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1.发明公开SUBSTITUTED 2-(4-HETEROCYCLYLBENZYL)ISOINDOLIN-1-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 有权取代的2-（4-HETEROCYCLYLBENZYL）异吲哚啉-1-酮类似物作为毒蕈碱正变构乙酰胆碱受体M1的调节剂
公开(公告)号：EP2770997A1
公开(公告)日：2014-09-03
申请号：EP12843949.4
申请日：2012-10-28
发明人： LINDSLEY, Craig, W. , CONN, P., Jeffrey , WOOD, Michael, R. , HOPKINS, Corey, R. , MELANCON, Bruce, J. , POSLUSNEY, Michael, S. , ENGERS, Darren, W.
IPC分类号： A61K31/435 , A61K31/4353 , A61P25/00 , C07D471/04 , C07D487/04 , C07D491/04
CPC分类号： C07D471/04 , C07D275/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D417/10 , C07D487/04 , C07D519/00
摘要： In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin- 1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M
1 (mAChR M
1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.-
2.发明公开ARYL AND HETEROARYL SULFONES AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION 审中-公开芳和HETEROARYLSULFONE变构增效剂mGluR4，因此组合物和治疗神经功能障碍的方法
公开(公告)号：EP2498781A2
公开(公告)日：2012-09-19
申请号：EP10829242.6
申请日：2010-11-08
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , HOPKINS, Corey, R. , WEAVER, Charles, David , NISWENDER, Colleen, M. , CHEUNG, Yiu-Yin
IPC分类号： A61K31/53
CPC分类号： C07D401/04 , C07D213/81 , C07D239/28 , C07D307/56 , C07D417/04
摘要： In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
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3.发明公开MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION 审中-公开变构增效剂mGluR4，组成和方法用于治疗神经机能障碍
公开(公告)号：EP2490529A1
公开(公告)日：2012-08-29
申请号：EP10825779.1
申请日：2010-10-22
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , HOPKINS, Corey, R. , NISWENDER, Colleen, M. , GOGLIOTTI, Rocco, D. , SALOVICH, James, M.
IPC分类号： A01N41/10
CPC分类号： A61K45/06 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/538 , C07D207/48 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12
摘要： Pyrrole compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
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公开(公告)号：EP3153167B1
公开(公告)日：2019-10-02
申请号：EP16185778.4
申请日：2012-10-28
发明人： LINDSLEY, Craig, W. , CONN, P., Jeffrey , WOOD, Michael, R. , HOPKINS, Corey, R. , MELANCON, Bruce, J. , POSLUSNEY, Michael, S. , ENGERS, Darren, W.
IPC分类号： A61K31/435 , A61K31/4353 , A61P25/00 , C07D471/04 , C07D487/04 , C07D491/04 , C07D401/14 , C07D519/00
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公开(公告)号：EP2900238B1
公开(公告)日：2017-12-06
申请号：EP13840866.1
申请日：2013-03-15
IPC分类号： C07D471/04 , C07D487/04 , C07D519/00 , A61K31/437 , A61K31/438 , A61K31/4709 , A61K31/5025 , A61K31/519 , A61P1/16 , A61P7/02 , A61P9/00 , A61P17/00 , A61P29/00 , A61P35/00
CPC分类号： C07D471/04 , A61K31/4709 , A61K31/5025 , A61K31/519 , C07D487/04 , C07D519/00
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6.发明公开HETEROCYCLIC SULFONE MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION 审中-公开杂环磺酸盐MGLUR4变体增效剂，组合物和治疗神经功能障碍的方法
公开(公告)号：EP2568809A1
公开(公告)日：2013-03-20
申请号：EP11781297.4
申请日：2011-05-12
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , HOPKINS, Corey, R. , WEAVER, Charles, David , NISWENDER, Colleen, M. , GOGLIOTTI, Rocco, D. , CHEUNG, Yiu-Yin , SALOVICH, James, M. , ENGERS, Darren, W.
