidentate organic ligand coordinated to M which allows complexing of MA.sub.y with X;y is an integer having a value of 2, 3 or 4; each of the A ligands may be the same or different; andX is a monodentate or multidentate ligand coordinated to M and containing one or more atoms independently selected from the group consisting of atoms of the elements C, N, H, S, O and F.The metal M may be selected from the group consisting of Cu, Ba, Sr, La, Nd, Ce, Pr, Sm, Eu, Th, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Bi, Tl, Y, Pb, Ni, Pd, Pt, Al, Ga, In, Ag, Au, Co, Rh, Ir, Fe, Ru, Sn, Li, Na, K, Rb, Cs, Ca, Mg, Ti, Zr, Hf, V, Nb, Ta, Cr, Mo, and W. A may be selected from the group consisting of .beta.-diketonates and their sulfur and nitrogen analogs, .beta.-ketoesters and their sulfur and nitrogen analogs, cyclopentadienyls, alkyls, perfluoroalkyls, alkoxides, perfluoroalkoxides, and Schiff bases.

Abstract: A physiologically acceptable, radiolabelled compound of general formula (I) consisting of a compound of the ##STR1## where k is an integer from 2 to 5l is an integer from 1 to 5X and Y are independently selected from phenyl, naphthyl, pyridine or quinoline radical, each having at position 2 one of --OH, --SH, --NH.sub.2 or --COOH and each of X and Y can be optionally substituted by one or more amino, halogen, hydroxy, mercapto, nitro, cyano, thiocyano, alkyl, alkoxy, halogenoalkyl, acyl, acylamino, acyloxy, carboxyl, alkoxycarbonyl, carbamoyl, pyridoylamino, N-carboxyalkyl-carbamoyl, sulpho, sulphamoyl, mono- or dialkylated or phenylated sulphamoyl which can also carry one or more substituents R', alkylsulphonyl, alkoxysulphonyl, or by an optionally hydroxy-containing phenylsulphonyl or phenoxysulphonyl; where R' is as defined for X and Y; or pharmaceutically acceptable salts thereof.

Abstract: Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comnprisinga metal, preferably radionuclide of rhenium or technetium;a hypoxia-localizing moiety; and,a complexing ligand, wherein said ligand and said radionuclide combined have cell membrane permeabilities greater than that of sucrose, are disclosed.

Abstract: The invention provides polymeric polychelants containing polymer repeat units of formula ?L--Ch--L--B! (where Ch is a polydentate chelant moiety; L is an amide or ester linkage; B is a hydrophobic group providing a carbon chain of at least 4 carbon atoms between the L linkages it interconnects) or a salt or chelate thereof, with the proviso that where Ch is 2,5-biscarboxymethyl-2,5-diazahex-1,6-diyl, the polychelant is metallated with lanthanide or manganese ions or B provides a carbon chain of at least 10 carbon atoms between the L linkages it interconnects and their salts and chelates. The paramagnetic polychelates of the polychelants of the invention have remarkably high R.sub.1 relaxivities.

Abstract: The invention relates to a method of detecting a site of infection or inflammation, and a method for treating such infection or inflammation, in an individual by administering to the individual a diagnostically or therapeutically effective amount of detectably labeled, therapeutic, or therapeutically-conjugated, chemotactic peptide that accumulates substantially at the infected or inflamed site, said chemotactic peptide having the general structureX--Y--Leu--Phe--?Z!.sub.n --Wwherein:X is an amino protecting group,Y is an amino acid residue,Z is a spacer sequence,n is 0 or 1, andW is a labeling or attachment substituent.

Abstract: The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein "azavesamicols" in which the cyclohexyl group of vesamicol is replaced with a heterocycle of similar size, the piperidyl ring. The compounds bind to the vesamicol receptor, a cytoplasmically-oriented site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.

Abstract: Radiopharmaceutical formulations for complexes comprising at least one radionuclide complexed with a ligand, or its physiologically-acceptable salts thereof, especially .sup.153 samarium-ethylenediaminetetramethylenephosphonic acid, which optionally contains a divalent metal ion, e.g. calcium, and is frozen, thawed, and then administered by injection.

