US2004142957A1PendingUtilityA1

Quinolonecarboxylic acid derivatives

58
Assignee: DAIICHI SEIYAKU COPriority: Mar 31, 2000Filed: Jan 9, 2004Published: Jul 22, 2004
Est. expiryMar 31, 2020(expired)· nominal 20-yr term from priority
Inventors:Makoto TakemuraHisashi TakahashiKatsuhiro KawakamiMasao ItohTetsuya SuzukiTsuyoshi OhtaniMasayasu SekiguchiRie MiyauchiIsao Hayakawa
A61K 31/4709A61P 31/04C07D 401/04
58
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Claims

Abstract

(−)-7-[(7S)-7-Amino-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R, 2S)-2-fluoro-1-cyclopropyl]-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid.1HCl.1H 2 O and antibacterial compositions containing this compound. The compound of the present invention exhibits not only excellent antibacterial activity and safety, but also remarkable stability against light and humidity, and is thus useful as an antibacterial agent.

Claims

exact text as granted — not AI-modified
1 . A compound represented by the following formula (1).  
       
         
           
           
               
               
           
         
       
     
     
         2 . A compound as claimed in  claim 1 , which assumes crystals exhibiting characteristic peaks in the vicinity of angles of diffraction (2θ) of 6.9, 10.5, 14.4, 23.1, 26.9, and 27.8(°) when subjected to powder X-ray diffractometry.  
     
     
         3 . An antibacterial composition containing a compound represented by the following formula (1a), an acid addition salt of the compound, or a hydrate of the formula (1a) compound or the acid addition salt.  
       
         
           
           
               
               
           
         
       
     
     
         4 . The antibacterial composition as claimed in  claim 3 , containing an acid addition salt of a compound represented by formula (1a), or a hydrate of the acid addition salt.  
     
     
         5 . The antibacterial composition as claimed in  claim 4 , wherein the acid addition salt is a hydrochloric acid salt.  
     
     
         6 . An antibacterial composition containing a compound represented by the following formula (1).  
       
         
           
           
               
               
           
         
       
     
     
         7 . An antibacterial composition as claimed in  claim 4 , wherein the compound of formula (1) assumes crystals exhibiting characteristic peaks in the vicinity of angles of diffraction (2θ) of 6.9, 10.5, 14.4, 23.1, 26.9, and 27.8(°) when subjected to powder X-ray diffractometry.  
     
     
         8 . Use, in the manufacture of a drug for the treatment of infectious diseases, of a compound represented by the following formula (1a), an acid addition salt of the compound, or a hydrate of the formula (1a) compound or the acid addition salt.  
       
         
           
           
               
               
           
         
       
     
     
         9 . The use as claimed in  claim 8 , which employs an acid addition salt of the compound represented by formula (1a), or a hydrate of the acid addition salt.  
     
     
         10 . The use as claimed in  claim 9 , wherein the acid addition salt is a hydrochloric acid salt.  
     
     
         11 . Use, in the manufacture of a drug for the treatment of infectious diseases, of a compound represented by the following formula (1).  
       
         
           
           
               
               
           
         
       
     
     
         12 . The use as claimed in  claim 11 , wherein the compound of formula (1) assumes crystals exhibiting characteristic peaks in the vicinity of angles of diffraction (2θ) of 6.9, 10.5, 14.4, 23.1, 26.9, and 27.8(°) when subjected to powder X-ray diffractometry.  
     
     
         13 . A method for the treatment of infectious diseases, which is characterized by administering an effective amount of a compound represented by the following formula (1a), an acid addition salt of the compound, or a hydrate of the formula (1a) compound or the acid addition salt.  
       
         
           
           
               
               
           
         
       
     
     
         14 . The method as claimed in  claim 13 , which employs an acid additional salt of the compound represented by formula (1a), or a hydrate of the acid addition salt.  
     
     
         15 . The method as claimed in  claim 14 , wherein the acid additional salt is a hydrochloric acid salt.  
     
     
         16 . A method for the treatment of infectious diseases, which is characterized by administering an effect amount of a compound represented by the following formula (1).  
       
         
           
           
               
               
           
         
       
     
     
         17 . The method as claimed in  claim 16 , wherein the compound of formula (1) assumes crystals exhibiting characteristic peaks in the vicinity of angles of diffraction (2θ) of 6.9, 10.5, 14.4, 23.1, 26.9, and 27.8(°) when subjected to powder X-ray diffractometry.

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