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1. 发明授权

US5968934A Morpholine derivatives and their use as therapeutic agents 失效
标题翻译：吗啉衍生物及其作为治疗剂的用途
公开(公告)号：US5968934A
公开(公告)日：1999-10-19
申请号：US68818
申请日：1998-05-14
申请人： Christopher John Swain , Martin Richard Teall , Brian John Williams
发明人： Christopher John Swain , Martin Richard Teall , Brian John Williams
IPC分类号： A61K31/00 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P25/06 , A61P29/00 , A61P43/00 , C07D413/04 , C07D417/04
CPC分类号： C07D413/04 , C07D417/04
摘要： The present invention relates to compounds of formula (I) ##STR1## wherein X is a 5- or 6-membered C-linked heteroaromatic ring containing 1 to 4 nitrogen atoms and optionally containing in the ring one oxygen or sulphur atom; Y is a group of the formula --(CH.sub.2).sub.n NR.sup.6 R.sup.7 or a methylene- or ethylene-linked imidazolyl group; Z is hydrogen or C.sub.1-4 alkyl optionally substituted by a hydroxy group; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.9a and R.sup.9b are a variety of substituents; R.sup.6 is hydrogen, C.sub.1-6 akyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2-4 akyl substituted by C.sub.1-4 alkoxy or hydroxy, R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2-4 alkyl substituted by one or two substituents selected from C.sub.1-4 alkoxy, hydroxy or a 4-, 5- or 6-membered heteroaliphatic ring containing one or two heteroatoms selected from N, O and S; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, form a saturated or partially saturated heterocyclic ring or a non-aromatic azabicyclic ring system; and n is zero, 1 or 2; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherapeutic neuralgia.
摘要翻译： PCT No.PCT / GB96 / 02766 Sec。 371日期：1998年5月14日 102（e）日期1998年5月14日PCT 1996年11月13日PCT公布。 WO97 / 18206 PCT公开号日期：1997年5月22日本发明涉及式（I）化合物，其中X为含有1至4个氮原子且任选地在环中含有一个氧或硫原子的5-或6-元C-连接的杂芳环; Y是式 - （CH2）nNR6R7或亚甲基或乙烯连接的咪唑基的基团; Z是氢或任选被羟基取代的C 1-4烷基; R1，R2，R3，R4，R5，R9a和R9b是多种取代基; R 6是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基或被C 1-4烷氧基或羟基取代的C 2-4烷基，R 7是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基或被一个或两个选自C 1-4烷氧基，羟基或含有一个或两个选自N，O和S的杂原子的4-，5-或6-元杂脂肪族环取代的C 2-4烷基; 或R6和R7与它们所连接的氮原子一起形成饱和或部分饱和的杂环或非芳族氮杂双环体系; n为零，1或2; 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，呕吐和治疗后神经痛。

2. 发明授权

US07598386B2 Sulphones which modulate the action of gamma-secretase 有权
标题翻译：调节γ-分泌酶的作用的手机
公开(公告)号：US07598386B2
公开(公告)日：2009-10-06
申请号：US11788888
申请日：2007-04-23
申请人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
发明人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
IPC分类号： C07D211/00 , C07D211/68 , C07D211/40 , C07D211/70 , C07D309/00
CPC分类号： C07D207/27 , C07C317/14 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07D207/12 , C07D207/404 , C07D211/18 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/40 , C07D233/56 , C07D233/64 , C07D241/18 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/38 , C07D263/44 , C07D271/06 , C07D277/26 , C07D285/12 , C07D295/088 , C07D295/096 , C07D295/182 , C07D307/52 , C07D309/08 , C07D309/10 , C07D317/48 , C07D317/72 , C07D491/10 , C07F7/0812
摘要： Novel sulphones of Formula I are disclosed: wherein A completes a 4-7 membered ring optionally comprising up to two heteroatoms. The compounds modulate the action of γ-secretase and are therefore useful in the treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式I的新型砜：其中A完成任选包含最多两个杂原子的4-7元环。该化合物调节γ-分泌酶的作用，因此可用于治疗或预防阿尔茨海默氏病。

3. 发明授权

US07595344B2 Sulphones which modulate the action of gamma secretase 有权
标题翻译：调节γ分泌酶作用的手机
公开(公告)号：US07595344B2
公开(公告)日：2009-09-29
申请号：US12151296
申请日：2008-05-06
申请人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
发明人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
IPC分类号： A61K31/65
CPC分类号： C07D207/27 , C07C317/14 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07D207/12 , C07D207/404 , C07D211/18 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/40 , C07D233/56 , C07D233/64 , C07D241/18 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/38 , C07D263/44 , C07D271/06 , C07D277/26 , C07D285/12 , C07D295/088 , C07D295/096 , C07D295/182 , C07D307/52 , C07D309/08 , C07D309/10 , C07D317/48 , C07D317/72 , C07D491/10 , C07F7/0812
摘要： Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.
摘要翻译：公开了调节γ-分泌酶作用的唾液。该化合物可用于治疗或预防阿尔茨海默病。

5. 发明授权

US07304094B2 Cyclohexyl sulphones 有权
标题翻译：环己基砜
公开(公告)号：US07304094B2
公开(公告)日：2007-12-04
申请号：US11261365
申请日：2005-10-28
申请人： Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams , Brian John Williams
发明人： Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams , Brian John Williams
IPC分类号： A61K31/165 , C07C321/24
CPC分类号： C07D213/40 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/27 , C07D207/404 , C07D211/44 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/36 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/56 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/72 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/44 , C07D271/06 , C07D271/10 , C07D277/26 , C07D285/12 , C07D295/096 , C07D295/185
摘要： Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
摘要翻译：公式I的新型手机被公开：

