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    7-Phenylsulfonyl-tetrahydro-3-benzazepine derivatives as antipsychotic agents
    2.
    发明申请
    7-Phenylsulfonyl-tetrahydro-3-benzazepine derivatives as antipsychotic agents 审中-公开

    公开(公告)号：US20050245507A1

    公开(公告)日：2005-11-03

    申请号：US10516065

    申请日：2003-05-28

    申请人： Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne ,  Graham Walker

    发明人： Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne ,  Graham Walker

    IPC分类号： A61K31/55 ,  A61P1/08 ,  A61P3/04 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D209/44 ,  C07D217/02 ,  C07D217/04 ,  C07D223/16

    CPC分类号： C07D223/16 ,  C07D209/44 ,  C07D217/02 ,  C07D217/04

    摘要： 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, —CO2NR5R6, —SO2NR5R6, —(CH2)pNR5R6, —(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; R4 represents 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.

    AROMATIC SULFONES AND THEIR MEDICAL USE
    4.
    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

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

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

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

    CPC分类号： C07D223/16 ,  C07D209/44 ,  C07D217/02

    摘要： 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.

    Compounds which have activity at M1 receptor and their uses in medicine.
    5.
    发明申请
    Compounds which have activity at M1 receptor and their uses in medicine. 失效
    具有M1受体活性的化合物及其在药物中的用途。

    公开(公告)号：US20080058378A1

    公开(公告)日：2008-03-06

    申请号：US11852455

    申请日：2007-09-10

    申请人： Brian Budzik ,  David Cooper ,  Ian Forbes ,  Vincenzo Garzya ,  Jian Jin ,  Dongchuan Shi ,  Graham Walker

    发明人： Brian Budzik ,  David Cooper ,  Ian Forbes ,  Vincenzo Garzya ,  Jian Jin ,  Dongchuan Shi ,  Graham Walker

    IPC分类号： A61K31/445 ,  A61P43/00

    CPC分类号： C07D405/12 ,  C07D235/26

    摘要： Compounds of formula (I) and salts and solvates are provided: wherein R4 is fluoro, R5 is selected from hydrogen, halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6alkoxy, and C1-6alkoxy substituted with one or more fluorine atoms; and R6 is selected from halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6alkoxy and C1-6alkoxy substituted with one or more fluorine atoms, and Q is hydrogen or C1-6alkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.

    摘要翻译： 提供式（I）化合物和盐和溶剂化物：其中R 4是氟，R 5选自氢，卤素，氰基，C 1〜 C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基和C 1-6 - 被一个或多个氟原子取代的烷氧基; 和R 6选自卤素，氰基，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基， C 3-6环烷基，被一个或多个氟原子取代的C 3-6环烷基，C 1-6烷氧基和C 1-6烷基， 1-6个被一个或多个氟原子取代的烷氧基，Q是氢或C 1-6烷基。 预期化合物可用于治疗，例如治疗精神病和认知障碍。

    Compounds which have activity at M1 receptor and their uses in medicine
    8.
    发明授权
    Compounds which have activity at M1 receptor and their uses in medicine 失效
    具有M1受体活性的化合物及其在药物中的用途

    公开(公告)号：US08288412B2

    公开(公告)日：2012-10-16

    申请号：US12088451

    申请日：2006-09-27

    申请人： Brian Budzik ,  David Gwyn Cooper ,  Ian Thomson Forbes ,  Vincenzo Garzya ,  Jian Jin ,  Dongchuan Shi ,  Paul William Smith ,  Graham Walker

    发明人： Brian Budzik ,  David Gwyn Cooper ,  Ian Thomson Forbes ,  Vincenzo Garzya ,  Jian Jin ,  Dongchuan Shi ,  Paul William Smith ,  Graham Walker

    IPC分类号： A61K31/454 ,  C07D405/04

    CPC分类号： C07D401/14

    摘要： Compounds of formula (I) and salts are provided: wherein R5 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; R6 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.

    摘要翻译： 提供式（I）和盐的化合物：其中R 5选自卤素，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基， 和氰基; R 6选自卤素，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 3-6环烷基，被一个或多个氟原子取代的C 3-6环烷基，C 1-6烷氧基，被一个或多个 氟原子和氰基; Q是氢或C 1-6烷基。 化合物是M1激动剂，可用于治疗，例如治疗精神病和认知障碍。