The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 16, 2003

Filed:

Jul. 21, 1994
Applicant:
Inventors:

Raghavan Rajagopalan, Maryland Heights, MO (US);

Ananthachari Srinivasan, St. Charles, MO (US);

Leon R. Lyle, Webster Groves, MO (US);

Assignee:

Biosynthema, Inc., St. Louis, MO (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07K 1/600 ;
U.S. Cl.
CPC ...
C07K 1/600 ;
Abstract

Stable analogs of cyclic peptides containing disulfide linkages are disclosed. The disulfide linkage is modified by one of four methods: (a) sulfide contraction, (b) isosteric substitution, (c) thioketal expansion, or (d) alkylation expansion. In sulfide contraction the disulfide bond (—S—S—) is replaced with a monosulfide bond (—S—) in which a bifunctional effector molecule, such as a ligand or chemotoxic agent, is bound to the new peptide linkage. In isosteric substitution, one sulfur atom is replaced with a carbon atom and at least one of the carbon atoms at the modified site is a bifunctional effector molecule. In thioketal expansion, an alkylidene unit (—CR C —) is inserted between the two sulfur atoms. In alkylation expansion, an alkyl moiety of from C to C , is inserted between the two sulfur atoms.


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