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1. 发明授权

US5807857A Piperazine, piperidine and tetrahydropyridine derivative of indol-3-alkyl as 5-HT.sub.1D-.alpha. agonists 失效
标题翻译：吲哚-3-烷基的哌嗪，哌啶和四氢吡啶衍生物作为5-HT1D-α激动剂
公开(公告)号：US5807857A
公开(公告)日：1998-09-15
申请号：US737769
申请日：1996-11-15
申请人： Jose Luis Castro Pineiro , Mark Stuart Chambers , Sarah Christine Hobbs , Austin John Reeve , Graham Andrew Showell , Leslie Joseph Street , Victor Giulio Matassa
发明人： Jose Luis Castro Pineiro , Mark Stuart Chambers , Sarah Christine Hobbs , Austin John Reeve , Graham Andrew Showell , Leslie Joseph Street , Victor Giulio Matassa
IPC分类号： C07D401/14 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/495 , A61P9/00 , A61P25/04 , A61P25/06 , A61P43/00 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04
摘要： Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1 to 6 carbon atoms, optionally substituted in any position by a hydroxy group; T represents nitrogen or CH; U represents nitrogen or C--R.sup.2 ; V represents oxygen, sulphur or N--R.sup.3 ; --F--G-- represents --CH2--N--, --CH2--CH-- or --CH.dbd.C--; R.sup.1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, any of which groups may be optionally substituted; and R.sup.2 and R.sup.3 independently represent hydrogen or C.sub.1-6 alkyl are selective agonists of 5-HT1D receptors, being potent agonists of the human 5-HT1Dalpha receptor subtype, while possessing at least a 10-fold selective affinity for the 5-HT1Dalpha receptor subtype, relative to the 5-HT1Dbeta subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
摘要翻译： PCT No.PCT / GB95 / 01129 Sec。 371日期1996年11月15日 102（e）日期1996年11月15日PCT提交1995年5月18日PCT公布。公开号WO95 / 32196 （I）式（I）化合物或其盐或前药，其中Z表示选自呋喃，噻吩，吡咯，恶唑，噻唑，异恶唑的任选取代的五元杂芳环，异噻唑，咪唑，吡唑，恶二唑，噻二唑，三唑和四唑; E表示化学键或含有1至4个碳原子的直链或支链亚烷基链; Q表示任选被羟基取代的含有1至6个碳原子的直链或支链亚烷基链; T表示氮或CH; U表示氮或C-R2; V表示氧，硫或N-R3; -F-G-表示-CH 2 -N，-CH 2 -CH-或-CH = C-; R 1表示C 3-6烯基，C 3-6炔基，芳基（C 1-6）烷基或杂芳基（C 1-6）烷基，其中任何基团可以任选被取代; 并且R 2和R 3独立地表示氢或C 1-6烷基是5-HT1D受体的选择性激动剂，它是人5-HT1Dalpha受体亚型的有效激动剂，同时对5-HT1Dalpha受体亚型具有至少10倍的选择性亲和力，相对于5-HT1Dbeta亚型; 因此，它们可用于治疗和/或预防临床症状，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

2. 发明授权

US5854268A Azetidine, pyrrolidine and piperidine derivatives 失效
标题翻译：氮杂环丁烷，吡咯烷，哌啶衍生物
公开(公告)号：US5854268A
公开(公告)日：1998-12-29
申请号：US776024
申请日：1997-01-22
申请人： Raymond Baker , Sylvie Bourrain , Jose Luis Castro Pineiro , Mark Stuart Chambers , Alexander Richard Guiblin , Sarah Christine Hobbs , Richard Alexander Jelley , Andrew Madin , Victor Giulio Matassa , Austin John Reeve , Michael Geoffrey Russell , Graham Andrew Showell , Francine Sternfeld , Leslie Joseph Street , Monique Bodil Van Niel
发明人： Raymond Baker , Sylvie Bourrain , Jose Luis Castro Pineiro , Mark Stuart Chambers , Alexander Richard Guiblin , Sarah Christine Hobbs , Richard Alexander Jelley , Andrew Madin , Victor Giulio Matassa , Austin John Reeve , Michael Geoffrey Russell , Graham Andrew Showell , Francine Sternfeld , Leslie Joseph Street , Monique Bodil Van Niel
IPC分类号： C07D401/14 , A61K31/41 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/475 , A61P9/00 , A61P25/04 , A61P43/00 , C07D403/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
摘要翻译： PCT No.PCT / GB95 / 01819 Sec。 371日期1997年1月22日 102（e）1997年1月22日PCT PCT 1995年8月1日PCT公布。公开号WO96 / 04274 日期1996年2月15日一类取代的氮杂环丁烷，吡咯烷和哌啶衍生物是5-HT1样受体的选择性激动剂，它是人类5-HT1Dα受体亚型的有效激动剂，同时具有至少10倍的选择性亲和力 5-HT1Dα受体亚型相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

