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1. 发明申请

US20110300165A1 SUBSTITUTED ISOXAZOLE COMPOUNDS 有权
标题翻译：取代的异丙唑化合物
公开(公告)号：US20110300165A1
公开(公告)日：2011-12-08
申请号：US13145730
申请日：2010-01-22
申请人： Scott Hunter Watterson , Alaric J. Dyckman , William J. Pitts , Steven H. Spergel
发明人： Scott Hunter Watterson , Alaric J. Dyckman , William J. Pitts , Steven H. Spergel
IPC分类号： A61K31/4245 , A61P29/00 , A61P37/06 , A61P19/02 , A61P25/00 , A61P17/06 , A61P11/06 , C07D413/14 , A61P3/10
CPC分类号： C07D413/14
摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein Q is R1 is alkyl or aryl, said aryl optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐，其中Q为R 1为烷基或芳基，所述芳基任选被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，-OR 4和/ 或卤素; 并且R 2，R 3，R 4和n在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

2. 发明授权

US08404672B2 Substituted heterocyclic compounds 有权
标题翻译：取代的杂环化合物
公开(公告)号：US08404672B2
公开(公告)日：2013-03-26
申请号：US13145721
申请日：2010-01-22
申请人： William J. Pitts , Alaric J. Dyckman , Steven H. Spergel , Scott Hunter Watterson
发明人： William J. Pitts , Alaric J. Dyckman , Steven H. Spergel , Scott Hunter Watterson
IPC分类号： A61K31/4402 , C07D413/14
CPC分类号： C07D413/14
摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein Q is R1 is cycloalkyl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as vascular disease and autoimmune diseases.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐，其中Q为R 1为环烷基，杂芳基或杂环基，各自任选被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，-OR 4，和/或卤素; 并且R 2，R 3，R 4和n在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如血管疾病和自身免疫性疾病）中疾病或病症的发展。

3. 发明授权

US08354398B2 Substituted isoxazole compounds 有权
标题翻译：取代的异恶唑化合物
公开(公告)号：US08354398B2
公开(公告)日：2013-01-15
申请号：US13145730
申请日：2010-01-22
申请人： Scott Hunter Watterson , Alaric J. Dyckman , William J. Pitts , Steven H. Spergel
发明人： Scott Hunter Watterson , Alaric J. Dyckman , William J. Pitts , Steven H. Spergel
IPC分类号： A61K31/4245 , C07D413/14
CPC分类号： C07D413/14
摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein Q is R1 is alkyl or aryl, said aryl optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐，其中Q为R 1为烷基或芳基，所述芳基任选被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，-OR 4和/ 或卤素; 并且R 2，R 3，R 4和n在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。

4. 发明申请

US20120022041A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS 有权
标题翻译：取代的杂环化合物
公开(公告)号：US20120022041A1
公开(公告)日：2012-01-26
申请号：US13145721
申请日：2010-01-22
申请人： William J. Pitts , Alaric J. Dyckman , Steven H. Spergel , Scott Hunter Watterson
发明人： William J. Pitts , Alaric J. Dyckman , Steven H. Spergel , Scott Hunter Watterson
IPC分类号： A61K31/4439 , A61P37/06 , A61P29/00 , C07D413/14
CPC分类号： C07D413/14
摘要： Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein Q is R1 is cycloalkyl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as vascular disease and autoimmune diseases.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐，其中Q为R 1为环烷基，杂芳基或杂环基，各自任选被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，-OR 4，和/或卤素; 并且R 2，R 3，R 4和n在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如血管疾病和自身免疫性疾病）中疾病或病症的发展。

5. 发明申请

US20110275610A1 SUBSTITUTED PYRAZOLE COMPOUNDS 有权
标题翻译：取代的吡唑化合物
公开(公告)号：US20110275610A1
公开(公告)日：2011-11-10
申请号：US13145728
申请日：2010-01-22
申请人： Alaric J. Dyckman , William J. Pitts , Scott Hunter Watterson
发明人： Alaric J. Dyckman , William J. Pitts , Scott Hunter Watterson
IPC分类号： A61K31/4245 , A61P29/00 , A61P37/00 , C07D413/14
CPC分类号： C07D413/14
摘要： Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, benzyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物或其药学上可接受的盐，其中：n为0或选自1至4的整数; R 1是环烷基，芳基，杂芳基或杂环基，各自任选地被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，苄基，-OR 4和/或卤素的取代基取代。并且R 2，R 3，R 4和n在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

6. 发明授权

US08389509B2 Substituted pyrazole compounds 有权
标题翻译：取代的吡唑化合物
公开(公告)号：US08389509B2
公开(公告)日：2013-03-05
申请号：US13145728
申请日：2010-01-22
申请人： Alaric J. Dyckman , William J. Pitts , Scott Hunter Watterson
发明人： Alaric J. Dyckman , William J. Pitts , Scott Hunter Watterson
IPC分类号： A61K31/4155 , A61K31/397 , A61K31/4245 , C07D231/10 , C07D271/06 , C07D205/04
CPC分类号： C07D413/14
摘要： Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, benzyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物或其药学上可接受的盐，其中：n为0或选自1至4的整数; R 1是环烷基，芳基，杂芳基或杂环基，各自任选地被一至五个独立地选自C 1至C 6烷基，C 1至C 4卤代烷基，苄基，-OR 4和/或卤素的取代基取代。并且R 2，R 3，R 4和n在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

