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：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：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：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：US20050222124A1

公开(公告)日：2005-10-06

申请号：US10504111

申请日：2003-02-13

申请人： Steven Bromidge ,  David Cooper ,  Ian Forbes ,  Andrew Gribble ,  Christopher Johnson ,  Andrew Plightfoot ,  Stephen Moss ,  Andrew Payne ,  Shahzad Rahman ,  David Witty

发明人： Steven Bromidge ,  David Cooper ,  Ian Forbes ,  Andrew Gribble ,  Christopher Johnson ,  Andrew Plightfoot ,  Stephen Moss ,  Andrew Payne ,  Shahzad Rahman ,  David Witty

IPC分类号： A61K31/40 ,  A61K31/4035 ,  A61K31/47 ,  A61K31/472 ,  A61K31/55 ,  A61P1/08 ,  A61P3/04 ,  A61P15/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D209/44 ,  C07D217/02 ,  C07D217/04 ,  C07D223/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D407/10 ,  C07D409/10 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12

CPC分类号： C07D223/16 ,  A61K31/40 ,  A61K31/47 ,  A61K31/55 ,  C07D209/44 ,  C07D217/02 ,  C07D217/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

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, C1-6alkoxyC1-6alkyl, C3-7cycloalkylC1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonylC1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, C1-6alkylsulfonamido, C1-6alkylsulfonamidoC1-6alkyl, —(CH2)pNR7R8, C1-6alkylamidoC1-6alkyl, —(CH2)pNR7COR8, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-6alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, aroylC1-6alkyl, arylC1-6alkanoyl, —SO2NR7R8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl, or a group CONR7R8 or SO2NR7R8 wherein R7 and R8 together may be fused to form a 5- 7-membered aromatic or non-aromatic heterocyclic ring optionally interrupted by an O or S atom; R3 represents hydrogen or C1-6alkyl; Ar represents optionally substituted phenyl or optionally substituted monocyclic heteroaryl group; R4 represents optionally substituted aryl or optionally substituted heteroaryl; R7 and R8 each independently represent hydrogen, C1-6alkyl or together form a 5- to 7-membered heterocyclic ring; Z represents a bond, an oxygen atom or C1-6alkyl; Y 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 represents an integer from 1 to 3; r represents an integer from 1 to 4; or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful in therapy, in particular as antipsychotic agents.

公开(公告)号：US08573602B2

公开(公告)日：2013-11-05

申请号：US13215528

申请日：2011-08-23

申请人： Andrew Payne ,  Brent R. Sedlar ,  David M. Toth ,  Frederick R. Hatch

发明人： Andrew Payne ,  Brent R. Sedlar ,  David M. Toth ,  Frederick R. Hatch

IPC分类号： F16J15/32

CPC分类号： F16J15/3224 ,  F16J15/3244

摘要： A radial shaft seal configured for receipt in a housing and about a shaft to sealingly isolate an air-side of the shaft seal from an oil-side of the shaft seal is provided. The seal includes an annular mounting portion and a seal lip operably attached to the mounting portion. The seal lip has an annular inner sealing surface extending axially between an oil-side end and a free air-side end. The inner sealing surface has a first groove region extending along the shaft in sealed engagement therewith and a second groove region extending along the shaft in sealed engagement therewith. The first groove region and the second groove region are spaced axially from one another by an intermediate non-grooved region. The first groove region is configured to direct contamination toward the air-side of the seal and the second groove region is configured to direct lubrication toward the oil-side of the seal.

摘要翻译： 提供了一种径向轴密封件，其构造成用于容纳在壳体中并且围绕轴，以将轴封的空气侧与轴封的油侧密封隔离。 密封件包括可操作地附接到安装部分的环形安装部分和密封唇缘。 密封唇缘具有在油侧端部和自由空气侧端部之间轴向延伸的环形内部密封表面。 内部密封表面具有沿着轴与密封接合的第一槽区域和沿着轴密封接合的第二槽区域。 第一凹槽区域和第二凹槽区域通过中间非凹槽区域彼此轴向隔开。 第一槽区域构造成将污染物引导到密封件的空气侧，并且第二槽区域构造成朝向密封件的油侧引导润滑。

公开(公告)号：US20070259347A1

公开(公告)日：2007-11-08

申请号：US11417353

申请日：2006-05-03

申请人： David B. Gordon ,  Andrew Payne

发明人： David B. Gordon ,  Andrew Payne

IPC分类号： C12Q1/68 ,  C07H21/04 ,  C12M3/00

CPC分类号： C07H21/04 ,  C12Q1/6837 ,  C12Q2565/507 ,  C12Q2525/197

摘要： Methods and articles for analyzing nucleotide sequences of nucleic acid molecules, e.g., using multiple probes per spot of an array, are described. In some embodiments, the methods and articles can reduce the numbers of arrays necessary to probe regions of interest in a biological sample, and/or increase the resolution at which biological events are probed. In some cases, these methods exploit the vertical aspect of an array in order to decrease the number of arrays or spots required for an assay. These probes may be in the form of compound probes, which comprise at least first and second probes, including first and second nucleotide sequences capable of hybridizing to first and second target nucleotide sequences, respectively, in a nucleic acid molecule of interest.

