IP Library › Granted Patent US 7,385,042
Granted Patent B2
US 7,385,042 · App. 11/486,338 · Granted Jun 10, 2008

Therapeutic and diagnostic compounds, compositions, and methods

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Quick Facts
Patent No.
US 7,385,042
App. No.
11/486,338
Granted
Jun 10, 2008
Kind
B2
Abstract

One embodiment provides a composition comprising a) a compound of formula I: wherein R 1 , X and n have any of the values described in the specification, or a pharmaceutically acceptable salt thereof; b) a radionuclide; and c) a radioprotectant.

Claims (24)

1. A composition comprising:

a) a compound of formula (I):

wherein:

each R 1 is independently hydrogen or (C 1 -C 4 )alkyl, optionally substituted with carboxy;

each X is independently (CH 2 ) n or

and each n is independently 2, 3, or 4;

wherein the compound of formula I is substituted on one or more carbons other than a carbon of R 1 with one or more groups —Y(PO 3 H 2 ) m ; wherein Y is a linker group; and m is 1, 2, 3, 4, 5, or 6; or a pharmaceutically acceptable salt thereof;

b) a detectable or therapeutic radionuclide; and

c) a radioprotectant.

2. The composition of claim 1 , which comprises a detectable radionuclide.

3. The composition of claim 2 , wherein the detectable radionuclide is Technetium-99m, Ruthenium-97, Indium-111, Gallium-67 or -68 or Lead-203.

4. The composition of claim 1 , which comprises a therapeutic radionuclide.

5. The composition of claim 4 , wherein the therapeutic radionuclide is Holmium-166, Yttrium-90, Samarium-153, or Gadolinium-159.

6. The composition of claim 1 , wherein the radioprotectant is an anti-oxidant.

7. The composition of claim 1 , wherein the radioprotectant is ascorbic acid, gentisic acid, nicotinic acid, ascorbyl palmitate, HOP(O)H 2 , monthioglycerol, sodium formaldehyde sulfoxylate, Na 2 S 2 O 5 , Na 2 S 2 O 3 , or SO 2 .

8. The composition of claim 1 , wherein the radioprotect is a reducing agent combined with BHA, BHT, pyrogallate or tocopherol.

9. The composition of claim 1 , wherein the radioprotectant is ascorbic acid.

10. The composition of claim 9 , wherein the ascorbic acid is present in the amount of about 35-75 mg/mL of liquid composition.

11. The composition of claim 1 , wherein the composition is buffered to a pH of 7-8.

12. The composition of claim 1 further comprising a pharmaceutically acceptable carrier.

13. A method of preparing the composition of claim 1 comprising admixing a compound of formula (I), a radionuclide and a radioprotectant.

14. The method of claim 13 , further comprising admixing a pharmaceutically acceptable carrier.

15. A kit comprising the composition of claim 1 .

16. The kit of claim 15 further comprising a pharmaceutically acceptable carrier.