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Cycloalkyl-substituted aminomethylpyrrolidine derivatives

A technology of substituents and alkyl groups, which is applied in the field of quinolones synthetic antibacterial agents, can solve the problems of no disclosure and no record of compound safety

Inactive Publication Date: 2002-01-30
ROHTO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, in this gazette, there is no disclosure of the details of the examples related to 3-[1-amino-1-cyclopropyl]methylpyrrolidin-1-yl, which is an optically active substance.
[0016] In addition, there is no description at all about the safety of the compound represented by formula (c)

Method used

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  • Cycloalkyl-substituted aminomethylpyrrolidine derivatives

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0137] Preparation example 1 (capsule):

Embodiment 2

[0138] Compound 100.0mg of Example 2

[0139] Corn starch 23.0mg

[0140]Calcium CMC 22.5mg

[0141] Hydroxymethylcellulose 3.0mg

[0142] Magnesium Stearate 1.5mg

[0143] Total 150.0mg

preparation example 2

[0144] Preparation example 2 (solution):

[0145] The compound 1~10g of embodiment 2

[0146] Sodium acetate or sodium hydroxide 0.5~2g

[0147] Ethyl p-hydroxybenzoate 0.1g

[0148] Purified water 88.9~98.4g

[0149] Total 100g

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Abstract

This invention provides a quinolone derivative which exerts strong antibacterial action upon various bacteria and has high safety, and it relates to a compound having a structure of formula (I), its salts and hydrates thereof: <CHEM> äR<1> and R<2>: hydrogen, alkyl; n: 1 to 4; Q: following structure (Ia): <CHEM> ÄR<3>: alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl, alkylamino; R<4>: hydrogen, alkylthio; R<5>: hydrogen, amino, hydroxyl, thiol, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; X<1>: halogen, hydrogen, A<1>: nitrogen, structure of formula (II): <CHEM> (X<2>: hydrogen, amino, halogen, cyano, halogenomethyl, halogenomethoxyl, alkyl, alkenyl, alkynyl, alkoxyl; R<4> and R<3> or X<2> and R<3> may together form a cyclic structure; Y: hydrogen, various ester forming groupsÜü.

Description

technical field [0001] The invention relates to a quinolone synthetic antibacterial agent suitable for use as a medicine, veterinary medicine, aquatic medicine or antibacterial preservative. [0002] Furthermore, the present invention relates to derivatives of 6-fluoro-1-[2-(S)-fluoro-1-(R)-cyclopropyl]-1,4-dihydro-4-oxoquinoline-3-carboxylic acid or 2,3-dihydro-3-(S)-methyl-7-oxo-7H-pyrido[1,2,3-de][1.4]benzoxazine-6-carboxylic acid derivative This is a class of quinolone synthetic antibacterial drugs, the structure of the substituent at the 7-position of the 1,4-dihydro-4-oxoquinoline skeleton or the structure of the substituent at the 2,3-dihydro-7-oxo- The structure of the substituent on the 10-position of the 7H-pyrido[1,2,3-de][1.4]benzoxazine skeleton plays a major role in the exertion of pharmacological effects such as antibacterial activity, pharmacokinetics in vivo, and safety. effect, when the 7-position of the former skeleton or the 10-position of the latter skel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/56A61K31/4709A61P31/04C07D213/64C07D401/04C07D498/06
CPCC07D401/04A61P31/04C07D413/04
Inventor 竹村真高桥寿宫内理江武田聪之早川勇夫
Owner ROHTO PHARM CO LTD
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