Alvin D Joran

US Patent:

52684237, Dec 7, 1993

Filed:

Feb 28, 1992

Appl. No.:

7/843115

Inventors:

Alvin D. Joran - New York NY

Assignee:

New York University - New York NY

International Classification:

C08F28300
C08G 1400
C08G 1600
C08L 6100

US Classification:

525 5411

Abstract:

A solid phase resin useful as a support for peptide synthesis is synthesized stepwise from a solid phase polymer by reacting a solid phase phenyl ether resin with an alkoxy benzoyl halide to form a solid phase having (alkoxybenzoyl)phenoxymethyl groups bound thereto. The hydroxy group of the benzoyl moiety may be converted to a free amine by reacting with an ammonium salt of a carboxylic acid and then hydrolyzing with alkali. Novel resins produced by this method include those in which the solid phase phenyl ether resin is a resin having alkyl phenyl moieties linked to alkoxy phenyl groups by an ether linkage.

US Patent:

53648510, Nov 15, 1994

Filed:

Jun 14, 1991

Appl. No.:

7/714167

Inventors:

Alvin D. Joran - New York NY

Assignee:

International Synthecon, LLC - New York NY

International Classification:

C07K 100
C25B 300

US Classification:

530345

Abstract:

Electrochemical methods, preferably the Kolbe coupling reaction, are utilized to create intramolecularly bridged peptides, segments or peptide isosteres which are conformationally restricted and preferably, biologically active. Preferably, the peptide analogues contain methylene groups bridging particular amino acid side chains. Analogues of a variety of peptide hormones, including insulin, insulin-like growth factors, somatostatin, melanocyte stimulating hormone, and the like are prepared by the above methods. Such peptides are useful as agonists or antagonists for treatment of diseases associated with deficiency of the hormone or dysregulation of hormone activity, as well as for mechanistic studies to understand the interactions between peptide hormones and cells.