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1. 发明授权

US06262103B1 Thienycyclohexanone derivatives as ligands of the GABAA &agr;5 receptor subtype 失效
标题翻译：噻吩环己酮衍生物作为GABAAα5受体亚型的配体
公开(公告)号：US06262103B1
公开(公告)日：2001-07-17
申请号：US09284591
申请日：1999-04-16
申请人： Howard Barff Broughton , Mark Stewart Chambers , Sarah Christine Hobbs , Angus Murray MacLeod , Austin John Reeve
发明人： Howard Barff Broughton , Mark Stewart Chambers , Sarah Christine Hobbs , Angus Murray MacLeod , Austin John Reeve
IPC分类号： A61K314155
CPC分类号： C07D417/14 , A61K31/381 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4436 , A61K31/4439 , A61K31/496 , A61K31/497 , A61K31/506 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要： A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.
摘要翻译：药用组合物包含式（I）化合物或其药学上可接受的盐，其中A为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基，芳基C 1-6烷基，芳基，S（O ）pR1。

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

US5681833A Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US5681833A
公开(公告)日：1997-10-28
申请号：US302936
申请日：1994-09-20
申请人： Jose Luis Castro Pineiro , Mark Stuart Chambers , Sarah Christine Hobbs , Victor Giulio Matassa
发明人： Jose Luis Castro Pineiro , Mark Stuart Chambers , Sarah Christine Hobbs , Victor Giulio Matassa
IPC分类号： A61K31/55 , A61K31/551 , A61P1/04 , A61P25/04 , A61P25/20 , C07D243/14 , C07D243/24 , C07D403/04 , C07D403/12 , C07D403/14
CPC分类号： C07D403/12 , C07D243/14 , C07D243/24 , C07D403/14
摘要： Compounds of Formula (I), and salts and prodrugs thereof, wherein said formula, R.sup.1 represents certain optionally substituted alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents (II) or (III), where m is 0, 1, 2 or 3; R.sup.9 is H or C.sub.1-6 alkyl; R.sup.10 is imidazolyl, triazolyl or tetrazolyl, and R.sup.11 is H, C.sub.1-6 alkyl or halo; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 is C.sub.1-7 alkyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkylC.sub.1-4 alkyl, C.sub.6-10 bicycloalkyl, optionally substituted aryl, or NR.sub.12 R.sub.13 ; R.sup.5 is H or C.sub.1-4 alkyl; n is 0, 1, 2 or 3; which are CCK and/or gastrin antagonists useful in therapy.
摘要翻译： PCT No.PCT / GB93 / 00599 Sec。 371日期1994年9月20日 102（e）1994年9月20日PCT 1993年3月23日PCT公布。出版物WO93 / 19052 （III）式（I）化合物及其盐和前药，其中所述式R1表示某些任选取代的烷基或C 3 -C 10烷基， 7环烷基; R2表示（II）或（III），其中m为0,1,2或3; R9是H或C1-6烷基; R10是咪唑基，三唑基或四唑基，R11是H，C1-6烷基或卤素; R3是C1-6烷基，卤素或NR6R7; R 4是C 1-7烷基，C 3-10环烷基，C 3-10环烷基C 1-4烷基，C 6-10二环烷基，任选取代的芳基或NR 12 R 13; R5是H或C1-4烷基; n为0,1,2或3; 其是可用于治疗的CCK和/或胃泌素拮抗剂。

