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公开(公告)号：EP4267569A1
公开(公告)日：2023-11-01
申请号：EP21848382.4
申请日：2021-12-22
发明人： BENDER, Aaron, M. , SPOCK, Matthew , KORKMAZ-VAISYS, Melissa, A. , MALINKY, Cori, A. , CONN, P., Jeffrey , LINDSLEY, Craig, W.
IPC分类号： C07D405/14 , A61K31/501 , A61P25/00 , A61P25/14 , A61P25/28
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2.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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3.发明公开BENZISOXAZOLES AND AZABENZISOXAZOLES AS mgluR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION 审中-公开苯并异恶唑AZABENZISOXAZOLE变构增强剂mGluR4和构成，并用于治疗神经机能障碍
公开(公告)号：EP2533642A1
公开(公告)日：2012-12-19
申请号：EP11742914.2
申请日：2011-02-11
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , HOPKINS, Corey, R. , WEAVER, Charles, David , NISWENDER, Colleen, M. , ENGERS, Darren, W.
CPC分类号： C07D498/04 , A61K31/42 , A61K31/423 , A61K31/4355 , A61K31/437 , A61K45/06 , C07D261/20 , C07D491/048
摘要： Benzisoxazole and azabenzisoxazole 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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4.发明公开PYRAZOLOPYRIDINE, PYRAZOLOPYRAZINE, PYRAZOLOPYRIMIDINE, PYRAZOLOTHIOPHENE AND PYRAZOLOTHIAZOLE COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOUNDS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION 审中-公开吡唑并吡啶，吡唑并吡嗪，吡唑并嘧啶，吡唑并噻吩和吡唑并噻唑化合物作为MGLUR4变体增效剂，化合物和治疗神经功能障碍的方法
公开(公告)号：EP2533639A1
公开(公告)日：2012-12-19
申请号：EP11742910.0
申请日：2011-02-11
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , HOPKINS, Corey, R. , NISWENDER, Colleen, M. , GOGLIOTTI, Rocco, D. , SALOVICH, James, M. , ENGERS, Darren, W. , CHEUNG, Yiu-Yin
IPC分类号： A01N43/56 , A61K31/415
CPC分类号： C07D471/04 , A61K31/415 , A61K31/4188 , A61K31/429 , A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D487/04 , C07D513/04
摘要： Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole 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.
摘要翻译： 吡唑并吡啶，吡唑并吡嗪，吡唑并嘧啶，吡唑并噻吩和吡唑并噻唑化合物，其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; 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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5.发明公开SULFONYL-AZETIDIN-3-YL-METHYLAMINE AMIDE ANALOGS AS GLYT1 INHIBITORS, METHODS FOR MAKING SAME, AND USE OF SAME IN TREATING PSYCHIATRIC DISORDERS 审中-公开磺酰基 - 氮杂环丁烷-3-基 - 甲基胺酰胺类似物ALS GlyT1抑制剂，生产和使用，用于治疗精神疾病方法
公开(公告)号：EP2413701A1
公开(公告)日：2012-02-08
申请号：EP10759346.9
申请日：2010-03-31
发明人： LINDSLEY, Craig, W. , CONN, P., Jeffrey , WILLIAMS, Richard , JONES, Carrie, K. , SHEFFLER, Douglas, J.
IPC分类号： A01N65/00
CPC分类号： C07D401/14 , C07D205/04 , C07D403/12 , C07D409/14
摘要： In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GIyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GIyT1) activity 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.
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6.发明公开
公开(公告)号：EP4168406A1
公开(公告)日：2023-04-26
申请号：EP21740400.3
申请日：2021-06-18
发明人： FELTS, Andrew, S. , HAN, Changho , CAPSTICK, Rory, A. , ORSI, Douglas, L. , WHOMBLE, David, L. , LINDSLEY, Craig, W. , CONN, P., Jeffrey
IPC分类号： C07D417/14 , C07D417/12 , C07D405/14 , C07D471/04 , C07D513/04 , A61K31/454 , A61K31/4523 , A61P25/18
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公开(公告)号：EP4037677A1
公开(公告)日：2022-08-10
申请号：EP20873262.8
申请日：2020-10-02
IPC分类号： A61K31/403 , A61K31/5025 , C07D417/12 , A61P25/00
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8.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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9.发明公开SUBSTITUTED BICYCLIC ALKOXY PYRAZOLE ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS 审中-公开取代的双环烷氧基吡唑类似物作为MGLUR5受体的共振调节剂
公开(公告)号：EP2863912A1
公开(公告)日：2015-04-29
申请号：EP13807306.9
申请日：2013-06-19
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , STAUFFER, Shaun, R. , BARTOLOME-NEBREDA, Jose, Manuel , MACDONALD, Gregor, James , CONDE-CEIDE, Susana , TONG, Han, Min , ALCAZAR-VACA, Manuel, Jesus , ANDRÉS-GIL, José Ignacio , PENA-PIÑON, Miguel, Angel
IPC分类号： A61K31/4985 , C07D471/04
CPC分类号： A61K31/4985 , A61K31/506 , A61K31/551 , C07D487/04
摘要： In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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.
摘要翻译： 一方面，本发明涉及取代的双环烷氧基吡唑类似物，其衍生物和相关化合物，其可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂; 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 以及使用所述化合物和组合物治疗与谷氨酸功能障碍有关的神经和精神障碍的方法。 该摘要旨在作为用于在特定领域中进行搜索的目的的扫描工具，并且不旨在限制本发明。
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10.发明公开BICYCLIC OXAZOLE AND THIAZOLE COMPOUNDS AND THEIR USE AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS 审中-公开双环恶唑和噻唑化合物及其作为代谢型谷氨酸受体的变构调节剂5个受体使用
公开(公告)号：EP2611298A1
公开(公告)日：2013-07-10
申请号：EP11822606.7
申请日：2011-08-31
发明人： CONN, P., Jeffrey , LINDSLEY, Craig, W. , STAUFFER, Shaun, R. , JONES, Carrie, K. , BARTOLOME-NEBREDA, Jose, Manuel , CONDE-CEIDE, Susana , MACDONALD, Gregor, James , ALCAZAR VACA, Manuel, Jesus
CPC分类号： C07D513/04 , C07D498/04
摘要： In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ("mGluR5"); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. 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.
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