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    OSTEOPOROSIS REMEDY AND TRIAZEPINE COMPOUND
    4.
    发明公开
    OSTEOPOROSIS REMEDY AND TRIAZEPINE COMPOUND 失效
    OSTEOPOROSIS-MEDIKAMENT UND TRIAZEPINVERBINDUNG

    公开(公告)号：EP0792880A1

    公开(公告)日：1997-09-03

    申请号：EP95938016.3

    申请日：1995-11-15

    Applicant: Japan Tobacco Inc.

    Inventor： NAKAMURA, Takeshi, Central Phar. Res. Ins. of ,  KOGA, Yoshihisa, Central Phar. Res. Ins. of Japan ,  SHINDO, Masanori, Central Phar. Res. Ins. of Japan

    IPC: C07D487/04 ,  C07D495/14 ,  C07D495/04 ,  C07D255/04 ,  C07D401/06 ,  C07D409/12 ,  A61K31/55

    CPC classification number: C07D401/06 ,  C07D255/04 ,  C07D487/04 ,  C07D495/04 ,  C07D495/14

    Abstract: Therapeutic agents for osteoporosis comprising, as an active ingredient, a triazepine compound of the formula [I]
    wherein R 1 is aryl or heteroaryl; R 2 is hydrogen atom, hydroxy, halogen atom or lower alkyl; R 4 is hydrogen atom or halogen atom, or R 2 and R 4 form carbonyl combinedly together with the carbon atom to which they bond; R 3 is hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, -X-Y wherein X is -(CH 2 ) m -, -CO-, -COCH 2 -, -NH-, -NHCH 2 -, -CH 2 NH-, -CH 2 NHCO-, -OCH 2 -, -(CH 2 ) n O- or -CH 2 S- and Y is halogen atom, cycloalkyl, aryl or heteroaryl; and A is benzene ring or thiophene ring, or a salt thereof, novel triazepine compounds, and intermediate triazepine compounds for producing these triazepine compounds. The triazepine compounds of the formula [I] have superior bone resorption-inhibitory action and are useful as therapeutic agents for osteoporosis.

    Abstract translation: 用于骨质疏松症的治疗剂包括作为活性成分的下式的三氮化合物其中R 1为芳基或杂芳基; R 2是氢原子，羟基，卤素原子或低级烷基; R 4是氢原子或卤素原子，或者R 2和R 4与它们键合的碳原子一起形成羰基; R 3是氢原子，低级烷基，低级烷氧基，环烷基，芳基，杂芳基，-XY，其中X是 - （CH 2）m - ， - CO - ， - COCH 2 - ， - NH - ， - NHCH 2 - ， - CH 2 NH - ， - CH 2 NHCO - ， - OCH 2 - ， - （CH 2）n O-或-CH 2 S-，Y是卤素原子，环烷基，芳基或杂芳基; A是苯环或噻吩环，或其盐，新的三氮化合物和用于制备这些三氮化合物的中间体三氮化合物。 式ÄIÜ的三氮化合物具有优异的骨吸收抑制作用，可用作骨质疏松症的治疗剂。

    Peptoid compounds
    10.
    发明公开
    Peptoid compounds 有权
    拟肽连接

    公开(公告)号：EP2343285A3

    公开(公告)日：2011-08-10

    申请号：EP11158209.4

    申请日：2002-06-28

    Applicant: UNIVERSITY OF WOLLONGONG

    Inventor： Bremner, John ,  Pyne, Stephen ,  Keller, Paul ,  Coghlan, Dan ,  Garas, Adel ,  Witchard, Helen ,  Boyle, Tim ,  Coates, Jonathan

    IPC: C07D245/04 ,  C07D255/04 ,  C07D273/08 ,  C07D273/02 ,  C07D487/02 ,  C07D209/18 ,  C07D209/88 ,  C07C233/31 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  A61K38/12 ,  A61K38/06 ,  A61P31/04 ,  C07D209/86 ,  C07D487/04 ,  C07C229/36 ,  C07C233/47 ,  C07C237/22 ,  C07C251/24

    CPC classification number: C07C229/36 ,  A61K38/00 ,  C07C233/47 ,  C07C237/22 ,  C07C251/24 ,  C07C279/14 ,  C07D209/86 ,  C07D245/04 ,  C07D255/04 ,  C07D273/02 ,  C07D487/04 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/0812 ,  C07K5/1016

    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 α side chains of α-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 α-amino acid residue, a β-amino acid residue or an α,α-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.

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