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    Benzoxazinone derivatives, their preparation and use
    1.
    发明授权
    Benzoxazinone derivatives, their preparation and use 失效

    公开(公告)号：US06939871B2

    公开(公告)日：2005-09-06

    申请号：US10415119

    申请日：2001-10-22

    申请人： Christopher Norbert Johnson ,  Harshad Kantilal Rami ,  Geoffrey Stemp ,  Kevin Thewlis ,  Mervyn Thompson ,  Antonio Keuok Keong Vong

    发明人： Christopher Norbert Johnson ,  Harshad Kantilal Rami ,  Geoffrey Stemp ,  Kevin Thewlis ,  Mervyn Thompson ,  Antonio Keuok Keong Vong

    IPC分类号： A61K31/538 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  C07D413/12 ,  C07D413/14 ,  C07D413/10 ,  A61P25/18

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is phenyl, naphthyl, a monocyclic heteroaromatic group or a bicyclic heteroaromatic group, said Ar group being optionally substituted by 1-4 substituents, which may be the same or different, and which are selected from the group consisting of: halogen, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-6alkyl, trifluoromethanesulfonyloxy, pentafluoroethyl, C1-6alkoxy, arylC1-6alkoxy, C1-6alkylthio, C1-6alkoxyC1-6-alkyl, C3-7cycloalkylC1-6alkoxy, C1-6alkanoyl, C1-6alkoxycarbonyl, C1-6alkylsulfonyl, C1-6alkylsulfinyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonylC1-6alkyl, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-6alkyl, C1-6alkylsulfonamido, C1-6alkylamido, C1-6alkylsulfonamidoC1-6alkyl, C1-6alkylamidoC1-6alkyl, arylsulfonamido, arylcarboxamido, alkylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, arolC1-6alkyl, arylC1-6alkanoyl, a group R OCO(CH2)s, R CON(R )(CH2)s, R R NCO(CH2)s or R R NSO2(CH2) where each of R and R independently represents a hydrogen atom or C1-4alkyl or R and R form part of a C3-6azacyloalkane or C3-6(2-oxo)azacycloalkane ring and s represents zero or an integer from 1 to 4, and a group Ar Z, wherein Z represents a single bond, O, S or CH2 and Ar represents a phenyl or a monocyclic heteroaromatic group, said Ar group being optionally substituted by 1-3 substituents, which may be the same or different, and which are selected from the group consisting of a halogen, hydroxy, cyano, trifluoromethyl, C1-6alkyl, C1-6alkoxy or C1-6alkanoyl; when Ar is a phenyl or a monocyclic heteroaromatic group, substitutents positioned ortho to one another may be linked to form a 5- or 6-membered ring; R is hydrogen, C1-6alkyl, C3-6alkenyl, C3-6alkynyl or arylC1-6alkyl; R is halogen, C1-6alkyl, cyano, CF3, C1-6alkanoyl, C1-6alkoxy or hydroxy; X is CH or N; Y is a single bond, O, or C═O; p is 0, 1 or 2; r is 0, 1, 2 or 3; m is 2, 3 or 4; n and q are independently 1 or 2. Processes for preparing the compounds, pharmaceutical compositions containing them and their use as medicaments for various CNS disorders, including deression and/or anxiety, are also disclosed.

    N-aroyl cyclic amines
    6.
    发明授权
    N-aroyl cyclic amines 失效
    N-芳酰基环胺

    公开(公告)号：US07432270B2

    公开(公告)日：2008-10-07

    申请号：US10477008

    申请日：2002-05-02

    申请人： Clive Leslie Branch ,  Steven Coulton ,  Amanda Johns ,  Christopher Norbert Johnson ,  Roderick Alan Porter ,  Geoffrey Stemp ,  Kevin Thewlis

    发明人： Clive Leslie Branch ,  Steven Coulton ,  Amanda Johns ,  Christopher Norbert Johnson ,  Roderick Alan Porter ,  Geoffrey Stemp ,  Kevin Thewlis

    IPC分类号： A61K31/498 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

    摘要： This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3; m represents 1, 2, or 3; p represents ) or 1; X is NR, wherein R is H or (C1-4)alkyl; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; any of which may be optionally substituted; A2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R1 represents hydrogen, optionally substituted (C1-4)alkoxy, halo, cyano, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S; when Ar1 is aryl p is not 1, or a pharmaceutical acceptable salt thereof.

    摘要翻译： 本发明涉及N-芳酰基环胺衍生物及其作为食欲素拮抗剂的用途，其中：Y表示键，氧或基团（CH 2）n，其中n 代表1,2或3; m表示1,2或3; p表示）或1; X是NR，其中R是H或（C 1-4 - ）烷基; Ar 1是芳基或含有至多3个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; 代表苯基或含有至多3个选自N，O和S的杂原子的5或6元杂环基，其中苯基或杂环基被R 1取代， SUP>和另外任选的取代基; 或Ar 2表示含有至多3个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 1表示氢，任选取代的（C 1-4 - ）烷氧基，卤素，氰基，任选取代的（C 1-6 - ）烷基， 或任选取代的苯基，或任选取代的含有至多4个选自N，O和S的杂原子的5或6元杂环基; 当Ar 1是芳基p不为1时，或其药学上可接受的盐。

    Piperdines for use as orexin receptor antagonists
    7.
    发明授权
    Piperdines for use as orexin receptor antagonists 失效
    用作食欲肽受体拮抗剂的Pi子

    公开(公告)号：US06677354B2

    公开(公告)日：2004-01-13

    申请号：US10311445

    申请日：2002-12-16

    申请人： Clive Leslie Branch ,  Christopher Norbert Johnson ,  Geoffrey Stemp ,  Kevin Thewlis

    发明人： Clive Leslie Branch ,  Christopher Norbert Johnson ,  Geoffrey Stemp ,  Kevin Thewlis

    IPC分类号： A61K314545

    CPC分类号： C07D401/06 ,  C07D211/26 ,  C07D401/10 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04

    摘要： Disclosed are compounds of formula (I): wherein: Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered heteroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R5 represents an optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to 3 heteroatoms selected from N, O and S; or pharmaceutically acceptable salts thereof.

    摘要翻译： 公开了式（I）的化合物：其中：Y表示基团（CH 2）n，其中n表示0,1或2; R 1是苯基，萘基，含有至多3个选自杂原子的单或双环杂芳基 来自N，O和S; 或NR 3或R 4基团，其中R 3和R 4中的一个是氢或任选取代的（C 1-4）烷基，另一个是苯基，萘基或含有上述的单或双环杂芳基 至3个选自N，O和S的杂原子，或R 3和R 4与它们所连接的N原子一起形成具有任选稠合的苯环的5至7元环胺; 任何R 1可以任选被取代; R 2表示苯基或含有至多3个选自N，O和S的杂原子的5-或6-元杂芳基，其中苯基或杂芳基被取代 R 5和另外任选的取代基; 或R 2表示含有至多3个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 5表示任选取代的（C 1-4）烷氧基，卤素，任选取代的（C1- 6）烷基，任选取代的苯基或含有至多3个选自N，O和S的杂原子的任选取代的5或6元杂环; 或其药学上可接受的盐。