CPC分类号： A61K31/4439 , A61K45/06 , C07D401/12 , C07D413/12 , C07D417/12
摘要： Heterocyclic sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
摘要翻译： 可用作代谢型谷氨酸受体亚型4（mGluR4）的变构增效剂/正变构调节剂的杂环砜化合物; 和使用这些化合物的方法，例如，用于治疗与谷氨酸功能障碍相关的神经和精神疾病或其他疾病状态。
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7.发明授权SUBSTITUTED 2-(4-HETEROCYCLYLBENZYL)ISOINDOLIN-1-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 有权替代2-（4-羟基苄基苄基）异吲哚啉-1-对 - 阿拉伯糖酸盐阳性胰岛素调节蛋白酶抑制剂乙酰胆碱酯酶M1
公开(公告)号：EP2770997B1
公开(公告)日：2016-09-14
申请号：EP12843949.4
申请日：2012-10-28
发明人： LINDSLEY, Craig, W. , CONN, P., Jeffrey , WOOD, Michael, R. , HOPKINS, Corey, R. , MELANCON, Bruce, J. , POSLUSNEY, Michael, S. , ENGERS, Darren, W.
IPC分类号： A61K31/435 , A61K31/4353 , A61P25/00 , C07D471/04 , C07D487/04 , C07D491/04
CPC分类号： C07D471/04 , C07D275/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D417/10 , C07D487/04 , C07D519/00
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8.发明公开FUSED HETEROCYCLIC COMPOUNDS AS SELECTIVE BMP INHIBITORS 有权KENENSIERTE HETEROCYCLISCHE VERBINDUNGEN ALS SELEKTIVE BMP-INHIBITOREN
公开(公告)号：EP2900238A1
公开(公告)日：2015-08-05
申请号：EP13840866.1
申请日：2013-03-15
IPC分类号： A61K31/437 , A61K31/438 , A61K31/357 , A61K31/5375 , A61P29/00 , A61P9/00
CPC分类号： C07D471/04 , A61K31/4709 , A61K31/5025 , A61K31/519 , C07D487/04 , C07D519/00
摘要： The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.
摘要翻译： 本发明提供BMP信号传导的小分子抑制剂。 这些化合物可用于调节细胞生长，分化，增殖和凋亡，因此可用于治疗与BMP信号相关的疾病或病症，包括炎症，心血管疾病，血液疾病，癌症和骨骼疾病，以及 用于调节细胞分化和/或增殖。
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9.发明公开MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION 审中-公开MGLUR4变体增效剂，组合物和治疗神经功能障碍的方法
公开(公告)号：EP2490537A1
公开(公告)日：2012-08-29
申请号：EP10825772.6
申请日：2010-10-22
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , HOPKINS, Corey, R. , NISWENDER, Colleen, M. , GOGLIOTTI, Rocco, D.
IPC分类号： A01N43/56
CPC分类号： A61K45/06 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/538 , C07D207/48 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12
摘要： Pyrrole compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
摘要翻译： 可用作代谢型谷氨酸受体亚型4（mGluR4）的变构增效剂/正变构调节剂的吡咯化合物; 用于制备该化合物的合成方法; 包含该化合物的药物组合物 和使用这些化合物的方法，例如，用于治疗与谷氨酸功能障碍相关的神经和精神疾病或其他疾病状态。
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10.发明公开SUBSTITUTED 2-(4-HETEROCYCLYLBENZYL)ISOINDOLIN-1-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 审中-公开替代2-（4-杂环苄基）异吲哚-1-酮ANALOGA ALS阳性ALLOSTERISCHE MODULATOREN DES MUSKARINISCHEN乙酰胆碱酯酶M1
公开(公告)号：EP3153167A1
公开(公告)日：2017-04-12
申请号：EP16185778.4
申请日：2012-10-28
发明人： LINDSLEY, Craig, W. , CONN, P., Jeffrey , WOOD, Michael, R. , HOPKINS, Corey, R. , MELANCON, Bruce, J. , POSLUSNEY, Michael, S. , ENGERS, Darren, W.
IPC分类号： A61K31/435 , A61K31/4353 , A61P25/00 , C07D471/04 , C07D487/04 , C07D491/04 , C07D401/14 , C07D519/00
摘要： In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
摘要翻译： 一方面，本发明涉及可用作毒蕈碱乙酰胆碱受体M 1（mAChR M 1）的正变构调节剂的取代的2-（4-杂环基苄基）异二氢吲哚-1-酮类似物化合物，其衍生物和相关化合物。 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用该化合物和组合物治疗与毒蕈碱性乙酰胆碱受体功能障碍相关的神经和精神疾病的方法。
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