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48 条记录 (耗时 0.028 秒)

    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。

    Substituted quinoline-4-carboxylic hydrazides as NK-2/NK-3 receptor ligands
    2.
    发明授权
    Substituted quinoline-4-carboxylic hydrazides as NK-2/NK-3 receptor ligands 失效
    取代的喹啉-4-羧酸酰肼作为NK-2 / NK-3受体配体

    公开(公告)号：US07482457B2

    公开(公告)日：2009-01-27

    申请号：US10544440

    申请日：2004-02-03

    申请人： Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod

    发明人： Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod

    IPC分类号： C07D215/38

    CPC分类号： C07D215/52

    摘要： The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR′R″ or C1-6 alkyl-NR′R″ where R′ and R″ are independently chosen from hydrogen and C1-4 alkyl and where R′ and R″, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR′R″ as defined above or R2 is C1-6 alkoxy substituted by NR′R″ as defined above; R3 is hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl or aryl C1-6 alkyl; R5 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl, aryl C1-6 alkyl or C1-6 alkoxycarbonyl; or R4 and R5, together with the nitrogen atom to which they are attached, form a C3-C10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF3, halogen and C1-4 alkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome.

    摘要翻译： 本发明公开了式（I）的化合物：其中：R1是芳基或杂芳基环; R 2是羟基，C 1-6烷氧基，C 1-6烷基，氨基，NR'R“或C 1-6烷基-NR'R”，其中R'和R“独立地选自氢和C 1-4烷基， 其中R'和R“与它们所连接的氮原子一起形成任选含有另外的氮原子并且任选地被如上所定义的NR'R”取代的饱和含氮3-7元杂环或R2 是由如上定义的NR'R“取代的C 1-6烷氧基; R3是氢或C1-6烷基; R4是氢，C1-8烷基，C2-8烯基，C2-8炔基，C3-8环烷基，芳基或芳基C1-6烷基; R5是氢，C1-8烷基，C2-8烯基，C2-8炔基，C3-8环烷基，芳基，芳基C1-6烷基或C1-6烷氧基羰基; 或R 4和R 5与它们所连接的氮原子一起形成C 3 -C 10单环或双环饱和环; X和Y独立地选自氢，羟基，硝基，氨基，氰基，CF 3，卤素和C 1-4烷基; 或其药学上可接受的盐; 作为用于治疗精神分裂症，COPD，哮喘或肠易激综合征的NK-2 / NK-3配体。

    Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
    5.
    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
    7.
    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。

    Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition
    9.
    发明授权
    Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition 失效
    取代的1,2,3-三唑并[1,5-a]喹唑啉用于增强认知

    公开(公告)号：US07144887B2

    公开(公告)日：2006-12-05

    申请号：US10149852

    申请日：2000-12-11

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

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

    IPC分类号： A61K471/04 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a linking portion and X is generally an aromatic or non-aromatic heterocycle, alkyl or alkylcarbonyl and Z is generally a heterocycle such as 5-methylisoxazol-3-yl, and pharmaceutically acceptable salts thereof for enhancing cognition in conditions such as Alzheimer's Disease, pharmaceutical compositions comprising them, their use for manufacturing medicaments and methods of treatment using them

    摘要翻译： 本发明提供式（I）化合物，其中R 1通常是氢或CF 3，R 2通常是氢，W 是环状胺，杂环或LYX基团，其中LY是连接部分，X通常是芳族或非芳族杂环，烷基或烷基羰基，Z通常是杂环，例如5-甲基异恶唑-3-基和药学上 用于增强诸如阿尔茨海默氏病等疾病的认知的可接受的盐，包含它们的药物组合物，其用于制备药物的用途和使用它们的治疗方法

    Piperidine and tetrahydropyridine derivatives
    10.
    发明授权
    Piperidine and tetrahydropyridine derivatives 失效
    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。