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    BENZOXAZINONE DERIVATIVES, THEIR PREPARATION AND USE
    46.
    发明申请
    BENZOXAZINONE DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
    苯并恶嗪酮衍生物及其制备和使用

    公开(公告)号：WO0234754A3

    公开(公告)日：2002-07-11

    申请号：PCT/EP0112344

    申请日：2001-10-22

    Applicant: SMITHKLINE BEECHAM PLC ,  JOHNSON CHRISTOPHER NORBERT ,  RAMI HARSHAD KANTILAL ,  STEMP GEOFFREY ,  THEWLIS KEVIN ,  THOMPSON MERVYN ,  VONG ANTONIO KUOK KEONG

    Inventor： JOHNSON CHRISTOPHER NORBERT ,  RAMI HARSHAD KANTILAL ,  STEMP GEOFFREY ,  THEWLIS KEVIN ,  THOMPSON MERVYN ,  VONG ANTONIO KUOK KEONG

    IPC: A61K31/538 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  C07D413/12 ,  C07D413/14 ,  C07D498/00 ,  A61K31/445

    CPC classification number: C07D413/12 ,  C07D413/14

    Abstract: 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, C1-6alkoxyC1-6alkyl, 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, arylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, aroylC1-6alkyl, 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 pheyl 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, substitutens 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.

    Abstract translation: 本发明涉及式（I）的新化合物或其药学上可接受的盐，其中Ar为苯基，萘基，单环杂芳基或双环杂芳基，所述Ar基团任选被1-4个取代基取代，所述取代基可以 它们选自卤素，羟基，氰基，硝基，三氟甲基，三氟甲氧基，C1-6烷基，三氟甲磺酰氧基，五氟乙基，C1-6烷氧基，芳基C1-6烷氧基，C1-6烷硫基，C1- C 1-6烷基磺酰基，C 1-6烷基磺酰氧基，C 1-6烷基磺酰基C 1-6烷基，芳基磺酰基，芳基磺酰氧基，芳基磺酰基C 1-6烷基，C 1-6烷基磺酰氨基，C 1-6烷氧基C 1-6烷氧基， C 1-6烷基酰氨基C 1-6烷基，芳基磺酰氨基，芳基甲酰氨基，芳基磺酰氨基C 1-6烷基，芳基甲酰氨基C 1-6烷基，芳酰基，芳酰基C 1-6烷基，芳基C 1-6烷酰基，基团R 3 OCO（CH 2） R 3 CON（R 4）（CH 2）s，R 3 R 4 NCO（CH 2）s或R 3 R 4 NSO 2（CH 2），其中R 3和 R 4独立地表示氢原子或C 1-4烷基，或者R 3和R 4形成C 3-6氮杂环烷烃或C 3-6（2-氧代）氮杂环烷烃环的一部分，并且s表示0或1的整数 其中Z表示单键，O，S或CH 2且Ar 1表示苯基或单环杂芳族基团，所述Ar 1基团任选被1至4个碳原子取代， 3个取代基，其可以相同或不同，并且选自卤素，羟基，氰基，三氟甲基，C 1-6烷基，C 1-6烷氧基或C 1-6烷酰基; 当Ar是苯基或单环杂芳族基团时，位于彼此邻位的取代基可以连接形成5-或6-元环; R 1是氢，C 1-6烷基，C 3-6烯基，C 3-6炔基或芳基C 1-6烷基; R 2是卤素，C 1-6烷基，氰基，CF 3，C 1-6烷酰基，C 1-6烷氧基或羟基; X是CH或N; Y是单键，O或C = O; p是0,1或2; r是0,1,2或3; m是2,3或4; n和q独立地为1或2.还公开了制备该化合物的方法，含有它们的药物组合物以及它们作为各种CNS病症（包括抑郁症和/或焦虑症）的药物的用途。

    BENZOXAZINONE DERIVATIVES, THEIR PREPARATION AND USE
    47.
    发明申请
    BENZOXAZINONE DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
    苯并恶嗪衍生物，其制备和使用

    公开(公告)号：WO02034754A2

    公开(公告)日：2002-05-02

    申请号：PCT/EP2001/012344

    申请日：2001-10-22

    IPC: A61K31/538 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  C07D413/12 ,  C07D413/14 ,  C07D498/00

    CPC classification number: C07D413/12 ,  C07D413/14

    Abstract: 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, C1-6alkoxyC1-6alkyl, 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, arylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, aroylC1-6alkyl, 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 pheyl 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, substitutens 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.

