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：US20130261107A1

公开(公告)日：2013-10-03

申请号：US13819273

申请日：2011-08-31

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Carrie K. Jones ,  Jose Manuel Bartolome-Nebreda ,  Susana Conde-Ceide ,  James Gregor MacDonald ,  Manuel Jesus Alcazar Vaca

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Carrie K. Jones ,  Jose Manuel Bartolome-Nebreda ,  Susana Conde-Ceide ,  James Gregor MacDonald ,  Manuel Jesus Alcazar Vaca

IPC分类号： C07D513/04 ,  C07D498/04

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.

摘要翻译： 一方面，本发明涉及作为代谢型谷氨酸受体亚型5（“mGluR5”）的正变构调节剂的新型双环恶唑和噻唑化合物。 制备化合物的合成方法; 包含该化合物的药物组合物; 使用该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; 以及用于治疗或预防与谷氨酸功能障碍相关的病症和其中涉及mGluR5亚型亚型的疾病的方法。 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：US20110183980A1

公开(公告)日：2011-07-28

申请号：US12886950

申请日：2010-09-21

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Charles David Weaver ,  Shaun Stauffer ,  Richard Williams ,  Gregor MacDonald ,  Ya Zhou ,  José Manuel Bartolomé-Nebreda

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Charles David Weaver ,  Shaun Stauffer ,  Richard Williams ,  Gregor MacDonald ,  Ya Zhou ,  José Manuel Bartolomé-Nebreda

IPC分类号： A61K31/5377 ,  C07D213/62 ,  C07D213/78 ,  C07D401/12 ,  C07D417/12 ,  C07D403/12 ,  C07D413/12 ,  A61K31/444 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/00

CPC分类号： A61K31/44 ,  C07D213/80 ,  C07D213/85 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： In one aspect, the invention relates to O-benzyl nicotinamide 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O-苄基烟酰胺类似物，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）的阳性变构调节剂; 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：US20110294858A1

公开(公告)日：2011-12-01

申请号：US13114958

申请日：2011-05-24

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Ya Zhou ,  Jason Manka ,  Gregor McDonald ,  José Manuel Bartolome-Nebreda

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Ya Zhou ,  Jason Manka ,  Gregor McDonald ,  José Manuel Bartolome-Nebreda

IPC分类号： A61K31/455 ,  C07D213/82 ,  C07D417/12 ,  A61K31/4439 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/30 ,  A61P25/14 ,  A61P25/08 ,  A61P25/06 ,  A61P3/10 ,  A61P21/00 ,  A61P3/04 ,  A61P3/00 ,  A61P25/22 ,  A61P25/24 ,  C07D213/80

CPC分类号： A61K31/44

摘要： In one aspect, the invention relates to substituted 6-methylnicotinamide 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6-甲基烟酰胺类似物，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：US08969389B2

公开(公告)日：2015-03-03

申请号：US13114958

申请日：2011-05-24

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Ya Zhou ,  Jason Manka ,  Gregor McDonald ,  José Manuel Bartolome-Nebreda

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Ya Zhou ,  Jason Manka ,  Gregor McDonald ,  José Manuel Bartolome-Nebreda

IPC分类号： A61K31/44

CPC分类号： A61K31/44

摘要： In one aspect, the invention relates to substituted 6-methylnicotinamide 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6-甲基烟酰胺类似物，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：US08501757B2

公开(公告)日：2013-08-06

申请号：US12885420

申请日：2010-09-17

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Charles David Weaver ,  Alice L. Rodriguez ,  Andrew S. Felts ,  Carrie K. Jones ,  Brittney S. Bates ,  Brian A. Chauder

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Charles David Weaver ,  Alice L. Rodriguez ,  Andrew S. Felts ,  Carrie K. Jones ,  Brittney S. Bates ,  Brian A. Chauder

IPC分类号： A61K31/505 ,  A61K31/44 ,  C07D239/02 ,  C07D403/12 ,  C07D401/12 ,  C07D213/62 ,  A61K31/4965

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.

摘要翻译： 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：US20120028956A1

公开(公告)日：2012-02-02

申请号：US13269977

申请日：2011-10-10

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Charles David Weaver ,  Alice L. Rodriguez ,  Colleen M. Niswender ,  Carrie K. Jones ,  Richard Williams

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Charles David Weaver ,  Alice L. Rodriguez ,  Colleen M. Niswender ,  Carrie K. Jones ,  Richard Williams

IPC分类号： A61K31/4725 ,  A61K31/496 ,  A61K31/4375 ,  A61K31/472 ,  C07D413/06 ,  C07D401/06 ,  C07D471/04 ,  C07D217/24 ,  A61P25/24 ,  C07D401/12 ,  A61P25/28 ,  A61P25/00 ,  A61P25/18 ,  A61P25/30 ,  A61P25/08 ,  A61P25/06 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00 ,  A61P25/20 ,  A61P25/22 ,  A61K31/5377

CPC分类号： A61K31/397 ,  A61K31/4704 ,  A61K31/5377 ,  C07D209/46 ,  C07D209/48 ,  C07D217/24 ,  C07D401/06

摘要： In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, 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：US20110172248A1

公开(公告)日：2011-07-14

申请号：US12885289

申请日：2010-09-17

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Charles David Weaver ,  Alice L. Rodriguez ,  Andrew S. Felts ,  Carrie K. Jones ,  Brittney S. Bates

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Charles David Weaver ,  Alice L. Rodriguez ,  Andrew S. Felts ,  Carrie K. Jones ,  Brittney S. Bates

IPC分类号： A61K31/497 ,  C07D213/65 ,  C07D239/34 ,  C07D401/12 ,  C07D403/14 ,  C07D401/14 ,  A61K31/444 ,  A61K31/506 ,  A61P25/00 ,  A61P25/22 ,  A61P25/30 ,  A61P25/16 ,  A61P1/04

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.

摘要翻译： 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：US20110152299A1

公开(公告)日：2011-06-23

申请号：US12885378

申请日：2010-09-17

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Charles David Weaver ,  Alice L. Rodriguez ,  Andrew S. Felts ,  Carrie K. Jones

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Charles David Weaver ,  Alice L. Rodriguez ,  Andrew S. Felts ,  Carrie K. Jones

IPC分类号： A61K31/506 ,  C07D401/12 ,  A61K31/4439 ,  C07D403/12 ,  A61P25/22 ,  A61P25/16 ,  A61P29/00 ,  A61P1/04

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

摘要翻译： 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：US09085562B2

公开(公告)日：2015-07-21

申请号：US14002309

申请日：2012-03-05

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Alice L. Rodriguez ,  Andrew S. Felts ,  Carrie K. Jones ,  Brittney S. Bates ,  Brian A. Chauder

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Kyle A. Emmitte ,  Alice L. Rodriguez ,  Andrew S. Felts ,  Carrie K. Jones ,  Brittney S. Bates ,  Brian A. Chauder

IPC分类号： C07D401/14 ,  A61K31/513 ,  C07D213/81 ,  C07D401/12

CPC分类号： C07D401/14 ,  A61K31/513 ,  C07D213/81 ,  C07D401/12

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.

摘要翻译： 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。