摘要翻译： 描述了分析核酸分子的核苷酸序列的方法和制品，例如每阵列阵列使用多个探针。 在一些实施方案中，所述方法和制品可以减少探测生物样品中感兴趣区域所需的阵列数量和/或增加探测生物学事件的分辨率。 在某些情况下，这些方法利用阵列的垂直方面，以减少测定所需的阵列数或点数。 这些探针可以是化合物探针的形式，其包含至少第一和第二探针，包括分别在目的核酸分子中能够与第一和第二靶核苷酸序列杂交的第一和第二核苷酸序列。

公开(公告)号：US20050014938A1

公开(公告)日：2005-01-20

申请号：US10495414

申请日：2002-11-14

申请人： Laramie Gaster ,  John Harling ,  Jag Heer ,  Thomas Heightman ,  Andrew Payne

发明人： Laramie Gaster ,  John Harling ,  Jag Heer ,  Thomas Heightman ,  Andrew Payne

IPC分类号： A61K31/4192 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/538 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P3/12 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P43/00 ,  C07D249/06 ,  C07D265/36 ,  C07D285/14 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D417/02 ,  C07D413/02 ,  C07

CPC分类号： C07D285/14 ,  C07D249/06 ,  C07D265/36 ,  C07D471/04

摘要： Phenyl substituted triazoles of formula (I) wherein R1 is naphthyl or phenyl optionally substituted with one or more substituents selected from halo, —O—C1-6alkyl, —S—C1-6alkyl, C1-6alkyl, C1-6haloalkyl, —O—(CH2)n-Ph, —S—(CH2)n-Ph, cyano, phenyl, and CO2R, wherein R is hydrogen or C1-6alkyl, and n is 0, 1, 2 or 3; or R1 is phenyl or pyridyl fused with an aromatic or non-aromatic cyclic ring of 5-7 members wherein said cyclic ring optionally contains up to three heteroatoms, independently selected from N, O and S, and N may be further optionally substituted by C1-6 alkyl, and wherein the cyclic ring may be optionally substituted by ═O; R2 and R3 are independently selected from H, C1-6alkyl, C1-6alkoxy, phenyl, NH(CH2)n-Ph, NH—C1-6alkyl, halo, alkoxy, CN, NO2, CONHR and SO2NHR; two of X1, X2 and X3 are N and the other is NR4 wherein R4 is hydrogen, C1-6alkyl, C3-7cycloalkyl, —(CH2)p—CN, —(CH2)p—CO2H, —(CH2)p—CONHR5R6, —(CH2)pCOR5, —(CH2)q(CR7)2, —(CH2)pOR5, (CH2)qCH═CH—CN, —(CH2)q—CH═CH—CO2H, —(CH2)p—CH═CH—CONHR5R6, —(CH2)pNHCOR8 or —(CH2)pNR9R10; R5 and R6 are independently hydrogen or C1-6alkyl; R7 is C1-6alkyl; R8 is C1-7alkyl, or optionally substituted aryl, heteroaryl, arylC1-6alkyl or heteroaryl C1-6alkyl; R9 and R10 are independently selected from hydrogen, C1-6alkyl, aryl and arylC1-6alkyl; p is 0-4; and q is 1-4 and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.

摘要翻译： 式（I）的苯基取代的三唑，其中R 1是萘基或任选被一个或多个选自卤素，-OC 1-6烷基，-S-C 1-6烷基，C 1-6烷基，C 1-6卤代烷基，-O- （CH 2）n-Ph，-S-（CH 2）n-Ph，氰基，苯基和CO 2 R，其中R是氢或C 1-6烷基，n是0,1,2或3; 或R 1是与5-7个成员的芳族或非芳族环的稠合的苯基或吡啶基，其中所述环任选地含有至多三个独立地选自N，O和S的杂原子，并且N可以进一步任选地被C1 -6烷基，并且其中所述环状环可以任选地被= O取代; R2和R3独立地选自H，C1-6烷基，C1-6烷氧基，苯基，NH（CH2）n-Ph，NH-C1-6烷基，卤素，烷氧基，CN，NO2，CONHR和SO2NHR; X1，X2和X3中的两个是N，另一个是NR4，其中R4是氢，C1-6烷基，C3-7环烷基， - （CH2）p-CN， - （CH2）p-CO2H， - （CH2）p-CONHR5R6 ， - （CH2）pCOR5， - （CH2）q（CR7）2， - （CH2）pOR5，（CH2）qCH = CH-CN， - （CH2）q-CH = CH-CO2H， - （CH2） CH = CH-CONHR5R6， - （CH2）pNHCOR8或 - （CH2）p