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公开(公告)号：US20080108663A1
公开(公告)日：2008-05-08
申请号：US11664190
申请日：2005-09-26
IPC分类号： C07D211/96 , A61K31/445 , A61P25/00 , A61P25/18
CPC分类号： C07D211/96
摘要： The present invention is directed to cyclopropyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neuro-transmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
摘要翻译： 本发明涉及抑制甘氨酸转运蛋白GlyT1的环丙基哌啶化合物，其可用于治疗与甘氨酸能或谷氨酸能神经传递功能障碍相关的神经和精神疾病以及其中涉及甘氨酸转运蛋白GlyT1的疾病。
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公开(公告)号：US07304063B2
公开(公告)日：2007-12-04
申请号：US10554186
申请日：2004-04-20
IPC分类号： C07D401/10 , C07D403/10 , A61K31/53 , A61P35/00 , C07D253/06
CPC分类号： C07D417/14 , C07D253/065 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention is directed to compounds which contain a heterocyclic triazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
摘要翻译： 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的杂环三嗪部分的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。
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公开(公告)号：US20120214832A1
公开(公告)日：2012-08-23
申请号：US13386397
申请日：2010-07-23
IPC分类号： A61K31/438 , A61P35/00 , C07D471/10
CPC分类号： C07D471/10
摘要： Disclosed are isoform selective Phospholipase D inhibitors. In one aspect, the disclosed compounds can have a structure represented by a formula (I): Also disclosed are methods of making and using the compounds. Also disclosed are pharmaceutical compositions and kits comprising the compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译： 公开了同工型选择性磷脂酶D抑制剂。 一方面，所公开的化合物可以具有由式（I）表示的结构：还公开了制备和使用该化合物的方法。 还公开了包含该化合物的药物组合物和试剂盒。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。
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公开(公告)号：US20110288090A1
公开(公告)日：2011-11-24
申请号：US13147392
申请日：2010-01-25
申请人： Donna J. Armstrong , Yasuhiro Goto , Takashi Hashihayata , Tetsuya Kato , Michael J. Kelly, III , Mark E. Layton , Craig W. Lindsley , Yoshio Ogino , Yu Onozaki , Kenvin J. Rodzinak , Michael A. Rossi , Philip E. Sanderson , Jiabing Wang , Melissa M. Yaroschak
发明人： Donna J. Armstrong , Yasuhiro Goto , Takashi Hashihayata , Tetsuya Kato , Michael J. Kelly, III , Mark E. Layton , Craig W. Lindsley , Yoshio Ogino , Yu Onozaki , Kenvin J. Rodzinak , Michael A. Rossi , Philip E. Sanderson , Jiabing Wang , Melissa M. Yaroschak
IPC分类号： A61K31/5377 , A61K31/4985 , A61K31/496 , A61K31/506 , A61K31/498 , A61K31/438 , A61K31/4375 , C07D475/04 , C07D471/04 , C07D401/12 , A61P35/00 , A61K31/519
CPC分类号： C07D471/04 , C07D217/24 , C07D241/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D475/02 , C07D475/04 , C07D487/04 , C07D519/00
摘要： The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 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给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：US07834031B2
公开(公告)日：2010-11-16
申请号：US11991727
申请日：2006-09-25
IPC分类号： A61K31/445 , C07D211/06 , C07D401/04
CPC分类号： C07D211/64 , A61K51/0455 , C07B59/002 , C07D401/04
摘要： The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.
