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Title:
予測的生理学的ゲート駆動のための方法およびシステム
Document Type and Number:
Japanese Patent JP2005504734
Kind Code:
A
Abstract:
A compound of the formula (I): wherein A is an aromatic or heteroaromatic ring system or partially or fully reduced derivatives thereof; Q is hydrogen, C 1 -C 12 straight chain, branched or cyclic alkyl substituted with one or more hydroxy groups, or a mono- or di-saccharide moiety; Z is -CR 10 R 11 -, -NR 12 -, -C(O)O-, -C(O)NR 12 - or -O-, where R 10 and R 11 are independently selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 6 -C 10 aryl, C 1 -C 6 alkoxy and -N(R 13 ) 2 and where each R 13 is independently selected from hydrogen and C 1 -C 6 alkyl, and where R 12 is selected from hydrogen and C 1 -C 6 alkyl; R 1 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -NR(R 13 ) 2 and -N(R 12 )-COR 14 ; where R 12 and R 13 are as defined above, and where R 14 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy and -NR 12 ; R 2 is selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -N(R 13 ) 2 and -N(R 12 )-COCHR 2a R 2b ; where R 2a and R 2b are selected from hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, -N(R 13 ) 2 and -N(R 12 )-COR 14 ; where R 12 , R 13 and R 14 are as defined above; R 3 , R 4 and R 5 are independently selected from hydrogen, C 1 -C 6 alkyl and ± side chains of ±-amino acids or their enantiomers or their derivatives; R 6 is -CO 2 R 15 , -CONHR 16 , -CONHOR 16 , -CONHNHR 16 , -SO 2 N(R 16 ) 2 , -SO 2 R 17 or -P(O)(OR 18 )(OR 18 ) where each R 15 , R 16 , R 17 and R 18 is independently selected from hydrogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 6 -C 10 aryl and C 7 -C 10 arylalkyl; B is an ±-amino acid residue, a ²-amino acid residue or an ±,±-disubstituted amino acid residue, such residue forming amide linkages with the adjacent molecules; W is -O- or CR 10 R 11 where R 10 and R 11 are as defined above; Y is an optionally substituted amino group, a moiety containing an optionally substituted amino group or a salt thereof: ------ is a single or double bond; R 7 and R 8a are hydrogen or are absent if ------ is a double bond; and R 8b and R 9 are hydrogen, and X is selected from (CR 10 R 11 ) u , -(CR 10 R 11 ) u -CH=CH-, -NR 12 (CR 10 R 11 ) u -, -(CR 10 R 11 ) u NR 12 -, -O(CR 10 R 11 ) u -, -(CR 10 R 11 ) u O- or -O(CR 10 R 11 )CH=CH- where R 10 , R 11 and R 12 are as defined above; or R 8b and R 9 together form a covalent bond between X and the carbon to which R 8b is attached, and X is selected from (CR 10 R 11 ) x , -NR 12 (CR 10 R 11 ) x -, -(CR 10 R 11 ) x NR 12 -, -O(CR 10 R 11 ) x - or -(CR 10 R 11 ) x O-, where R 10 , R 11 and R 12 are as defined above; n, m, r and t are independently selected from 0 or 1; s is an integer selected from 0 to 3; p is an integer selected from 0 to 6, provided that when W is -O-, p is at least 1; and u, x and q are independently selected from 0 to 4; and salts and pharmaceutically acceptable derivatives thereof. The compound of formula (I) are useful in the treatment of bacterial infections.

Inventors:
John Blemner
Steven Pine
Paul Keller
Dan Kofran
Adele Glass
Helen Witchard
Tim Boyle
Jonathan Coates
Application Number:
JP2003508926A
Publication Date:
February 17, 2005
Filing Date:
June 28, 2002
Export Citation:
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Assignee:
UNIVERSITY OF WOLLONGONG
International Classes:
A61K38/00; A61K38/06; A61K38/12; A61P31/04; C07C229/36; C07C233/31; C07C233/47; C07C237/22; C07C251/24; C07D209/18; C07D209/86; C07D209/88; C07D245/04; C07D255/04; C07D273/02; C07D273/08; C07D487/02; C07D487/04; C07K5/02; C07K5/068; C07K5/087; C07K5/107; (IPC1-7): C07K5/02; A61K38/00; A61P31/04; C07K5/087
Attorney, Agent or Firm:
Kyousei Tamura
Nagatoshi Shinagawa