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    QUINOXALINEDIONE NMDA RECEPTOR ANTAGONISTS
    1.
    发明公开
    QUINOXALINEDIONE NMDA RECEPTOR ANTAGONISTS 失效
    QUINOXALINDION，NMDA受体拮抗剂

    公开(公告)号：EP0781279A1

    公开(公告)日：1997-07-02

    申请号：EP95931989.0

    申请日：1995-09-01

    申请人： Pfizer Limited ,  Pfizer Research and Development Company, N.V./S.A.

    发明人： MOWBRAY, Charles, Eric ,  STOBIE, Alan ,  BULL, David, John ,  CARR, Christopher, Lee ,  FRAY, Michael, Johnathan

    IPC分类号： C07D401 ,  A61K31 ,  A61P25 ,  A61P43 ,  C07D403

    CPC分类号： C07D403/06

    摘要： Compounds of formula (I) wherein R?1 and R2¿ are each independently F, Cl, Br, CH¿3?, CH2CH3 or CF3; R?3¿ is H, CH¿3? or CH2CH3; and X is a 5-membered heterocyclic group containing up to four nitrogen atoms, attached via a nitrogen atom, the said group being optionally benzofused and/or substituted by C1-C6 alkyl or (CH2)nNR?4R5¿, wherein n is an integer from 1 to 5 and R?4 and R5¿ are each independently H, C¿1?-C6 alkyl, C3-C6 cycloalkyl or C1-C4 alkyl substituted by phenyl or pyridyl, or R?4 and R5¿ are linked to form, together with the nitrogen atom to which they are attached, a pyrrolidine, piperidine, piperazine, N-(C¿1?-C4 alkyl) piperazine, morpholine or azepine group; and their pharmaceutically acceptable salts, are NMDA antagonists of utility in the treatment of acute neurodegenerative disorders, e.g. arising from stroke or traumatic head injury and in chronic neurological disorders, e.g. senile dementia and Alzheimer's disease.

    QUINOXALINEDIONE NMDA RECEPTOR ANTAGONISTS
    3.
    发明授权
    QUINOXALINEDIONE NMDA RECEPTOR ANTAGONISTS 失效
    喹唑啉酮 - NMDA反应物

    公开(公告)号：EP0781279B1

    公开(公告)日：2001-06-13

    申请号：EP95931989.8

    申请日：1995-09-01

    申请人： Pfizer Limited ,  Pfizer Research and Development Company, N.V./S.A.

    发明人： MOWBRAY, Charles, Eric ,  STOBIE, Alan ,  BULL, David, John ,  CARR, Christopher, Lee ,  FRAY, Michael, Johnathan

    IPC分类号： C07D403/06 ,  A61K31/495 ,  A61P25/28

    CPC分类号： C07D403/06

    摘要： Compounds of formula (I) wherein R?1 and R2¿ are each independently F, Cl, Br, CH¿3?, CH2CH3 or CF3; R?3¿ is H, CH¿3? or CH2CH3; and X is a 5-membered heterocyclic group containing up to four nitrogen atoms, attached via a nitrogen atom, the said group being optionally benzofused and/or substituted by C1-C6 alkyl or (CH2)nNR?4R5¿, wherein n is an integer from 1 to 5 and R?4 and R5¿ are each independently H, C¿1?-C6 alkyl, C3-C6 cycloalkyl or C1-C4 alkyl substituted by phenyl or pyridyl, or R?4 and R5¿ are linked to form, together with the nitrogen atom to which they are attached, a pyrrolidine, piperidine, piperazine, N-(C¿1?-C4 alkyl) piperazine, morpholine or azepine group; and their pharmaceutically acceptable salts, are NMDA antagonists of utility in the treatment of acute neurodegenerative disorders, e.g. arising from stroke or traumatic head injury and in chronic neurological disorders, e.g. senile dementia and Alzheimer's disease.

    QUINOXALINEDIONES
    6.
    发明公开
    QUINOXALINEDIONES 失效

    公开(公告)号：EP0885212A1

    公开(公告)日：1998-12-23

    申请号：EP97908156.0

    申请日：1997-02-27

    申请人： Pfizer Research and Development Company, N.V./S.A.

