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公开(公告)号:US20100016371A1
公开(公告)日:2010-01-21
申请号:US12373307
申请日:2007-07-09
申请人: Gerard Martin Paul Giblin , Adrian Hall , David Nigel Hurst , Tiziana Scoccitti , Pamela Joan Theobald
发明人: Gerard Martin Paul Giblin , Adrian Hall , David Nigel Hurst , Tiziana Scoccitti , Pamela Joan Theobald
IPC分类号: A61K31/427 , C07D417/04 , C07D401/04 , A61K31/4439 , A61P25/00
CPC分类号: C07D417/04 , C07D209/08 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/06
摘要: The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof; wherein X, R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译: 本申请涉及式(I)化合物或其药学上可接受的衍生物; 其中X,R 1,R 2和R 3如本说明书中所定义,制备这些化合物的方法,包含这些化合物的药物组合物以及这些化合物在医药中的用途。
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公开(公告)号:US20090298866A1
公开(公告)日:2009-12-03
申请号:US12373315
申请日:2007-07-09
IPC分类号: A61K31/437 , C07D277/28 , C07D277/24 , C07D417/14 , C07D471/04 , A61K31/427 , A61K31/44 , A61P37/04
CPC分类号: C07D417/04 , C07D413/04
摘要: The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein X, R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译: 本申请涉及式(I)化合物或其药学上可接受的衍生物:其中X,R 1,R 2和R 3如说明书中所定义的式(I),制备这些化合物的方法,药物组合物,包含 这些化合物和这些化合物在医药中的应用。
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3.
公开(公告)号:US20100204242A1
公开(公告)日:2010-08-12
申请号:US12676158
申请日:2008-09-04
申请人: Desmond John Best , Sing Yeung Mak , Barry Sidney Orlek , Geracimos Rassias , Pamela Joan Theobald
发明人: Desmond John Best , Sing Yeung Mak , Barry Sidney Orlek , Geracimos Rassias , Pamela Joan Theobald
IPC分类号: A61K31/496 , C07D405/12 , A61P25/00 , A61P25/28
CPC分类号: C07D309/12
摘要: The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}piperazine or a pharmaceutically acceptable salt thereof, in particular the hydrochloride salt thereof and crystalline forms of the hydrochloride salt; to processes for the preparation of the compound or its salt; to compositions containing it; and to its use in the treatment or prophylaxis of neurological or psychiatric diseases, such as cognitive impairment, fatigue or a sleep disorder, for example in a mammal such as a human.The compound or a salt thereof has affinity for and is an antagonist and/or inverse agonist of the histamine H3 receptor.
摘要翻译: 本发明涉及1-(1-甲基乙基)-4 - {[4-(四氢-2H-吡喃-4-基氧基)苯基]羰基}哌嗪或其药学上可接受的盐,特别是其盐酸盐和结晶 形式的盐酸盐; 制备化合物或其盐的方法; 含有它的组合物; 以及其在治疗或预防神经或精神疾病如认知障碍,疲劳或睡眠障碍中的用途,例如在哺乳动物如人中的用途。 该化合物或其盐对组胺H3受体具有亲和性,并且是拮抗剂和/或反向激动剂。
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公开(公告)号:US20110046137A1
公开(公告)日:2011-02-24
申请号:US12599416
申请日:2008-05-08
申请人: Paul John Beswick , Laura Jane Chambers , Iain Patrick Chessell , David John Davies , Emmanuel Hubert Demont , Robert James Gleave , David George Hubert Livermore , Pamela Joan Theobald , Mythily Vimal , Daryl Simon Walter
发明人: Paul John Beswick , Laura Jane Chambers , Iain Patrick Chessell , David John Davies , Emmanuel Hubert Demont , Robert James Gleave , David George Hubert Livermore , Pamela Joan Theobald , Mythily Vimal , Daryl Simon Walter
IPC分类号: A61K31/415 , C07D231/12 , C07D403/06 , A61K31/4178 , C07D401/04 , A61K31/4439 , C07D417/04 , A61K31/427 , C07D403/04 , A61K31/501 , A61K31/506 , C07D471/08 , A61K31/439 , C07D413/06 , A61K31/5377 , A61P29/00 , A61P25/28
CPC分类号: C07D231/12 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D405/12 , C07D417/04 , C07D417/06 , C07D471/08
摘要: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The pyrazole derivatives of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐:式(I)的吡唑衍生物或其盐调节P2X7受体功能,并能够拮抗ATP在P2X7受体(P2X7受体) 拮抗剂)。 本发明还涉及这些化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的疾病/疾病中的用途,例如疼痛,炎症或神经变性疾病。
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5.
