IP Library › Patent Application 12197007
Patent Application
App. No. 12/197,007

DEUTERIUM-ENRICHED FONDAPARINUX

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Patent No.
US None
App. No.
12/197,007
Abstract

The present application describes deuterium-enriched fondaparinux, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Claims (26)

1 . A deuterium-enriched compound of formula I or a pharmaceutically acceptable salt thereof:

wherein R 1 -R 43 are independently selected from H and D; and

the abundance of deuterium in R 1 -R 43 is at least 2%.

2 . A deuterium-enriched compound of claim 1 , wherein the abundance of deuterium in R 1 -R 43 is selected from at least 2%, at least 5%, at least 9%, at least 14%, at least 19%, at least 23%, at least 28%, at least 33%, at least 37%, at least 42%, at least 47%, at least 51%, at least 56%, at least 60%, at least 65%, at least 70%, at least 74%, at least 79%, at least 84%, at least 88%, at least 93%, at least 98%, and 100%.

3 . A deuterium-enriched compound of claim 1 , wherein the abundance of deuterium in R 1 -R 9 is selected from at least 11%, at least 22%, at least 33%, at least 44%, at least 56%, at least 67%, at least 78%, and 100%.

4 . A deuterium-enriched compound of claim 1 , wherein the abundance of deuterium in R 10 -R 16 is selected from at least 14%, at least 29%, at least 43%, at least 57%, at least 71%, at least 86%, and 100%.

5 . A deuterium-enriched compound of claim 1 , wherein the abundance of deuterium in R 17 -R 21 is selected from at least 20%, at least 40%, at least 60%, at least 80%, and 100%.

6 . A deuterium-enriched compound of claim 1 , wherein the abundance of deuterium in R 22 -R 28 is selected from at least 14%, at least 29%, at least 43%, at least 57%, at least 71%, at least 86%, and 100%.

7 . A deuterium-enriched compound of claim 1 , wherein the abundance of deuterium in R 29 -R 33 is selected from at least 20%, at least 40%, at least 60%, at least 80%, and 100%.

8 . A deuterium-enriched compound of claim 1 , wherein the abundance of deuterium in R 34 -R 40 is selected from at least 14%, at least 29%, at least 43%, at least 57%, at least 71%, at least 86%, and 100%.

9 . A deuterium-enriched compound of claim 1 , wherein the abundance of deuterium in R 41 -R 43 is selected from at least 33%, at least 67%, and 100%.

10 . A deuterium-enriched compound of claim 1 , wherein the compound is selected from compounds 1-8 of Table 1.

11 . A deuterium-enriched compound of claim 1 , wherein the compound is selected from compounds 9-16 of Table 2.

12 . An isolated deuterium-enriched compound of formula I or a pharmaceutically acceptable salt thereof:

wherein R 1 -R 43 are independently selected from H and D; and

the abundance of deuterium in R 1 -R 43 is at least 2%.

13 . An isolated deuterium-enriched compound of claim 12 , wherein the abundance of deuterium in R 1 -R 43 is selected from at least 2%, at least 5%, at least 9%, at least 14%, at least 19%, at least 23%, at least 28%, at least 33%, at least 37%, at least 42%, at least 47%, at least 51%, at least 56%, at least 60%, at least 65%, at least 70%, at least 74%, at least 79%, at least 84%, at least 88%, at least 93%, at least 98%, and 100%.

14 . An isolated deuterium-enriched compound of claim 12 , wherein the compound is selected from compounds 1-8 of Table 1.

15 . An isolated deuterium-enriched compound of claim 12 , wherein the compound is selected from compounds 9-16 of Table 2.

16 . A mixture of deuterium-enriched compounds of formula I or a pharmaceutically acceptable salt thereof:

wherein R 1 -R 43 are independently selected from H and D; and

the abundance of deuterium in R 1 -R 43 is at least 2%.

17 . A mixture of deuterium-enriched compound of claim 16 , wherein the compound is selected from compounds 1-8 of Table 1.

18 . A mixture of deuterium-enriched compound of claim 16 , wherein the compound is selected from compounds 9-16 of Table 2.

19 . A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt form thereof.

20 . A method for treating deep vein thrombosis comprising: administering, to a patient in need thereof, a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt form thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 24, 2008
From: CZARNIK, ANTHONY W
To: PROTIA, LLC
Reel/Frame 021733/0840 →