Claims for Patent: 11,896,597

Summary for Patent: 11,896,597

Title:	ErbB/BTK inhibitors
Abstract:	Disclosed are compounds inhibiting ErbBs (e.g., EGFR or Her 2), especially mutant forms of ErbBs, and BTK, pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition can effectively treat ErbBs (especially mutant forms of ErbBs) or BTK associated diseases, including cancer.
Inventor(s):	Zhenfan YANG, Xiaolin Zhang
Assignee:	Dizal Jiangsu Pharmaceutical Co Ltd
Application Number:	US18/045,838
Patent Claims:	1. A method of treating an ErbB associated disease in a subject, comprising administering to the subject about 50 mg to about 500 mg per day of (R)—N-(5-(4-(5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenylamino)pyrimidin-2-ylamino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide, or a pharmaceutically acceptable salt, hydrate, solvate or stereoisomer thereof, wherein the ErbB associated disease is lung cancer. 2. The method according to claim 1, wherein the subject is a warm blooded-animal. 3. The method according to claim 2, wherein the warm blooded-animal is man. 4. The method according to claim 1, wherein the subject is a non-small cell lung cancer patient with EGFR exon20 insertion mutations. 5. The method according to claim 4, wherein the patient is pretreated by platinum-based chemotherapy. 6. The method according to claim 5, wherein the patient has brain metastasis. 7. The method according to claim 1, wherein the lung cancer is non-small cell lung cancer. 8. The method according to claim 1, wherein the lung cancer is non-small cell lung cancer with central nervous system metastasis. 9. The method according to claim 1, wherein the lung cancer is non-small cell lung cancer with brain metastasis. 10. The method according to claim 1, wherein the lung cancer is non-small cell lung cancer with EGFR exon20 insertion mutations. 11. The method according to claim 10, comprising administering to the subject about 100 mg, about 200 mg, about 300 mg or about 400 mg per day of (R)—N-(5-(4-(5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenylamino)pyrimidin-2-ylamino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide, or a pharmaceutically acceptable salt, hydrate, solvate or stereoisomer thereof. 12. The method according to claim 1, wherein the lung cancer is non-small cell lung cancer with EGFR exon19 deletion mutation, EGFR L858R mutation, EGFR exon 19 deletion/L858R and T790M double mutations, or less common EGFR non-resistant mutation selected from the group consisting of Gly719Xaa, Leu861Gln, and Ser768Ile mutation. 13. The method according to claim 12, comprising administering to the subject about 50 mg to about 500 mg per day of (R)—N-(5-(4-(5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenylamino)pyrimidin-2-ylamino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide, or a pharmaceutically acceptable salt, hydrate, solvate or stereoisomer thereof. 14. The method according to claim 1, wherein (R)—N-(5-(4-(5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenylamino)pyrimidin-2-ylamino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide, or a pharmaceutically acceptable salt, hydrate, solvate or stereoisomer thereof is administered to the subject orally. 15. A pharmaceutical composition formulated in a unit-dosage form comprising about 50 mg-about 500 mg (R)—N-(5-(4-(5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenylamino)pyrimidin-2-ylamino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide, or a pharmaceutically acceptable salt, hydrate, solvate or stereoisomer thereof. 16. The composition according to claim 15, comprising about 50 mg, about 100 mg, about 200 mg, about 300 mg, about 400 mg or about 500 mg (R)—N-(5-(4-(5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenylamino)pyrimidin-2-ylamino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide, or a pharmaceutically acceptable salt, hydrate, solvate or stereoisomer thereof. 17. The composition according to claim 15 formulated in a unit-dosage form for oral administration. 18. A pharmaceutical composition comprising about 50 mg-about 500 mg (R)—N-(5-(4-(5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenylamino)pyrimidin-2-ylamino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide, or a pharmaceutically acceptable salt, hydrate, solvate or stereoisomer thereof. 19. The composition according to claim 18, comprising about 50 mg, about 100 mg, about 200 mg, about 300 mg, about 400 mg or about 500 mg (R)—N-(5-(4-(5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenylamino)pyrimidin-2-ylamino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide, or a pharmaceutically acceptable salt, hydrate, solvate or stereoisomer thereof. 20. The composition according to claim 18 formulated for oral administration.