6. 发明授权

US06984663B2 Cyclohexyl sulphones 有权
标题翻译：环己基砜
公开(公告)号：US06984663B2
公开(公告)日：2006-01-10
申请号：US10223993
申请日：2002-08-20
申请人： Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams , Brian John Williams
发明人： Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams , Brian John Williams
IPC分类号： A61K31/19 , C07C317/12 , C07C317/14
CPC分类号： C07D213/40 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/27 , C07D207/404 , C07D211/44 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/36 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/56 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/72 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/44 , C07D271/06 , C07D271/10 , C07D277/26 , C07D285/12 , C07D295/096 , C07D295/185
摘要： Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式I的新型砜：该化合物通过γ-分泌酶调节淀粉样蛋白前体蛋白的加工，因此可用于治疗或预防阿尔茨海默氏病。

7. 发明授权

US6096729A Use of NK-1 receptor antagonists for treating amnestic disorders 失效
标题翻译：使用NK-1受体拮抗剂治疗遗忘性疾病
公开(公告)号：US6096729A
公开(公告)日：2000-08-01
申请号：US980928
申请日：1997-12-01
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
IPC分类号： C07D491/107 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/4525 , A61K31/5375 , A61K31/5377 , A61K31/675 , A61K45/00 , A61P9/10 , A61P25/28 , C07D211/56 , C07D265/32 , C07D413/06 , C07D491/10 , A61K31/44 , A61K31/535
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides methods for the treatment or prevention of amnestic disorders which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist.
摘要翻译：本发明提供了治疗或预防遗忘性疾病的方法，其包括口服活性的长效中枢神经系统（CNS）渗透的NK-1受体拮抗剂的口服给药。

8. 发明授权

US5985874A Substituted morpholine derivative and its use as a therapeutic agent 失效
标题翻译：取代的吗啉衍生物及其作为治疗剂的用途
公开(公告)号：US5985874A
公开(公告)日：1999-11-16
申请号：US306957
申请日：1999-05-07
申请人： Simon Neil Owen , Christopher John Swain , Brian John Williams
发明人： Simon Neil Owen , Christopher John Swain , Brian John Williams
IPC分类号： C07D413/06 , A61K31/535
CPC分类号： C07D413/06
摘要： The present invention relates to the compound of formula (I) or a pharmaceutically acceptable salt thereof.The compounds are of particular use in the treatment or prevention of pain or inflammation, migraine, emesis, postherpetic neuralgia, depression or anxiety.
摘要翻译：本发明涉及式（I）化合物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或炎症，偏头痛，呕吐，带状疱疹后神经痛，抑郁症或焦虑症。

9. 发明授权

US6087348A Use of NK-1 receptor antagonists for treating stress disorders 有权
标题翻译：使用NK-1受体拮抗剂治疗应激障碍
公开(公告)号：US6087348A
公开(公告)日：2000-07-11
申请号：US328743
申请日：1999-06-09
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
IPC分类号： A61K31/44 , A61K31/535 , A61K31/675 , A61K31/4445
CPC分类号： A61K31/44 , A61K31/535 , A61K31/675
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of stress disorders without concomitant therapy with other anti-stress agents, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.
摘要翻译：本发明提供口服活性的长效CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防应激障碍的药物中的用途，而不与其它抗应激剂同时治疗，使用这样的NK-1受体拮抗剂的药物组合物的方法和包含它的药物组合物。

10. 发明授权

US6060469A Spiro-piperidine derivatives and their use as tachykinin antagonists 失效
标题翻译：螺哌啶衍生物及其作为速激肽拮抗剂的用途
公开(公告)号：US6060469A
公开(公告)日：2000-05-09
申请号：US77063
申请日：1998-05-18
申请人： Raymond Baker , Timothy Harrison , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Timothy Harrison , Christopher John Swain , Brian John Williams
IPC分类号： A61K31/00 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61K31/505 , A61K31/506 , A61P1/00 , A61P1/08 , A61P25/06 , A61P29/00 , A61P43/00 , C07D491/10 , C07D491/107 , C07D471/10
CPC分类号： C07D491/10
摘要： The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.10 are a variety of substituents defined in the specification; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, emesis and postherpetic neuralgia.
摘要翻译： PCT No.PCT / GB96 / 02853 Sec。 371日期1998年5月18日 102（e）日期1998年5月18日PCT提交1996年11月20日PCT公布。公开号WO97 / 19084 日期：1997年5月29日本发明涉及式（I）化合物，其中R 1表示卤素，羟基，任选被一个或三个氟原子取代的C 1-6烷基，任选被一至三个氟原子取代的C 1-6烷氧基，或任选被一至三个氟原子取代的C 1-6烷硫基; R 2表示氢，卤素，C 1-6烷基或C 1-6烷氧基; 或者当R 2与R 1相邻时，它们可以连接在一起，使得形成含有一个或两个氧原子的5-或6-元饱和或不饱和环; R3表示含有1,2,3或4个选自氮，氧和硫的杂原子的任选取代的5-或6-元芳族杂环基; m为0-3，n为0-3，条件是m + n的总和为2或3; p为零或1; q为1或2; 当m为1且n为1或2时，虚线表示任选的双键; R4，R5，R6，R9和R10是说明书中定义的各种取代基; 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，呕吐和带状疱疹后神经痛。

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