Epidermal growth factor receptor binding compounds for positron

Details Epidermal growth factor receptor binding compounds for positron Epidermal growth factor receptor binding compounds for positron

1999-06-01

2000-10-03

Berch, Mark

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

In an organic compound

544293, 382131, C07D23994, A61K 5104

Patent

active

061269174

ABSTRACT:
A radiolabeled compound of a formula: ##STR1## is described. R1 and R2 are each independently selected from the group consisting of hydrogen, alkyl, hydroxy, alkoxy, halo, haloalkyl, carboxy, carbalkoxy and salts thereof; and A, B, C and D are each independently selected from the group consisting of a hydrogen and an electron withdrawing group, provided that at least one of A, B, C and D is [18]fluorine.

REFERENCES:
patent: 5710158 (1998-01-01), Myers et al.
Lowry and Richardson, Mechanism and Theory in Organic Chemistry, 3rd Edition, Harper and Row, New York, 1987, p. 633.
Roberts and Caserio, "Basic Principles of Organic Chemistry", Wa A. Benjamin, New York, 1964, p. 800-802.
Bridges et al, "Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035, a Potent Inhibitor of the Epidermal Growth Factor Receptor", J. Med. Chem., 39: 267-276, 1996.
Johnstrom et al, "Synthesis of [methoxy-.sup.11 C]PD153035, a Selective EGF Receptor Tyrosine Kinase Inhibitor", J. Labelled Compounds and Radiopharmaceuticals, 41(7): 623-629, 1998 (abstract).
Mulholland et al, "Synthesis and Biodistribution of New C-11 and F-18 Labeled Epidermal Growth Factor Receptor Ligands", J. Nucl. Med., 36 (Suppl): 71P.

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