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    7-Phenylsulfonyl-Tetrahydro-3-Benzazepine Dervatives as Antipsychotic Agents
    2.
    发明申请
    7-Phenylsulfonyl-Tetrahydro-3-Benzazepine Dervatives as Antipsychotic Agents 审中-公开
    7-苯基磺酰基 - 四氢-3-苯并氮杂作为抗精神病药

    公开(公告)号：US20070225276A1

    公开(公告)日：2007-09-27

    申请号：US10580641

    申请日：2004-11-25

    Applicant: Ian Forbes ,  Gabriella Gentile ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne ,  Alexander Smith

    Inventor： Ian Forbes ,  Gabriella Gentile ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne ,  Alexander Smith

    IPC: A61K31/55 ,  C07D223/16

    CPC classification number: C07D223/16 ,  C07D413/12

    Abstract: The invention provides one or more chemical entities selected from a compound of formula (I): wherein R1 represents C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halo, cyano, 5-methyl-1,2,4-oxadiazol-3-yl or a group —SO2X; R2 represents hydrogen, C1-6alkyl, C1-6alkoxy, halo or cyano; X is C1-6alkyl, —NR3R4 or morpholino; R3 and R4 independently represent hydrogen or C1-6alkyl; and a pharmaceutically acceptable salt and solvate thereof; with the proviso that the compound {8-[4-(4-fluoro-benzyl)-benzenesulfonyl]-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl}-dimethyl-amine is excluded. The compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof are useful in therapy, in particular as antipsychotic agents.

    Abstract translation: 本发明提供一种或多种选自式（I）化合物的化学实体：其中R 1表示C 1-6烷基，C 1-6烷基， 三氟甲基，三氟甲氧基，卤素，氰基，5-甲基-1,2,4-恶二唑-3-基或基团-SO 2 X; R 2表示氢，C 1-6烷基，C 1-6烷氧基，卤素或氰基; X是C 1-6烷基，-NR 3 R 4或吗啉代; R 3和R 4独立地表示氢或C 1-6烷基; 及其药学上可接受的盐和溶剂合物; 条件是化合物{8- [4-（4-氟 - 苄基） - 苯磺酰基] -3-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因-7-基} - 二甲基 - 胺被排除。 式（I）化合物及其药学上可接受的盐和溶剂合物可用于治疗，特别是抗精神病药。

    Sulfonamide derivatives as antipsychotic agents
    3.
    发明申请
    Sulfonamide derivatives as antipsychotic agents 失效
    磺酰胺衍生物作为抗精神病药

    公开(公告)号：US20060063757A1

    公开(公告)日：2006-03-23

    申请号：US10530538

    申请日：2003-10-06

    Applicant: Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne

    Inventor： Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne

    IPC: A61K31/55 ,  C07D409/02

    CPC classification number: C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    Abstract: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR5R6, —SO2NR5R6, —(CH2)NR5R6, —(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R3 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8 or —(CH2)pNR7COR8; R4represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, trifluoromethyl, trifluoromethoxy, halogen, —OSO2CF3, —(CH2)pC3-6cycloalkyl, —(CH2)qOC1-6alkyl or —(CH2)pOC3-6cycloalkyl; R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; R7 and R8 each independently represent hydrogen or C1-6alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; q independently represents an integer selected from 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that the compounds 8-hydroxy-3-methyl-7-phenylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 8-hydroxy-7-4-(hydroxyphenyl)sulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 7-phenylsulfonyl- 1,2,3,4-tetrahydroisoquinoline and 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline hydrochloride are excluded. The compounds are useful in therapy, in particular as antipsychotic agents

    Abstract translation: 本发明提供式（I）化合物：

    AROMATIC SULFONES AND THEIR MEDICAL USE
    6.
    发明申请
    AROMATIC SULFONES AND THEIR MEDICAL USE 审中-公开

    公开(公告)号：US20080269197A1

    公开(公告)日：2008-10-30

    申请号：US12144917

    申请日：2008-06-24

    Applicant: Ian Thomson Forbes ,  Vincenzo Garzya ,  Andrew Derrick Gribble ,  Andrew Lightfoot ,  Andrew H. Payne ,  Graham Walker

    Inventor： Ian Thomson Forbes ,  Vincenzo Garzya ,  Andrew Derrick Gribble ,  Andrew Lightfoot ,  Andrew H. Payne ,  Graham Walker

    IPC: A61K31/55 ,  C07D223/16 ,  C07D217/00 ,  A61K31/472 ,  C07D209/48 ,  A61K31/4035 ,  A61P3/00 ,  A61P15/00 ,  A61P25/00

    CPC classification number: C07D223/16 ,  C07D209/44 ,  C07D217/02

    Abstract: The invention provides compounds of formula (I): whereinA and B represent the groups —(CH2)m— and —(CH2)n— respectively;R1 represents hydrogen or C1-6alkyl;R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxy C1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR5R6, —SO2NR5R6, —(CH2)pNR5R6, —(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring;R3 represents optionally substituted aryl ring or optionally substituted heteroaryl ring;R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halogen, —OSO2CF3, —(CH2)pC3-6cycloalkyl, —(CH2)qOC1-6alkyl or —(CH2)pOC3-6cycloalkyl;R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring;Z represents —(CH2)rX— wherein the —(CH2)r— group is attached to R3, or —X(CH2)r— wherein X is attached to R3, and wherein any of the —CH2— groups may be optionally substituted by one or more C1-6alkyl groups;X represents oxygen, —NR7 or —CH2— wherein the —CH2— group may be optionally substituted by one or more C1-6alkyl groups;R7 represents hydrogen or C1-6alkyl;m and n independently represent an integer selected from 1 and 2;p independently represents an integer selected from 0, 1, 2 and 3;q independently represents an integer selected from 1, 2 and 3;r independently represents an integer selected from 0, 1, and 2;or a pharmaceutically acceptable salt or solvate thereof.The compounds are useful in therapy, in particular as antipsychotic agents.

    Dopamine receptor modulators as antipsychotic agents
    7.
    发明申请
    Dopamine receptor modulators as antipsychotic agents 审中-公开

    公开(公告)号：US20070043026A1

    公开(公告)日：2007-02-22

    申请号：US10513919

    申请日：2003-05-09

    Applicant: David Cooper ,  Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne

    Inventor： David Cooper ,  Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne

    IPC: A61K31/55 ,  A61K31/47 ,  C07D223/16

    CPC classification number: C07D223/16 ,  C07D217/04

    Abstract: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m—and —(CH2)n-respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8—(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R3 represents hydrogen or C1-6alkyl; R4 represents optionally substituted aryl or optionally substituted heteroaryl; R5 and R6each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R7 and R8 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; and either: Z represents —CR9R10X— or —XCR9R10— and X represents oxygen, sulfur, —SO— or —SO2, or Z represents —CONR11— or —NR9CO— and X represents —CH2—, oxygen, sulfur, —SO— or —SO2; R9 and R10 each independently represent hydrogen, C1-6alkyl or fluoro; R11 represents hydrogen or C1-6alkyl; or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention are useful in therapy, in particular as antipsychotic agents.

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