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    • 8. 发明授权
      US06677354B2 Piperdines for use as orexin receptor antagonists 失效
    • Piperdines for use as orexin receptor antagonists
    • 用作食欲肽受体拮抗剂的Pi子
    • US06677354B2
    • 2004-01-13
    • US10311445
    • 2002-12-16
    • Clive Leslie Branch , Christopher Norbert Johnson , Geoffrey Stemp , Kevin Thewlis
    • Clive Leslie Branch , Christopher Norbert Johnson , Geoffrey Stemp , Kevin Thewlis
    • A61K314545
    • C07D401/06 , C07D211/26 , C07D401/10 , C07D405/06 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/04
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US06939871B2 Benzoxazinone derivatives, their preparation and use 失效
    • Benzoxazinone derivatives, their preparation and use
    • US06939871B2
    • 2005-09-06
    • US10415119
    • 2001-10-22
    • Christopher Norbert Johnson , Harshad Kantilal Rami , Geoffrey Stemp , Kevin Thewlis , Mervyn Thompson , Antonio Keuok Keong Vong
    • Christopher Norbert Johnson , Harshad Kantilal Rami , Geoffrey Stemp , Kevin Thewlis , Mervyn Thompson , Antonio Keuok Keong Vong
    • A61K31/538 , A61P25/00 , A61P25/22 , A61P25/24 , C07D413/12 , C07D413/14 , C07D413/10 , A61P25/18
    • C07D413/12 , C07D413/14
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 10. 发明申请
      US20070270471A1 Compounds Which Potentiate Glutamate Receptor and Uses Thereof in Medicine 审中-公开
    • Compounds Which Potentiate Glutamate Receptor and Uses Thereof in Medicine
    • US20070270471A1
    • 2007-11-22
    • US11573366
    • 2005-08-05
    • Kevin Thewlis , Simon Ward
    • Kevin Thewlis , Simon Ward
    • A61K31/40 , A61K31/4439 , A61P25/18 , C07D207/14 , C07D401/10
    • C07D207/14 , C07D403/10 , C07D409/10
    • This case discloses compounds of formula (I) wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; B is —N(R4)— or —O—; A and D, which may be the same or different, are —C(R5)2—; each R2, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; n is 0, 1 or 2; R3 is C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, —(CH2)pNR3aSO2R3b, —(CH2)pNR3a(C═O)R3b, —(CH2)pNR3a(C═O)N(R3c)2, —(CH2)p(C═O)R3d, —(CH2)pSO2R3e, phenyl or heterocyclyl, wherein when R3 is phenyl or heterocyclyl, it is optionally substituted by one or more groups independently selected from: C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, —(CH2)pNR3aSO2R3b, —(CH2)pNR3a(C═O)R3b, —(CH2)pNR3a(C═O)N(R3c)2, —(CH2)p(C═O)R3d and —(CH2)pSO2R3e; where R3a and each R3c, which may be the same or different, is hydrogen or C1-6alkyl; R3b and R3e are C1-6alkyl or haloC1-6alkyl; R3d is C1-6alkyl, C1-4alkoxy or haloC1-6alkyl; or R3a and R3b, or R3a and R3c, together with the interconnecting atoms, may form a 5- or 6-membered ring; and p is 0, 1, or 2; R4 is carbocyclyl or carbocyclylC1-4alkyl, wherein the carbocyclyl group of either is optionally substituted by one or more groups independently selected from C1-6alkyl and halogen; or R4 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkylcarbonyl, C1-6alkylsulfonyl or C1-6alkylaminocarbonyl; each R5, which may be the same or different, is hydrogen, C1-6alkyl or halogen; and R6 is hydrogen or fluorine.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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