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    PHARMACEUTICAL COMPOSITION CONTAINING BICYCLIC TYPE COMPOUNDS
    4.
    发明申请
    PHARMACEUTICAL COMPOSITION CONTAINING BICYCLIC TYPE COMPOUNDS 审中-公开
    含有双相类型化合物的药物组合物

    公开(公告)号：WO1994013657A1

    公开(公告)日：1994-06-23

    申请号：PCT/GB1993002513

    申请日：1993-12-08

    Applicant: SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM CORPORATION ,  CHAN, Wai, Ngor ,  EVANS, John, Morris ,  STEMP, Geoffrey ,  UPTON, Neil ,  WILLETTE, Robert, Nicholas

    Inventor： SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM CORPORATION

    IPC: C07D311/68

    CPC classification number: C07D409/06 ,  C07D311/68 ,  C07D409/12

    Abstract: A compound of formula (I) or pharmaceutically acceptable salt thereof wherein: either Y is N and R2 is hydrogen, or Y is C-R1 where: either one of R1 and R2 is hydrogen and the other is selected from the class of hydrogen, C3-8 cycloalkyl, C1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C1-6 alkoxy or substituted aminocarbonyl, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF3S, or a group CF3-A-, where A is -CF2-, -CO-, -CH2-, CH(OH), SO2, SO, CH2-O, or CONH, or a group CF2H-A'- where A' is oxygen, sulphur, SO, SO2, CF2 or CFH; trifluoromethoxy, C1-6 alkylsulphinyl, perfluoro C2-6 alkylsulphonyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl in which any aromatic moiety is optionally substituted, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, 1-mercapto C2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, any amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkylsulphinylamino, C1-6 alkylsulphonylamino, C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or -C(C1-6 alkyl)NOH or -C(C1-6 alkyl)NNH2, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C1-6 alkyl or by C2-7 alkanoyl; or R1 and R2 together are -(CH2)4- or -CH CH-CH CH-, or form an optionally substituted triazole or oxadiazole ring; and X is oxygen or NR10 where R10 is hydrogen or C1-6 alkyl with the proviso that the compound is not racemic cis-4-benzoylamino-6-cyano-3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3-ol.

    Abstract translation: 式（I）化合物或其药学上可接受的盐，其中：Y是N，R2是氢，或Y是C-R1，其中：R1和R2中的任一个是氢，另一个选自氢， C 3-6烷氧基，C 1-6烷氧基，硝基，氰基，C 1-6烷基， 卤素，三氟甲基，CF 3 S或基团CF 3 -A，其中A是-CF 2 - ， - CO - ， - CH 2 - ，CH（OH），SO 2，SO，CH 2 -O或CONH，或CF 2 H- A'-其中A'为氧，硫，SO，SO2，CF2或CFH; 三氟甲氧基，C 1-6烷基亚磺酰基，全氟C 2-6烷基磺酰基，C 1-6烷基磺酰基，C 1-6烷氧基亚磺酰基，C 1-6烷氧基磺酰基，芳基，杂芳基，芳基羰基，杂芳基羰基，膦酰基，芳基羰基氧基，杂芳基羰氧基，芳基亚磺酰基，杂芳基亚磺酰基，芳基磺酰基，杂芳基磺酰基 任何芳族部分任选被取代，C 1-6烷基羰基氨基，C 1-6烷氧基羰基氨基，C 1-6烷基 - 硫代羰基，C 1-6烷氧基 - 硫代羰基，C 1-6烷基 - 硫代羰基氧基，1-巯基C 2-7烷基，甲酰基或 氨基亚磺酰基，氨基磺酰基或氨基羰基，任选被一个或两个C 1-6烷基取代的氨基部分，或C 1-6烷基亚磺酰氨基，C 1-6烷基磺酰基氨基，C 1-6烷氧基亚磺酰氨基或C 1-6烷氧基磺酰基氨基，或被C 1 -C 6末端取代的亚乙基， 6烷基羰基，硝基或氰基或-C（C 1-6烷基）NOH或-C（C 1-6烷基）NNH 2，或R 1和R 2之一是硝基，氰基或C 1-3烷基羰基，另一个是甲氧基或氨基 可选地替代 d由一个或两个C 1-6烷基或C 2-7烷酰基取代; 或者R 1和R 2一起是 - （CH 2）4 - 或-CH 3 CH-CH，或形成任选取代的三唑或恶二唑环; 并且X是氧或NR 10，其中R 10是氢或C 1-6烷基，条件是该化合物不是外消旋的顺式-4-苯甲酰基氨基-6-氰基-3,4-二氢-2,2-二甲基-2H-苯并[ b]吡喃-3-醇。

