Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1995-11-27
1998-12-01
Tsang, Cecilia J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
530314, 530315, 530316, 530327, 568604, 568591, A61K 3809, C07K 723
Patent
active
058439030
ABSTRACT:
This invention is in the field of the chemistry of targeting anticancer anthracycline derivatives. More particularly, it concerns doxorubicin (DOX) or its daunosamine modified derivatives (DM-DOX) linked covalently to analogs of peptide hormones such as LH-RH, bombesin and somatostatin. These covalent conjugates are targeted to various tumors bearing receptors for the peptide hormone analogs. The compounds of this invention are represented by General Formula Q.sup.14 --O--R--P wherein Q has the general formula ##STR1## wherein: Q.sup.14 signifies a Q moiety with a side chain at the 14 position, R-- is H or --C(O)--(CH.sub.2).sub.n --C(O)-- and n=0-7, R' is NH.sub.2 or an aromatic, saturated or partially saturated 5 or 6 membered heterocyclic compounds having at least one ring nitrogen and optionally having a butadiene moiety bonded to adjacent carbon atoms of said ring to form a bicyclic system; P is H or a peptide moiety, suitably an LHRH, somatostatin or bombesin analogs. Nevertheless where R' is NH.sub.2 then R and P are other than H. When R and P are H, then R' is other than NH.sub.2. A novel synthetic reaction has been discovered in the course of this work to form partially saturated heterocyclic moieties from vicinal and disjunct i.e., .alpha., .beta., or .alpha., .gamma. hydroxy primary amines.
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Cai Ren-Zhi
Nagy Attila A.
Schally Andrew V.
Behr Esq. Omri M.
Gupa Anish
The Administrators of the Tulane Educational Fund
Tsang Cecilia J.
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