公开(公告)号:US08288389B2
公开(公告)日:2012-10-16
申请号:US12676158
申请日:2008-09-04
申请人: Desmond John Best , Sing Yeung Mak , Barry Sidney Orlek , Geracimos Rassias , Pamela Joan Theobald
发明人: Desmond John Best , Sing Yeung Mak , Barry Sidney Orlek , Geracimos Rassias , Pamela Joan Theobald
IPC分类号: A61K31/496 , C07D309/12
CPC分类号: C07D309/12
摘要: The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}piperazine or a pharmaceutically acceptable salt thereof, in particular the hydrochloride salt thereof and crystalline forms of the hydrochloride salt; to processes for the preparation of the compound or its salt; to compositions containing it; and to its use in the treatment or prophylaxis of neurological or psychiatric diseases, such as cognitive impairment, fatigue or a sleep disorder, for example in a mammal such as a human. The compound or a salt thereof has affinity for and is an antagonist and/or inverse agonist of the histamine H3 receptor.
摘要翻译: 本发明涉及1-(1-甲基乙基)-4 - {[4-(四氢-2H-吡喃-4-基氧基)苯基]羰基}哌嗪或其药学上可接受的盐,特别是其盐酸盐和结晶 形式的盐酸盐; 制备化合物或其盐的方法; 含有它的组合物; 以及其用于治疗或预防神经或精神疾病,例如认知障碍,疲劳或睡眠障碍,例如在哺乳动物如人中的用途。 该化合物或其盐对组胺H3受体具有亲和性,并且是拮抗剂和/或反向激动剂。
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6.
公开(公告)号:US20090170869A1
公开(公告)日:2009-07-02
申请号:US12203946
申请日:2008-09-04
申请人: Desmond John BEST , Sing Yeung Mak , Barry Sidney Orlek , Geracimos Rassias , Pamela Joan Theobald
发明人: Desmond John BEST , Sing Yeung Mak , Barry Sidney Orlek , Geracimos Rassias , Pamela Joan Theobald
IPC分类号: A61K31/497 , C07D405/12
CPC分类号: C07D309/12
摘要: The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}piperazine or a pharmaceutically acceptable salt thereof, in particular the hydrochloride salt thereof and crystalline forms of the hydrochloride salt; to processes for the preparation of the compound or its salt; to compositions containing it; and to its use in the treatment or prophylaxis of neurological or psychiatric diseases, such as cognitive impairment, fatigue or a sleep disorder, for example in a mammal such as a human.The compound or a salt thereof has affinity for and is an antagonist and/or inverse agonist of the histamine H3 receptor.
摘要翻译: 本发明涉及1-(1-甲基乙基)-4 - {[4-(四氢-2H-吡喃-4-基氧基)苯基]羰基}哌嗪或其药学上可接受的盐,特别是其盐酸盐和结晶 形式的盐酸盐; 制备化合物或其盐的方法; 含有它的组合物; 以及其用于治疗或预防神经或精神疾病,例如认知障碍,疲劳或睡眠障碍,例如在哺乳动物如人中的用途。 该化合物或其盐对组胺H3受体具有亲和性,并且是拮抗剂和/或反向激动剂。
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