Title:
ペプトイド化合物
Document Type and Number:
Japanese Patent JP4446736
Kind Code:
B2
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
Steven Pine
Paul Keller
Dan Kofran
Adele Glass
Helen Witchard
Tim Boyle
Jonathan Coates
Application Number:
JP2003508926A
Publication Date:
April 07, 2010
Filing Date:
June 28, 2002
Export Citation:
Assignee:
UNIVERSITY OF WOLLONGONG
International Classes:
A61K38/00; C07K5/02; 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; C07K5/068; C07K5/087; C07K5/107
Other References:
Synlett.,2002年 2月,No.2,pp.219-222
J. Comb. Chem.,2001年 5月,Vol.3,pp.257-266
Chemistry: A European Journal,1999年,Vol.5, No.11,pp.3261-3272
J. Comb. Chem.,2001年 5月,Vol.3,pp.257-266
Chemistry: A European Journal,1999年,Vol.5, No.11,pp.3261-3272
Attorney, Agent or Firm:
Kyousei Tamura
Samejima Mutsumi
Masahiro Nitta
Nagatoshi Shinagawa
Samejima Mutsumi
Masahiro Nitta
Nagatoshi Shinagawa