7. 发明授权

US08268855B2 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same 有权
标题翻译： 1,6-二氢-1,3,5,6-四氮杂 - 引入并三烯基的三环化合物和包含它们的药物组合物
公开(公告)号：US08268855B2
公开(公告)日：2012-09-18
申请号：US12765932
申请日：2010-04-23
申请人： William J. Pitts , James Kempson , Junqing Guo , Jagabandhu Das , Charles M. Langevine , Steven H. Spergel , Scott Hunter Watterson
发明人： William J. Pitts , James Kempson , Junqing Guo , Jagabandhu Das , Charles M. Langevine , Steven H. Spergel , Scott Hunter Watterson
IPC分类号： C07D471/16 , C07D471/14 , A61K31/437
CPC分类号： C07D471/14
摘要： The present invention provides for tricyclic compounds having the formula (I), wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
摘要翻译：本发明提供具有式（I）的三环化合物，其中R 1，R 2，R 5，R 6，R 7和R 8如本文所述。本发明还提供包含这些化合物的药物组合物，以及这些化合物用于治疗炎症和免疫疾病的用途。

8. 发明申请

US20100210629A1 1,6-DIHYDRO-1,3,5,6-TETRAAZA-AS-INDACENE BASED TRICYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME 有权
标题翻译： 1,6-二氢-1,3,5,6-四氢异喹喔啉基异柠檬酸的三聚体化合物和包含其的药物组合物
公开(公告)号：US20100210629A1
公开(公告)日：2010-08-19
申请号：US12765932
申请日：2010-04-23
申请人： William J. Pitts , James Kempson , Junqing Guo , Jagabandhu Das , Charles M. Langevine , Steven H. Spergel , Scott Hunter Watterson
发明人： William J. Pitts , James Kempson , Junqing Guo , Jagabandhu Das , Charles M. Langevine , Steven H. Spergel , Scott Hunter Watterson
IPC分类号： A61K31/551 , C07D471/14 , A61K31/437 , C07D413/10 , A61K31/5377 , C07D279/12 , A61K31/541 , C07D401/14 , A61K31/496 , C07D403/14 , A61K31/497 , C07D243/08 , A61P19/02 , A61P11/06 , A61P1/02 , A61P17/06
CPC分类号： C07D471/14
摘要： The present invention provides for tricyclic compounds having the formula (I), wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
摘要翻译：本发明提供具有式（I）的三环化合物，其中R 1，R 2，R 5，R 6，R 7和R 8如本文所述。本发明还提供包含这些化合物的药物组合物，以及这些化合物用于治疗炎症和免疫疾病的用途。

9. 发明授权

US07737279B2 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same 有权
标题翻译： 1,6-二氢-1,3,5,6-四氮杂 - 引入并三烯基的三环化合物和包含它们的药物组合物
公开(公告)号：US07737279B2
公开(公告)日：2010-06-15
申请号：US11430215
申请日：2006-05-08
申请人： William J. Pitts , James Kempson , Junqing Guo , Jagabandhu Das , Charles M. Langevine , Steven H. Spergel , Scott Hunter Watterson
发明人： William J. Pitts , James Kempson , Junqing Guo , Jagabandhu Das , Charles M. Langevine , Steven H. Spergel , Scott Hunter Watterson
IPC分类号： C07D471/14 , A61K31/437 , A61K31/4375
CPC分类号： C07D471/14
摘要： The present invention provides for tricyclic compounds having the formula (I), wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
摘要翻译：本发明提供具有式（I）的三环化合物，其中R 1，R 2，R 5，R 6，R 7和R 8如本文所述。本发明还提供包含这些化合物的药物组合物，以及这些化合物用于治疗炎症和免疫疾病的用途。

10. 发明申请

US20120214767A1 TRICYCLIC HETEROCYCLIC COMPOUNDS 有权
标题翻译：三元杂环化合物
公开(公告)号：US20120214767A1
公开(公告)日：2012-08-23
申请号：US13504541
申请日：2010-10-29
申请人： T.G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das
发明人： T.G. Murali Dhar , Hai-Yun Xiao , Scott Hunter Watterson , Soo S. Ko , Alaric J. Dyckman , Charles M. Langevine , Jagabandhu Das
IPC分类号： A61K31/423 , C07D498/04 , A61K31/454 , C07D413/04 , A61P37/00 , A61K31/5377 , C07F9/09 , A61K31/675 , A61P35/00 , A61P7/00 , C07D413/14 , A61K31/506
CPC分类号： C07D413/04 , C07D231/54 , C07D261/20 , C07D277/84 , C07D403/06 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D487/10 , C07D498/04
摘要： Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译：公开了式（I）的化合物或其立体异构体或其盐，其中：X1，X2，X3，W，Q1，Q2和G2在本文中定义。还公开了使用这种化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。

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