Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, SPECT and PET imaging

Mease, R C; Mausner, L F; Srivastava, S C

Title: Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, SPECT and PET imaging

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Abstract

A simple method for the synthesis of 1,4,7, 10-tetraazacyclododecane N,N{prime}N{double_prime},N{prime}{double_prime}-tetraacetic acid and 1,4,8,11-tetraazacyclotetradecane N,N{prime},N{double_prime},N{prime}{double_prime}-tetraacetic acid involves cyanomethylating 1,4,7,10-tetraazacyclododecane or 1,4,8,11-tetraazacyclotetradecane to form a tetranitrile and hydrolyzing the tetranitrile. These macrocyclic compounds are functionalized through one of the carboxylates and then conjugated to various biological molecules including monoclonal antibodies. The resulting conjugated molecules are labeled with radiometals for SPECT and PET imaging and for radiotherapy. 4 figs.

Inventors:: Mease, R C; Mausner, L F; Srivastava, S C

Issue Date:: 1997-06-17

Research Org.:: Associated Universities Inc

Sponsoring Org.:: USDOE, Washington, DC (United States); National Insts. of Health, Bethesda, MD (United States)

OSTI Identifier:: 512425

Patent Number(s):: 5639879

Application Number:: PAN: 8-382,522; CNN: Grant CA-51958; TRN: 97:013495

Assignee:: Associated Universities, Inc., Washington, DC (United States)

DOE Contract Number:: AC02-76CH00016

Resource Type:: Patent

Resource Relation:: Other Information: PBD: 17 Jun 1997

Country of Publication:: United States

Language:: English

Subject:: 55 BIOLOGY AND MEDICINE, BASIC STUDIES; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; DIAGNOSTIC USES; THERAPEUTIC USES; POSITRON COMPUTED TOMOGRAPHY; SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY; RADIOIMMUNOTHERAPY

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                    Mease, R C, Mausner, L F, and Srivastava, S C. Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, SPECT and PET imaging.  United States: N. p., 1997. 
        Web.

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                    Mease, R C, Mausner, L F, & Srivastava, S C. Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, SPECT and PET imaging.  United States.

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                    Mease, R C, Mausner, L F, and Srivastava, S C. Tue .  
        "Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, SPECT and PET imaging".  United States.

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@article{osti_512425,

  title        = {Macrocyclic polyaminocarboxylates for stable radiometal antibody conjugates for therapy, SPECT and PET imaging},

  author       = {Mease, R C and Mausner, L F and Srivastava, S C},

  abstractNote = {A simple method for the synthesis of 1,4,7, 10-tetraazacyclododecane N,N{prime}N{double_prime},N{prime}{double_prime}-tetraacetic acid and 1,4,8,11-tetraazacyclotetradecane N,N{prime},N{double_prime},N{prime}{double_prime}-tetraacetic acid involves cyanomethylating 1,4,7,10-tetraazacyclododecane or 1,4,8,11-tetraazacyclotetradecane to form a tetranitrile and hydrolyzing the tetranitrile. These macrocyclic compounds are functionalized through one of the carboxylates and then conjugated to various biological molecules including monoclonal antibodies. The resulting conjugated molecules are labeled with radiometals for SPECT and PET imaging and for radiotherapy. 4 figs.},

  doi          = {},

  journal      = {},
number       = ,

  volume       = ,

  place        = {United States},

  year         = {1997},

  month        = {6}

}

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