US2020317624A1PendingUtilityA1

Bicyclic quinazolinone derivatives

Assignee: HOFFMANN LA ROCHEPriority: Apr 10, 2015Filed: Feb 18, 2020Published: Oct 8, 2020
Est. expiryApr 10, 2035(~8.7 yrs left)· nominal 20-yr term from priority
C07D 239/88C07D 403/04A61K 31/496C07D 471/04A61K 31/517C07D 403/02C07D 413/12A61P 1/16A61P 29/00C07D 239/90A61P 35/00C07D 401/04C07D 401/12A61P 25/00C07D 405/12A61P 37/06A61P 17/04A61P 11/00A61P 9/00A61P 3/00A61P 13/12C07D 403/12A61P 43/00A61P 27/02A61P 27/06C07D 413/14C07D 405/14
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Claims

Abstract

wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R12, R13, R14, A1, A2, A3, n and m are as described herein.

Claims

exact text as granted — not AI-modified
1 - 42 . (canceled) 
     
     
         43 . A compound, wherein the compound is:
 (3R)-3-[[2-[6-(4-acetylpiperazin-1-yl)-4-oxoquinazolin-3-yl]acetyl]amino]-N-benzyl-3-[4-(trifluoromethyl)phenyl]propanamide;   2-[6-(4-acetylpiperazin-1-yl)-2,4-dioxo-1H-quinazolin-3-yl]-N-[(3,4-dichlorophenyl)methyl]acetamide;   2-[6-(4-acetylpiperazin-1-yl)-4-oxoquinazolin-3-yl]-N-[2-(3,4-dichlorophenyl)ethyl]acetamide;   2-[6-(4-acetylpiperazin-1-yl)-4-oxoquinazolin-3-yl]-N-[[3-(4-chlorophenyl)-1,2-oxazol-5-yl]methyl]acetamide; or   2-[6-(4-acetylpiperazin-1-yl)-4-oxoquinazolin-3-yl]-N-[[5-(4-chlorophenyl)-1,2,4-oxadiazol-3-yl]methyl]acetamide;   or a pharmaceutically acceptable salt thereof.   
     
     
         44 . The compound of  claim 43 , wherein the compound is (3R)-3-[[2-[6-(4-acetylpiperazin-1-yl)-4-oxoquinazolin-3-yl]acetyl]amino]-N-benzyl-3-[4-(trifluoromethyl)phenyl]propanamide, or a pharmaceutically acceptable salt thereof. 
     
     
         45 . The compound of  claim 43 , wherein the compound is 2-[6-(4-acetylpiperazin-1-yl)-2,4-dioxo-1H-quinazolin-3-yl]-N-[(3,4-dichlorophenyl)methyl]acetamide, or a pharmaceutically acceptable salt thereof. 
     
     
         46 . The compound of  claim 43 , wherein the compound is 2-[6-(4-acetylpiperazin-1-yl)-4-oxoquinazolin-3-yl]-N-[2-(3,4-dichlorophenyl)ethyl]acetamide, or a pharmaceutically acceptable salt thereof. 
     
     
         47 . The compound of  claim 43 , wherein the compound is 2-[6-(4-acetylpiperazin-1-yl)-4-oxoquinazolin-3-yl]-N-[[3-(4-chlorophenyl)-1,2-oxazol-5-yl]methyl]acetamide, or a pharmaceutically acceptable salt thereof. 
     
     
         48 . The compound of  claim 43 , wherein the compound is 2-[6-(4-acetylpiperazin-1-yl)-4-oxoquinazolin-3-yl]-N-[[5-(4-chlorophenyl)-1,2,4-oxadiazol-3-yl]methyl]acetamide, or a pharmaceutically acceptable salt thereof. 
     
     
         49 . A pharmaceutical composition, comprising a compound according to  claim 43 , or a pharmaceutically acceptable salt thereof, and a therapeutically inert carrier. 
     
     
         50 . A method for the treatment of a condition, comprising administering a compound according to  claim 43 , or a pharmaceutically acceptable salt thereof,
 wherein the condition is selected from the group consisting of renal conditions, liver conditions, inflammatory conditions, conditions of the nervous system, conditions of the respiratory system, vascular and cardiovascular conditions, fibrotic diseases, cancer, ocular conditions, metabolic conditions, cholestatic and other forms of chronic pruritus, and acute and chronic organ transplant rejection.   
     
     
         51 . The method of  claim 45 , wherein the condition is an ocular condition. 
     
     
         52 . The method of  claim 46 , wherein the ocular condition is proliferative retinopathy, non-proliferative diabetic retinopathy, dry age-related macular degeneration, wet age-related macular degeneration, macular edema, central arterial occlusion, central venous occlusion, traumatic injury, or glaucoma. 
     
     
         53 . The method of  claim 47 , wherein the condition is glaucoma.

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