3. 发明授权

US6140347A Azetidine, pyrrolidine and piperidine derivatives as 5-HT receptor agonists 失效
标题翻译：氮杂环丁烷，吡咯烷和哌啶衍生物作为5-HT受体激动剂
公开(公告)号：US6140347A
公开(公告)日：2000-10-31
申请号：US171208
申请日：1998-10-14
申请人： Jose Luis Castro Pineiro , Andrew Madin , Joseph George Neduvelil , Graham Andrew Showell , Leslie Joseph Street , Monique Bodil Van Niel
发明人： Jose Luis Castro Pineiro , Andrew Madin , Joseph George Neduvelil , Graham Andrew Showell , Leslie Joseph Street , Monique Bodil Van Niel
IPC分类号： C07D521/00 , A61K31/445 , A61K31/415 , C07D401/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A class of compounds of formula (I) wherein Z, E, Q, T, U, V, W, M, R.sup.1, R.sup.7 and R.sup.8 are as defined herein; are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists. ##STR1##
摘要翻译： PCT No.PCT / GB97 / 01137 Sec。 371日期：1998年10月14日 102（e）日期1998年10月14日PCT 1997年4月24日PCT公布。出版物WO97 / 42189 日期：1997年11月13日一类其中Z，E，Q，T，U，V，W，M，R 1，R 7和R 8如本文所定义的式（I）化合物; 是5-HT1样受体的选择性激动剂，其是人类5-HT1Dα受体亚型的有效激动剂，同时相对于5-HT1Dβ亚型对5-HT1Dα受体亚型具有至少10倍的选择性亲和力; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

4. 发明授权

US6048878A Substituted piperidine derivatives as selective agonists of 5-HT receptors 失效
标题翻译：取代的哌啶衍生物作为5-HT受体的选择性激动剂
公开(公告)号：US6048878A
公开(公告)日：2000-04-11
申请号：US68752
申请日：1998-05-13
申请人： Jose Luis Castro Pineiro , Ian James Collins , Angus Murray MacLeod , Christopher Richard Moyes , Michael Rowley , Graham Andrew Showell
发明人： Jose Luis Castro Pineiro , Ian James Collins , Angus Murray MacLeod , Christopher Richard Moyes , Michael Rowley , Graham Andrew Showell
IPC分类号： C07D521/00 , A61K31/445 , C07D401/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A compound of formula (I), or a salt or prodrug thereof, is described, wherein G is attached at position 3 or 4 of the piperidine ring and represents halogen or C.sub.1-6 alkoxy; R1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl (C.sub.1-6)alkyl, any of which groups may be optionally substituted; processes for its preparation and its use in therapy, particularly in the treatment of migraine.
摘要翻译： PCT No.PCT / GB96 / 02765 Sec。 371日期1998年5月13日 102（e）1998年5月13日PCT PCT 1996年11月13日PCT公布。公开号WO97 / 18202 PCT 日期：1997年5月22日描述了式（I）化合物或其盐或前药，其中G连接在哌啶环的3或4位，代表卤素或C 1-6烷氧基; R 1表示C 3-6烯基，C 3-6炔基，芳基（C 1-6）烷基或杂芳基（C 1-6）烷基，其中任何一个可以任选被取代; 其制备方法及其在治疗中的应用，特别是治疗偏头痛。

