公开(公告)号：US10227343B2

公开(公告)日：2019-03-12

申请号：US15547775

申请日：2016-02-01

Applicant: Vanderbilt University

Inventor： P. Jeffrey Conn ,  Craig W. Lindsley ,  Colleen M. Niswender ,  Corey R. Hopkins ,  Joanne Bronson ,  Yong-Jin Wu ,  Kyle Emmitte ,  Joe Panarese ,  Darren W. Engers ,  Julie Engers

IPC: C07D471/04 ,  A61K31/496 ,  A61K31/437 ,  A61K31/554 ,  A61K31/553 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/4725 ,  A61K31/541 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/502 ,  C07D401/12 ,  A61K31/4375 ,  C07D519/00 ,  A61K31/519 ,  A61K45/06

Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); 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.

公开(公告)号：US10221175B2

公开(公告)日：2019-03-05

申请号：US15568936

申请日：2016-04-22

Applicant: Vanderbilt University

Inventor： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Changho Han ,  Julie L. Engers ,  Aaron M. Bender

IPC: A61K31/395 ,  C07D471/14 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61P25/28 ,  A61P25/00

Abstract: Substituted pyrrolopyridine, imidazopyridine and triazolopyridine compounds having a formula are positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1) and the compounds and their pharmaceutical compositions may be useful in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction. Compounds of the invention may be prepared in several steps from 2-halo-5,6-dihydro-7H-pyrrolo[3,4-b]pyridin-7-one intermediates.

公开(公告)号：US20180057490A1

公开(公告)日：2018-03-01

申请号：US15694465

申请日：2017-09-01

Applicant: Vanderbilt University

Inventor： P. Jeffrey Conn ,  Craig W. Lindsley ,  Andrew Felts

IPC: C07D471/04 ,  A61K31/538 ,  A61K45/06

CPC classification number: C07D471/04 ,  A61K31/538 ,  A61K45/06

Abstract: 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.

公开(公告)号：US20170369505A1

公开(公告)日：2017-12-28

申请号：US15630200

申请日：2017-06-22

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Sean Bollinger ,  James C. Tarr ,  Paul Spearing ,  Julie L. Engers ,  Madeline Long ,  Thomas M. Bridges

IPC: C07D495/14 ,  C07D519/00 ,  C07D493/14

CPC classification number: C07D495/14 ,  C07D493/14 ,  C07D519/00

Abstract: Disclosed herein are tricyclic compounds, including pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine-8-amine, pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine-4-amine, pyrazino[2′,3′:4,5]thieno[3,2-d]pyrimidin-4-amine, pyrido[3′,2′:4,5]furo[3, 2-d]pyrimidin-4-amine, and pyrimido[4′,5′:4,5]furo[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of 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.

公开(公告)号：US09708278B2

公开(公告)日：2017-07-18

申请号：US15039763

申请日：2014-11-18

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Shaun R. Stauffer ,  Joseph D. Panarese

IPC: C07D265/36 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14

CPC classification number: C07D265/36 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14

Abstract: In one aspect, the invention relates to N-substituted 3,4-dihydro-benzo[£][1,4]oxazine-2-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); 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.

公开(公告)号：US09637498B2

公开(公告)日：2017-05-02

申请号：US14913266

申请日：2014-08-22

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Michael R. Wood ,  Michael S. Poslusney ,  James C. Tarr ,  Bruce J. Melancon

IPC: C07D495/04 ,  A61K31/5025

CPC classification number: C07D495/04

Abstract: 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 M4 (mAChR M4); 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.

公开(公告)号：US09586964B2

公开(公告)日：2017-03-07

申请号：US14354560

申请日：2012-10-28

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Michael R. Wood ,  Corey R. Hopkins ,  Bruce J. Melancon ,  Michael S. Poslusney ,  Darren W. Engers

IPC: C07D519/00 ,  C07D403/10 ,  C07D487/04 ,  C07D401/10 ,  C07D401/14 ,  C07D471/04 ,  C07D417/10 ,  C07D405/10 ,  C07D275/06

CPC classification number: C07D471/04 ,  C07D275/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/10 ,  C07D417/10 ,  C07D487/04 ,  C07D519/00

Abstract: 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 M1 (mAChR M1); 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.

Abstract translation: 一方面，本发明涉及用作毒蕈碱乙酰胆碱受体M1（mAChR M1）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。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不是限制本发明。

公开(公告)号：US20170022173A1

公开(公告)日：2017-01-26

申请号：US15039763

申请日：2014-11-18

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Shaun R. Stauffer ,  Joseph D. Panarese

IPC: C07D265/36 ,  C07D413/14 ,  C07D413/06 ,  C07D413/10

CPC classification number: C07D265/36 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14

Abstract: In one aspect, the invention relates to N-substituted 3,4-dihydro-benzo[£][1,4]oxazine-2-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); 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.

Abstract translation: 一方面，本发明涉及N-取代的3,4-二氢 - 苯并[[]] [1,4]恶嗪-2-甲酰胺类似物，其衍生物和相关化合物，其可用作毒蕈碱的正变构调节剂 乙酰胆碱受体M1（mAChR M1）; 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。 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。

公开(公告)号：US20160289227A1

公开(公告)日：2016-10-06

申请号：US15037320

申请日：2014-11-18

Applicant: VANDERBILT UNIVERSITY

Inventor： Kyle A. Emmitte ,  Craig W. Lindsley ,  P. Jeffrey Conn ,  Andrew S. Felts ,  Alice L. Rodriguez ,  Katrina A. Smith ,  Carrie K. Jones

IPC: C07D471/04 ,  A61K31/506 ,  A61K45/06 ,  A61K31/444

CPC classification number: A61K31/444 ,  A61K31/506 ,  A61K45/06 ,  C07D471/04

Abstract: 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.

Abstract translation: 公开了代谢型谷氨酸受体亚型5（mGluR5）的负变构调节剂; 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官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。

公开(公告)号：US20160207935A1

公开(公告)日：2016-07-21

申请号：US14913266

申请日：2014-08-22

Applicant: VANDERBILT UNIVERSITY

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Michael R. Wood ,  Michael S. Poslusney ,  James C. Tarr ,  Bruce J. Melancon

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: 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 M4 (mAChR M4); 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.

Abstract translation: 一方面，本发明涉及用作毒蕈碱乙酰胆碱受体M4（mAChR M4）的正变构调节剂的取代的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， ; 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。 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。