    Abstract translation: 本发明涉及新的式（I）化合物或其药学上可接受的盐，其中Ar为苯基，萘基，单环杂芳族基团或双环杂芳族基团，所述Ar基团任选被1-4个取代基取代， 选自卤素，羟基，氰基，硝基，三氟甲基，三氟甲氧基，C 1-6烷基，三氟甲磺酰氧基，五氟乙基，C 1-6烷氧基，芳基C 1-6烷氧基，C 1-6烷硫基，C 1 -C 6烷氧基， 6-烷氧基C 1-6烷基，C 3-7环烷基C 1-6烷氧基，C 1-6烷酰基，C 1-6烷氧基羰基，C 1-6烷基磺酰基，C 1-6烷基亚磺酰基，C 1-6烷基磺酰氧基，C 1-6烷基磺酰基C 1-6烷基，芳基磺酰基，芳基磺酰氧基，芳基磺酰基C 1-6烷基，C 1-6烷基磺酰氨基， C 1-6烷基酰氨基C 1-6烷基，C 1-6烷基氨基C 1-6烷基，芳基磺酰氨基，芳基羧酰胺基，芳基亚磺酰氨基C 1-6烷基，芳基羧酰胺基C 1-6烷基，芳酰基，芳酰基C 1-6烷基，芳基C 1-6烷酰基，R 3 OCO（CH 2） R 3 CON（R 4）（CH 2）s，R 3 R 4 NCO（CH 2）s或R 3 R 4 NSO 2（CH 2）其中R 3和 R 4独立地表示氢原子或C 1-4烷基或R 3和R 4形成C3-6氮杂环烷或C3-6（2-氧代）氮杂环烷烃环的一部分，s表示0或1的整数 其中Z表示单键，O，S或CH 2，Ar 1表示苯乙烯基或单环杂芳族基团，所述Ar 1基团任选被1- 3个取代基，其可以相同或不同，并且选自卤素，羟基，氰基，三氟甲基，C 1-6烷基，C 1-6烷氧基或C 1-6烷酰基; 当Ar是苯基或单环杂芳族基团时，彼此邻位置换可以连接形成5-或6-元环; R 1是氢，C 1-6烷基，C 3-6烯基，C 3-6炔基或芳基C 1-6烷基; R 2是卤素，C 1-6烷基，氰基，CF 3，C 1-6烷酰基，C 1-6烷氧基或羟基; X是CH或N; Y是单键，O或C = O; p为0,1或2; r为0,1,2或3; m为2,3或4; n和q独立地为1或2.还公开了制备化合物的方法，含有它们的药物组合物及其作为各种CNS障碍的药物的用途，包括抑郁和/或焦虑。

    BIOLOGICALLY ACTIVE MACROLIDES, COMPOSITIONS, AND USES THEREOF
    48.
    发明申请
    BIOLOGICALLY ACTIVE MACROLIDES, COMPOSITIONS, AND USES THEREOF 审中-公开
    生物活性成分，组合物及其用途

    公开(公告)号：WO02008231A2

    公开(公告)日：2002-01-31

    申请号：PCT/US2001/023633

    申请日：2001-07-24

    IPC: A61K31/395 ,  A61P13/02 ,  A61P15/08 ,  A61P19/10 ,  A61P25/28 ,  A61P27/06 ,  A61P35/00 ,  A61P43/00 ,  C07D498/08 ,  C07D498/00

    CPC classification number: A61K31/395 ,  A61K31/365 ,  A61K31/7048 ,  C07D498/06 ,  C07D498/08

