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。

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。

公开(公告)号：US20110190274A1

公开(公告)日：2011-08-04

申请号：US13058559

申请日：2009-08-14

申请人： Caroline Jane Day ,  Trevor Raymond Keel ,  Geracimos Rassias

发明人： Caroline Jane Day ,  Trevor Raymond Keel ,  Geracimos Rassias

IPC分类号： A61K31/551 ,  C07D243/08 ,  A61P11/00

CPC分类号： C07D309/12 ,  Y02P20/55

摘要： The invention relates to 1-isopropyl-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}hexahydro-1H-1,4-diazepine mono-maleate, and crystalline Form 1 thereof.

摘要翻译： 本发明涉及1-异丙基-4 - {[4-（四氢-2H-吡喃-4-基氧基）苯基]羰基}六氢-1H-1,4-二氮杂单马来酸酯及其晶型1。

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。