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1. 发明授权

US07393858B2 Tetrahydropyran compounds as tachykinin antagonists 失效
标题翻译：四氢吡喃化合物作为速激肽拮抗剂
公开(公告)号：US07393858B2
公开(公告)日：2008-07-01
申请号：US10548678
申请日：2004-03-04
申请人： Olivier Dirat , Jason Matthew Elliott , Ian Thomas Huscroft , Richard Alexander Jelley , Janusz Jozef Kulagowski , Piotr Antoni Raubo , Duncan Edward Shaw , Francine Sternfeld , Christopher John Swain
发明人： Olivier Dirat , Jason Matthew Elliott , Ian Thomas Huscroft , Richard Alexander Jelley , Janusz Jozef Kulagowski , Piotr Antoni Raubo , Duncan Edward Shaw , Francine Sternfeld , Christopher John Swain
IPC分类号： A61K31/438 , C07D491/10
CPC分类号： C07D405/04 , C07D405/06 , C07D407/12 , C07D417/04 , C07D491/10
摘要： The present invention relates to compounds of formula (Ia) wherein A, B, n, m, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are defined herein, and pharmaceutically acceptable salts thereof; the compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
摘要翻译：本发明涉及式（Ia）化合物，其中A，B，n，m，R 1，R 2，R 3， R 4，R 5，R 6，R 7，R 8，本文定义R 9，R 10和R 11和其药学上可接受的盐; 该化合物特别用于治疗或预防抑郁，焦虑，疼痛，炎症，偏头痛，呕吐或带状疱疹后神经痛。

2. 发明授权

US06727249B2 Azabicyclic ether derivatives and their use as therapeutic agents 失效
标题翻译：偶氮二环醚衍生物及其作为治疗剂的用途
公开(公告)号：US06727249B2
公开(公告)日：2004-04-27
申请号：US10113117
申请日：2002-04-01
申请人： Neil Roy Curtis , Ian Thomas Huscroft , Janusz Jozef Kulagowski , Piotr Antoni Raubo
发明人： Neil Roy Curtis , Ian Thomas Huscroft , Janusz Jozef Kulagowski , Piotr Antoni Raubo
IPC分类号： A61K31535
CPC分类号： C07D451/02
摘要： The present invention relates compounds of the formula (I): wherein X represents hydrogen, C1-4alkyl optionally substituted by a hydroxy, methoxy or benzyloxy group, or CO2(C1-2alkyl); Z is —CR9R10CH2— or —CH2CR9R10—; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
摘要翻译：本发明涉及式（I）化合物：其中X代表氢，任选被羟基，甲氧基或苄氧基取代的C 1-4烷基或CO 2（C 1-2烷基）; Z是-CR 9 R 10 CH - 或-CH 2 CR 9 R 10 - ，R 1，R 2，R 3，R 4，R 5和R 6如本文所定义。化合物特别用于治疗或预防抑郁，焦虑，疼痛，炎症，迁移物，呕吐或带状疱疹后神经痛。

3. 发明授权

US06479486B2 Azabicyclic spiroether derivatives and their use as therapeutic agents 失效
标题翻译：氮杂双环螺醚衍生物及其作为治疗剂的用途
公开(公告)号：US06479486B2
公开(公告)日：2002-11-12
申请号：US10115629
申请日：2002-04-01
申请人： Ian Thomas Huscroft , Janusz Jozef Kulagowski , Piotr Antoni Raubo
发明人： Ian Thomas Huscroft , Janusz Jozef Kulagowski , Piotr Antoni Raubo
IPC分类号： A61K31438
CPC分类号： C07D491/20
摘要： The present invention relates compounds of the formula (I): wherein Z is —CR9R10CH2— or —CH2CR9R10—; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
摘要翻译：本发明涉及式（I）的化合物：其中Z是-CR 9 R 10 CH 2 - 或-CH 2 CR 9 R 10 - ;且R 1，R 2，R 3，R 4，R 5和R 6如本文所定义。这些化合物特别用于治疗或预防抑郁，焦虑，疼痛，炎症，迁移物，呕吐或带状疱疹后神经痛。

