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公开(公告)号：US07825135B2
公开(公告)日：2010-11-02
申请号：US10593950
申请日：2005-03-23
申请人： Wesley Blackaby , Mark E. Duggan , David Hallett , George D. Hartman , Andrew S. Jennings , William H. Leister , Richard T. Lewis , Craig W. Lindsley , Elizabeth Naylor , Leslie J. Street , Yi Wang , David D. Wisnoski , Scott E. Wolkenberg , Zhijian Zhao
发明人： Wesley Blackaby , Mark E. Duggan , David Hallett , George D. Hartman , Andrew S. Jennings , William H. Leister , Richard T. Lewis , Craig W. Lindsley , Elizabeth Naylor , Leslie J. Street , Yi Wang , David D. Wisnoski , Scott E. Wolkenberg , Zhijian Zhao
IPC分类号： A61K31/435 , A61K31/445
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D413/14
摘要： The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl 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的吡啶基，哒嗪基，嘧啶基和吡嗪基哌啶化合物，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：US07947714B2
公开(公告)日：2011-05-24
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： A61K31/445 , C07D211/32
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：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：US07776886B2
公开(公告)日：2010-08-17
申请号：US11664190
申请日：2005-09-26
IPC分类号： A61K31/445 , C07D211/96
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：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：US20100179122A1
公开(公告)日：2010-07-15
申请号：US11922681
申请日：2006-06-23
IPC分类号： A61K31/404 , C07D413/12 , A61K31/5377 , C07D209/40 , C07D405/12 , C07D401/12 , A61K31/4439 , A61K31/454 , A61K31/427 , C07D417/12 , C07D401/14 , A61K31/496 , A61P31/18
CPC分类号： C07D413/12 , C07D209/40 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D417/14
摘要： Compounds of Formula (I): are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 式（I）的化合物是HIV逆转录酶抑制剂，其中R1，R2，R3，R4和R5如本文所定义。 式（I）化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗艾滋病毒感染以及预防，延迟发作和治疗艾滋病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US20090258853A1
公开(公告)日：2009-10-15
申请号：US12225027
申请日：2007-03-09
IPC分类号： A61K31/4709 , C07D401/14 , A61K31/506
CPC分类号： C07D409/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D417/14
摘要： This invention relates to compounds which are agonists of somatostatin and selective toward somatostatin receptor subtype SSTR2. The compounds are useful in the treatment and prevention of diabetes, and diabetes-related pathologies, including retinopathy, neuropathy and nephropathy. Many of the compounds are orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostatin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof.
摘要翻译： 本发明涉及作为生长抑素的激动剂并且对生长抑素受体亚型SSTR2有选择性的化合物。 该化合物可用于治疗和预防糖尿病以及糖尿病相关病理学，包括视网膜病变，神经病变和肾病。 许多化合物是口服活性的。 因此，本发明的目的是描述这些化合物。 进一步的目的是描述生长抑素激动剂的具体优选的立体异构体。 另一个目的是描述制备这些化合物的方法。 另一个目的是描述使用这些化合物作为其活性成分的方法和组合物。
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公开(公告)号：US20100222322A1
公开(公告)日：2010-09-02
申请号：US11922682
申请日：2006-06-23
IPC分类号： A61K31/404 , A61P31/18 , C07D403/12 , C07D401/12 , A61K31/454 , A61K31/496
CPC分类号： A61K31/551 , C07D209/42 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 式（I）的吲哚化合物是HIV逆转录酶抑制剂，其中R 1，R 2，R 3，R 4和R 5在本文中定义。 式（I）化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗艾滋病毒感染以及预防，延迟发作和治疗艾滋病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US20100168097A1
公开(公告)日：2010-07-01
申请号：US11922672
申请日：2006-06-23
IPC分类号： A61K31/5377 , C07D403/04 , A61K31/4178 , C07D413/14 , C07D417/14 , A61K31/4245 , A61K31/4439 , A61P31/18
CPC分类号： C07D413/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： Compounds of Formula I: Formula (I); are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 式I化合物：式（I）; 是HIV逆转录酶抑制剂，其中R 1，R 2，R 3，R 4和R 5在本文中定义。 式（I）化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗艾滋病毒感染以及预防，延迟发作和治疗艾滋病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US07576083B2
公开(公告)日：2009-08-18
申请号：US11579234
申请日：2005-04-29
IPC分类号： A61K31/5377 , C07D413/06 , C07D413/14
CPC分类号： C07D211/62 , C07D211/96 , C07D405/12 , C07D417/12
摘要： The present invention is directed to morpholinyl 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的吗啉基哌啶化合物，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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