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    Substituted 1,4-piperazine-heteroaryl derivatives as 5-HT.sub.1D receptor agonists
    1.
    发明授权
    Substituted 1,4-piperazine-heteroaryl derivatives as 5-HT.sub.1D receptor agonists 失效
    取代的1,4-哌嗪 - 杂芳基衍生物作为5-HT1D受体激动剂

    公开(公告)号：US5849746A

    公开(公告)日：1998-12-15

    申请号：US894302

    申请日：1997-07-22

    申请人： Mark Stuart Chambers ,  Angus Murray MacLeod ,  Victor Giulio Matassa

    发明人： Mark Stuart Chambers ,  Angus Murray MacLeod ,  Victor Giulio Matassa

    IPC分类号： A61K31/495 ,  A61P9/00 ,  A61P25/04 ,  A61P43/00 ,  C07D403/14 ,  C07D413/14

    CPC分类号： C07D403/14

    摘要： A class of 1,4-disubstituted piperazine derivatives, further substituted on one of the carbon atoms of the piperazine ring, 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, 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 / 00179 Sec。 371日期1997年7月22日 102（e）日期1997年7月22日PCT提交1996年1月29日PCT公布。 出版物WO96 / 23785 日期1996年8月8日一类在哌嗪环的一个碳原子上进一步取代的1,4-二取代哌嗪衍生物是5-HT1样受体的选择性激动剂，是人5-HT1Dα的有效激动剂 受体亚型，而相对于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。

    Piperazine, piperidine and tetrahydropyridine derivative of indol-3-alkyl as 5-HT.sub.1D-.alpha. agonists
    2.
    发明授权
    Piperazine, piperidine and tetrahydropyridine derivative of indol-3-alkyl as 5-HT.sub.1D-.alpha. agonists 失效
    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。

    Benzodiazepine derivatives
    4.
    发明授权
    Benzodiazepine derivatives 失效
    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。

    Indoline and azaindoline derivatives as 5-HT.sub.1D alpha receptor agonists
    5.
    发明授权
    Indoline and azaindoline derivatives as 5-HT.sub.1D alpha receptor agonists 失效
    二氢吲哚和唑啉衍生物作为5-HT1Dα受体激动剂

    公开(公告)号：US5919783A

    公开(公告)日：1999-07-06

    申请号：US776626

    申请日：1997-01-21

    申请人： Mark Stuart Chambers ,  Victor Giulio Matassa ,  Leslie Joseph Street

    发明人： Mark Stuart Chambers ,  Victor Giulio Matassa ,  Leslie Joseph Street

    IPC分类号： C07D521/00 ,  A61K31/495 ,  C07D403/14 ,  C07D471/04

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    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 1-4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1-6 carbon atoms; T represents nitrogen or CH; R.sup.1 represents aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, either of which groups may be optionally substituted; and R.sup.2 represents hydrogen or C.sub.1-6 alkyl 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 / GB95 / 01756 Sec。 371日期1997年1月21日 102（e）1997年1月21日PCT PCT 1995年7月24日PCT公布。 出版物WO96 / 04269 日期：2002年2月15日式（I）化合物或其盐或前体药物，其中Z表示选自呋喃，噻吩，吡咯，恶唑，噻唑，异恶唑，异噻唑，咪唑，吡唑等的任选取代的五元杂芳族环， 恶二唑，噻二唑，三唑和四唑; E表示化学键或含有1-4个碳原子的直链或支链亚烷基链; Q表示含有1-6个碳原子的直链或支链亚烷基链; T表示氮或CH; R1表示芳基（C1-6）烷基或杂芳基（C1-6）烷基，其中任一个可以任选被取代; 并且R 2表示氢或C 1-6烷基是5-HT1样受体的选择性激动剂，其是人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。

    Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
    8.
    发明授权
    Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition 失效
    氮取代的1,2,4-三唑并[3,4-a]酞嗪衍生物用于增强认知

    公开(公告)号：US06900209B2

    公开(公告)日：2005-05-31

    申请号：US10432391

    申请日：2001-11-22

    申请人： Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey ,  Helen Jane Szekeres

    发明人： Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey ,  Helen Jane Szekeres

    IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61P25/28

    CPC分类号： C07D487/04

    摘要： The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.

    摘要翻译： 本发明提供式（I）的化合物，其中A是任选取代的C 1-4烷基或键，R 20和R 21， / SO 2是氢，烷基或杂环基，R 1和R 2是小取代基或氢，L是O，S或取代的N，X是5 - 或6-元杂芳环，Y是C 1-4 - 亚烷基，Z是5-或6-元杂芳环; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗; 其用于制备用于治疗神经退行性疾病的药物和使用其增强认知的方法。

    Substituted indolylpropyl-piperazine derivatives as 5-HT.sub.1D .alpha. agonists
    10.
    发明授权
    Substituted indolylpropyl-piperazine derivatives as 5-HT.sub.1D .alpha. agonists 失效
    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。