-
公开(公告)号:US20080090822A1
公开(公告)日:2008-04-17
申请号:US11908149
申请日:2006-03-09
申请人: Daniel Bradley , Clive Branch , Bethany Brown , Wai Chan , Steven Coulton , Martin Gilpin , Sharon Gough , Jacqueline MacRitchie , Howard Marshall , David Nash , Roderick Porter , Anthony Dean , Paul Doyle , Brian Evans , Luigi Stasi
发明人: Daniel Bradley , Clive Branch , Bethany Brown , Wai Chan , Steven Coulton , Martin Gilpin , Sharon Gough , Jacqueline MacRitchie , Howard Marshall , David Nash , Roderick Porter , Anthony Dean , Paul Doyle , Brian Evans , Luigi Stasi
IPC分类号: A61K31/535 , A61K31/497 , A61P25/18 , C07D401/02 , C07D401/14
CPC分类号: C07D213/73 , C07D213/75 , C07D213/85 , C07D215/38 , C07D239/42 , C07D241/44 , C07D295/192 , C07D487/04
摘要: The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译: 本发明提供式(I)化合物或其盐或溶剂合物:其中R 1,n,X,Y和Z如说明书中所定义,以及这些化合物的用途。 该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍,包括精神分裂症。
-
公开(公告)号:US20060040937A1
公开(公告)日:2006-02-23
申请号:US10527833
申请日:2003-09-17
申请人: Clive Branch , Steven Coulton , Amanda Johns , David Nash , Roderick Porter , Geoffrey Stemp
发明人: Clive Branch , Steven Coulton , Amanda Johns , David Nash , Roderick Porter , Geoffrey Stemp
IPC分类号: A61K31/5377 , A61K31/506 , A61K31/496 , C07D413/02 , C07D403/02
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D417/14
摘要: This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals.
摘要翻译: 本发明涉及N-芳酰基环胺衍生物及其作为药物的用途。
-
3.Broadspectrum heterocyclic substituted phenyl containing sulfonamide hiv protease inhibitors 失效
标题翻译: 支链杂环取代苯基含磺酰胺hiv蛋白酶抑制剂公开(公告)号:US20050222215A1
公开(公告)日:2005-10-06
申请号:US10499221
申请日:2002-12-20
申请人: Steven Coulton , Michael Hadley , Hugh Herdon , Jian Jin , Graham Joiner , Roderick Porter , Shahzad Rahman
发明人: Steven Coulton , Michael Hadley , Hugh Herdon , Jian Jin , Graham Joiner , Roderick Porter , Shahzad Rahman
IPC分类号: C07D233/64 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/4188 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/429 , A61K31/443 , A61K31/497 , A61K31/506 , A61K31/53 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/18 , C07D231/12 , C07D233/54 , C07D233/88 , C07D263/32 , C07D277/20 , C07D277/40 , C07D277/42 , C07D277/46 , C07D417/04 , C07D417/12 , C07D417/14 , C07D493/04 , C07D513/04 , C07D519/00 , A61K31/44 , A61K31/16 , A61K31/277 , A61K31/40
CPC分类号: C07D231/12 , C07C311/18 , C07C2603/18 , C07D233/64 , C07D233/88 , C07D263/32 , C07D277/40 , C07D277/42 , C07D277/46 , C07D417/04 , C07D417/12 , C07D417/14 , C07D493/04 , C07D513/04
摘要: The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, (R7a)n-M-R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and -A-R6; and on (ii) a nitrogen atom if present by hydroxy or -A-R6. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
摘要翻译: 本发明涉及具有式(I),N-氧化物,盐,立体异构形式,外消旋混合物,前药,酯和代谢物的化合物,其中Haryl是具有3至14个环成员的芳族单环,双环或三环杂环, 含有一个或多个选自氮,氧和硫的杂原子环成员,并且其可任选地在(i)一个或多个碳原子上被C 1-6烷基取代,卤素,羟基, 或二取代的氨基,硝基,氰基,卤代C 1-6烷基,羧基,C 3-7环烷基,任选的单或二取代的氨基羰基,甲硫基,甲基磺酰基,芳基,( H< 1>和< 2>;< 2> 其中任何氨基官能团上的任选取代基独立地选自R 5和-A-R 6; 和(ii)如果存在羟基或-A-R 6的氮原子。 它还涉及它们作为广谱的HIV蛋白酶抑制剂,其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。 它还涉及与另一种抗逆转录病毒剂的组合,以及它们在测定中用作参考化合物或作为试剂。
-
4.Ethylene diamine derivatives and their use as orexin-receptor antagonists 失效
标题翻译: 乙二胺衍生物及其作为食欲素受体拮抗剂的用途公开(公告)号:US20050159421A1
公开(公告)日:2005-07-21
申请号:US10498884
申请日:2002-12-13
申请人: Steven Coulton , Amanda Johns , Roderick Porter
发明人: Steven Coulton , Amanda Johns , Roderick Porter
IPC分类号: C07D215/46 , A61K31/427 , A61K31/47 , A61K31/498 , A61K31/506 , A61P1/04 , A61P1/08 , A61P3/04 , A61P3/10 , A61P5/02 , A61P5/06 , A61P5/38 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P35/00 , A61P37/08 , A61P43/00 , C07D403/12 , C07D417/12 , C07K14/575 , A61K31/423 , A61K31/426 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号: C07D403/12 , C07D417/12
摘要: This invention relates to heterocyclic substituted ethylene diamine derivatives and their use as pharmaceuticals.
