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Last Updated: March 28, 2024

Claims for Patent: 9,938,288


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Summary for Patent: 9,938,288
Title:Macrocyclic compound and uses thereof
Abstract: The present invention provides novel Compound (1) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, and a medical uses thereof. ##STR00001##
Inventor(s): Kishi; Yoshito (Cambridge, MA), Kira; Kazunobu (Tsukuba, JP), Ito; Ken (Tsukuba, JP)
Assignee: President and Fellows of Harvard College (Cambridge, MA) Eisai R&D Management Co., LTD. (Tokyo, JP)
Application Number:15/814,105
Patent Claims:1. A compound of the following structure: ##STR00030## or a pharmaceutically acceptable salt thereof.

2. The compound or pharmaceutically acceptable salt thereof according to claim 1 for use in inhibiting growth of tumor or cancer characterized by angiogenesis, invasion, or metastasis.

3. The compound or pharmaceutically acceptable salt thereof according to claim 1 for use in the treatment of tumor or cancer characterized by angiogenesis, invasion, or metastasis.

4. A pharmaceutical composition comprising the compound of claim 1, or pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.

5. A method for treating a tumor or cancer characterized by angiogenesis, invasion or metastasis in a subject comprising administering to the subject the compound of claim 1, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

6. The method of claim 5, wherein the cancer or tumor is head and neck cancer, breast cancer, esophageal cancer, uterine cancer, ovarian cancer, colorectal cancer, endometrial cancer, or a sarcoma.

7. The method of claim 6, wherein the cancer or tumor is head and neck cancer.

8. The method of claim 7, wherein the cancer or tumor is squamous cell carcinoma of the head and neck (SCCHN).

9. The method of claim 6, wherein the cancer or tumor is breast cancer.

10. The method of claim 9, wherein the cancer or tumor is HER2-positive breast cancer.

11. The method of claim 9, wherein the cancer or tumor is HER2-negative breast cancer.

12. The method of claim 9, wherein the cancer or tumor is triple negative breast cancer.

13. The method of claim 6, wherein the cancer or tumor is colorectal cancer.

14. The method of claim 6, wherein the cancer or tumor is esophageal cancer.

15. The method of claim 14, wherein the cancer or tumor is esophageal adenocarcinoma.

16. The method of claim 6, wherein the cancer or tumor is uterine cancer.

17. The method of claim 6, wherein the cancer or tumor is ovarian cancer.

18. The method of claim 6, wherein the cancer or tumor is a sarcoma.

19. The method of claim 18, wherein the cancer or tumor is uterine sarcoma, fibrosarcoma, or angiosarcoma.

20. The method of claim 5 comprising further treating the subject with radiation therapy.

21. The method of claim 5 comprising further treating the subject with a Programmed Death 1 protein (PD-1) antibody.

22. The method of claim 5 comprising further treating the subject with an anti-EGFR (epidermal growth factor receptor) mAb.

23. The method of claim 22, wherein the cancer or tumor is head and neck cancer.

24. The method of claim 23, wherein the cancer or tumor is squamous cell carcinoma of the head and neck (SCCHN).

25. The method of claim 22, wherein the anti-EGFR (epidermal growth factor receptor) mAb is cetuximab.

26. The method of claim 5 comprising further treating the subject with an HER2 (human epidermal growth factor receptor) mAb.

27. The method of claim 26, wherein the cancer is breast cancer.

28. The method of according to claim 26, wherein the HER2 (human epidermal growth factor receptor) mAb is trastuzumab.

29. A method for treating HER2-negative breast cancer or squamous cell carcinoma of the head and neck (SCCHN) in a subject comprising administering to the subject the compound of claim 1, or a pharmaceutically acceptable salt thereof.

Details for Patent 9,938,288

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2037-04-05
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2037-04-05
Eli Lilly And Company ERBITUX cetuximab Injection 125084 02/12/2004 ⤷  Try a Trial 2037-04-05
Eli Lilly And Company ERBITUX cetuximab Injection 125084 03/28/2007 ⤷  Try a Trial 2037-04-05
Genentech, Inc. HERCEPTIN HYLECTA trastuzumab and hyaluronidase-oysk Injection 761106 02/28/2019 ⤷  Try a Trial 2037-04-05
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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