    N-ARYL ACETYL CYCLIC AMINE DERIVATIVES AS OREXIN ANTAGONISTS
    6.
    发明申请
    N-ARYL ACETYL CYCLIC AMINE DERIVATIVES AS OREXIN ANTAGONISTS 审中-公开
    N-ARYL ACETYL循环胺衍生物作为OREXIN ANTAGONISTS

    公开(公告)号：WO2004041791A1

    公开(公告)日：2004-05-21

    申请号：PCT/EP2003/012407

    申请日：2003-11-04

    Applicant: GLAXO GROUP LIMITED ,  CHAN, Wai, Ngor ,  NASH, David, John ,  PORTER, Roderick, Alan ,  STEAD, Rachel, Elizabeth, Anne

    Inventor： CHAN, Wai, Ngor ,  NASH, David, John ,  PORTER, Roderick, Alan ,  STEAD, Rachel, Elizabeth, Anne

    IPC: C07D241/44

    CPC classification number: C07D401/12 ,  C07D405/14

    Abstract: The present invention provides N -aryl acetyl cyclic amine derivatives which are non-peptide antagonists of human orexin receptors, in particular orexin-1 receptors. In particular, theses compounds are of potential use in the treatment of obesity, including obesity observed in Type 2 (non-insulin-dependent) diabetes patients, and/or sleep disorders. Additionally these compounds are useful in the treatment of stroke, particularly ischemic or haemorrhagic stroke, and/or blocking the emetic response, i.e. useful in the treatment of nausea and vomiting. (I) wherein: Y represents a bond, oxygen, NQ or a group (CH 2 ) n , wherein n represents 1, 2 or 3 m is 0 or 1; X is NR, wherein R is H or (C 1-4 )alkyl; Q is H or (C 1-4 )alkyl; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar 2 represents optionally substituted phenyl, an optionally substituted 5- or 6- membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S, or an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 4 heteroatoms selected from N, O and S; R 1 and R 2 independently represent hydrogen, optionally substituted amino, optionally substituted (C 1-6 )alkyl or optionally substituted phenyl; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明提供作为人食欲素受体的非肽拮抗剂的N-芳基乙酰基环胺衍生物，特别是食欲素-1受体。 特别地，这些化合物可用于治疗肥胖症，包括在2型（非胰岛素依赖性）糖尿病患者中观察到的肥胖症和/或睡眠障碍。 另外，这些化合物可用于治疗中风，特别是缺血性或出血性中风，和/或阻断催吐反应，即可用于治疗恶心和呕吐。 （I）其中：Y表示键，氧，NQ或基团（CH 2）n，其中n表示1,2或3m为0或1; X是NR，其中R是H或（C 1-4）烷基; Q是H或（C 1-4）烷基; Ar 1是芳基或含有至多4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; Ar 2表示任选取代的苯基，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，或含有至多4个选自以下的杂原子的任选取代的双环芳族或双环杂芳族基团： N，O和S; R 1和R 2独立地表示氢，任选取代的氨基，任选取代的（C 1-6）烷基或任选取代的苯基; 或其药学上可接受的盐。

    BICYCLIC COMPOUNDS WITH PHARMACEUTICAL ACTIVITY
    7.
    发明申请
    BICYCLIC COMPOUNDS WITH PHARMACEUTICAL ACTIVITY 审中-公开
    具有药物活性的双环化合物