4. 发明授权

US5998415A Bicyclic heteroaryl-alkylene-(homo)piperazinones and thione analogues thereof, their preparation, and their use of as selective agonists of 5-HT.sub.1 -like receptors 失效
标题翻译：双环杂芳基 - 亚烷基 - （同）哌嗪酮及其硫酮类似物，其制备及其作为5-HT1样受体选择性激动剂的用途
公开(公告)号：US5998415A
公开(公告)日：1999-12-07
申请号：US065020
申请日：1998-04-17
申请人： Mark Stuart Chambers , Sarah Christine Hobbs , Leslie Joseph Street
发明人： Mark Stuart Chambers , Sarah Christine Hobbs , Leslie Joseph Street
IPC分类号： C07D403/06 , C07D521/00 , A61K31/495 , C07D403/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/06
摘要： A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while 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, while 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 / GB96 / 02624。 371日期：1998年4月17日 102（e）1998年4月17日PCT PCT 1996年10月28日PCT公布。公开号WO97 / 16446 日期1997年5月9日一类哌嗪酮，高哌嗪酮和其硫酮类似物在1位被任选取代的烯基，炔基，芳基 - 烷基或杂芳基 - 烷基部分取代，并通过亚烷基间隔基在4-位连接至稠合双环杂芳族部分，通常为吲哚基，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，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力相对于5-HT1Dβ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。

5. 发明授权

US6156761A Substituted tetralone derivatives for enhancing cognition 失效
标题翻译：用于增强认知的取代的四氢萘酮衍生物
公开(公告)号：US6156761A
公开(公告)日：2000-12-05
申请号：US296847
申请日：1999-04-22
申请人： Helen Jane Bryant , Mark Stuart Chambers , Sarah Christine Hobbs
发明人： Helen Jane Bryant , Mark Stuart Chambers , Sarah Christine Hobbs
IPC分类号： C07D213/50 , C07D213/89 , C07D239/26 , C07D241/12 , C07D261/08 , C07D277/24 , C07D277/26 , C07D277/28 , C07D405/12 , C07D409/12 , C07D417/12 , C07D213/46 , A61K31/4418
CPC分类号： C07D213/89 , C07D213/50 , C07D239/26 , C07D241/12 , C07D261/08 , C07D277/24 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein A, B, R2, R3 and q are as defined in the disclosure, pharmaceutical compositions containing them; methods for their production; their use in therapy and methods of treatment of disease states where cognition enhancement is required, such as Alzheimer's disease.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐：其中A，B，R2，R3和q如本公开所定义，含有它们的药物组合物; 生产方法; 它们在治疗中的应用和治疗需要认知增强的疾病状态的方法，例如阿尔茨海默病。

6. 发明授权

US5973156A Piperidine and tetrahydropyridine derivatives 失效
标题翻译：哌啶和四氢吡啶衍生物
公开(公告)号：US5973156A
公开(公告)日：1999-10-26
申请号：US68723
申请日：1998-05-13
申请人： Mark Stuart Chambers , Sarah Christine Hobbs , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant
发明人： Mark Stuart Chambers , Sarah Christine Hobbs , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant
IPC分类号： C07D401/06 , C07D413/14 , C07D521/00 , C07D401/14 , A61K31/445 , C07D409/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D413/14
摘要： A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, 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.spsb..alpha. receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT.sub.1D.spsb..alpha. receptor subtype relative to the 5-HT.sub.1D.spsb..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 / GB96 / 02795 Sec。 371日期1998年5月13日 102（e）日期1998年5月13日PCT 1996年11月14日PCT PCT。公开号WO97 / 19073 日期1997年5月29日一类取代的哌啶和四氢吡啶衍生物，其通过其4-位通过亚烷基链连接到稠合的双环杂芳族部分如吲哚基，并且在1位被进一步被任选取代的烷基，烯基，炔基，环烷基 - 烷基，芳基 - 烷基或杂芳基 - 烷基部分是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，同时处理至少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。

