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。

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：

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.

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.

公开(公告)号：US20050261279A1

公开(公告)日：2005-11-24

申请号：US10515998

申请日：2003-05-28

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

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

IPC分类号： C07D217/22 ,  A61K20060101 ,  A61K31/4035 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/472 ,  A61K31/55 ,  A61P20060101 ,  A61P1/00 ,  A61P1/08 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/36 ,  A61P43/00 ,  C07D20060101 ,  C07D209/44 ,  C07D217/02 ,  C07D223/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D223/16 ,  C07D209/44 ,  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 C1-6alkyl; 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, —(CF)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.

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.

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.

公开(公告)号：US20050176759A1

公开(公告)日：2005-08-11

申请号：US10499776

申请日：2002-12-20

申请人： Mahmood Ahmed ,  Steven Bromidge ,  Ian Forbes ,  Andrew Gribble ,  Christopher Johnson ,  Francis King ,  Andrew Lightfoot ,  Gregor Macdonald ,  Stephen Moss ,  Mervyn Thompson ,  David Witty

发明人： Mahmood Ahmed ,  Steven Bromidge ,  Ian Forbes ,  Andrew Gribble ,  Christopher Johnson ,  Francis King ,  Andrew Lightfoot ,  Gregor Macdonald ,  Stephen Moss ,  Mervyn Thompson ,  David Witty

IPC分类号： C07D223/14 ,  A61K31/55 ,  A61P1/08 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  A61K31/47 ,  A61K31/4035

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12

摘要： Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

摘要翻译： 发明的是非肽TPO模拟物。 还发明了一种在有需要的哺乳动物（包括人）中治疗血小板减少症的方法，其包括向所述哺乳动物施用有效量的选择的羟基-1-偶氮苯衍生物。

公开(公告)号：US08796283B2

公开(公告)日：2014-08-05

申请号：US13501418

申请日：2010-10-14

申请人： Kevin Dinnell ,  Andrew Lightfoot ,  Gillian Elizabeth Lunniss

发明人： Kevin Dinnell ,  Andrew Lightfoot ,  Gillian Elizabeth Lunniss

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

CPC分类号： C07D471/04 ,  A61K31/506 ,  C07D403/12

摘要： This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I): or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐调节α7烟碱乙酰胆碱受体（nAChR）。

公开(公告)号：US07429579B2

公开(公告)日：2008-09-30

申请号：US10416377

申请日：2001-11-12

申请人： Michael Stewart Hadley ,  Andrew Lightfoot ,  Gregor James MacDonald ,  Geoffrey Stemp

发明人： Michael Stewart Hadley ,  Andrew Lightfoot ,  Gregor James MacDonald ,  Geoffrey Stemp

IPC分类号： A61P25/18 ,  A61K31/55 ,  C07D223/16

CPC分类号： C07D223/16 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04

摘要： The invention provides compounds of formula (I): wherein: R2 and R3 independently represent various substituents; R1 and R4 independently represent H, F, Cl, Br, C1-2alkyl, C1alkoxy, OH, CN, or NO2; B represents a sulfur atom or a —CH2-group; t represents 3 or 4; and A represents an optionally substituted 5- or 6-membered aromatic heterocyclic ring, or an optionally substituted bicyclic heterocyclic ring system in which at least the ring bound to the group B in Formula (I) is aromatic; or a salt thereof. Preferably, A is selected from one of the groups (i), (ii) or (iii): wherein X1 and X2 are independently N or CR8, and X3 is NR8, O or S; Y1 and Y3 are independently N or CR9, and Y2 is NR9, O or S; Z1 is NR10, O or S, and Z2 and Z3 are independently N or CR10; R8, R9, and R10 are as herein defined, and R7 is H, a halogen atom, OH, cyano, nitro, C1-4alkyl, C1-4alkoxy, C1-4alkylenedioxy, C1-4alkanoyl, or C1-4alkylsulfonyl, an optionally substituted 3-, 4-, 5- or 6-membered cycloalkyl ring, or a group of the formula (a), (b), (c) or (d) as defined by the formulas (a), (b), (c) or (d). The compounds are modulators of dopamine D3 receptors and have potential in the treatment of psychotic conditions (e.g. schizophrenia) or substance abuse.