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Last Updated: March 29, 2024

Claims for Patent: 9,045,453


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Summary for Patent: 9,045,453
Title:Substituted dioxopiperidinyl phthalimide derivatives
Abstract: This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent.
Inventor(s): Tung; Roger (Lexington, MA)
Assignee: Concert Pharmaceuticals, Inc. (Lexington, MA)
Application Number:13/107,873
Patent Claims:1. A compound of Formula Ia: ##STR00020## or a pharmaceutically acceptable salt thereof, wherein: each of W.sup.1, W.sup.2, and W.sup.3 is independently selected from hydrogen or deuterium; each of Y.sup.1 and Y.sup.2 is independently selected from hydrogen or deuterium; and each of Z.sup.1 Z.sup.2, Z.sup.3 and Z.sup.4 is independently selected from hydrogen or deuterium; wherein the compound comprises less than 25% of the other enantiomer, and wherein each position designated as D or deuterium has at least 75% incorporation of deuterium, and wherein any atom not designated as deuterium is present at its natural isotopic abundance.

2. The compound of claim 1, wherein Z.sup.3 and Z.sup.4 are deuterium; W.sup.1, W.sup.2 and W.sup.3 are simultaneously hydrogen or simultaneously deuterium; Z.sup.1 and Z.sup.2 are simultaneously hydrogen; and Y.sup.1 and Y.sup.2 are simultaneously hydrogen.

3. The compound of claim 1, wherein Z.sup.3 and Z.sup.4 are deuterium; W.sup.1, W.sup.2 and W.sup.3 are simultaneously hydrogen or simultaneously deuterium; Z.sup.1 and Z.sup.2 are simultaneously hydrogen; and Y.sup.1 and Y.sup.2 are simultaneously deuterium.

4. The compound of claim 1, wherein W.sup.1, W.sup.2 and W.sup.3 are the same.

5. The compound of claim 4, wherein W.sup.1, W.sup.2 and W.sup.3 are simultaneously hydrogen.

6. The compound of claim 5, wherein Z.sup.1, Z.sup.2, Z.sup.3 and Z.sup.4 are the same.

7. The compound of claim 6, wherein Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 are simultaneously deuterium.

8. The compound of claim 7, wherein each Y is simultaneously deuterium.

9. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00021## or a pharmaceutically acceptable salt thereof.

10. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00022## or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1, wherein the compound is selected from the group consisting of: ##STR00023## or a pharmaceutically acceptable salt thereof.

12. A pyrogen-free pharmaceutical composition comprising a compound of claim 1, and a pharmaceutically acceptable carrier.

13. The composition of claim 12, additionally comprising a second therapeutic agent selected from pemetrexed, topotecan, doxorubicin, bortezomib, gemcitabine, dacarbazine, dexamethasone, biaxin, doxil, vincristine, decadron, azacitidine, rituximab, prednisone, docetaxel, melphalan, and combinations thereof.

14. A method of treating a disease or condition selected from myelodysplastic syndromes, multiple myeloma, Non-Hodgkins lymphoma; chronic lymphocytic leukemia, amyloidosis, malignant gliomas, chronic myelomonocytic leukemia, follicular lymphoma, myeloid leukemia, mantle cell lymphoma, non-small cell lung cancer, Hodgkin's lymphoma, large cell lymphoma, and Waldenstrom's macroglobulinemia in a patient in need thereof, the method comprising the step of administering to the patient a composition of claim 12.

15. The method of claim 14, wherein the disease is selected from myelodysplastic syndromes and multiple myeloma.

16. The compound of claim 1, wherein the compound comprises less than 10% of the other enantiomer.

17. The compound of claim 1, wherein the compound comprises less than 5% of the other enantiomer.

18. The compound of claim 1, wherein the compound comprises less than 2% of the other enantiomer.

19. The compound of claim 1, wherein each position designated as D or deuterium has at least 90% incorporation of deuterium.

20. The compound of claim 1, wherein each position designated as D or deuterium has at least 95% incorporation of deuterium.

21. The compound of claim 1, wherein the compound comprises less than 10% of the other enantiomer and wherein each position designated as D or deuterium has at least 90% incorporation of deuterium.

22. The compound of claim 1, wherein the compound comprises less than 5% of the other enantiomer and wherein each position designated as D or deuterium has at least 90% incorporation of deuterium.

23. The compound of claim 1, wherein the compound comprises less than 2% of the other enantiomer and wherein each position designated as D or deuterium has at least 95% incorporation of deuterium.

Details for Patent 9,045,453

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. RITUXAN rituximab Injection 103705 11/26/1997 ⤷  Try a Trial 2028-11-14
Idec Pharmaceuticals Corp. RITUXAN rituximab Injection 103737 02/19/2002 ⤷  Try a Trial 2028-11-14
Genentech, Inc. RITUXAN HYCELA rituximab and hyaluronidase human Injection 761064 06/22/2017 ⤷  Try a Trial 2028-11-14
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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