5. 发明授权

US5696110A Benzodiazepine derivatives and their use as antagonists of cholecystokinin and/or gastrin receptors 失效
标题翻译：苯并二氮杂衍生物及其作为胆囊收缩素和/或胃泌素受体拮抗剂的用途
公开(公告)号：US5696110A
公开(公告)日：1997-12-09
申请号：US523661
申请日：1995-09-05
申请人： Sylvie Bourrain , Stephen Robert Fletcher , Victor Giulio Matassa , Graham Andrew Showell
发明人： Sylvie Bourrain , Stephen Robert Fletcher , Victor Giulio Matassa , Graham Andrew Showell
IPC分类号： C07D243/20 , C07D403/04 , A61K31/55 , C07D401/04 , C07D413/04
CPC分类号： C07D403/04 , C07D243/20
摘要： ##STR1## Compounds of formula (I), and salts and prodrugs thereof, wherein X is O,S,NR
4 or CH
2 ; R
1 represents H, certain optionally substituted C
1-6 alkyl, or C
3-7 cycloalkyl; R
2 represents phenyl having certain optional substituents; R
3 represents C
1-6 alkyl, halo or NR
6 R
7 ; m is 2,3 or 4; n is 1,2,3,4,5,6 7 or 8 when X is CH
2 or 2,3,4,5,6,7 or 8 when X is O, S or NR
4 ; and x is 0,1,2, or 3; are CCK and/or gastrin antagonists. They and compositions thereof are therefore useful in therapy.
摘要翻译：式（I）化合物及其盐和前体药物，其中X为O，S，NR4或CH2; R1表示H，某些任选取代的C 1-6烷基或C 3-7环烷基; R2表示具有某些任选取代基的苯基; R 3表示C 1-6烷基，卤代或NR 6 R 7; m是2,3或4; 当X为CH 2时，n为1,2,3,4,5,6,7或8，X为O，S或NR4时为2,3,4,5,6,7或8; x为0,1,2或3; 是CCK和/或胃泌素拮抗剂。因此，它们及其组合物可用于治疗。

6. 发明授权

US06211219B1 Aminocyclohexane derivatives as 5-HT receptor agonists 失效
标题翻译：氨基环己烷衍生物作为5-HT受体激动剂
公开(公告)号：US06211219B1
公开(公告)日：2001-04-03
申请号：US09214343
申请日：1999-01-04
申请人： Angus Murray MacLeod , Graham Andrew Showell , Leslie Joseph Street
发明人： Angus Murray MacLeod , Graham Andrew Showell , Leslie Joseph Street
IPC分类号： C07D40306
CPC分类号： C07D231/12 , C07D209/14 , C07D233/56 , C07D249/08
摘要： A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
摘要翻译：一类取代的氨基环己烷衍生物是5-HT1样受体的选择性激动剂，它是人类5-HT1Dalpha受体亚型的有效激动剂，同时对5-HT1Dalpha受体亚型具有至少10倍的选择性亲和力， HT1Dbeta亚型; 因此，它们可用于治疗和/或预防临床症状，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起更少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

7. 发明授权

US5998416A Piperazine, piperidine and tetrahydropyridine derivatives as 5-HT receptor agonists 失效
标题翻译：哌嗪，哌啶和四氢吡啶衍生物作为5-HT受体激动剂
公开(公告)号：US5998416A
公开(公告)日：1999-12-07
申请号：US171930
申请日：1998-10-26
申请人： Sylvie Bourrain , Angus Murray MacLeod , Graham Andrew Showell , Leslie Joseph Street
发明人： Sylvie Bourrain , Angus Murray MacLeod , Graham Andrew Showell , Leslie Joseph Street
IPC分类号： C07D405/04 , C07D405/14 , A61K31/495 , A61K31/505
CPC分类号： C07D405/04 , C07D405/14
摘要： A class of N-substituted piperazine, piperidine, and tetrahydropyridine derivatives, further subltitutedat the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
摘要翻译： PCT No.PCT / GB97 / 01329 Sec。 371日期：1998年10月26日 102（e）日期1998年10月26日PCT提交1997年5月15日PCT公布。出版物WO97 / 45432 PCT 日期1997年12月4日一类N-取代的哌嗪，哌啶和四氢吡啶衍生物，通过任选取代的烯基，炔基，芳基 - 烷基或杂芳基 - 烷基部分进一步在4-位上被取代为5-HT1- 作为人5-HT1Dα受体亚型的有效激动剂，同时相对于5-HT1Dβ亚型对5-HT1Dα受体亚型具有至少10倍的选择性亲和力; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

