US2022096444A1PendingUtilityA1

Prophylactic or therapeutic agent for delirium

Assignee: TAKEDA PHARMACEUTICALS COPriority: Jan 8, 2016Filed: Oct 7, 2021Published: Mar 31, 2022
Est. expiryJan 8, 2036(~9.4 yrs left)· nominal 20-yr term from priority
A61P 25/20A61K 31/428A61K 31/423A61K 31/4439A61P 25/00
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Claims

Abstract

The present invention provides a prophylactic or therapeutic agent for delirium containing compound (I) having melatonin receptor affinity. A compound represented by the formula:wherein each symbol is as described in the specification, or a salt thereof.

Claims

exact text as granted — not AI-modified
1 . A method for preventing or treating delirium comprising administering an effective amount of a compound selected from
 (N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]oxazol-8-ylidene)ethyl]acetamide,   N-[2-(2-methyl-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]oxazol-8-ylidene)ethyl]propionamide,   N-{2-[2-(4-phenylbutyl)-6,7-dihydro-8H-indeno[5,4-d][I,3]oxazol-8-ylidene]ethyl}acetamide,   N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]thiazol-8-ylidene)ethyl]acetamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]propionamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]propionamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]propionamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]thiazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]thiazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]thiazol-8-yl)ethyl]acetamide,   N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide, and   (S)—N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide   or a salt thereof to a mammal in need thereof.   
     
     
         2 . A pharmaceutical composition comprising a compound selected from
 N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]oxazol-8-ylidene)ethyl]acetamide,   N-[2-(2-methyl-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]oxazol-8-ylidene)ethyl]propionamide,   N-{2-[2-(4-phenylbutyl)-6,7-dihydro-8H-indeno[5,4-d][1,3]oxazol-8-ylidene]ethyl}acetamide,   N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]thiazol-8-ylidene)ethyl]acetamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]propionamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]propionamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]propionamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]thiazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]thiazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]thiazol-8-yl)ethyl]acetamide,   N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide, and   (S)—N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide or a salt thereof and   one or more pharmacologically acceptable carriers.   
     
     
         3 . (canceled) 
     
     
         4 . A method for preparing a pharmaceutical composition, the method comprising combining a compound of
 N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]oxazol-8-ylidene)ethyl]acetamide,   N-[2-(2-methyl-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]oxazol-8-ylidene)ethyl]propionamide,   N-{2-[2-(4-phenylbutyl)-6,7-dihydro-8H-indeno[5,4-d][1,3]oxazol-8-ylidene]ethyl}acetamide,   N-[2-(2-methyl-6,7-dihydro-8H-indeno[5,4-d][I,3]thiazol-8-ylidene)ethyl]acetamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]propionamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]propionamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]propionamide,   N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]thiazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]thiazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-methyl-7,8-dihydro-6H-indeno[5,4-d][I,3]thiazol-8-yl)ethyl]acetamide,   N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   (S)—N-[2-(2-ethyl-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide,   (R)—N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][I,3]oxazol-8-yl)ethyl]acetamide, and   (S)—N-[2-(2-methoxy-7,8-dihydro-6H-indeno[5,4-d][1,3]oxazol-8-yl)ethyl]acetamide   or a salt thereof with one or more pharmacologically acceptable carriers.   
     
     
         5 . (canceled)

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