Abstract: A metal chelate comprising a compound having the following formula and one or more metal ions which metal ions are a radionucleotide or a paramagnetic metal ion: ##STR1##

Abstract: The present disclosure details the preparation of hydroxamic-acid based bifunctional chelators and their use in conjugating metal ions to proteins and nucleic acids for tumor or tissue imaging or therapy purposes. Some preferred aspects of the disclosure involve the preparation of trisuccin, chemical name N-?tris(2-N- benzyloxyaminocarbonylethyl)! methylsuccinamic acid, which is a hydroxamic acid/succinate based structure that is particularly useful for binding radionuclides such as .sup.99m Tc, .sup.186 Re and .sup.67 Cu.

Abstract: The present invention is directed to a method of labeling a protein conjugate with a radionuclide to form a radioconjugate comprising reacting:(a) the radionuclide; and(b) the protein conjugate in an acetate buffer for a time period and under conditions sufficient to form said radioconjugate.Preferably, the protein conjugate is comprised of a complexing agent moiety and a free epsilon amino group-containing protein moiety. The completing agent moiety is preferably a terpyridine analog. The terpyridine analog is preferably TMT.Preferably, the free epsilon amino group-containing protein moiety is an immunoreactive protein. The immunoreactive protein is preferably the monoclonal antibody ING-1.In a preferred embodiment, the protein conjugate is TMT-ING-1, and the radionuclide is .sup.90 Y.In a further preferred embodiment, the radioconjugate is chelated to greater than 98 percent of the radionuclide.

Abstract: Compounds such as 4-(s'-methoxy)phenyl-?2'-N-2"-pyridinyl)-p-iodobenzamido! ethylpiperazine have affinity and specificity for serotonin 5-HT.sub.1A receptors.

Abstract: The invention relates to polyhydric phenol compounds of the general formula ##STR1## wherein R is a hydrogen atom or a saccharide moiety;A and B are hydrogen atoms or form together a C--C bond;R.sub.1 is a hydroxy group and R.sub.2 is a hydrogen atom, orR.sub.1 and R.sub.2 form together an oxygen atom;Z is a hydroxy group, an amino group, a carboxy group or a N-(carboxymethyl)carbamoyl group;X* is a radioactive halogen isotope; andm and n are 0 or 1, with the proviso, that m is 1 if n is 0, and that m is 0 if n is 1.The radiolabelled phenol compounds can be used for diagnosis and therapy.

Abstract: Bicyclopolyazamacrocyclophosphonic acid compounds are disclosed which may form inert complexes with Gd, Mn or Fe ions. The overall charge of the complex can be varied to alter the in vivo biolocalization. Such complexes can be covalently attached to an antibody, antibody fragment or other biologically active molecule to form conjugates. The complexes and conjugates are useful as contrast agents for diagnostic purposes.

Abstract: A group of functionalized polyaminocarboxamide modified chelators, such as 1,4 7,10-tetraaza-1-N-(1-carboxy-3-(4-aminophenyl)propyl)-7-N-(1-carboxymethyl )bis-4,10-N,N-(carboxamidomethyl)cyclododecane and 1,4 7,10-tetraaza-1-N-(1-carboxy-3-(4-aminophenyl)propyl)bis-4,7-N,N-(1-carbox ymethyl)-10-N-(carboxamidomethyl)cyclododecane are disclosed. These modified chelators are capable of forming complexes with rare earth-type metal ions. When the complexes are covalently attached to an antibody or antibody fragment, they can be used in therapeutic and diagnostic applications.

Abstract: Novel compounds useful as intermediates in the synthesis of compounds having high affinity for specific cocaine receptors in the brain have the formula ##STR1## wherein R is (CH.sub.2).sub.n CH.sub.2 Y, and wherein Y is H or F, X is a pharmaceutically acceptable anion, andwherein Sn (R.sup.1, R.sup.2, R.sup.3) is ortho, meta or para and wherein R.sup.1, R.sup.2, R.sup.3 are independently alkyl of 1-6 carbon atoms and n is an integer of 0-5.

Abstract: The preparation and use of organometallic complexes of Group III metals having the formula:Me(Ar)(AlX.sub.3 R).sub.3 (I)wherein Me, Ar, X and R are as defined herein, to stereospecifically polymerize unsaturated monomers is provided.