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Last Updated: April 25, 2024

Claims for Patent: 9,968,606

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Summary for Patent: 9,968,606

Title:	Deuterated compounds for treating cancer and related diseases and conditions, and compositions and methods thereof
Abstract:	The invention provides novel chemical compounds useful for treating cancer or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof.
Inventor(s):	Huang; Chaoran (Auburndale, MA), Cheng; Changfu (Northborough, MA)
Assignee:	NeuForm Pharmaceuticals, Inc. (Auburndale, MA)
Application Number:	15/599,415
Patent Claims:	1. A compound having the structural formula of: ##STR00031## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.9 is independently selected from H and D, or a pharmaceutically acceptable form thereof. 2. The compound of claim 1, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.9 is H. 3. The compound of claim 1, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, is D and each R.sub.9 is H. 4. The compound of claim 1, wherein R.sub.9 is D, having the following structural formula, ##STR00032## 5. The compound of claim 4, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is H. 6. The compound of claim 1, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is D, having the following structural formula, ##STR00033## 7. The compound of claim 1, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.9 is D, having the following structural formula, ##STR00034## 8. The compound of claim 1, wherein the compound is in the form of a mesylate salt. 9. A pharmaceutical composition comprising a compound having the structural formula of: ##STR00035## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.9 is independently selected from H and D, or a pharmaceutically acceptable form thereof, effective to treat cancer, or a related disease or disorder thereof, in a mammal, including a human, and a pharmaceutically acceptable excipient, carrier, or diluent. 10. The pharmaceutical composition of claim 9, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.9 is H. 11. The pharmaceutical composition of claim 9, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, is D and each R.sub.9 is H. 12. The pharmaceutical composition of claim 9, wherein each of R.sub.9 is D, having the following structural formula, ##STR00036## 13. The pharmaceutical composition of claim 12, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is H. 14. The pharmaceutical composition of claim 9, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is D, having the following structural formula, ##STR00037## 15. The pharmaceutical composition of claim 9, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.9 is D, having the following structural formula, ##STR00038## 16. The pharmaceutical composition of claim 9, wherein the compound is in the form of a mesylate salt. 17. A unit dosage form comprising the pharmaceutical composition of claim 16. 18. A method for treating cancer or a related disease or disorder, comprising: administering to a subject in need thereof a pharmaceutical composition comprising a compound having the formula of: ##STR00039## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.9 is independently selected from H and D, or a pharmaceutically acceptable form thereof. 19. The method of claim 18, wherein the cancer is lung cancer. 20. The method of claim 18, wherein the cancer is non-small cell lung cancer. 21. The method of claim 18, wherein the cancer is non-small cell lung cancer with EGFR T790M mutation. 22. The method of claim 18, wherein the pharmaceutical composition is administered to a subject with EGFRm+ and EGFR T790M mutation. 23. The method of claim 18, wherein each of R.sub.9 is D, having the following structural formula, ##STR00040## 24. The method of claim 23, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is H. 25. The method of claim 18, wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is D, having the following structural formula, ##STR00041## 26. The method of claim 18, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 is D, having the following structural formula, ##STR00042## 27. The method of claim 18, wherein the compound is in the form of a mesylate salt. 28. The method of claim 18, wherein the compound is administered in combination with one or more other anticancer agents selected from methotrexate, afatinib dimaleate, alectinib, pemetrexed disodium, bevacizumab, carboplatin, ceritinib, crizotinib, ramucirumab, docetaxel, erlotinib hydrochloride, methotrexate, gefitinib, gemcitabine hydrochloride, pembrolizumab, mechlorethamine hydrochloride, vinorelbine tartrate, necitumumab, nivolumab, paclitaxel, and erlotinib hydrochloride. 29. The method of claim 25, wherein each R.sub.9 is H.

Details for Patent 9,968,606

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Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	AVASTIN	bevacizumab	Injection	125085	02/26/2004	⤷ Try a Trial	2035-12-27
Eli Lilly And Company	CYRAMZA	ramucirumab	Injection	125477	04/21/2014	⤷ Try a Trial	2035-12-27
Merck Sharp & Dohme Corp.	KEYTRUDA	pembrolizumab	For Injection	125514	09/04/2014	⤷ Try a Trial	2035-12-27
Merck Sharp & Dohme Corp.	KEYTRUDA	pembrolizumab	Injection	125514	01/15/2015	⤷ Try a Trial	2035-12-27
Eli Lilly And Company	PORTRAZZA	necitumumab	Injection	125547	11/24/2015	⤷ Try a Trial	2035-12-27
Bristol-myers Squibb Company	OPDIVO	nivolumab	Injection	125554	12/22/2014	⤷ Try a Trial	2035-12-27
Bristol-myers Squibb Company	OPDIVO	nivolumab	Injection	125554	10/04/2017	⤷ Try a Trial	2035-12-27
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

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