Transcobalamin receptor binding conjugates useful for treating abnormal cellular proliferation

• US 7,531,162 B2
• Filed: 02/13/2006
• Issued: 05/12/2009
• Est. Priority Date: 10/25/2000
• Status: Expired due to Fees

• Current Assignee: Regents of The University of Minnesota (University of Minnesota)
• Original Assignee: Mayo Foundation For Medical Education And Research (Mayo Clinic), Regents of The University of Minnesota (University of Minnesota)
• Inventors: Hogenkamp, Henricus P. C., Collins, Douglas A.
• Primary Examiner(s): McIntosh, III; Traviss C
• Application Number:
  US11/353,810
• Publication Number:
  US 20060166862A1
• Time in Patent Office: 1,184 Days
• Field of Search: None
• US Class Current: 424/1.73
• CPC Class Codes: A61K 47/551 one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07H 23/00 Compounds containing boron, silicon, or a metal, e.g. chelates, vitamin B12 esters with inorganic acids C07H11/00; metal salts, see parent compounds

Abstract

An agent, composition and method for the treatment, prophylaxis and/or diagnosis of proliferative disorders, which is highly and efficiently absorbed at the site of abnormal cellular proliferation is disclosed.

Claims

1. A compound of the formula (I):

6. A pharmaceutical composition for the diagnosis of a proliferative disorder in a host comprising a compound of claim 1, 2, 3, and 4, or the pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier.

7. A pharmaceutical composition for the diagnosis of a proliferative disorder in a host comprising a compound of claim 1, 2, 3, and 4, or the pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, in combination with one or more other diagnostic agent(s).

8. The pharmaceutical composition of claim 6, wherein the host is a human.

9. The pharmaceutical composition of claim 7, wherein the host is a human.

2. A compound of the formula (I):

5. The compound of claim 2 or 4, wherein —

NR′

(alkylene-NR′

)_nalkyleneNR′

is selected from the group consisting of—

NR′

(CH₂)₃NR′

(CH₂)₄NR′

(CH₂)₃NR′

R′

;

—

NR′

(CH₂)₃NR′

(CH₂)₄NR′

R′

;

decamethylene tetraamine and pentamethylene hexamine.

3. A compound of the formula (I):

4. A compound of the formula (I):