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

    公开(公告)号：US20070093473A1

    公开(公告)日：2007-04-26

    申请号：US10571220

    申请日：2004-09-09

    申请人： David Cooper ,  Ian Forbes ,  Vincenzo Garzya ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne ,  Alexander Smith

    发明人： David Cooper ,  Ian Forbes ,  Vincenzo Garzya ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne ,  Alexander Smith

    IPC分类号： A61K31/55 ,  C07D403/02 ,  C07D409/02

    CPC分类号： C04B35/632 ,  C07D401/12 ,  C07D409/12

    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, —CO2NR3R4, —SO2NR3R4, —(CH2)pNR3R4, —(CH2)pNR3COR4, optionally substituted aryl ring, optionally substituted heteroaryl ring, a fused bicyclic heteroaromatic ring system or optionally substituted heterocyclyl ring; Ar1 represents optionally substituted heteroaryl ring; Ar2 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; Z represents —(CH2)qX— wherein the —(CH2)q— group is attached to Ar2, or —X(CH2)q— wherein X is attached to Ar2, and wherein any of the —CH2— groups may be optionally substituted by one or more C1-6alkyl groups; X represents oxygen, —CH(OR5)—, —NR5— or —CH2— wherein the —CH2— group may be optionally substituted by one or more C1-6alkyl groups; R3 and R4 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; R5 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 0, 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that when Ar1 is a pyridyl group, and Z is —CH2X— where X is attached to the Ar1 group, X is selected from —CH(OR5)—, —NR5— and —CH2— wherein the —CH2— group may be optionally substituted by one or more C1-6alkyl groups. The compounds of formula (I) are useful in therapy, in particular as antipsychotic agents.

    Dopamine receptor modulators as antipsychotic agents
    4.
    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

    申请人： David Cooper ,  Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne

    发明人： David Cooper ,  Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne

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

    CPC分类号： C07D223/16 ,  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, —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.

    7-Phenylsulfonyl-tetrahydro-3-benzazepine derivatives as antipsychotic agents
    5.
    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.

    7-Phenylsulfonyl-Tetrahydro-3-Benzazepine Dervatives as Antipsychotic Agents
    7.
    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

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

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

    IPC分类号： A61K31/55 ,  C07D223/16

    CPC分类号： C07D223/16 ,  C07D413/12

    摘要： 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.

    摘要翻译： 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
    8.
    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

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

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

    IPC分类号： A61K31/55 ,  C07D409/02

    CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    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, —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

    摘要翻译： 本发明提供式（I）化合物：

    Benzenesulfonamide derivatives
    9.
    发明申请
    Benzenesulfonamide derivatives 审中-公开

    公开(公告)号：US20050085461A1

    公开(公告)日：2005-04-21

    申请号：US10504110

    申请日：2003-02-13

    申请人： David Cooper ,  Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot

    发明人： David Cooper ,  Ian Forbes ,  Andrew Gribble ,  Andrew Lightfoot

    IPC分类号： C07D217/02 ,  A61K31/395 ,  A61K31/4035 ,  A61K31/47 ,  A61K31/472 ,  A61K31/55 ,  A61P1/00 ,  A61P1/08 ,  A61P3/04 ,  A61P15/02 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07C307/00 ,  C07D209/44 ,  C07D217/22 ,  C07D223/16 ,  C07D405/12 ,  C07D409/12

    CPC分类号： C07D223/16 ,  C07D217/02

    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 C1-4alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S-C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R3 represents hydrogen or C1-6alkyl; R4 represents halogen, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl or —(CH2)pC3-6cycloalkyloxy; R5 and R6 each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; 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; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that the compounds 4-methyl-N-(1,2,3,4-tetrahydroisoquinolin-6-yl)-benzenesulfonamide, 7-(4-chlorophenyl)sulfonamido-1,2,3,4-tetrahydroisoquinoline hydrochloride and N-(2-ethyl-5-isoindolinyl)-p-toluenesulfonamide are excluded. The compounds are useful in therapy, in particular as antipsychotic agents.

    Compounds which have activity at M1 receptor and their uses in medicine.
    10.
    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。