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    PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES
    4.
    发明授权
    PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES 有权
    哌嗪取代的芳基苯并二氮杂

    公开(公告)号：EP1546134B1

    公开(公告)日：2007-05-02

    申请号：EP03784411.5

    申请日：2003-07-28

    申请人： ELI LILLY AND COMPANY

    发明人： AICHER, Thomas, Daniel ,  CHEN, Zhaogen House 10A, Phase V. Green Villa ,  LE HUEROU, Yvan ,  MARTIN, Fionna Mitchell Eli Lilly and Company Ltd. ,  PINEIRO-NUNEZ, Marta, Maria ,  ROCCO, Vincent, Patrick ,  RULEY, Kevin, Michael ,  SCHAUS, John, Mehnert ,  SPINAZZE, Patrick, Gianpietro ,  TUPPER, David Edward Eli Lilly and Company

    IPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61P25/18

    CPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04

    摘要： Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or -CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, N02, CN, COR4, C(O)OR4, CONR5R6 , NR5R6, S02NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen, (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyl is unsubsituted or substituted with a phenyl; R4 is hydrogen, (C1-6 alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treament of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).

    摘要翻译： 本文描述的是式（I）的化合物，其中：是任选苯并稠合的五元或六元芳族环，其具有0至3个独立地选自N，S和O的杂原子; Alk是（C1-4）亚烷基或羟基取代的（C1-4）亚烷基; X是氧或硫; （C 1-4）烷基是未取代的或被羟基，甲氧基，乙氧基，OCH 2 CH 2 OH或-CN取代的（C 1-4）烷基，（C 1-6）氟代烷基， ; （C1-6）氟代烷基，（C1-6）环烷基，OR4，SR4，NO2，CN，COR4，C（O）OR4，CONR5R6，NR5R6，SO2NR5R6，NR5COR4，NR5SO2R4，任选取代的芳族， 或（C 1-6）烷基，其中（C 1-6）烷基未被取代或被羟基取代; （C1-4）氟烷基，（C2-6）链烯基，Ar，（C1-4）烷基-Ar或（C1-4）烷基未被取代或被苯基取代的（C1-4） ; （C 1-6烷基，（C 1-6）氟烷基或任选取代的芳族基; R 5和R 6独立地为氢，（C 1-6）烷基或任选取代的芳族基团，R 7为氢，（C 1-6） 烷基，（C 1-6）氟烷基或任选取代的芳族基团; R 8和R 9独立地为氢，（C 1-6）烷基或任选取代的芳族基团; Ar为任选取代的苯基，萘基，单环杂芳族或双环杂芳族; Z 1和Z 2 （C 1-6）烷基，（C 1-6）氟烷基，OR 7，SR 7，NO 2，CN，COR 7，CONR 8 R 9，NR 8 R 9和任选取代的芳族基团;以及所有的盐，溶剂合物， （I）化合物作为多巴胺D2受体的拮抗剂的用途，以及作为治疗精神病和双相性精神障碍的药剂的用途，以及式（I）化合物的药物制剂 ）。

    PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES
    10.
    发明公开
    PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES 有权
    苯丙酸甲酯

    公开(公告)号：EP1546134A1

    公开(公告)日：2005-06-29

    申请号：EP03784411.5

    申请日：2003-07-28

    申请人： ELI LILLY AND COMPANY

    发明人： AICHER, Thomas, Daniel ,  CHEN, Zhaogen ,  LE HUEROU, Yvan ,  MARTIN, Fionna MitchellEli Lilly and Company Ltd. ,  PINEIRO-NUNEZ, Marta, Maria ,  ROCCO, Vincent, Patrick ,  RULEY, Kevin, Michael ,  SCHAUS, John, Mehnert ,  SPINAZZE, Patrick, Gianpietro ,  TUPPER, David EdwardEli Lilly and Company

    IPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61P25/18

    CPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04

    摘要： Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or -CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, N02, CN, COR4, C(O)OR4, CONR5R6 , NR5R6, S02NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen, (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyl is unsubsituted or substituted with a phenyl; R4 is hydrogen, (C1-6 alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treament of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).