    Abstract: The present invention provides a compound of the formula (I) or (II), wherein R is H, alkyl, alkenyl or aryl, R is H, alkyl or aryl, R is H, a alkyl, alkenyl or aryl, R and R -R are independently R , C(O)R or SO2R , wherein R is H, alkyl, alkenyl or aryl, and R is R , C(O)R or SO2R , wherein R is H, alkyl, alkenyl or aryl. R can be unsubstituted or substituted with one or more oxo(=O), OR , OC(O)R , OSO2R , NHR , NHC(O)R and NHSO2R groups. R is H, alkyl, alkenyl, or aryl. R can be unsubstituted or substituted with one or more groups such as oxo(=O), OR , CO2R , CO2R and OC(O)R . R is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.

    Abstract translation: 本发明提供式（I）或（II）的化合物，其中R 1是H，烷基，烯基或芳基，R 2是H，烷基或芳基，R 3是H， 烷基，烯基或芳基，R 4和R 4 -R 8独立地是R 10，C（O）R 10或SO 2 R 10，其中R 10是H，烷基 ，烯基或芳基，R 9是R 9a，C（O）R 9a或SO 2 R 9a，其中R 9a是H，烷基，烯基或芳基。 R 9a可以是未取代的或被一个或多个氧代（= O），OR 9b，OC（O）R 9b，OSO 2 R 9b，NHR 9b，NHC（O）R 9b， 和NHSO 2 R 9b基团。 R 9b是H，烷基，烯基或芳基。 R 9b可以是未取代的或被一个或多个基团取代，例如氧代（= O），OR 9c，CO 2 R 9c，CO 2 R 9c和OC（O）R 9c。 R 9c是H或未取代或取代的烷基，烯基或芳基。 本发明还提供包含至少一种本发明化合物和药学上可接受的载体的组合物，其单独或与至少一种另外的活性剂组合。 本发明还提供一种治疗通过抑制液泡型（H +）-ATP酶可治疗的病症的方法和一种治疗癌症的方法。

    NOVEL BI- AND TRI-CYCLIC AZA COMPOUNDS AND THEIR USES
    49.
    发明申请
    NOVEL BI- AND TRI-CYCLIC AZA COMPOUNDS AND THEIR USES 审中-公开
    新型双 - 和三环AZA化合物及其用途

    公开(公告)号：WO00007994A1

    公开(公告)日：2000-02-17

    申请号：PCT/US1999/017860

    申请日：1999-08-05

    IPC: C07D487/08 ,  A61K31/437 ,  A61K31/46 ,  A61P1/14 ,  A61P3/04 ,  A61P15/10 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D451/02 ,  C07D471/08 ,  C07D471/18 ,  C07D487/18 ,  C07D221/02 ,  C07D215/36 ,  C07D221/22 ,  C07D453/00 ,  C07D455/00 ,  C07D491/00 ,  C07D498/00 ,  C07D513/00

    CPC classification number: C07D451/02 ,  C07D471/08

    Abstract: The present invention provides tropane-derived monoamine neurotransmitter re-uptake inhibitors which predictably exhibit selectivity for either the serotonin or dopamine transporter, pharmaceutical compositions thereof and methods for their use. The serotonin-selective re-uptake inhibitors are particularly useful for treating neurological disorders associated with the serotonergic neural system of the brain, such as depression, with significantly reduced side-effects. The dopamine-selective re-uptake inhibitors are particularly useful for treating disorders associated with dopamine re-uptake and/or acetylcholine release.

    Abstract translation: 本发明提供了可预测地显示5-羟色胺或多巴胺转运蛋白选择性的托烷衍生的单胺神经递质再摄取抑制剂，其药物组合物及其使用方法。 5-羟色胺选择性再摄取抑制剂特别可用于治疗与脑的血清素能神经系统相关的神经系统疾病，例如抑郁症，具有显着降低的副作用。 多巴胺选择性再摄取抑制剂特别可用于治疗与多巴胺再摄取和/或乙酰胆碱释放相关的疾病。

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