4. 发明授权

US07101892B2 Sulfone derivatives as 5-HT7 receptor ligands 失效
标题翻译：砜衍生物作为5-HT7受体配体
公开(公告)号：US07101892B2
公开(公告)日：2006-09-05
申请号：US10845847
申请日：2004-05-14
申请人： Sylvie Bourrain , Peter Alan Hunt , Ian Thomas Huscroft , Janusz Jozef Kulagowski , Clare London , Elizabeth Mary Naylor , Piotr Antoni Raubo , Eileen Mary Seward
发明人： Sylvie Bourrain , Peter Alan Hunt , Ian Thomas Huscroft , Janusz Jozef Kulagowski , Clare London , Elizabeth Mary Naylor , Piotr Antoni Raubo , Eileen Mary Seward
IPC分类号： A61K31/44
CPC分类号： C07D241/38 , C07D207/06 , C07D207/16 , C07D209/44 , C07D209/52 , C07D209/60 , C07D209/62 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/32 , C07D211/60 , C07D211/70 , C07D217/04 , C07D233/04 , C07D295/084 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/08
摘要： The present invention relates to sulfone derivatives of formula (I): Ar—SO2—CR2R3-L-N(R1)2I wherein Ar, L, R1, R2 and R3 are as defined herein, and pharmaceutically acceptable salts and N-oxides thereof, useful in the treatment of a condition which is susceptible to treatment by modulation of 5-HT7 receptor activity, such as depression or a sleep disorder.
摘要翻译：本发明涉及式（I）的砜衍生物：<？in-line-formula description =“In-line Formulas”end =“lead”→Ar-SO 2 -CR > 2 3 其中Ar，L，R 1，R 2和R 3如本文所定义，并且药学上可接受的是式可接受的盐和N-氧化物，其可用于治疗通过调节5-HT 7受体活性（例如抑郁症或睡眠障碍）进行治疗的病症。

5. 发明授权

US6071928A Spiro-piperidine derivatives and their use as therapeutic agents 失效
标题翻译：螺哌啶衍生物及其作为治疗剂的用途
公开(公告)号：US6071928A
公开(公告)日：2000-06-06
申请号：US202551
申请日：1998-12-16
申请人： Neil Roy Curtis , Ian Thomas Huscroft , Janusz Jozef Kulagowski , Christopher John Swain
发明人： Neil Roy Curtis , Ian Thomas Huscroft , Janusz Jozef Kulagowski , Christopher John Swain
IPC分类号： H04L12/28 , A61K31/438 , C07D491/10 , C07D491/107 , A61K31/44 , C07D221/00 , C07D239/00 , C07D251/00 , C07D403/00
CPC分类号： C07D491/10 , A61K31/438
摘要： The present invention relates to compounds of formula (I), wherein R is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, which groups are optionally substituted by hydroxy, C.sub.1-4 alkoxy or NR.sup.a R.sup.b, where R.sup.a and R.sup.b each independently repesent hydrogen or C.sub.1-4 alkyl; or R is C.sub.1-4 alkyl substituted by Ar, and optionally further substituted by one or both of R.sup.4 and R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 represent a variety of substituents; R.sup.9 and R.sup.10 are each hydrogen, halogen, C.sub.1-6 alkyl, CH.sub.2 OR.sup.c, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b where R.sup.c represents hydrogen, C.sub.1-6 alkyl or phenyl; X is --CH.sub.2, or --CH.sub.2 CH.sub.2 --; Y is --CH--, --CH.sub.2 --, --CH.sub.2 CH-- or --CH.sub.2 CH.sub.2 --, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when Y is --CH-- or --CH.sub.2 CH--, the broken line is a double bond; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, anesis and postherpetic neuralgia. ##STR1##
摘要翻译： PCT No.PCT / GB97 / 01710 Sec。 371日期1998年12月16日第 102（e）日期1998年12月16日PCT提交1997年6月24日PCT公布。出版物WO98 / 01450 日本1月15日，1998本发明涉及式（I）化合物，其中R为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，该基团任选被羟基取代， C 1-4烷氧基或NR a R b，其中R a和R b各自独立地代表氢或C 1-4烷基; 或R为被Ar取代的C 1-4烷基，并且任选进一步被R4和R5中的一个或两个取代; R1，R2和R3代表各种取代基; R 9和R 10各自为氢，卤素，C 1-6烷基，CH 2 OR c，氧代，CO 2 R a或CONR a R b，其中R c表示氢，C 1-6烷基或苯基; X是-CH 2或-CH 2 CH 2 - ; Y是-CH-，-CH 2 - ， - CH 2 CH-或-CH 2 CH 2 - ，条件是X + Y中的碳原子总数为2或3; 当Y为-CH-或-CH 2 CH-时，虚线为双键; 或其药学上可接受的盐。该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。

