摘要:
The invention provides targeting radioactive immunoreagents comprising a metal radionuclide ion, a complexing agent having structure A-I, as defined in the specification, and an immunoreactive group covalently bonded to the complexing agent. The present invention also provides novel complexing agents having the structure A-I, as defined in the specification. The targeting radioactive immunoreagents are particularly useful in therapeutic and diagnostic imaging compositions and methods.
摘要:
A compound of formula ##STR1## where the two R.sup.2 groups, taken together, represent the atoms necessary to complete a macrocyclic ring structure containing at least one heteroatom coordinating site and at least one alkylene group forming part of the ring structure; R.sup.3 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; and R.sup.4 represents hydrogen or a protein reactive group, provided that at least one of the R.sup.4 groups is a protein reactive group, and salts, complexes and protein conjugates thereof.
摘要翻译:其中两个R 2基团一起表示完成含有至少一个杂原子配位位点和至少一个形成环结构部分的亚烷基的大环环结构所必需的原子的化合物 R 3表示氢,烷基,烷氧基,烷硫基,烷基氨基,烷基酰氨基,芳基,芳氧基,杂环基或蛋白质反应性基团; 并且R 4表示氢或蛋白质反应性基团,条件是至少一个R 4基团是蛋白质反应性基团,以及其盐,复合物和蛋白质缀合物。
摘要:
Tripyridyl macrocyclic compounds that are employed in the production of a complexing agent for use in targeting radioactive immunoreagents with the following formula are disclosed: ##STR1## wherein R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group;the two R.sup.2 groups, taken together, represent a bridging group serving to complete a macrocyclic ring, the bridging group containing at least one heteroatom and at least one alkylene group which form part of the resulting macrocyclic ring;R.sup.3 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl, or a protein reactive group;R.sup.5 represents alkyl or alkoxy; andR.sup.6 represents a protein reactive group.
摘要:
Novel chromogenic derivatives of 1,2-bis-(o-aminoaryloxy)ethane-N,N,N',N'-tetraacetic acid are useful for the determination of calcium ions in both solution and dry assays. These compounds comprise a dye moiety which is directly conjugated to the acetic acid substituted-nitrogen atom and which enables the compounds to exhibit maximum absorbance at a wavelength generally greater than 400 nm before complexation. When the compounds are complexed with calcium ions, the absorbance shifts to a shorter wavelength.
摘要:
This invention provides therapeutic and diagnostic imaging compositions and methods featuring a polymer comprising units containing a poly(alkylene oxide) moiety linked to the residue of a chelating agent, said polymer having a cytotoxic agent associated therewith.
摘要:
This invention provides compositions useful in MR imaging comprising a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, the polymer having a paramagetic metal ion associated therewith.
摘要:
A composition suitable for use in diagnostic imaging or as a cell killing agent comprising a chelating residue linked via an amide linkage to a poly(alkylene oxide) moiety, said composition having a molecular weight of at least 4,500; ##STR1## wherein: Z is a chelating residue; Q is a divalent poly(alkylene oxidylene) moiety having a carbon terminus at R and at L; L represents an amide linkage; E.sup.(b) is one or more counterions each having a charge of b; b is an integer from 1, 2 and 3; n is an integer selected from the group 1, 2, 3 and 4; w is zero or an integer from 1 to 5; M.sup.(+a) is a cation, having a charge of +a; a is an integer from 1 to 4; r is 0 or an integer from 1 to 3, provided that when r is 2-3, each M.sup.(+a) can be the same or different cation; d is the total charge on the chelating residue and is an integer from 0 to 10; d+.SIGMA.(b.multidot.w)+.SIGMA.(a.multidot.r)=O; and R is a capping moiety chosen from the group consisting of hydrogen, hydroxyl, C.sub.1 -C.sub.4 alkyl, aryl containing 6 to 24 carbon atoms, C.sub.2 -C.sub.5 alkanoyloxyl and C.sub.1 -C.sub.4 alkoxy, or R is an immunoreactive group or cytotoxic drug linked to Q by a chemical bond or a linking group.
摘要:
A composition suitable for use in diagnostic imaging or as a cell killing agent comprising a chelating residue linked via an amide linkage to a poly(alkylene oxide) moiety, said compisition having a molecular weight of at least 4,500; ##STR1## wherein: Z is a chelating residue;Q is a divalent poly(alkylene oxidylene) moiety having a carbon terminus at R and at L;L represents an amide linkage;E.sup.(b) is one or more counterions each having a charge of b;b is an integer from 1, 2 and 3;n is an integer selected from the group 1, 2, 3 and 4;w is zero or an integer from 1 to 5;M.sup.(+a) is a cation, having a charge of +a;a is an integer from 1 to 4;r is 0 or an integer from 1 to 3, provided that when r is 2-3, each M.sup.(+a) can be the same or different cation;d is the total charge on the chelating residue and is an integer from 0 to 10;d+.SIGMA.(b.multidot.w)+.SIGMA.(a.multidot.r)=O; andR is a capping moiety chosen from the group consisting of hydrogen, hydroxyl, C.sub.1 -C.sub.4 alkyl, aryl containing 6 to 24 carbon atoms, C.sub.2 -C.sub.5 alkanoyloxyl and C.sub.1 -C.sub.4 alkoxy, or R is an immunoreactive group or cytotoxic drug linked to Q by a chemical bond or a linking group.
摘要:
This invention provides compositions useful in MR imaging comprising a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, the polymer having a paramagetic metal ion associated therewith.