Claims for Patent: 11,021,456

Summary for Patent: 11,021,456

Title:	Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
Abstract:	Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
Inventor(s):	Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
Assignee:	Alcon Inc
Application Number:	US16/730,085
Patent Claims:	1. A method of treating glaucoma, comprising ocular administration of a composition comprising a Rho kinase inhibitor and a pharmaceutically acceptable carrier to a subject in need thereof, wherein the administration is daily administration, weekly administration, or monthly administration and wherein the Rho kinase inhibitor is a compound of formula (I): or a pharmaceutically acceptable salt thereof; wherein R1 and R2 are, independently, hydrogen, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 carbonyl, or C1-C4 carboxyl, or R1 and R2 combine to form a heterocycloalkyl ring of at least 5 and at most 8 member atoms, or R1 and R3 combine to form a heterocycloalkyl ring of at least 5 and at most 8 member atoms; one of R3 and R4 is an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, C1-C8 alkenyl, and the other of R3 and R4 is hydrogen or C1-C4 alkyl; and X1 and X2 are, independently, hydrogen, hydroxyl, halogen, C1-C4 alkyl, C2-C4 alkenyl, amino, nitro, or cyano. 2. The method of claim 1, wherein one of R3 and R4 is aryl or heteroaryl. 3. The method of claim 1, wherein the amount of the Rho kinase inhibitor administered is about 0.01 to about 1,000 μg/kg subject body weight. 4. The method of claim 2, wherein the amount of the Rho kinase inhibitor administered is about 0.01 to about 1,000 μg/kg subject body weight. 5. The method of claim 1, wherein the amount of the Rho kinase inhibitor administered is about 0.1 to about 100 μg/kg subject body weight. 6. The method of claim 2, wherein the amount of the Rho kinase inhibitor administered is about 0.1 to about 100 μg/kg subject body weight. 7. The method of claim 1, wherein the amount of the Rho kinase inhibitor administered is about 1 to about 50 μg/kg subject body weight. 8. The method of claim 2, wherein the amount of the Rho kinase inhibitor administered is about 1 to about 50 μg/kg subject body weight. 9. The method of claim 1, wherein the administration is once daily, twice per day, or 4 times per day. 10. The method of claim 2, wherein the administration is once daily, twice per day, or 4 times per day. 11. The method of claim 3, wherein the administration is once daily, twice per day, or 4 times per day. 12. The method of claim 4, wherein the administration is once daily, twice per day, or 4 times per day. 13. The method of claim 5, wherein the administration is once daily, twice per day, or 4 times per day. 14. The method of claim 6, wherein the administration is once daily, twice per day, or 4 times per day. 15. The method of claim 7, wherein the administration is once daily, twice per day, or 4 times per day. 16. The method of claim 8, wherein the administration is once daily, twice per day, or 4 times per day. 17. The method of claim 1, wherein the administration is once weekly or twice weekly. 18. The method of claim 2, wherein the administration is once weekly or twice weekly. 19. The method of claim 3, wherein the administration is once weekly or twice weekly. 20. The method of claim 4, wherein the administration is once weekly or twice weekly. 21. The method of claim 5, wherein the administration is once weekly or twice weekly. 22. The method of claim 6, wherein the administration is once weekly or twice weekly. 23. The method of claim 7, wherein the administration is once weekly or twice weekly. 24. The method of claim 8, wherein the administration is once weekly or twice weekly. 25. The method of claim 1, wherein the administration is once a month. 26. The method of claim 2, wherein the administration is once a month. 27. The method of claim 3, wherein the administration is once a month. 28. The method of claim 4, wherein the administration is once a month. 29. The method of claim 5, wherein the administration is once a month. 30. The method of claim 6, wherein the administration is once a month. 31. The method of claim 7, wherein the administration is once a month. 32. The method of claim 8, wherein the administration is once a month. 33. The method of claim 1, wherein R1 and R2 are hydrogen; R4 is C6H5; R3 is hydrogen; and X1 and X2 are hydrogen.