摘要翻译: 本发明涉及杂环取代的乙二胺衍生物及其作为药物的用途。
-
公开(公告)号:US20050020584A1
公开(公告)日:2005-01-27
申请号:US10494011
申请日:2002-10-30
申请人: Wai Chan , Amanda Johns , Roderick Porter , Rachel Stead , Mythily Vimal
发明人: Wai Chan , Amanda Johns , Roderick Porter , Rachel Stead , Mythily Vimal
IPC分类号: A61K31/166 , A61K31/277 , A61K31/343 , A61K31/36 , A61K31/415 , A61K31/4192 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/47 , A61K31/472 , A61P3/00 , A61P3/04 , A61P3/10 , A61P5/02 , A61P5/06 , A61P5/10 , A61P7/00 , A61P7/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/28 , A61P43/00 , C07C233/73 , C07C233/76 , C07C233/77 , C07C233/78 , C07C233/87 , C07C235/46 , C07C235/48 , C07C235/84 , C07C255/50 , C07C255/57 , C07C317/14 , C07D215/48 , C07D215/50 , C07D217/26 , C07D231/14 , C07D249/06 , C07D271/06 , C07D271/12 , C07D277/20 , C07D277/56 , C07D277/62 , C07D285/14 , C07D307/79 , C07D317/50 , C07D317/68 , C07D279/12 , A61K31/165 , A61K31/401 , A61K31/421 , A61K31/495 , A61K31/537 , A61K31/54
CPC分类号: C07D271/06 , C07C233/73 , C07C233/77 , C07C233/87 , C07C235/46 , C07C235/84 , C07C255/57 , C07C2603/18 , C07D215/48 , C07D215/50 , C07D217/26 , C07D231/14 , C07D249/06 , C07D277/56 , C07D307/79 , C07D317/68
摘要: This invention relates to certain benzamide derivatives and their use as pharmaceuticals.
摘要翻译: 本发明涉及某些苯甲酰胺衍生物及其作为药物的用途。
-
6.N-'4-4(4-MORPHOLINYL) PHENYL!- '(4-PIPERIDINYL) METHYL! CARBOXAMIDE DERIVATIVES AND THEIR USE AS GLYCINE TRANSPORTER INHIBITORS 审中-公开
标题翻译: N-4 - (4-吗啉代)苯基 - (4-哌啶子基)甲基! 羧酰胺衍生物及其作为甘氨酸运输抑制剂的用途公开(公告)号:US20090253700A1
公开(公告)日:2009-10-08
申请号:US11568044
申请日:2005-04-15
IPC分类号: A61K31/5377 , C07D413/12 , A61P25/18 , A61P25/00
CPC分类号: C07D211/26 , C07D405/12
摘要: The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, n and Ar are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译: 本发明提供式(I)化合物或其盐或溶剂化物:其中R1,R2,R3,R4,R5,R6,R7,R8,R9,R10,R11,n和Ar如说明书中所定义, 和这些化合物的用途。 该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍,包括精神分裂症。
-
-
-
-
-