6. 发明授权

US08163956B2 Inhibitors of GLYT1 transporters 有权
标题翻译： GLYT1转运蛋白的抑制剂
公开(公告)号：US08163956B2
公开(公告)日：2012-04-24
申请号：US11922074
申请日：2006-06-13
申请人： Wesley Peter Blackaby , Ian Thomas Huscroft , Linda Elizabeth Keown , Richard Thomas Lewis , Piotr Antoni Raubo , Leslie Joseph Street , Christopher George Thomson , Joanne Thomson
发明人： Wesley Peter Blackaby , Ian Thomas Huscroft , Linda Elizabeth Keown , Richard Thomas Lewis , Piotr Antoni Raubo , Leslie Joseph Street , Christopher George Thomson , Joanne Thomson
IPC分类号： C07C303/00 , C07C233/00 , C07C237/00 , C07C323/00 , A61K31/16 , A61K31/165
CPC分类号： C07D249/04 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/08 , C07D207/09 , C07D211/26 , C07D211/28 , C07D211/60 , C07D213/40 , C07D249/12 , C07D295/067 , C07D309/04 , C07D401/12
摘要： A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.
摘要翻译：公开了式（I）化合物：其中R 1，R 2，R 3，R 4，Ar，A，n和m如本文所定义，被公开为GlyT1抑制剂; 还公开了含有式（I）化合物的药物组合物，它们在医学中的用途，例如在精神分裂症的治疗中。

7. 发明申请

US20090286765A1 Therapeutic Agents 有权
标题翻译：治疗剂
公开(公告)号：US20090286765A1
公开(公告)日：2009-11-19
申请号：US11922074
申请日：2006-06-13
申请人： Wesley Peter Blackaby , Ian Thomas Huscroft , Linda Elizabeth Keown , Richard Thomas Lewis , Piotr Antoni Raubo , Leslie Joseph Street , Christopher George Thomson , Joanne Thomson
发明人： Wesley Peter Blackaby , Ian Thomas Huscroft , Linda Elizabeth Keown , Richard Thomas Lewis , Piotr Antoni Raubo , Leslie Joseph Street , Christopher George Thomson , Joanne Thomson
IPC分类号： A61K31/397 , C07C233/00 , A61K31/165 , C07D211/32 , A61K31/445 , C07D413/14 , A61K31/5377
CPC分类号： C07D249/04 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/08 , C07D207/09 , C07D211/26 , C07D211/28 , C07D211/60 , C07D213/40 , C07D249/12 , C07D295/067 , C07D309/04 , C07D401/12
摘要： A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.
摘要翻译：公开了式（I）化合物：其中R 1，R 2，R 3，R 4，Ar，A，n和m如本文所定义，被公开为GlyT1抑制剂; 还公开了含有式（I）化合物的药物组合物，它们在医学中的用途，例如在精神分裂症的治疗中。

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