.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 4,705,849

« Back to Dashboard

Claims for Patent: 4,705,849

Title: Boronic acid adducts of technetium-99m dioxime complexes
Abstract:Boronic acid adducts of technetium-99m dioxime complexes are useful for imaging the myocardium, hepatobiliary system, brain and blood pool in humans and other mammalian species.
Inventor(s): Nunn; Adrian D. (Hopewell, NJ), Feld; Thomas A. (Califon, NJ), Treher; Elizabeth N. (Washington Crossing, PA)
Assignee: E. R. Squibb & Sons, Inc. (Princeton, NJ)
Application Number:06/723,601
Patent Claims: 1. A boronic acid adduct of technetium-99m dioxime complexes having the formula

wherein

X is an anion;

Y is a vicinal dioxime having the formula ##STR6## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R.sub.1 and R.sub.2 are --(CR.sub.8 R.sub.9).sub.n --wherein n is 3, 4, 5 or 6 and R.sub.8 and R.sub.9 are each independently hydrogen or alkyl; and

Z is a boron derivative of the formula

wherein R.sub.3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxyalkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl or (R.sub.4 R.sub.5 N)-alkyl and R.sub.4 and R.sub.5 are each independently hydrogen, alkyl, or arylalkyl, or R.sub.4 and R.sub.5 when taken together with the nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle.

2. A boronic acid adduct in accordance with claim 1, wherein X is a halide.

3. A boronic acid adduct in accordance with claim 1, wherein X is chloride or bromide.

4. A boronic acid adduct in accordance with claim 1, wherein X is chloride.

5. A boronic acid adduct in accordance with claim 1, wherein Y is dimethyl glyoxime, 1,2-cyclohexanedione dioxime, 1,2-ethanedione dioxime, .alpha.-furyldioxime, 1,2-cyclopentanedione dioxime, or 3-methyl-1,2-cyclopentanedione dioxime.

6. A boronic acid adduct in accordance with claim 1, wherein Y is dimethyl glyoxime

7. A boronic acid adduct in accordance with claim 1, wherein Y is 1,2-cyclohexanedione dioxime.

8. A boronic acid adduct in accordance with claim 1, wherein Y is 1,2-ethanedione dioxime.

9. A boronic acid adduct in accordance with claim 1, wherein Y is .alpha.-furyldioxime.

10. A boronic acid adduct in accordance with claim 1, wherein the boron derivative Z is B-alkyl.

11. A boronic acid adduct in accordance with claim 1, wherein the boron derivative Z is B-alkoxy.

12. A boronic acid adduct in accordance with claim 1, wherein the boron derivative Z is B-benzyl.

13. A boronic acid adduct in accordance with claim 1, wherein the boron derivative Z is B-cycloalkyl.

14. The boronic acid adduct in accordance with claim 1, 99mTc (chlorine) (1,2-cyclohexanedione dioxime).sub.3 methyl boron.

15. The boronic acid adduct in accordance with claim 1, 99mTc (chlorine)(dimethyl glyoxime).sub.3 1-methylpropyl boron.

16. The boronic acid adduct in accordance with claim 1, 99mTc (chlorine)(dimethyl glyoxime).sub.3 4-methylphenyl boron.

17. The boronic acid adduct in accordance with claim 1, 99mTc (chlorine)(dimethyl glyoxime).sub.3 cyclopentyl boron.

18. The boronic acid adduct in accordance with claim 1, 99mTc (chlorine) 1,2-cyclohexanedione dioxime).sub.3 ethyl boron.

19. The boronic acid adduct in accordance with claim 1, 99mTc (chlorine)(dimethyl glyoxime).sub.3 4-(t-butyl)phenyl boron.

20. The boronic acid adduct in accordance with claim 1, 99mTc (chlorine) (dimethyl glyoxime).sub.3 2-methyl-1-propyl boron.

21. The boronic acid adduct in accordance with claim 1, 99mTc (chlorine) (1,2-cyclohexanedione dioxime).sub.3 hydroxy boron.

22. A kit suitable for labeling with technetium-99m, said kit comprising:

(i) a source of anion;

(ii) a boronic acid derivative, or compounds which can react in situ to form a boronic acid derivative, having the formula ##STR7## or a pharmaceutically acceptable salt thereof, wherein R.sub.3 is hydroxy, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, carboxyalkyl, carboxyalkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, alkoxy-alkenyl, haloalkyl, haloalkenyl, aryl, arylalkyl, or R.sub.4 R.sub.5 N-alkyl and R.sub.4 and R.sub.5 are each independently hydrogen, alkyl, or arylalkyl, or R.sub.4 and R.sub.5 when taken together with nitrogen atom to which they are attached form a 5 or 6-membered nitrogen containing heterocycle, and R.sub.7 is hydrogen, alkyl or aryl;

(iii) a dioxime having the formula ##STR8## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, halogen, alkyl, aryl, amino or a 5 or 6-membered nitrogen or oxygen containing heterocycle, or together R.sub.1 and R.sub.2 are --(CR.sub.8 R.sub.9).sub.n --wherein n is 3, 4, 5 or 6 and R.sub.8 and R.sub.9 are each independently hydrogen or alkyl; and

(iv) a reducing agent.

23. A kit in accordance with claim 22, wherein the source of anion is a source of halide.

24. A kit in accordance with claim 22, wherein the source of anion is a source of chloride or bromide.

25. A kit in accordance with claim 22 wherein the dioxime is dimethyl glyoxime, 1,2-cyclohexanedione dioxime, 1,2-ethanedione dioxime or .alpha.-furyldioxime.

26. A kit in accordance with claim 22, wherein the dioxime is dimethyl glyoxime.

27. A kit in accordance with claim 22, wherein the dioxime is 1,2-cyclohexanedione dioxime.

28. A kit in accordance with claim 22, wherein the reducing agent is a stannous salt.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc