公开(公告)号：US20230014109A1

公开(公告)日：2023-01-19

申请号：US17469178

申请日：2021-09-08

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

发明人： 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分类号： C07D495/14 ,  C07D493/14 ,  C07D519/00

摘要： 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：US08865725B2

公开(公告)日：2014-10-21

申请号：US13420333

申请日：2012-03-14

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Jose Manuel Bartolome-Nebreda ,  Gregor James MacDonald ,  Susana Conde-Ceide ,  Carrie K. Jones ,  Maria Luz Martin-Martin ,  Han Min Tong

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Jose Manuel Bartolome-Nebreda ,  Gregor James MacDonald ,  Susana Conde-Ceide ,  Carrie K. Jones ,  Maria Luz Martin-Martin ,  Han Min Tong

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC分类号： C07D487/04

摘要： In one aspect, the invention relates to imidazopyrimidin-5(6H)-one 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，本发明涉及可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂的咪唑并嘧啶-5（6H） - 酮类似物及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：US08703946B2

公开(公告)日：2014-04-22

申请号：US13314117

申请日：2011-12-07

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Carrie K. Jones ,  Shaun R. Stauffer ,  José Manuel Bartolome-Nebreda ,  Gregor James McDonald ,  Susana Conde-Ceide ,  Han Min Tong

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Carrie K. Jones ,  Shaun R. Stauffer ,  José Manuel Bartolome-Nebreda ,  Gregor James McDonald ,  Susana Conde-Ceide ,  Han Min Tong

IPC分类号： C07D471/00

CPC分类号： C07D487/04

摘要： In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazine 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.

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）的正变构调节剂的取代的吡唑并[1,5-a]吡嗪化合物，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：US08497289B2

公开(公告)日：2013-07-30

申请号：US12648972

申请日：2009-12-29

申请人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Richard Williams ,  Carrie K. Jones ,  Douglas J. Sheffler

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Richard Williams ,  Carrie K. Jones ,  Douglas J. Sheffler

IPC分类号： A61K31/44 ,  C07D403/02

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 inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) 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.

摘要翻译： 一方面，本发明涉及可用作1型甘氨酸转运蛋白（GlyT1）活性抑制剂的化合物; 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甘氨酸1型转运蛋白（GlyT1）活性相关的病症的方法。 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：US08431700B2

公开(公告)日：2013-04-30

申请号：US12716748

申请日：2010-03-03

申请人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Richard Williams ,  Carrie K. Jones ,  Douglas J. Sheffler

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Richard Williams ,  Carrie K. Jones ,  Douglas J. Sheffler

IPC分类号： C07D401/00

CPC分类号： C07D221/20 ,  C07D401/12 ,  C07D409/12

摘要： In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) 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.

摘要翻译： 一方面，本发明涉及可用作1型甘氨酸转运蛋白（GlyT1）活性抑制剂的化合物; 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甘氨酸1型转运蛋白（GlyT1）活性相关的病症的方法。 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：US20120295913A1

公开(公告)日：2012-11-22

申请号：US13314117

申请日：2011-12-07

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Carrie K. Jones ,  Shaun R. Stauffer ,  José Manuel Bartolome-Nebreda ,  Gregor James McDonald ,  Susana Conde-Ceide ,  Han Min Tong

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Carrie K. Jones ,  Shaun R. Stauffer ,  José Manuel Bartolome-Nebreda ,  Gregor James McDonald ,  Susana Conde-Ceide ,  Han Min Tong

IPC分类号： A61K31/4985 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/30 ,  A61P35/00 ,  A61P25/08 ,  A61P25/06 ,  A61P3/10 ,  A61P3/04 ,  A61P25/22 ,  A61P25/24 ,  C07D487/04 ,  A61P25/14

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.

摘要翻译： 一方面，本发明涉及双代吡唑化合物，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; 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：US20120172391A1

公开(公告)日：2012-07-05

申请号：US13340641

申请日：2011-12-29

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Jason Manka ,  Jon Jacobs ,  Ya Zhou ,  José Manuel Bartolomé-Nebreda ,  Gregor James Macdonald ,  Susana Conde-Ceide ,  Carrie K. Jones

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Jason Manka ,  Jon Jacobs ,  Ya Zhou ,  José Manuel Bartolomé-Nebreda ,  Gregor James Macdonald ,  Susana Conde-Ceide ,  Carrie K. Jones

IPC分类号： A61K31/4375 ,  A61P25/00 ,  A61P25/18 ,  A61P25/14 ,  A61P25/24 ,  A61P25/06 ,  A61P3/10 ,  A61P3/04 ,  A61P25/20 ,  A61P25/22 ,  C07D471/04 ,  A61P25/08

CPC分类号： C07D471/04 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/10 ,  A61K9/2018 ,  A61K31/4375

摘要： In one aspect, the invention relates to naphthyridinone 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，本发明涉及可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂的萘啶酮类似物，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：US20100249167A1

公开(公告)日：2010-09-30

申请号：US12716748

申请日：2010-03-03

申请人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Richard Williams ,  Carrie K. Jones ,  Douglas J. Sheffler

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Richard Williams ,  Carrie K. Jones ,  Douglas J. Sheffler

IPC分类号： A61K31/438 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/14 ,  C07D309/14

CPC分类号： C07D221/20 ,  C07D401/12 ,  C07D409/12

摘要： In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) 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.

摘要翻译： 一方面，本发明涉及可用作1型甘氨酸转运蛋白（GlyT1）活性抑制剂的化合物; 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甘氨酸1型转运蛋白（GlyT1）活性相关的病症的方法。 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：US20100222387A1

公开(公告)日：2010-09-02

申请号：US11922390

申请日：2006-06-21

申请人： James C. Barrow ,  Craig W. Lindsley ,  William D. Shipe ,  Zhi-Qiang Yang

发明人： James C. Barrow ,  Craig W. Lindsley ,  William D. Shipe ,  Zhi-Qiang Yang

IPC分类号： A61K31/4545 ,  C07D211/14 ,  A61K31/445 ,  C07D401/06 ,  A61P25/02 ,  A61P25/16 ,  A61P25/28 ,  A61P25/20 ,  A61P25/22 ,  A61P25/00 ,  A61K31/4523 ,  C07D413/06

CPC分类号： C07D211/38 ,  C07D405/06 ,  C07D413/06

摘要： The present invention is directed to 3-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

摘要翻译： 本发明涉及作为T型钙通道拮抗剂的3-氟哌啶化合物，其可用于治疗或预防其中涉及T型钙通道的神经和精神疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道的疾病中的用途。

公开(公告)号：US20100222322A1

公开(公告)日：2010-09-02

申请号：US11922682

申请日：2006-06-23

申请人： Scott E. Wolkenberg ,  Zhijian Zhao ,  Craig W. Lindsley

发明人： Scott E. Wolkenberg ,  Zhijian Zhao ,  Craig W. Lindsley

IPC分类号： A61K31/404 ,  A61P31/18 ,  C07D403/12 ,  C07D401/12 ,  A61K31/454 ,  A61K31/496

CPC分类号： A61K31/551 ,  C07D209/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

摘要翻译： 式（I）的吲哚化合物是HIV逆转录酶抑制剂，其中R 1，R 2，R 3，R 4和R 5在本文中定义。 式（I）化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗艾滋病毒感染以及预防，延迟发作和治疗艾滋病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。