摘要翻译： 本发明涉及可用于哺乳动物中甘氨酸转运蛋白的标记和诊断成像的放射性标记的甘氨酸转运蛋白抑制剂。
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公开(公告)号：US20100216841A1
公开(公告)日：2010-08-26
申请号：US11922399
申请日：2006-06-28
IPC分类号： A61K31/445 , C07D211/34 , C07D405/06 , C07D403/06 , C07D413/06 , C07D417/06 , A61K31/453 , A61K31/454 , A61P25/00
CPC分类号： C07D211/38
摘要： The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
摘要翻译： 本发明涉及作为T型钙通道拮抗剂的4-氟哌啶化合物，其可用于治疗或预防涉及T型钙通道的神经和精神疾病及疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道的疾病中的用途。
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公开(公告)号：US20100041652A1
公开(公告)日：2010-02-18
申请号：US12605690
申请日：2009-10-26
IPC分类号： A61K31/5377 , A61K31/445 , A61K31/40 , A61K31/4523
CPC分类号： C07D403/12 , C07D209/42 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises an indole-sulfonamide moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
摘要翻译： 本发明涉及能够抑制，调节和/或调节受体型和非受体型酪氨酸激酶的信号转导的化合物。 本发明的化合物具有包含吲哚磺酰胺部分的核心结构。 本发明还涉及这些化合物的药学上可接受的盐，水合物和立体异构体。
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公开(公告)号：US20090270451A1
公开(公告)日：2009-10-29
申请号：US12084027
申请日：2006-10-27
申请人： David Hallett , Craig W. Lindsley , Elizabeth M. Naylor , Zhijian Zhao , Cory R. Theberge , Scott E. Wolkenberg , M. Brad Nolt
发明人： David Hallett , Craig W. Lindsley , Elizabeth M. Naylor , Zhijian Zhao , Cory R. Theberge , Scott E. Wolkenberg , M. Brad Nolt
IPC分类号： A61K31/4545 , C07D211/30 , A61P25/18 , C07D401/04 , C07D211/96 , A61K31/5355 , A61K31/497 , A61K31/445
CPC分类号： C07D211/96 , C07D401/04 , C07D405/06
摘要： The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
摘要翻译： 本发明涉及抑制甘氨酸转运蛋白GlyT1的哌啶化合物，其可用于治疗与甘氨酸能或谷氨酸能神经传递功能障碍相关的神经和精神疾病以及其中涉及甘氨酸转运蛋白GlyT1的疾病。
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公开(公告)号：US09453017B2
公开(公告)日：2016-09-27
申请号：US14348036
申请日：2012-09-30
申请人： Craig W. Lindsley , Alex H. Brown
发明人： Craig W. Lindsley , Alex H. Brown
IPC分类号： A61K31/44 , A61K31/70 , A61K31/35 , A61K31/215 , A61K31/13 , C07D471/10 , A61K45/06 , A61K31/05 , A61K31/138 , A61K31/4535 , A61K31/454 , A61K31/435 , A61K31/4709 , A61K31/498 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/231 , A61K31/661
CPC分类号： C07D471/10 , A61K31/05 , A61K31/138 , A61K31/231 , A61K31/435 , A61K31/4535 , A61K31/454 , A61K31/4709 , A61K31/498 , A61K31/661 , A61K45/06 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , A61K2300/00 , A61K31/683
摘要： Disclosed are methods of treating viral infections comprising, in one aspect, administering compounds that are phospholipase D inhibitors. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to antiviral therapies. For example, compounds having Phospholipase D activity (e.g., isoform selective Phospholipase D inhibitors) can be useful in antiviral therapies (e.g., influenza treatments).
摘要翻译： 公开了治疗病毒感染的方法，其一方面包括施用作为磷脂酶D抑制剂的化合物。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。 根据本发明的目的，如本文中体现和广泛描述的，本发明在一个方面涉及抗病毒疗法。 例如，具有磷脂酶D活性的化合物（例如，同种型选择性磷脂酶D抑制剂）可用于抗病毒疗法（例如流感病毒治疗）。
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公开(公告)号：US20090269278A1
公开(公告)日：2009-10-29
申请号：US11991727
申请日：2005-09-29
IPC分类号： A61K51/04 , C07D211/96 , C12Q1/02
CPC分类号： C07D211/64 , A61K51/0455 , C07B59/002 , C07D401/04
摘要： The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.
摘要翻译： 本发明涉及可用于哺乳动物中甘氨酸转运蛋白的标记和诊断成像的放射性标记的甘氨酸转运蛋白抑制剂。
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