公开(公告)号：US20080089858A1

公开(公告)日：2008-04-17

申请号：US11854600

申请日：2007-09-13

申请人： Brian McKittrick ,  Elizabeth Smith ,  Chad Bennett ,  Joel Harris ,  Eugenia Kiselgof ,  Chad Knutson ,  Peter Korakas ,  Deen Tulshian ,  Hyunjin Kim

发明人： Brian McKittrick ,  Elizabeth Smith ,  Chad Bennett ,  Joel Harris ,  Eugenia Kiselgof ,  Chad Knutson ,  Peter Korakas ,  Deen Tulshian ,  Hyunjin Kim

IPC分类号： A61K31/438 ,  A61K31/565 ,  A61K31/57 ,  A61K31/573 ,  A61K31/675 ,  A61K38/20 ,  A61P3/10 ,  C07D471/10

CPC分类号： C07D471/08

摘要： Disclosed are compounds of the formula: and compounds of the formula: wherein R1, R2, R3, R4, R5, u and v are as defined herein. Also disclosed are methods of treating pain (e.g., inflammatory pain, chronic pain, and neuropathic pain), methods of treating diabetes, and methods of inhibiting the absorption of cholesterol using compounds of formula I or IIA.

摘要翻译： 公开了下式的化合物和下式的化合物：其中R 1，R 2，R 3，R 4， u，v和u如本文所定义。 还公开了治疗疼痛（例如炎性疼痛，慢性疼痛和神经性疼痛）的方法，治疗糖尿病的方法，以及使用式I或IIA化合物抑制胆固醇吸收的方法。

公开(公告)号：US20090082336A1

公开(公告)日：2009-03-26

申请号：US12264676

申请日：2008-11-04

申请人： Julius J. Matasi ,  Deen Tulshian ,  Duane A. Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Donalski

发明人： Julius J. Matasi ,  Deen Tulshian ,  Duane A. Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Donalski

IPC分类号： A61K31/55 ,  C07D495/14 ,  A61K31/519 ,  C12N5/06 ,  A61K31/5377

CPC分类号： C07D471/14 ,  C07D491/14 ,  C07D495/04 ,  C07D495/14 ,  C09B57/00

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

摘要翻译： 在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂， 含有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代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

公开(公告)号：US07598259B2

公开(公告)日：2009-10-06

申请号：US11301672

申请日：2005-12-13

申请人： Julius J Matasi ,  Deen Tulshian ,  Duane A Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Domalski

发明人： Julius J Matasi ,  Deen Tulshian ,  Duane A Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Domalski

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC分类号： C07D495/14

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

公开(公告)号：US07485648B2

公开(公告)日：2009-02-03

申请号：US11152535

申请日：2005-06-14

申请人： Julius J. Matasi ,  Deen Tulshian ,  Duane A. Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Domalski

发明人： Julius J. Matasi ,  Deen Tulshian ,  Duane A. Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Domalski

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC分类号： C07D471/14 ,  C07D491/14 ,  C07D495/04 ,  C07D495/14 ,  C09B57/00

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1—R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

摘要翻译： 在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂， 含有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代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

公开(公告)号：US20060167029A1

公开(公告)日：2006-07-27

申请号：US11301672

申请日：2005-12-13

申请人： Julius Matasi ,  Deen Tulshian ,  Duane Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa Silverman ,  Thavalakulamgara Sasikumar ,  Li Qiang ,  Martin Domalski

发明人： Julius Matasi ,  Deen Tulshian ,  Duane Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa Silverman ,  Thavalakulamgara Sasikumar ,  Li Qiang ,  Martin Domalski

IPC分类号： A61K31/519 ,  C07D498/22

CPC分类号： C07D495/14

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

摘要翻译： 在其许多实施方案中，本发明提供式I的三环化合物（其中J 1，X 4和X 1，R 2，R 2， 可用作代谢型谷氨酸受体（mGluR）拮抗剂，特别是作为选择性代谢型谷氨酸受体1拮抗剂的药物组合物，以及使用该化合物和组合物治疗疾病的治疗方法 与代谢型谷氨酸受体（例如，mGluR1）相关，例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默氏病。