    发明人： BULL, David, John ,  CARR, Christopher, Lee ,  FRAY, Michael, Jonathan ,  GAUTIER, Elisabeth, Colette, Louise ,  MOWBRAY, Charles, Eric ,  STOBIE, Alan

    IPC分类号： A61K31 ,  A61P25 ,  A61P43 ,  C07D241 ,  C07D401 ,  C07D403 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D521

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： The invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is a 5-membered ring heteroaryl group containing 3 or 4 nitrogen heteroatoms which is linked to the quinoxalinedione ring by a ring carbon or nitrogen atom, or is a 6-membered ring heteroaryl group containing from 1 to 3 nitrogen heteroatoms which is linked to the quinoxalinedione ring by a ring carbon atom, either of said groups being optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by 1 or 2 substituents each independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, C3-C7 cycloalkyloxy, -COOH, C1-C4 alkoxycarbonyl, -CONR?3R4, -NR3R4¿, -S(O)¿p?(C1-C4 alkyl), -SO2NR?3R4¿, aryl, aryloxy, aryl(C¿1?-C4)alkoxy and het, said C1-C4 alkyl being optionally substituted by C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, halo(C1-C4)alkoxy, C3-C7 cycloalkyloxy, C3-C7 cycloalkyl(C1-C4)alkoxy, -COOH, C1-C4 alkoxycarbonyl, -CONR?3R4, -NR3R4¿, -S(O)¿p?(C1-C4 alkyl), -SO2(aryl), -SO2NR?3R4¿, morpholino, aryl, aryloxy, aryl(C¿1?-C4)alkoxy or het, and said C2-C4 alkenyl being optionally substituted by aryl; R?1 and R2¿ are each independently selected from H, fluoro, chloro, bromo, C¿1?-C4 alkyl and halo(C1-C4)alkyl; R?3 and R4¿ are either each independently selected from H and C¿1?-C4 alkyl or, when taken together, are C5-C7 alkylene; p is 0, 1 or 2; together with the preparation of, compositions containing, the uses of and intermediates used in the synthesis of, such compounds. The compounds are useful as NMDA receptor antagonists for treating acute neurodegenerative and chronic neurological disorders.

    摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，其中R为含有3或4个氮杂原子的5元环杂芳基，其通过环碳或氮原子与喹喔啉二酮环连接，或为 含有1至3个氮杂原子的6元环杂芳基基团，其通过环碳原子与喹喔啉二酮环连接，所述基团中的任一个任选被苯并稠合并且任选被取代，包括在苯并稠合部分中被1或 2个各自独立选自C 1 -C 4烷基，C 2 -C 4烯基，C 3 -C 7环烷基，卤素，羟基，C 1 -C 4烷氧基，C 3 -C 7环烷氧基，-COOH，C 1 -C 4烷氧基羰基，-CONR 3 R 4，-NR 3 R 4 （C 1 -C 4烷基）， - SO 2 NR 3 R 4，芳基，芳氧基，芳基（C 1 -C 4）烷氧基和het，所述C 1 -C 4烷基任选被C 3 （C 1 -C 4）烷氧基，C 3 -C 7环烷氧基，C 3 -C 7环烷基（C 1 -C 4）烷氧基，-COOH，C 1 -C 4卤代烷基， 烷氧基羰基，-CONR 3 R 4，-NR 3 R 4，-S（O） - ，（C 1 -C 4烷基），-SO 2（芳基），-SO 2 NR 3 R 4，吗啉代，芳基，芳氧基， -C4）烷氧基或het，并且所述C2-C4烯基任选被芳基取代; R 1和R 2各自独立地选自H，氟，氯，溴，C 1 -C 4烷基和卤代（C 1 -C 4）烷基; R 3和R 4'各自独立地选自H和C 1 -C 4烷基，或者当合在一起时为C 5 -C 7亚烷基; p是0,1或2; 以及含有这些化合物的合成中所使用的中间体和用途的组合物的制备。 该化合物可用作治疗急性神经变性和慢性神经疾病的NMDA受体拮抗剂。

    MORPHOLINE COMPOUNDS
    7.
    发明公开
    MORPHOLINE COMPOUNDS 审中-公开
    吗啉化合物

    公开(公告)号：EP1744754A1

    公开(公告)日：2007-01-24

    申请号：EP05733458.3

    申请日：2005-04-20

    申请人： Pfizer Limited ,  Pfizer, Inc.

