Efficient Synthesis of CN2097 and RC7 and Their Analogs

• US 20150038671A1
• Filed: 05/30/2014
• Published: 02/05/2015
• Est. Priority Date: 05/30/2013
• Status: Abandoned Application

• Current Assignee: Rhode Island Board of education (STATE OF RHODE ISLAND)
• Original Assignee: Rhode Island Board of education (STATE OF RHODE ISLAND)
• Inventors: Parang, Keykavous, Tiwari, Rakesh
• Application Number:
  US14/292,745
• Publication Number:
  US 20150038671A1
• Time in Patent Office: Days
• US Class Current: 530/317
• CPC Class Codes: C07K 7/06 having 5 to 11 amino acids
• CPC Class Codes: C07K 7/56 the cyclisation not occurring through 2,4-diamino-butanoic acid

Abstract

Synthesized macrocyclic ligand, CN2097 and analogs, optimized with systemic structure modifications to develop the compounds with lower molecular weights and less peptidic characters.

Claims

1. A compound comprising at least one substituted macrocyle selected from the group consisting of Formulas I-III:

2. The macrocyle compound of claim 1, wherein Formulas 1 is reduced by one amino acid selected from the group consisting of Formulas IV-VI:

4. The macrocyle compound of claim 1, wherein Formulas 1 is modified selected from the group consisting of myristoylated, polyarginine-based peptides, Szeto0Schillar peptide, N-terminal pegylation, KNYKKTEV, oligocarbamate, oligocarbonate, and oligoarginine.

3. A compound comprising a substituted macrocyle of Formula VIII, wherein