Claims for Patent: 9,096,569

Summary for Patent: 9,096,569

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:	US14/273,895
Patent Claims:	1. A compound of formula (I): or any optical isomer, diastereomer, enantiomer, tautomer, or physiologically 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; wherein 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 wherein X1 and X2 are, independently, hydrogen, hydroxyl, halogen, C1-C4 alkyl, C2-C4 alkenyl, amino, nitro, or cyano. 2. The compound according to claim 1, wherein one of R3 and R4 is aryl or heteroaryl. 3. The compound according to claim 2, wherein R1 and R2 are, independently, hydrogen or methyl. 4. The compound according to claim 1, wherein X1 and X2 are, independently, hydrogen, hydroxy, chloro or fluoro. 5. The compound according to claim 1, wherein one of R3 and R4 is aryl or heteroaryl; wherein R1 and R2 are, independently, hydrogen or methyl; and wherein X1 and X2 are, independently, hydrogen, hydroxyl, chloro or fluoro. 6. The compound according to claim 5, wherein the other of R3 and R4 is hydrogen. 7. The compound according to claim 1, wherein one of R3 and R4 is aryl or heteroaryl. 8. The compound according to claim 2, wherein one of R3 and R4 is thienyl. 9. The compound according to claim 2, wherein one of R3 and R4 is monosubstituted phenyl or monosubstituted thienyl. 10. The compound according to claim 9, wherein the substituent is fluoro, chloro or cyano. 11. The compound according to claim 2, wherein one of R3 and R4 is unsubstituted phenyl or unsubstituted thienyl. 12. The compound according to claim 1, wherein X1 is hydroxy and X2 is hydrogen. 13. The compound according to claim 1, wherein a hydroxy is at the 1-position. 14. The compound according to claim 1, wherein a hydrogen is at the 1-position. 15. The compound according to claim 1, wherein R1 and R2 are, independently, hydrogen or methyl; R3 is hydrogen, R4 is phenyl; X1 and X2 are hydrogen. 16. A compound of formula (II): or any optical isomer, diastereomer, enantiomer, tautomer, or physiologically 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; wherein one of R3, R4, and R5 is an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, C1-C8 alkyl, or C2-C8 alkenyl, and the other two of R3, R4, and R5 is hydrogen or C1-C4 alkyl; and wherein X1 and X2 are, independently, hydrogen, hydroxyl, halogen, C1-C4 alkyl, C2-C4 alkenyl, amino, nitro, or cyano. 17. The compound according to claim 16, wherein one of R3, R4 and R5 is aryl or heteroaryl. 18. The compound according to claim 17, wherein R1 and R2 are, independently, hydrogen or methyl. 19. The compound according to claim 16, wherein X1 and X2 are, independently, hydrogen, hydroxy, chloro or fluoro. 20. The compound according to claim 16, wherein one of R3, R4 and R5 is aryl or heteroaryl; wherein R1 and R2 are, independently, hydrogen or methyl; and wherein X1 and X2 are, independently, hydrogen, hydroxyl, chloro or fluoro. 21. The compound according to claim 20, wherein the other of R3, R4 and R5 are hydrogen. 22. The compound according to claim 16, wherein one of R3, R4 and R5 is aryl or heteroaryl. 23. The compound according to claim 22, wherein one of R3, R4 and R5 is thienyl. 24. The compound according to claim 22, wherein one of R3, R4 and R5 is monosubstituted phenyl or monosubstituted thienyl. 25. The compound according to claim 24, wherein the substituent is fluoro, chloro or cyano. 26. The compound according to claim 24, wherein one of R3, R4 and R5 is unsubstituted phenyl or unsubstituted thienyl. 27. The compound according to claim 16, wherein X1 is hydroxy and X2 is hydrogen. 28. The compound according to claim 16, wherein a hydroxy is at the 1-position. 29. The compound according to claim 16, wherein a hydrogen is at the 1-position. 30. The compound according to claim 16, wherein R1 and R2 are, independently, hydrogen or methyl; R3 and R4 are hydrogen, R5 is phenyl; X1 and X2 are hydrogen. 31. A composition comprising a compound according to claim 1 and a carrier. 32. The composition of claim 31, wherein the carrier is saline buffered to a pH of about 5.5 to about 6.5. 33. A composition comprising a compound according to claim 16 and a carrier. 34. The composition of claim 33, wherein the carrier is saline buffered to a pH of about 5.5 to about 6.5. 35. A method of treating a disease in a subject comprising: administering to a subject an effective amount of a compound according to claim 1; wherein the disease comprises eye disease. 36. The method of claim 35, wherein the eye disease comprises glaucoma or a neurodegenerative eye disease.