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公开(公告)号：US09139576B2
公开(公告)日：2015-09-22
申请号：US14115123
申请日：2012-04-30
申请人： Douglas C. Beshore , Robert M. Garbaccio , Scott D. Kuduk , Adam W. Johnson , Jason W. Skudlarek
发明人： Douglas C. Beshore , Robert M. Garbaccio , Scott D. Kuduk , Adam W. Johnson , Jason W. Skudlarek
IPC分类号： C07D413/12 , C07D401/14 , C07D403/10 , C07D249/18 , C07D401/10 , C07D401/12 , C07D413/10
CPC分类号： C07D413/12 , C07D249/18 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D413/10
摘要： The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors 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 metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增效剂的氨基甲基联芳基苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病 。 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代谢型谷氨酸受体的疾病中的用途。
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公开(公告)号：US08883850B2
公开(公告)日：2014-11-11
申请号：US13698288
申请日：2011-05-23
IPC分类号： A61K31/19 , A01N37/10 , A61K31/16 , A61K31/192
CPC分类号： A61K31/16 , A61K31/192
摘要： The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译： 本发明涉及作为M1受体阳性变构调节剂的式（I）的萘甲酰胺化合物，其可用于治疗涉及M1受体的疾病，例如阿尔茨海默病，精神分裂症，疼痛或睡眠障碍。 本发明还涉及包含该化合物的药物组合物以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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公开(公告)号：US20130059860A1
公开(公告)日：2013-03-07
申请号：US13698288
申请日：2011-05-23
IPC分类号： A61K31/44 , A61K31/4433 , A61K31/4439 , A61K31/415 , A61K31/192 , C07D403/04 , C07D401/04 , C07D405/12 , C07D213/56 , C07D231/12 , C07C63/36 , A61P25/00 , A61P25/28 , A61P25/18 , A61K31/496
CPC分类号： A61K31/16 , A61K31/192
摘要： The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译： 本发明涉及作为M1受体阳性变构调节剂的式（I）的萘甲酰胺化合物，其可用于治疗涉及M1受体的疾病，例如阿尔茨海默病，精神分裂症，疼痛或睡眠障碍。 本发明还涉及包含该化合物的药物组合物以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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公开(公告)号：US08008295B2
公开(公告)日：2011-08-30
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：US20170114056A1
公开(公告)日：2017-04-27
申请号：US15129206
申请日：2015-03-23
申请人： Helen MITCHELL , Mark E. FRALEY , Andrew J. COOKE , Craig A. STUMP , Yi Heng CHEN , Douglas C. BESHORE , Xu-Fank ZHANG , Casey C. MCCOMAS , Kathy SCHIRRIPA , Melody MCWHERTER , Swati P. MERCER , Keith P. MOORE , Ping LIU , Harold B. WOOD , Chun Sing LI , Qinghua MAO , Merck Sharp & Dohme Corp.
发明人： Helen Mitchell , Mark E. Fraley , Andrew J. Cooke , Craig A. Stump , Yi- Heng Chen , Xu-Fang Zhang , Casey C. McComas , Kathy Schirripa , Melody McWherter , Swati P. Mercer , Keith P. Moore , Ping Liu , Harold B. Wood , Chun Sing Li , Qinghua Mao , Douglas C. Beshore
IPC分类号： C07D471/04 , C07D513/04
CPC分类号： C07D403/12 , C07D401/12 , C07D403/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
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公开(公告)号：US20150065498A1
公开(公告)日：2015-03-05
申请号：US14117341
申请日：2012-05-11
IPC分类号： C07D519/00 , C07D471/04 , C07D471/08 , C07D209/64 , C07D403/06 , C07D405/14 , C07D401/14 , C07D401/06
CPC分类号： C07D519/00 , C07D209/64 , C07D401/06 , C07D401/08 , C07D401/14 , C07D403/06 , C07D403/08 , C07D405/14 , C07D417/08 , C07D471/04 , C07D471/08 , C07D487/08 , C07D491/10
摘要： The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译： 本发明涉及通式（I）的N-连接的内酰胺类化合物，其为M1受体阳性变构调节剂，可用于治疗涉及M1受体的疾病，例如阿尔茨海默病，精神分裂症，疼痛或 睡眠障碍 本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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公开(公告)号：US20140066443A1
公开(公告)日：2014-03-06
申请号：US14115123
申请日：2012-04-30
申请人： Douglas C. Beshore , Robert M. Garbaccio , Scott D. Kuduk , Adam W. Johnson , Jason W. Skudlarek
发明人： Douglas C. Beshore , Robert M. Garbaccio , Scott D. Kuduk , Adam W. Johnson , Jason W. Skudlarek
IPC分类号： C07D413/12 , C07D401/12 , C07D249/18 , C07D401/14 , C07D403/10
CPC分类号： C07D413/12 , C07D249/18 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D413/10
摘要： The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors 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 metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增效剂的氨基甲基联芳基苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病 。 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代谢型谷氨酸受体的疾病中的用途。
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公开(公告)号：US20130109686A1
公开(公告)日：2013-05-02
申请号：US13805346
申请日：2011-06-27
IPC分类号： C07D209/62 , C07D405/04 , C07D401/14 , C07D471/04 , C07D401/10 , C07D405/14
CPC分类号： C07D209/62 , C07D209/64 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/04 , C07D405/14 , C07D471/04
摘要： The present invention is directed to isoindolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译： 本发明涉及式（I）的异吲哚酮化合物，其为M1受体阳性变构调节剂，可用于治疗涉及M1受体的疾病，例如阿尔茨海默氏病，精神分裂症，疼痛或睡眠障碍。 本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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公开(公告)号：US20120149677A1
公开(公告)日：2012-06-14
申请号：US13391315
申请日：2010-08-16
申请人： Vadim Y. Dudkin , Mark E. Fraley , Cheng Wang , Robert M. Garbaccio , Douglas C. Beshore , Scott K. Kuduk , Jason W. Skudlarek
发明人： Vadim Y. Dudkin , Mark E. Fraley , Cheng Wang , Robert M. Garbaccio , Douglas C. Beshore , Scott K. Kuduk , Jason W. Skudlarek
IPC分类号： A61K31/4439 , C07D403/12 , C07D495/04 , C07D403/14 , C07D401/14 , C07D417/14 , A61K31/497 , A61K31/4709 , A61K31/506 , A61K31/519 , A61K31/444 , A61K31/541 , A61K31/438 , A61P25/00 , A61P25/18 , C07D401/12
CPC分类号： C07D417/14 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/506 , C07D249/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D495/04 , C07D498/04
摘要： The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors 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 metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增强剂的醚苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。 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代谢型谷氨酸受体的疾病中的用途。
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10.发明申请公开(公告)号：US20120040978A1
公开(公告)日：2012-02-16
申请号：US13264267
申请日：2010-04-13
申请人： Scott D. Kuduk , Douglas C. Beshore
发明人： Scott D. Kuduk , Douglas C. Beshore
IPC分类号： A61K31/5377 , C07D495/14 , A61P25/00 , A61P25/28 , A61P25/18 , C07D471/14 , A61K31/5025
CPC分类号： C07D471/14 , C07D495/14
摘要： The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译： 本发明涉及式（I）的杂环稠合噌啉化合物，其为M1受体阳性变构调节剂，可用于治疗阿尔茨海默病，精神分裂症，疼痛或睡眠障碍中的疾病。 本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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