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    • 2. 发明申请
    • BENZOTHIOPHENES AND RELATED COMPOUNDS AS ESTROGEN AGONISTS
    • 苯并噻唑和相关化合物作为雌激素激动剂
    • WO1995010513A1
    • 1995-04-20
    • PCT/IB1994000282
    • 1994-09-19
    • PFIZER INC.CAMERON, Kimberly, O.DA SILVA-JARDINE, PaulLARSON, Eric, R.HAUSKE, James, R.ROSATI, Robert, L.
    • PFIZER INC.
    • C07D333/56
    • C07D231/12C07D233/56C07D249/08C07D333/56C07D409/04C07D409/06C07D409/12C07D417/04
    • Benzothiophenes and related compounds of formula (1), wherein A, B, Z are independently -CH=, -CR4= or =N-; X is -S-, -O-, -NH-, -NR2, -CH2-CH2-, -CH2-CH2-CH2-, -CH2-O-; -OCH2-, -CH2-S-, -CO-, -SCH2-, -N=CR2- or -R2C=N-; Y is optionally substituted phenyl, alkyl, cycloalkyl, cycloalkenyl, heterocycle or bicyclic ring system; D is -CO-, -CR2R3-, -CONH-, -NHCO-, -CR2(OH)-, -CONR2, NOR1 CH-NO2 N-CN -NR2-CO-, -C-, -C-, -C-; E is a single bond, optionally substituted phenyl, heterocycle; Z is -(CH2)p W(CH2)q-, -O(CH2)p CR5R6- or -O(CH2)p W(CH2)q; G is -NR7R8, (a), (b), (c), a 5- or 6-membered saturated, unsaturated or partially unsaturated and optionally substituted heterocycle or a bicyclic amine containing 5 to 12 carbon atoms either bridged or fused and optionally substituted and R is halogen, -NR2R3, -NHCOR2, -NHSO2R2, -CR2R3OH, -CONR2R3, -SO2NR2R3, OH, -OR1, -O-COR1; are estrogen agonists which are useful for treating syndromes and diseases caused by estrogen deficiency.
    • 苯并噻吩和式(1)的相关化合物,其中A,B,Z独立地是-CH =,-CR 4 =或= N-; X是-S-,-O-,-NH-,-NR2,-CH2-CH2-,-CH2-CH2-CH2-,-CH2-O-; -OCH 2 - , - CH 2 -S-,-CO-,-SCH 2 - , - N = CR 2 - 或-R 2 C = N-; Y是任选取代的苯基,烷基,环烷基,环烯基,杂环或双环系统; D是-CO - , - CR 2 R 3 - , - CONH - , - NHCO-, - CR 2(OH) - , - CONR 2,NOR 1 CH-NO 2 N-CN -NR 2 -CO-, - C - , - C-; E是单键,任选取代的苯基,杂环; Z 1是 - (CH 2)p W(CH 2)q - , - O(CH 2)p CR 5 R 6 - 或-O(CH 2)p W(CH 2)q; G是-NR 7 R 8,(a),(b),(c),5或6元饱和,不饱和或部分不饱和和任选取代的杂环或含有5至12个碳原子的双环胺,其桥接或稠合, 取代的,R是卤素,-NR2R3,-NHCOR2,-NHSO2R2,-CR2R3OH,-CONR2R3,-SO2NR2R3,OH,-OR1,-O-COR1; 是雌激素激动剂,其可用于治疗由雌激素缺乏引起的综合征和疾病。