US2021253547A1PendingUtilityA1

Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds

78
Assignee: AERIE PHARMACEUTICALS INCPriority: Jul 25, 2008Filed: Apr 29, 2021Published: Aug 19, 2021
Est. expiryJul 25, 2028(~2 yrs left)· nominal 20-yr term from priority
Inventors:Mitchell A. DelongJill Marie SturdivantSusan M. Royalty
C07D 217/02A61P 11/00A61P 27/00A61P 11/02A61P 25/28A61P 11/06A61P 27/06A61P 1/16C07D 401/12A61P 43/00A61P 27/02A61P 1/04A61P 11/08A61K 31/4709A61P 15/18C07D 217/24A61P 1/00C07D 333/24A61P 9/10A61P 1/18C07D 213/56C07D 413/12C07D 409/12A61P 13/10A61P 3/04C07C 237/48C07D 417/12A61P 15/00A61K 31/381A61P 17/14A61P 35/00A61P 13/02A61P 13/12C07D 405/12A61K 31/16A61P 19/08A61P 17/00A61K 31/47C07C 237/04A61P 9/00A61P 9/12
78
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Claims

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.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A method of treating glaucoma, comprising administration via 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 
         R 1  and R 2  are, independently, hydrogen, C 1 -C 4  alkyl, C 2 -C 4  alkenyl, C 1 -C 4  carbonyl, or C 1 -C 4  carboxyl; or R 1  and R 2  combine to form a heterocycloalkyl ring of at least 5 and at most 8 member atoms, or R 1  and R 3  combine to form a heterocycloalkyl ring of at least 5 and at most 8 member atoms; 
         one of R 3  and R 4  is an aryl group, a heteroaryl group, a cycloalkyl group, a heterocycloalkyl group, C 1 -C 8  alkenyl, and the other of R 3  and R 4  is hydrogen or C 1 -C 4  alkyl; and 
         X 1  and X 2  are, independently, hydrogen, hydroxyl, halogen, C 1 -C 4  alkyl, C 2 -C 4  alkenyl, amino, nitro, or cyano. 
       
     
     
         2 . The method of  claim 1 , wherein one of R 3  and R 4  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 daily administration once daily, twice per day, or 4 times per day. 
     
     
         10 . The method of  claim 2 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         11 . The method of  claim 3 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         12 . The method of  claim 4 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         13 . The method of  claim 5 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         14 . The method of  claim 6 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         15 . The method of  claim 7 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         16 . The method of  claim 8 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         17 . The method of  claim 1 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         18 . The method of  claim 2 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         19 . The method of  claim 3 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         20 . The method of  claim 4 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         21 . The method of  claim 5 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         22 . The method of  claim 6 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         23 . The method of  claim 7 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         24 . The method of  claim 8 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         25 . The method of  claim 1 , wherein the administration is monthly administration once a month. 
     
     
         26 . The method of  claim 2 , wherein the administration is monthly administration once a month. 
     
     
         27 . The method of  claim 3 , wherein the administration is monthly administration once a month. 
     
     
         28 . The method of  claim 4 , wherein the administration is monthly administration once a month. 
     
     
         29 . The method of  claim 5 , wherein the administration is monthly administration once a month. 
     
     
         30 . The method of  claim 6 , wherein the administration is monthly administration once a month. 
     
     
         31 . The method of  claim 7 , wherein the administration is monthly administration once a month. 
     
     
         32 . The method of  claim 8 , wherein the administration is monthly administration once a month. 
     
     
         33 . A method of treating glaucoma, comprising administration via 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.   
     
     
         34 . The method of  claim 33 , wherein the amount of the Rho kinase inhibitor administered is about 0.01 to about 1,000 μg/kg subject body weight. 
     
     
         35 . The method of  claim 33 , wherein the amount of the Rho kinase inhibitor administered is about 0.1 to about 100 μg/kg subject body weight. 
     
     
         36 . The method of  claim 33 , wherein the amount of the Rho kinase inhibitor administered is about 1 to about 50 μg/kg subject body weight. 
     
     
         37 . The method of  claim 33 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         38 . The method of  claim 34 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         39 . The method of  claim 35 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         40 . The method of  claim 36 , wherein the administration is daily administration once daily, twice per day, or 4 times per day. 
     
     
         41 . The method of  claim 33 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         42 . The method of  claim 34 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         43 . The method of  claim 35 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         44 . The method of  claim 36 , wherein the administration is weekly administration once weekly or twice weekly. 
     
     
         45 . The method of  claim 33 , wherein the administration is monthly administration once a month. 
     
     
         46 . The method of  claim 34 , wherein the administration is monthly administration once a 
     
     
         47 . The method of  claim 35 , wherein the administration is monthly administration once a month. 
     
     
         48 . The method of  claim 36 , wherein the administration is monthly administration once a month.

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