    公开(公告)号：WO1994013656A1

    公开(公告)日：1994-06-23

    申请号：PCT/GB1993002512

    申请日：1993-12-08

    Applicant: SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM CORPORATION ,  THOMPSON, Mervyn ,  EVANS, John, Morris ,  UPTON, Neil ,  CHAN, Wai, Ngor ,  VONG, Kuok, Keong ,  WILLETTE, Robert, Nicholas

    Inventor： SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM CORPORATION

    IPC: C07D311/68

    CPC classification number: C07D405/12 ,  C07D311/68 ,  C07D407/12 ,  C07D409/12

    Abstract: A method of treatment and/or prophylaxis of disorders resulting from subarachnoid haemorrhage, neural shock, cerebral ischaemia, Parkinson's Disease, migraine and/or psychosis, in mammals, especially humans which comprises administering to the sufferer in need thereof an effective or prophylactic amount of a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein either Y is N and R2 is hydrogen, or Y is C-R1 where either one of R1 and R2 is hydrogen and the other is selected from the class of hydrogen, C3-8 cycloalkyl, C1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C1-6 alkoxy or substituted aminocarbonyl, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF3S, or a group CF3-A-, or a group CF2H-A'-; trifluoromethoxy, C1-6 alkylsulphinyl, perfluoro C2-6 alkylsulphonyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl in which any aromatic moiety is optionally substituted, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, 1-mercapto C2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, any amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkylsulphinylamino, C1-6 alkylsulphonylamino, C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or -C(C1-6 alkyl)NOH or -C(C1-6 alkyl)NNH2, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino group; or R1 and R2 together are -(CH2)4- or -CH CH-CH CH-, or form an optionally substituted triazole or oxadiazole ring; and X is oxygen or NR10.

    Abstract translation: 一种治疗和/或预防哺乳动物，特别是人的蛛网膜下腔出血，神经性休克，脑局部缺血，帕金森病，偏头痛和/或精神病引起的疾病的方法，包括向有需要的患者施用有效或预防量的 式（I）化合物或其药学上可接受的盐，其中Y为N且R 2为氢，或Y为C-R 1，其中R 1和R 2中的任一个为氢，另一个选自氢，C 3 -8环烷基，任选被氧中断或被羟基取代的C 1-6烷基，C 1-6烷氧基或取代的氨基羰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰氧基，C 1-6烷氧基，硝基，氰基，卤素 ，三氟甲基，CF 3 S或CF 3 -A-或CF 2 H-A'-基团; 三氟甲氧基，C 1-6烷基亚磺酰基，全氟C 2-6烷基磺酰基，C 1-6烷基磺酰基，C 1-6烷氧基亚磺酰基，C 1-6烷氧基磺酰基，芳基，杂芳基，芳基羰基，杂芳基羰基，膦酰基，芳基羰基氧基，杂芳基羰氧基，芳基亚磺酰基，杂芳基亚磺酰基，芳基磺酰基，杂芳基磺酰基 任何芳族部分任选被取代，C 1-6烷基羰基氨基，C 1-6烷氧基羰基氨基，C 1-6烷基 - 硫代羰基，C 1-6烷氧基 - 硫代羰基，C 1-6烷基 - 硫代羰基氧基，1-巯基C 2-7烷基，甲酰基或 氨基亚磺酰基，氨基磺酰基或氨基羰基，任选被一个或两个C 1-6烷基取代的氨基部分，或C 1-6烷基亚磺酰氨基，C 1-6烷基磺酰基氨基，C 1-6烷氧基亚磺酰氨基或C 1-6烷氧基磺酰基氨基，或被C 1 -C 6末端取代的亚乙基， 6烷基羰基，硝基或氰基或-C（C 1-6烷基）NOH或-C（C 1-6烷基）NNH 2，或R 1和R 2之一是硝基，氰基或C 1-3烷基羰基，另一个是甲氧基或氨基 组; 或者R 1和R 2一起是 - （CH 2）4 - 或-CH 3 CH-CH，或形成任选取代的三唑或恶二唑环; X是氧或NR 10。

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