Active agent delivery systems and methods for protecting and administering active agents

• US 7,427,600 B2
• Filed: 08/23/2004
• Issued: 09/23/2008
• Est. Priority Date: 08/22/2000
• Status: Expired due to Term

• Current Assignee: Takeda Pharmaceutical Company Limited
• Original Assignee: Shire LLC (Shire plc)
• Inventors: Piccariello, Thomas, Krishnan, Suma, Mickle, Travis, Moncrief, James Scott, Lauderback, Christopher, Kirk, Randal
• Primary Examiner(s): Russel; Jeffrey E
• Application Number:
  US10/923,088
• Publication Number:
  US 20070232529A1
• Time in Patent Office: 1,492 Days
• Field of Search: None
• US Class Current: 514/1.1
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 47/55 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• CPC Class Codes: A61K 47/62 the modifying agent being a protein, peptide or polyamino acid
• CPC Class Codes: A61K 47/64 Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent peptidic linkers A61K47/65

Abstract

The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

Claims

1. A method of treating inflammatory bowel disease comprising administering to a patient in need thereof an effective amount of a compound consisting of mesalamine covalently attached to a single amino acid selected from Valine, Alanine, Asparagine, Isoleucine, Proline, Lysine, Cysteine, Glutamine, Histidine, Methionine, Phenylalanine, Serine, Threonine, Tryptophan and Tyrosine or a pharmaceutically acceptable salt thereof.

7. The method of claim 1, wherein the compound is mesalamine covalently attached to Valine.

2. A compound consisting of mesalamine covalently attached to a single amino acid wherein said single amino acid is selected from Valine, Alanine, Asparagine, Isoleucine, Proline, Lysine, Cysteine, Glutamine, Histidine, Methionine, Phenylalanine, Serine, Threonine, Tryptophan and Tyrosine or a pharmaceutically acceptable salt thereof.

3. The compound of claim 2, wherein the amino acid is Valine.

4. A pharmaceutical composition comprising:

a compound consisting of mesalamine covalently attached to a single amino acid selected from Valine, Alanine, Asparagine, Isoleucine, Proline, Lysine, Cysteine, Glutamine, Histidine, Methionine, Phenylalanine, Serine, Threonine, Tryptophan and Tyrosine or a pharmaceutically acceptable salt thereof; and

a pharmaceutically acceptable excipient.

5. The pharmaceutical composition of claim 4, wherein said composition is an oral dosage form.

6. The pharmaceutical composition of claim 4, wherein the compound is mesalamine covalently attached to Valine.