Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-11-26
2000-02-15
Ghah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540145, 604 5, 534 13, 534 14, 534 15, 534 16, A61K 3166, A61K 3900, C07D48722
Patent
active
060253517
ABSTRACT:
Families of Diels Alder adducts and of metal complexes of Diels Alder adducts, which are useful as particularly active compounds for use in photodynamic therapy, are disclosed. The Diels Alder adducts and a preferred family of metal complexes have the structures of Formulas 3 and 4, below: ##STR1## where R1, R2, R3 and R4 can be the same or different, and each is methyl, ethyl, an amino acid moiety which is a part of an amide produced by reaction between an amine function of a naturally occurring amino acid and a carbonyl function of the adduct, or a monoclonal antibody moiety which is attached to the adduct moiety through a carbonyl which is a part of an amide produced by reaction between an amine function of a monoclonal antibody and a CO.sub.2 R', CH.sub.2 CO.sub.2 R' or CH.sub.2 CH.sub.2 CO.sub.2 R'group of the adduct, and wherein the moiety is of a monoclonal antibody which selectively binds to malignant tumors, R5, R6 and R7 can be the same or different, and each is ethyl, an amino acid moiety which is a part of an amide produced by reaction between an amine function of a naturally occurring amino acid and a carbonyl function of the adduct, or a monoclonal antibody moiety which is attached to the adduct moiety through a carbonyl which is a part of an amide produced by reaction between an amine function of a monoclonal antibody and a CO.sub.2 R', CH.sub.2 CO.sub.2 R' or CH.sub.2 CH.sub.2 CO.sub.2 R'group of the adduct, and wherein the moiety is of a monoclonal antibody which selectively binds to malignant tumors, M comprises 2H or a metal cation, e.g., Sn or Zn, that is complexed with two of the nitrogens of the adduct, and R8 is an alkyl group other than t-butyl having from one to four carbon atoms. The use of the adducts and complexes in PHD is also disclosed.
REFERENCES:
patent: 4878891 (1989-11-01), Judy et al.
Morgan et al; J. Med. Chem; 1990, 33 pp. 1258-1262.
Morgan Alan R.
Selman Steven H.
Ghah Mukund J.
Medical College of Ohio
Purdue David C.
Purdue John C.
Sripada Pavanaram K
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