7. 发明授权

US5925638A Substituted 1-indolylpropyl-4-benzylpiperazine derivatives 失效
标题翻译：取代的1-吲哚基丙基-4-苄基哌嗪衍生物
公开(公告)号：US5925638A
公开(公告)日：1999-07-20
申请号：US68072
申请日：1998-04-28
申请人： Mark Stuart Chambers , Sarah Christine Hobbs , Leslie Joseph Street
发明人： Mark Stuart Chambers , Sarah Christine Hobbs , Leslie Joseph Street
IPC分类号： C07D521/00 , A61K31/495 , C07D403/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A class of 1-�3-(1H-indol-3-yl)propyl!-4-benzylpiperazine derivatives of formula I, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by a range of substituted alkyl groups, 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 / GB96 / 02682 Sec。 371日期：1998年4月28日 102（e）1998年4月28日PCT PCT 1996年11月4日PCT公布。公开号WO97 / 17338 日期1997年5月15日将式I的1- [3-（1H-吲哚-3-基）丙基] -4-苄基哌嗪衍生物在吲哚核的5-位被1,2,4-三唑三唑-4-基部分，以及苄基部分亚甲基连接的一系列取代的烷基是5-HT1样受体的选择性激动剂，是人5-HT1Dα受体亚型的有效激动剂，同时具有对5-HT1Dα受体亚型相对于5-HT1Dβ亚型的至少10倍选择性亲和力; 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

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。

9. 发明授权

US06355638B1 Pyrazolo[1,5-d][1,2,4] triazines for enhancing cognition 有权
标题翻译：吡唑并[1,5-d] [1,2,4]三嗪用于增强认知
公开(公告)号：US06355638B1
公开(公告)日：2002-03-12
申请号：US09717423
申请日：2000-11-21
申请人： Helen Jane Bryant , William Robert Carling , Mark Stuart Chambers , Sarah Christine Hobbs , Philip Jones , Angus Murray MacLeod
发明人： Helen Jane Bryant , William Robert Carling , Mark Stuart Chambers , Sarah Christine Hobbs , Philip Jones , Angus Murray MacLeod
IPC分类号： C07D48714
CPC分类号： C07D487/04
摘要： Compounds according to Formula (I) or a salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition:
摘要翻译：根据式（I）的化合物或其盐是可用于增强认知的GABA-Aα5配体：

10. 发明授权

US5981529A Substituted indolylpropyl-piperazine derivatives as 5-HT.sub.1D .alpha. agonists 失效
标题翻译：取代的吲哚基丙基哌嗪衍生物作为5-HT1Dα激动剂
公开(公告)号：US5981529A
公开(公告)日：1999-11-09
申请号：US043440
申请日：1998-03-18
申请人： Raymond Baker , Mark Stuart Chambers , Sarah Christine Hobbs , Angus Murray MacLeod , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
发明人： Raymond Baker , Mark Stuart Chambers , Sarah Christine Hobbs , Angus Murray MacLeod , Austin John Reeve , Francine Sternfeld , Leslie Joseph Street
IPC分类号： C07D403/04 , A61K31/00 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/4196 , A61P25/06 , A61P43/00 , C07D403/06 , C07D521/00 , A61K31/495 , C07D403/14 , C07D413/14
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： A class of 1-[3-(1H-indol-3-yl)propyl]-4-(2-phenylethyl)piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, on one or other of the ethylene carbon atoms of the phenethyl moiety by halogen, trifluoromethyl, alkyl, hydroxyalkyl or alkoxyalkyl, and optionally on the phenyl ring of the phenethyl moiety by halogen, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, 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 / GB96 / 02309 Sec。 371日期1998年3月18日 102（e）1998年3月18日PCT PCT 1996年9月19日PCT公布。公开号WO97 / 11695 日期1997年4月3日一类1- [3-（1H-吲哚-3-基）丙基] -4-（2-苯基乙基）哌嗪衍生物，其在吲哚核的5-位被五元三氟甲基，烷基，羟基烷基或烷氧基烷基，以及任选地在苯乙基部分的苯环上被卤素，三氟甲基，烷氧基或恶唑烷酮基团任选地在苯乙基部分的一个或另外的乙烯碳原子上，一个或两个另外的取代基是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，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力 5-HT1D beta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。

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