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48 条记录 (耗时 0.049 秒)

    Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
    32.
    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 1-indolylpropyl-4-benzyl-tetrahydropyridine derivatives
    35.
    发明授权
    Substituted 1-indolylpropyl-4-benzyl-tetrahydropyridine derivatives 失效
    取代的1-吲哚基丙基-4-苄基 - 四氢吡啶衍生物

    公开(公告)号：US5994374A

    公开(公告)日：1999-11-30

    申请号：US068631

    申请日：1998-05-08

    申请人： Sylvie Bourrain ,  Angus Murray MacLeod ,  Joseph George Neduvelil ,  Graham Andrew Showell

    发明人： Sylvie Bourrain ,  Angus Murray MacLeod ,  Joseph George Neduvelil ,  Graham Andrew Showell

    IPC分类号： C07D521/00 ,  A61K31/44 ,  C07D401/14

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

    摘要： A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzyl-1,2,5,6-tetrahydropyridine derivatives, 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 an alkyl, alkoxy, or alkoxy-alkoxy substituent, 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 5HT.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.alpha. receptors is indicated, and are expected to have fewer undesirable cardiovascular and other side effects.

    摘要翻译： PCT No.PCT / GB96 / 02684。 371日期1998年5月8日 102（e）日期1998年5月8日PCT 1996年11月4日PCT PCT。 公开号WO97 / 17337 日期1997年5月15日一类在吲哚核的5-位被取代的1- [3-（1H-吲哚-3-基）丙基] -4-苄基-1,2,5,6-四氢吡啶衍生物 1,2,4-三唑-4-基部分，并且在烷基，烷氧基或烷氧基 - 烷氧基取代基上的苄基部分的亚甲基键是5-HT1样受体的选择性激动剂，其为 人类5-HT1Dα受体亚型，而对5HT1Dα受体亚型相对于5-HT1Dβ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-HT1Dα受体的亚型选择性激动剂，并且预期具有较少的不期望的心血管和其它副作用 。

    Piperazine, piperidine and tetrahydropyridine derivatives
    36.
    发明授权
    Piperazine, piperidine and tetrahydropyridine derivatives 失效
    哌嗪，哌啶和四氢吡啶衍生物

    公开(公告)号：US5977116A

    公开(公告)日：1999-11-02

    申请号：US68680

    申请日：1998-05-12

    申请人： Jose Luis Castro Pineiro ,  Angus Murray MacLeod ,  Michael Rowley ,  Monique Bodil Van Niel

    发明人： Jose Luis Castro Pineiro ,  Angus Murray MacLeod ,  Michael Rowley ,  Monique Bodil Van Niel

    IPC分类号： C07D521/00 ,  A01N43/60 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00

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

    摘要： A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at 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 recptor agonists.

    摘要翻译： PCT No.PCT / GB96 / 02762 Sec。 371日期：1998年5月12日 102（e）日期1998年5月12日PCT提交1996年11月13日PCT公布。 公开号WO97 / 18203 日期1997年5月22日一类N-取代的哌嗪，哌啶和四氢吡啶衍生物通过氟取代的亚烷基链连接到稠合双环杂芳族部分如吲哚基，并且在4-位被进一步被任选取代的烯基，炔基 ，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，是人类5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dα受体具有至少10倍的选择性亲和力 亚型相对于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。

    Substituted 1,4-piperazine-heteroaryl derivatives as 5-HT.sub.1D receptor agonists
    37.
    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。

    4-phenyl-4-phenylpropyl(enyl)-piperidines as tachykinin antagonists
    40.
    发明授权
    4-phenyl-4-phenylpropyl(enyl)-piperidines as tachykinin antagonists 失效

    公开(公告)号：US5663352A

    公开(公告)日：1997-09-02

    申请号：US583014

    申请日：1996-01-19

    申请人： Angus Murray MacLeod ,  Kevin John Merchant ,  Graeme Irvine Stevenson

    发明人： Angus Murray MacLeod ,  Kevin John Merchant ,  Graeme Irvine Stevenson

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61K31/53 ,  A61P1/08 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00 ,  C07D211/18 ,  C07D211/22 ,  C07D211/32 ,  C07D401/06 ,  C07D211/14 ,  C07D211/12

    CPC分类号： C07D401/06 ,  C07D211/18 ,  C07D211/22 ,  C07D211/32

    摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R.sup.1 represents optionally substituted phenyl; R.sup.2 represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R.sup.3 represents H, COR.sup.9, CO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, COCO.sub.2 R.sup.10, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, hydroxy, cyano, COR.sup.9, NR.sup.10 R.sup.11, C(NOH)NR.sup.10 R.sup.11, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15 and optionally substituted phenyl), Y--R.sup.8 or CO--Z--(CH.sub.2).sub.q --R.sup.12 ; R.sup.4 and R.sup.5 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, hydroxy or C.sub.1-6 alkoxy, or R.sup.4 and R.sup.5 together form a group .dbd.O; R.sup.6 and R.sup.7 each independent represents H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, hydroxy or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 together form a group .dbd.O; R.sup.8 represents an optionally substituted aromatic heterocycle; R.sup.9 represents H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, or phenyl; R.sup.10 and R.sup.11 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.3-5 cycloalkylmethyl; R.sup.12 represents NR.sup.13 R.sup.14 or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; R.sup.13 and R.sup.14 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, optionally substituted phenyl or phenylC.sub.1-4 alkyl; R.sup.15 represents C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, trifluoromethyl or optionally substituted phenyl; Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms which may optionally be substituted by oxo; Z represents CH.sub.2, O, S or NR.sup.10 ; and q represents 0, 1, 2, 3, 4, 5 or 6. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.