8. 发明授权

US6127388A Azetidine, pyrrolidine and piperidine derivatives as 5-HT.sub.1D receptor agonists 失效
标题翻译：氮杂环丁烷，吡咯烷和哌啶衍生物作为5-HT1D受体激动剂
公开(公告)号：US6127388A
公开(公告)日：2000-10-03
申请号：US171929
申请日：1998-10-26
申请人： Sylvie Bourrain , Angus Murray MacLeod , Graham Andrew Showell , Leslie Joseph Street
发明人： Sylvie Bourrain , Angus Murray MacLeod , Graham Andrew Showell , Leslie Joseph Street
IPC分类号： A61P25/06 , C07D405/14 , A61K31/443
CPC分类号： C07D405/14
摘要： A class of substituted azetidine, pyrrolidine and piperidine derivatives of Formula I are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists. ##STR1##
摘要翻译： PCT No.PCT / GB97 / 01330 Sec。 371日期：1998年10月26日 102（e）日期1998年10月26日PCT提交1997年5月15日PCT公布。公开号WO97 / 45426 PCT 日期1997年12月4日一类式I的取代的氮杂环丁烷，吡咯烷和哌啶衍生物是5-HT1样受体的选择性激动剂，是人类5-HT1Dα受体亚型的有效激动剂，同时具有至少10倍的选择性相对于5-HT1Dβ亚型的5-HT1Dα受体亚型的亲和力; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

9. 发明授权

US06852744B2 Pyrrolidine derivatives and their use as chymase inhibitor 失效
标题翻译：吡咯烷衍生物及其作为胃促胰酶抑制剂的用途
公开(公告)号：US06852744B2
公开(公告)日：2005-02-08
申请号：US10363036
申请日：2001-08-21
申请人： Takashi Deguchi , Ryotaro Shiratake , Fuminori Sato , Buichi Fujitani , Yayoi Honda , Akihiko Kiyoshi , Mitsue Notake , Graham Andrew Showell , Robert George Boyle , Sukhbinder Singh Klair
发明人： Takashi Deguchi , Ryotaro Shiratake , Fuminori Sato , Buichi Fujitani , Yayoi Honda , Akihiko Kiyoshi , Mitsue Notake , Graham Andrew Showell , Robert George Boyle , Sukhbinder Singh Klair
IPC分类号： C12N9/99 , A61K38/00 , A61P9/00 , A61P9/10 , A61P29/00 , A61P37/08 , A61P43/00 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/08 , C07K5/10 , A61K31/42 , A61K31/41 , C07D261/18 , C07D285/06
CPC分类号： C07K5/06026 , A61K38/00 , C07K5/06034 , C07K5/06191 , C07K5/0827 , C07K5/1027
摘要： Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein R1 is cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; R2 is H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; R3 is (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): R4 and R5 are independently H or OH, but R4 and R5 are not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof.
摘要翻译：新型吡咯烷衍生物可用作合成活性化合物的胃促胰酶抑制剂或中间体，其具有式（I）：其中R 1是环烷基，取代或未取代的苯基或萘基，茚满基，噻吩基，呋喃基，取代或未取代的吲哚基，苯并呋喃基，取代或未取代的苯并噻吩基等; R 2是H，烷基，苯基 - 低级烷基，环烷基或环烷基 - 低级烷基; R 3是（i）取代或未取代的单环杂环基，（ii）取代或未取代的苯 - 或吡啶稠合杂环基，或（iii）基团（a）：R 4和R 5是独立地是H或OH，但R 4和R 5不同时为H，或两者都形成氧代; n为0,1,2或3; 或其盐。

10. 发明申请

US20090291915A1 Silicon Compounds and Their Use 审中-公开
标题翻译：硅化合物及其用途
公开(公告)号：US20090291915A1
公开(公告)日：2009-11-26
申请号：US11721525
申请日：2001-12-16
申请人： Graham Andrew Showell , David John Miller
发明人： Graham Andrew Showell , David John Miller
IPC分类号： A61K31/695 , C07F7/10 , A61P3/10
CPC分类号： C07F7/0812 , C07F7/0814
摘要： A compound of any of formulae (I) to (III) wherein at least one of Y and Z includes a Si atom, is of utility in therapy.
摘要翻译：其中Y和Z中的至少一个包括Si原子的式（I）至（III）中任一项的化合物在治疗中是有用的。

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