公开(公告)号：US07989464B2

公开(公告)日：2011-08-02

申请号：US12356867

申请日：2009-01-21

申请人： Julius J. Matasi ,  Deen Tulshian ,  Duane A. Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Domalski

发明人： Julius J. Matasi ,  Deen Tulshian ,  Duane A. Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Domalski

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00

CPC分类号： C07D495/14

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

摘要翻译： 在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂， 含有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代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

公开(公告)号：US07638526B2

公开(公告)日：2009-12-29

申请号：US11854600

申请日：2007-09-13

申请人： Brian A. McKittrick ,  Elizabeth M. Smith ,  Chad E. Bennett ,  Joel M. Harris ,  Eugenia Y. Kiselgof ,  Chad E. Knutson ,  Peter Korakas ,  Deen Tulshian ,  Hyunjin Kim

发明人： Brian A. McKittrick ,  Elizabeth M. Smith ,  Chad E. Bennett ,  Joel M. Harris ,  Eugenia Y. Kiselgof ,  Chad E. Knutson ,  Peter Korakas ,  Deen Tulshian ,  Hyunjin Kim

IPC分类号： A61K31/438 ,  C07D471/10

CPC分类号： C07D471/08

摘要： Disclosed are compounds of the formula: and compounds of the formula: wherein R1, R2, R3, R4, R5, u and v are as defined herein. Also disclosed are methods of treating pain (e.g., inflammatory pain, chronic pain, and neuropathic pain), methods of treating diabetes, and methods of inhibiting the absorption of cholesterol using compounds of formula I or IIA.

摘要翻译： 公开了下式的化合物和下式的化合物：其中R 1，R 2，R 3，R 4，R 5，u和v如本文所定义。 还公开了治疗疼痛（例如炎性疼痛，慢性疼痛和神经性疼痛）的方法，治疗糖尿病的方法，以及使用式I或IIA化合物抑制胆固醇吸收的方法。

公开(公告)号：US20090192178A1

公开(公告)日：2009-07-30

申请号：US12356867

申请日：2009-01-21

申请人： Julius J. Matasi ,  Deen Tulshian ,  Duane A. Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Domalski

发明人： Julius J. Matasi ,  Deen Tulshian ,  Duane A. Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa S. Silverman ,  Thavalakulamgara K. Sasikumar ,  Li Qiang ,  Martin S. Domalski

IPC分类号： A61K31/519 ,  C07D495/14 ,  A61P25/00

CPC分类号： C07D495/14

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

摘要翻译： 在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂， 含有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代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

公开(公告)号：US20060009477A1

公开(公告)日：2006-01-12

申请号：US11152535

申请日：2005-06-14

申请人： Julius Matasi ,  Deen Tulshian ,  Duane Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa Silverman ,  Thavalakulamgara Sasikumar ,  Li Qiang ,  Martin Domalski

发明人： Julius Matasi ,  Deen Tulshian ,  Duane Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa Silverman ,  Thavalakulamgara Sasikumar ,  Li Qiang ,  Martin Domalski

IPC分类号： A61K31/519 ,  C07D487/14

CPC分类号： C07D471/14 ,  C07D491/14 ,  C07D495/04 ,  C07D495/14 ,  C09B57/00

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1—R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

摘要翻译： 在其许多实施方案中，本发明提供了式I的三环化合物（其中J 1，X 4和X 1，R 2， 可用作代谢型谷氨酸受体（mGluR）拮抗剂，特别是作为选择性代谢型谷氨酸受体1拮抗剂的药物组合物，以及使用该化合物和组合物治疗疾病的治疗方法 与代谢型谷氨酸受体（例如，mGluR1）相关，例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默氏病。