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标题翻译：三唑类化合物用于治疗脑损伤

公开(公告)号：WO2004037809A1

公开(公告)日：2004-05-06

申请号：PCT/IB2003/004587

申请日：2003-10-14

申请人： PFIZER LIMITED , PFIZER INC. , ARMOUR, Robert, Duncan , BAXTER, Andrew, Douglas , BRYANS, Justin, Stephen , DACK, Kevin, Neil , JOHNSON, Patrick, Stephen , LEWTHWAITE, Russell, Andrew , NEWMAN, Julie , RAWSON, David, James , RYCKMANS, Thomas

发明人： ARMOUR, Robert, Duncan , BAXTER, Andrew, Douglas , BRYANS, Justin, Stephen , DACK, Kevin, Neil , JOHNSON, Patrick, Stephen , LEWTHWAITE, Russell, Andrew , NEWMAN, Julie , RAWSON, David, James , RYCKMANS, Thomas

IPC分类号： C07D401/04

CPC分类号： C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14

摘要： A compound of formula (I), a pharmaceutically acceptable salt or solvate thereof, wherein R' represents C,-C6 alkyl, -(CH 2 ) c -[C 3 -C 8 cycloalkyl]-, -(CH 2 ) C -W or -(CH 2 ) C -Z-(CH 2 ) d W; W represents C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, -C0 2 [C 1 -C 6 alkyl], -CONR 4 R 5 , an optionally substituted phenyl group, NR 4 R 5 , het 2 or het 3 ; Z represents O or S(O) g ; g represents 0, 1 or 2; R 2 represents a phenyl group, optionally fused to a 5- or 6- membered aryl or heterocyclic group which may contain one or more heteroatoms selected from N, O or S; the phenyl group and the optionally fused group being optionally substituted; Ring A represents a 4-, 5- or 6- membered saturated heterocyclic group containing at least one N; Ring B represents a phenyl group or het 1 , each group being optionally substituted; R 7 independently represents H 1 C 1 -C 6 alkyl, OR 3 , -(CH 2 ) e -R 3 or -(CH 2 ) f -O-(CH 2 ) e -R 3 ; at each occurrence R 3 independently represents H 1 C 1 -C 6 alkyl optionally substituted by Y, -(CH 2 ) g [C 3 -C 8 cycloalkyl], phenyl, benzyl, pyridyl or pyrimidyl; at each occurrence R 4 and R 5 independently represent H 1 C l -C 6 alkyl (optionally substituted with C l -C 6 alkyloxy), (CH 2 ) g C0 2 -[C 1 -C 6 alkyl], -S0 2 Me, -(CH 2 ) g [C 3 -C 8 cycloalkyl], S0 2 Me, phenyl, benzyl, pyridyl or pyrimidyl; or R 4 and R 5 together with the N atom to which they are attached represent a heterocyclic group of from 3 to 8 atoms; Y independently represents a phenyl group, NR 4 R 5 or het 4 , the phenyl group being optionally substituted; het 1 represents a 4-, 5- or 6- membered saturated, or unsaturated, heterocyclic group containing at least one N (but which may also contain one or more O or S atoms); het 2 and het 4 represent an optionally substituted 4-, 5-, 6- or 7- membered saturated, or unsaturated, heterocyclic group containing at least one N (but which may 5 also contain one or more O or S atoms); het3 represents an optionally substituted 4-, 5-, 6- or 7- membered saturated, or unsaturated, heterocyclic group containing at least one O (but which may also contain one or mare N or S atoms); at each occurrence R 6 independently represents H 1 C 1 -C 6 alkyl optionally substituted by Y, =(CH 2 ) g [C 3 -C 8 cycloalkyl], phenyl, benzyl, pyridyl or pyrimidyl; a and b independently represent 0 or 1; c,, d, a end g independently represent 0, 1, 2, 3 or 4; . f índeperldently represents 1, 2, 3 or 4; provided that: (i) a + b cannot equal 0; and províded,that,when R 1 represents -(CH 2 ) c -Z-(CH 2 ) d -W and W represents.NR 4 R 5 or any N linked heterocyclic, group then d must not be, 0 or 1; and (iii), provided that when R 2 represents a phenyl group substituted by a group of, formula -(CH 2 ) e OR 3 , -(CH 2 ) e -OCOR 3 or -(CH 2 ) e ,OCOR 3 ;or het 1 ,and/or het 2 are substituted by a group of formula -(CH 2 ) e OR 3 , (CH 2 ),-CO 2 R 3 or -(CH 2 ) e OCOR 3 ; or when R 7 represents -OR 3 or -(CH 2 ) f -0-(CH 2 ) e -R 3 and e is 0; or when W represents a phenyl group substituted with -OR 3 or - C0 2 R 3 and R 3 represents an alkyl group substituted with Y, and Y represents NR 4 R 5 or an N-Finked het 3 ; then, R 3 , must,represent,C 2 -C 6 alkyl substituted with. Y. are useful in the treatment of dysmenorrhoea.

摘要翻译：式（I）化合物，其药学上可接受的盐或溶剂化物，其中R'表示C 1-6烷基， - （CH 2）c - [C 3 -C 8环烷基] - ， - （CH 2）C-W或 - （ CH2）CZ-（CH 2）一页; W表示C1-C6烷基，C1-C6烷氧基，-CO2 [C1-C6烷基]，-CONR4R5，任选取代的苯基，NR4R5，het2，或het <3>; Z表示O或S（O）g; g表示0,1或2; R 2表示苯基，任选地与可含有一个或多个选自N，O或S的杂原子的5-或6-元芳基或杂环基稠合; 苯基和任选稠合基团任选被取代; 环A表示含有至少一个N的4-，5-或6-元饱和杂环基; 环B表示苯基或het 1，每个基团任选被取代; R 7独立地表示H 1 C 1 -C 6烷基，OR 3， - （CH 2）e -R 3或 - （CH 2）f -O-（CH 2）e -R 3; 在每次出现时，R 3独立地表示任选被Y， - （CH 2）g [C 3 -C 8环烷基]，苯基，苄基，吡啶基或嘧啶基取代的H 1 C 1 -C 6烷基; 在每次出现时，R 4和R 5独立地表示H 1 C 1 -C 6烷基（任选被C 1 -C 6烷氧基取代），（CH 2）g CO 2 - [C 1 -C 6烷基]，-SO 2 Me， - （CH 2） C 3 -C 8环烷基]，SO 2 Me，苯基，苄基，吡啶基或嘧啶基; 或R 4和R 5与它们所连接的N原子一起表示3至8个原子的杂环基; Y独立地表示苯基，NR4R5或het4，苯基任选被取代; 表示含有至少一个N（但也可含有一个或多个O或S原子）的4-，5-或6-元饱和或不饱和杂环基; het 2和het 4代表任选被取代的含有至少一个N（但也可以含有一个或多个O或S的N，R 5，R 6，原子）; het3表示含有至少一个O（但也可含有一个或多个N或S原子）的任选取代的4-，5-，6-或7-元饱和或不饱和杂环基; 在每次出现时，R 6独立地表示任选被Y，=（CH 2）g [C 3 -C 8环烷基]，苯基，苄基，吡啶基或嘧啶基取代的H 1 C 1 -C 6烷基; a和b独立地表示0或1; c，d，末端g独立地表示0,1,2,3或4; 。 f，并且代表1,2,3或4; 条件是：（i）a + b不能等于0; 并证明当R 1表示 - （CH 2）c

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