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

申请人： Vanderbilt University

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

公开(公告)号：EP3534901A1

公开(公告)日：2019-09-11

申请号：EP17867018.8

申请日：2017-11-07

申请人： Vanderbilt University

发明人： LINDSLEY, Craig, W. ,  ENGERS, Darren, W. ,  CONN, P., Jeffrey ,  BOLLINGER, Sean, R. ,  ENGERS, Julie, L.

IPC分类号： A61K31/4365 ,  A61K31/4375 ,  A61K31/5025 ,  A61P25/00

公开(公告)号：EP3416639A1

公开(公告)日：2018-12-26

申请号：EP17753822.0

申请日：2017-02-16

申请人： Vanderbilt University

发明人： LINDSLEY, Craig, W. ,  CONN, P., Jeffrey ,  ENGERS, Darren, W. ,  BOLLINGER, Katrina, A. ,  ENGERS, Julie, L.

IPC分类号： A61K31/4365 ,  C07D495/04

CPC分类号： C07D495/04 ,  C07D471/04

摘要： Described are positive allosteric modulators of muscarinic acetylcholine receptor M1 (mAChR M1), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating neurological disorders, psychiatric disorders, or a combination thereof.

公开(公告)号：EP2817295A1

公开(公告)日：2014-12-31

申请号：EP13751391.7

申请日：2013-02-23

申请人： Vanderbilt University

发明人： LINDSLEY, Craig, W. ,  CONN, P., Jeffrey ,  WOOD, Michael, R. ,  MELANCON, Bruce, J. ,  TARR, James, C. ,  SALOVICH, James, M. ,  POSLUSNEY, Michael S.

IPC分类号： C07D237/26 ,  C07D409/02

CPC分类号： C07D495/04 ,  C07D237/26 ,  C07D409/04 ,  C07D519/00 ,  C07F7/1804

摘要： In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6- carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M
4 (mAChR M
4 ); 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.

摘要翻译： 在一个方面，本发明涉及取代的5-氨基噻吩并[2,3-c]哒嗪-6-甲酰胺类似物，其衍生物和相关化合物，其可用作毒蕈碱乙酰胆碱受体M 4的正变构调节剂（mAChR M 4）; 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有关的神经和精神疾病的方法。 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。

公开(公告)号：EP2648723A1

公开(公告)日：2013-10-16

申请号：EP11847759.5

申请日：2011-12-07

申请人： Vanderbilt University

发明人： CONN, P., Jeffrey ,  LINDSLEY, Craig, W. ,  STAUFFER, Shaun, R. ,  JONES, Carrie, K. ,  CONDE-CEIDE, Susana ,  TONG, Han Min ,  BARTOLOME-NEBREDA, Jose, Manuel ,  MACDONALD, Gregor, James

IPC分类号： A61K31/4162 ,  C07D231/54

CPC分类号： C07D487/04

摘要： In one aspect, the invention relates to bicyclic pyrazole compounds, 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.

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

申请人： Vanderbilt University

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.

IPC分类号： A01N41/10 ,  A61K31/10

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。

公开(公告)号：EP2477630A1

公开(公告)日：2012-07-25

申请号：EP10817950.8

申请日：2010-09-17

申请人： Vanderbilt University

发明人： CONN, P., Jeffrey ,  LINDSLEY, Craig, W. ,  EMMITTE, Kyle, A. ,  WEAVER, Charles, David ,  RODRIGUEZ, Alice, L. ,  FELTS, Andrew, S. ,  JONES, Carrie, K. ,  BATES, Brittney, S.

IPC分类号： A61K31/535

CPC分类号： A61K31/4406 ,  A61K31/497 ,  C07D401/12 ,  C07D401/14

摘要： Disclosed are negative 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.

公开(公告)号：EP2477629A1

公开(公告)日：2012-07-25

申请号：EP10817936.7

申请日：2010-09-17

申请人： Vanderbilt University

发明人： CONN, P., Jeffrey ,  LINDSLEY, Craig, W. ,  EMMITTE, Kyle, A. ,  WEAVER, Charles, David ,  RODRIGUEZ, Alice, L. ,  FELTS, Andrew, S. ,  JONES, Carrie, K. ,  BATES, Brittney, S.

IPC分类号： A61K31/535

CPC分类号： A61K31/4406 ,  A61K31/497 ,  C07D401/12 ,  C07D401/14

摘要： Disclosed are negative 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

公开(公告)号：EP2381941A1

公开(公告)日：2011-11-02

申请号：EP09837121.4

申请日：2009-12-29

申请人： VANDERBILT UNIVERSITY

发明人： LINDSLEY, Craig, W. ,  CONN, P., Jeffrey ,  WEAVER, Charles, David ,  NISWENDER, Colleen, M. ,  WILLIAMS, Richard ,  JONES, Carrie, K. ,  SHEFFLER, Douglas, J.

IPC分类号： A61K31/397 ,  A61K31/407

CPC分类号： C07D209/52 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GIyTl) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GIyTl) 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.

公开(公告)号：EP2162136A1

公开(公告)日：2010-03-17

申请号：EP08770045.6

申请日：2008-06-03

申请人： VANDERBILT UNIVERSITY

发明人： CONN, P., Jeffrey ,  LINDSLEY, Craig, W. ,  WEAVER, Charles, David ,  RODRIGUEZ, Alice, L. ,  NISWENDER, Colleen, M. ,  JONES, Carrie, K. ,  WILLIAMS, Richard

IPC分类号： A61K31/497

CPC分类号： C07D211/60 ,  A61K31/166 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4035 ,  A61K31/4245 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/451 ,  A61K31/4523 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/5377 ,  C07C233/65 ,  C07C233/66 ,  C07C233/69 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D205/04 ,  C07D207/09 ,  C07D209/46 ,  C07D209/48 ,  C07D211/18 ,  C07D211/22 ,  C07D211/42 ,  C07D211/44 ,  C07D211/46 ,  C07D211/52 ,  C07D211/58 ,  C07D213/74 ,  C07D217/06 ,  C07D217/24 ,  C07D271/06 ,  C07D295/13 ,  C07D295/14 ,  C07D295/192 ,  C07D295/30 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D409/04 ,  C07D413/12 ,  Y02A50/415

摘要： In one aspect, the invention relates to compounds, including benzamide derivatives and cyclic benzamide derivatives, 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，本发明涉及可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂的化合物，包括苯甲酰胺衍生物和环状苯甲酰胺衍生物。 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸功能障碍相关的神经和精神障碍的方法。 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。