The Dow Chemical Company

University of Missouri

Zynaxis, Inc.

David E Troutner

Jaime Simon

David A Wilson

Wynn A Volkert

William F Goeckeler

Joseph R Garlich

Christy S John

Maroor R Pillai

Paul K Horan

Sue Ellen Slezak

Bruce D Jensen

Katharine A Muirhead

Brian D Gray

Gregory A Kopia

Chia-En Lin

Kamleshkumar A Sheth

Davis A Wilson

Zhizhou Yu

Compounds are provided having the capability of binding therapeutically active substances to lipid containing bio-compatible particles, such as cells or viruses. These compounds include a bio-affecting moiety, comprising a therapeutically active substance, which is linked via a linking moiety to at least one hydrocarbon substituent selected so that the compounds is sufficiently non-polar to impart lipid binding capability to the compound. Thus, compounds of the invention are useful for site-selective delivery of therapeutic agents, and retention thereof at the selected site. Methods are provided for using various compounds of the invention in treatment of diseases or other pathological conditions. For example, methods are provided for treatment of: (1) post-angioplasty restenosis; (2) rheumatoid arthritis; (3) tumor cell proliferation, particularly tumor cells associated with ovarian cancer; and (4) psoriasis.

Compounds, compositions and methods for binding bio-affecting substances

A group of functionalized triamine chelants and their derivatives that form complexes with radioactive metal ions are disclosed. The complexes can be covalently attached to a protein or an antibody or antibody fragment and used for therapeutic and/or diagnostic purposes. The chelants are of the formula: ##STR1## wherein n, m, R, R.sup.1, R.sup.2 and L are defined in the specification.

Triamine chelants, their derivatives, complexes and conjugates

Particle-emitting radionuclides, e.g. Gd-159, Ho-166, Lu-177 and Yb-175, have been complexed with organic aminoalkylenephosphonic acids. These complexes have been found useful in compositions for the therapeutic treatment of calcific tumors or the relief of bone pain in animals.

Organic amine phosphonic acid complexes for the treatment of calcific

A group of functionalized triamine chelants and their derivatives that form complexes with radioactive metal ions are disclosed. The complexes can be covalently attached to a protein or an antibody or antibody fragment and used for therapeutic and/or diagnostic purposes.

Triamines and their derivatives as bifunctional chelating agents

Particle-emitting radionuclides, e.g. Gd-159, Ho-166, Lu-177 and Yb-175, have been complexed with organic aminoalkylenephosphonic acids wherein the nitrogen and phosphorus are interconnected by an alkylene group or substituted alkylene group. These complexes have been found useful in compositions for the therapeutic treatment of calcific tumors in animals and in relief of bone pain.

Radio labeled organic amine phosphonic acid complexes for the treatment

Particle emitting radionuclides, e.g. X-90, have been complexed with certain macrocyclic aminophosphonic acids wherein the nitrogen and phosphorus are interconnected by an alkylene group or substituted alkylene group. These complexes have been found useful in compositions and formulations for the therapeutic treatment of calcific tumors and the relief of bone pain in animals.

Macrocyclic aminophosphonic acid complexes, their formulations and use

Particle emitting radionuclides, e.g. Samarium-153, have been complexed with certain macrocyclic aminophosphonic acids wherein the nitrogen and phosphorus are interconnected by an alkylene group or substituted alkylene group. These complexes have been found useful in compositions and formulations for the therapeutic treatment of calcific tumors in animals.

Macrocyclic aminophosphonic acid complexes for the treatment of calcific

Particle-emitting radionuclides, e.g. Samarium-153, have been complexed with organic aminoalkylenephosphonic acids wherein the nitrogen and phosphorus are interconnected by an alkylene group or substituted alkylene group. These complexes have been found useful in compositions for the therapeutic treatment of calcific tumors in animals.

Organis amine phosphonic acid complexes for the treatment of calcific

Certain particle-emitting radionuclides, e.g. Samarium-153, have been complexed with certain alkylenepolyaminocarboxylic acid chelants. Compositions containing these complexes have been found useful in the treatment of calcific tumors in animals. The stability constant, log K, of the useful complexes is from about 14 to about 17 and the molar ratio of chelant to radionuclide in the compositions is such that the chelant is present in an amount sufficient to inhibit uptake of the radionuclide by soft tissue.

Radioactive compositions for the treatment of calcific tumors

Stable neutral-lipophilic complexes of technetium-99m (Tc-99m) useful as diagnostic radionuclidic imaging agents are formed by complexing technetium-99m pertechnetate with alkylene amine oximes (viz. propylene amine oxime) in aqueous solutions under reducing conditions. The complexes have a zero charge, contain an O--H--O ring closure bond, and are sufficiently stable for parental administration in imaging by scintillation scanning. Substituents can be attached to the C.sub.2 to C.sub.4 alkylene carbon backbone of the tetradentate amine oxime ligands to structurally modify them and produce a variety of Tc-99m-radiopharmaceuticals with specific body imaging applications.

Growing community of inventors

Columbia, MO, United States of America

David E Troutner