公开(公告)号：US10160763B2

公开(公告)日：2018-12-25

申请号：US15703289

申请日：2017-09-13

Applicant: Vanderbilt University

Inventor： Stephen W. Fesik ,  Shaun R. Stauffer ,  William P. Tansey ,  Edward T. Olejniczak ,  Jason Phan ,  Feng Wang ,  KyuOk Jeon ,  Rocco D. Gogliotti

IPC: C07D487/04 ,  C07B59/00

Abstract: Described are compounds that disrupt the WDR5-MLL1 protein-protein interaction, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.

公开(公告)号：US20180086767A1

公开(公告)日：2018-03-29

申请号：US15703289

申请日：2017-09-13

Applicant: Vanderbilt University

Inventor： Stephen W. Fesik ,  Shaun R. Stauffer ,  William P. Tansey ,  Edward T. Olejniczak ,  Jason Phan ,  Feng Wang ,  KyuOk Jeon ,  Rocco D. Gogliotti

IPC: C07D487/04 ,  C07B59/00

CPC classification number: C07D487/04 ,  C07B59/002 ,  C07B2200/05

Abstract: Described are compounds that disrupt the WDR5-MLL1 protein-protein interaction, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.

公开(公告)号：US09963466B2

公开(公告)日：2018-05-08

申请号：US15452686

申请日：2017-03-07

Applicant: Vanderbilt University

Inventor： Heidi E. Hamm ,  Shaun R. Stauffer ,  Craig W. Lindsley ,  Matthew T. Duvernay ,  Kayla J. Temple

IPC: C07D513/04

CPC classification number: C07D513/04

Abstract: Embodiments of the invention include compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.

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：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：US20160102090A1

公开(公告)日：2016-04-14

申请号：US14787722

申请日：2014-04-28

Applicant: VANDERBILT UNIVERSITY

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

IPC: C07D471/04 ,  C07D401/10

CPC classification number: C07D471/04 ,  C07D401/10 ,  C07D403/10

Abstract: In one aspect, the invention relates to 3-benzylquinazolin-4(3H)-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，本发明涉及可用作毒蕈碱乙酰胆碱受体M1（mAChR M1）的正变构调节剂的3-苄基喹唑啉-4（3H） - 酮类似物化合物及其衍生物及其相关化合物。 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。

公开(公告)号：US20140371239A1

公开(公告)日：2014-12-18

申请号：US14302219

申请日：2014-06-11

Applicant: The Regents of The University of Michigan ,  Vanderbilt University

Inventor： Jolanta Grembecka ,  Tomasz Cierpicki ,  Sunil Kumar Upadhyay ,  Shaun R. Stauffer ,  Rocco D. Gogliotti ,  Timothy J. Senter

IPC: C07D417/06 ,  C07D401/14 ,  C07D401/06 ,  C07D295/088 ,  C07D401/12

CPC classification number: C07D417/06 ,  C07D211/22 ,  C07D211/26 ,  C07D295/088 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin.

Abstract translation: 本发明一般涉及抑制menin和MLL或MLL融合蛋白结合的化合物及其使用方法。 在具体实施方案中，本发明提供包含含哌啶化合物的组合物及其用于抑制menin与MLL癌蛋白（例如MLL1，MLL2，MLL-融合癌蛋白）的相互作用的方法，例如用于治疗白血病， 固体癌症，糖尿病和依赖于MLL1，MLL2，MLL融合蛋白，MLL-PTD和/或menin活性的其它疾病。

公开(公告)号：US20130345206A1

公开(公告)日：2013-12-26

申请号：US13922230

申请日：2013-06-19

Applicant: Vanderbilt University

Inventor： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  José Manuel Bartolomé-Nebreda ,  Susana Conde-Ceide ,  Gregor James Macdonald ,  Han Min Tong ,  Miguel Angel Pena-Piñón ,  Manuel Jesús Alcázar-Vaca ,  José Ignacio Andrés-Gil

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: 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.

公开(公告)号：US11999716B2

公开(公告)日：2024-06-04

申请号：US17287492

申请日：2019-10-24

Applicant: Vanderbilt University

Inventor： Taekyu Lee ,  Joseph R. Alvarado ,  Jianhua Tian ,  Kenneth M. Meyers ,  Changho Han ,  Jonathan J. Mills ,  Kevin B. Teuscher ,  Shaun R. Stauffer ,  Stephen W. Fesik ,  Rocco D. Gogliotti

IPC: C07D401/14 ,  C07D217/16 ,  C07D401/06 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

CPC classification number: C07D401/14 ,  C07D217/16 ,  C07D401/06 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

Abstract: Isoquinolinone compounds and derivatives inhibit WDR5 and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

公开(公告)号：US20230012362A1

公开(公告)日：2023-01-12

申请号：US17287492

申请日：2019-10-24

Applicant: Vanderbilt University

Inventor： Taekyu Lee ,  Joseph R. Alvarado ,  Jianhua Tian ,  Kenneth M. Meyers ,  Changho Han ,  Jonathan J. Mills ,  Kevin B. Teuscher ,  Shaun R. Stauffer ,  Stephen W. Fesik

IPC: C07D401/14 ,  C07D401/06 ,  C07D487/04 ,  C07D405/14 ,  C07D417/14 ,  C07D417/06 ,  C07D413/14 ,  C07D217/16 ,  C07D413/06

Abstract: Isoquinolinone compounds and derivatives inhibit WDRS and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.