    发明人： FISH, Paul Vincent ,  MACKENNY, Malcolm Christian ,  STOBIE, Alan ,  WAKENHUT, Florian ,  WHITLOCK, Gavin Alistair

    IPC分类号： A61K31/535

    CPC分类号： C07D413/06 ,  A61K31/535 ,  C07D265/30 ,  C07D413/12

    摘要： The present invention provides compounds of Formula I: wherein R1, R2, R3, and n have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of conditions including urinary disorders, pain, premature ejaculation, ADHD and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.

    摘要翻译： 本发明提供式I化合物：其中R 1，R 2，R 3和n具有说​​明书中定义的任何值，及其药学上可接受的盐，其可用作治疗包括泌尿疾病，疼痛， 早泄，多动症和纤维肌痛。 还提供了包含一种或多种式I化合物的药物组合物。

    LACTAMS AS TACHYKININ ANTAGONISTS
    8.
    发明公开
    LACTAMS AS TACHYKININ ANTAGONISTS 审中-公开
    内酰胺ALS TACHYKININANTAGONISTEN

    公开(公告)号：EP1456200A1

    公开(公告)日：2004-09-15

    申请号：EP02804985.6

    申请日：2002-12-06

    申请人： Pfizer Limited ,  PFIZER INC.

    发明人： MIDDLETON, Donald Stuart ,  STOBIE, Alan

    IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D491/10 ,  C07D405/14 ,  C07D413/14 ,  A61K31/4545 ,  A61P13/10

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D405/14 ,  C07D413/14 ,  C07D491/10

    摘要： Compounds of the formula (I) or a pharmaceutically acceptable salt, prodrug, solvate or polymorph thereof, wherein: R is heta; R1 is phenyl optionally substituted by one or more substituents; m is 1-4; Z is selected from: a) N(R3)(R4X) wherein X is NR?3R5, OR5, Oaryl1, Ohetb, Ohetc, aryl1, hetb or hetc¿; b) N(R3)Y wherein Y is aryl?1, hetb or hetc¿; and c) a 4-7 membered N containing saturated or partially saturated heterocycle said heterocycle attached to the alkylene link via said nitrogen atom, said heterocycle optionally containing an additional 1-3 groups, each independently selected from C=O, NH, S(O)¿p? and O; optionally, said heterocycle is: (i) spirofused with het?b¿, such that both rings share 1 atom; or (ii) optionally independently substituted by 1-3 groups; wherein R?3 and R6¿ are both independently selected from H and C¿1-6?alkyl; wherein R?4¿ is selected from C¿1-6? alkylene; wherein R?5¿ is selected from C(O)OR3, S(O)¿pR?3, S(O)¿p?aryl?1, C(O)R3¿, and C(O)NR?3R6; hetb¿ is a 4-7 membered heterocycle containing 1-3 heteroatoms, each independently selected from N, O and S, said N being optionally substituted with O, said ring optionally containing 1-2 C=O groups, said ring being saturated or partially saturated, said ring being optionally benzofused, said ring being optionally substituted by 1-3 substituents; heta and hetc are a 5-7 membered aromatic heterocycle containing 1-3 heteroatoms each independently selected from N, O and S, said ring being optionally benzofused, said ring system as a whole being optionally substituted by 1-3 substituents; aryl1 is phenyl or naphthyl, each being optionally substituted by 1-3 substituents; p is 0, 1 or 2; and n is 0-4; are useful in treating or preventing a condition for which an NK¿2? antagonist is efficacious.