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公开(公告)号:US07381725B2
公开(公告)日:2008-06-03
申请号:US10524006
申请日:2003-08-04
IPC分类号: A61K31/501 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D237/14 , C07D237/20 , A61P25/28
CPC分类号: C07D401/04 , C07D401/14 , C07D403/04 , C07D409/04 , C07D471/04
摘要: A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译: 一类由任选取代的杂芳环在4-位取代的哒嗪衍生物是GABA A受体的选择性配体,特别是对α2和/或α3和/或其α5亚基具有高亲和力,因此有益于 治疗和/或预防中枢神经系统的不良状况,包括焦虑,抽搐和认知障碍。
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公开(公告)号:US20090170824A1
公开(公告)日:2009-07-02
申请号:US12316388
申请日:2008-12-12
申请人: Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alen Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
发明人: Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alen Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
IPC分类号: A61K31/397 , A61K31/47 , A61K31/335 , A61K31/10 , A61K31/535 , A61K31/497
CPC分类号: C07C317/28 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/36 , C07C317/42 , C07C317/44 , C07D205/04 , C07D207/10 , C07D211/38 , C07D211/72 , C07D213/34 , C07D213/71 , C07D217/24 , C07D231/12 , C07D233/64 , C07D241/08 , C07D249/08 , C07D261/08 , C07D271/10 , C07D277/26 , C07D295/096 , C07D317/62 , C07D319/18
摘要: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译: 式I化合物是人5-HT 2A受体的有效和选择性拮抗剂,因此可用于治疗CNS的多种不利条件。
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公开(公告)号:US07217740B2
公开(公告)日:2007-05-15
申请号:US11212789
申请日:2005-08-26
申请人: Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
发明人: Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
IPC分类号: A61K31/10 , C07C317/44
CPC分类号: C07C317/28 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/36 , C07C317/42 , C07C317/44 , C07D205/04 , C07D207/10 , C07D211/38 , C07D211/72 , C07D213/34 , C07D213/71 , C07D217/24 , C07D231/12 , C07D233/64 , C07D241/08 , C07D249/08 , C07D261/08 , C07D271/10 , C07D277/26 , C07D295/096 , C07D317/62 , C07D319/18
摘要: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译: 式I的化合物是人5-HT 2A 2A受体的有效和选择性拮抗剂,因此可用于治疗CNS的各种不利条件。
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公开(公告)号:US07468393B2
公开(公告)日:2008-12-23
申请号:US11796389
申请日:2007-04-27
申请人: Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
发明人: Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
IPC分类号: A61K31/10 , C07C317/24 , C07C317/32
CPC分类号: C07C317/28 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/36 , C07C317/42 , C07C317/44 , C07D205/04 , C07D207/10 , C07D211/38 , C07D211/72 , C07D213/34 , C07D213/71 , C07D217/24 , C07D231/12 , C07D233/64 , C07D241/08 , C07D249/08 , C07D261/08 , C07D271/10 , C07D277/26 , C07D295/096 , C07D317/62 , C07D319/18
摘要: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译: 式I化合物是人5-HT 2A受体的有效和选择性拮抗剂,因此可用于治疗CNS的多种不利条件。
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公开(公告)号:US09023865B2
公开(公告)日:2015-05-05
申请号:US14353381
申请日:2012-10-25
申请人: Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
发明人: Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
IPC分类号: C07D401/14 , A61K31/437 , C07D471/04 , C07D519/00 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06
CPC分类号: C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D519/00
摘要: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译: 公开了式(1)的ERK抑制剂及其药学上可接受的盐。 还公开了使用式(1)的化合物治疗癌症的方法。
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公开(公告)号:US08847715B2
公开(公告)日:2014-09-30
申请号:US13627233
申请日:2012-09-26
申请人: Kevin Wilson , Robert Tarzwell , Patrick McGuire
发明人: Kevin Wilson , Robert Tarzwell , Patrick McGuire
CPC分类号: H01H51/2281 , H01F7/0221 , H01H50/043 , H01H51/229 , H01H2050/007
摘要: A permanent magnet is pivotally mounted in a top spacer layer of a switching device and rests on a flex arm created in an underlying flex circuit layer. The underside of the flex arm rests on a thin bar formed in a lower spacer layer beneath which lies a base layer including an electromagnet. Activation of the electromagnet causes rotation of the flex arm to thereby close and open electrical contacts formed respectively on the underside of the flex arm and on the top surface of the base layer.
摘要翻译: 永磁体枢转地安装在开关装置的顶部间隔层中并且搁置在在下面的柔性电路层中产生的挠性臂上。 柔性臂的下侧搁置在形成在下部间隔层中的细条上,下部隔离层位于包括电磁体的基底层。 电磁体的激活导致柔性臂的旋转,从而闭合并打开分别形成在柔性臂的下侧和基底层的顶表面上的电触头。
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公开(公告)号:US20130116231A1
公开(公告)日:2013-05-09
申请号:US13809436
申请日:2011-07-07
IPC分类号: C07D411/14 , C07D403/14 , C07D403/04 , C07D401/14 , C07D401/12
CPC分类号: C07D411/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14
摘要: The present invention relates to 1,4-dihydropyridazinone derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译: 本发明涉及1,4-二氢哒嗪酮衍生物,其可用于治疗细胞增殖性疾病,用于治疗与MET活性相关的疾病,以及用于抑制受体酪氨酸激酶MET。 本发明还涉及包含这些化合物的组合物,以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号:US08420695B2
公开(公告)日:2013-04-16
申请号:US13002776
申请日:2009-07-01
申请人: Kevin Wilson , Gabriela de Almeida , Andrew Haidle , Kaleen Konrad , Michelle Machacek , Ann Zabierek
发明人: Kevin Wilson , Gabriela de Almeida , Andrew Haidle , Kaleen Konrad , Michelle Machacek , Ann Zabierek
IPC分类号: A61K31/38 , C07D333/36 , C07D333/42
CPC分类号: C07D333/38 , C07D409/04 , C07D409/12 , C07D413/12
摘要: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
摘要翻译: 本发明提供抑制四种已知的哺乳动物JAK激酶(JAK1,JAK2,JAK3和TYK2)的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物施用于需要治疗骨髓增生性疾病或癌症的患者的JAK1,JAK2,JAK3和TYK2的活性的方法。
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公开(公告)号:US08415346B2
公开(公告)日:2013-04-09
申请号:US13056180
申请日:2009-07-21
申请人: Michael Altman , Kevin Wilson
发明人: Michael Altman , Kevin Wilson
IPC分类号: A61K31/541 , A61K31/5377 , A61K31/496 , C07D231/38 , C07D413/12 , C07D403/12 , C07D417/12
CPC分类号: C07D231/38 , C07D401/12
摘要: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
摘要翻译: 本发明提供抑制四种已知的哺乳动物JAK激酶(JAK1,JAK2,JAK3和TYK2)的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物施用于需要治疗骨髓增生性疾病或癌症的患者的JAK1,JAK2,JAK3和TYK2的活性的方法。
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公开(公告)号:US08367706B2
公开(公告)日:2013-02-05
申请号:US12665045
申请日:2008-06-16
申请人: Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyun Chong Woo , Jonathan Young , Anna Zabierek
发明人: Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyun Chong Woo , Jonathan Young , Anna Zabierek
IPC分类号: A61K31/4436 , C07D409/12
CPC分类号: C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/65586 , C07F9/65685
摘要: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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