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公开(公告)号：US10150762B2
公开(公告)日：2018-12-11
申请号：US15664673
申请日：2017-07-31
发明人： Steven Goldberg , Hariharan Venkatesan , Olaf Kinzel , Christian Gege , Christoph Steeneck , Gerald Kleymann , Thomas Hoffmann
IPC分类号： C07D277/56 , A61K31/426 , C07D417/06 , A61K31/454 , A61K45/06 , C07D487/08 , A61K31/427 , C07D495/10 , C07D417/14 , A61K31/4709 , A61K31/541 , A61K31/4439
摘要： The present invention comprises methods of making 5-(2,3-dichloro-4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2-hydroxy-2-methylpropyl)-4-(R1-1-carbonyl)thiazole-2-carboxamide, wherein R1 is defined in the specification.
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公开(公告)号：US09845319B2
公开(公告)日：2017-12-19
申请号：US14927502
申请日：2015-10-30
发明人： Steven Goldberg , Hariharan Venkatesan , Virginia Tanis , Maud Urbanski , Aihua Wang , David Kummer , Christoph Steeneck , Christian Gege , Olaf Kinzel , Gerald Kleymann , Thomas Hoffmann , Anne M. Fourie , Xiaohua Xue
IPC分类号： C07D417/04 , C07D417/06 , C07D417/14 , A61K31/427 , A61K45/06 , A61K31/454 , A61K31/4439 , A61K31/4545
CPC分类号： C07D417/04 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D417/06 , C07D417/14
摘要： The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R5, A1, A2, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
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公开(公告)号：US09861618B2
公开(公告)日：2018-01-09
申请号：US14927501
申请日：2015-10-30
发明人： Steven Goldberg , Christoph Steeneck , Christian Gege , Olaf Kinzel , Gerald Kleymann , Thomas Hoffmann
IPC分类号： A61K31/426 , C07D417/04 , A61K31/427 , A61K45/06 , C07D417/14 , A61K31/5377 , A61K31/4725 , A61K31/454 , A61K31/433 , C07D277/30 , A61K31/506
CPC分类号： A61K31/426 , A61K31/427 , A61K31/433 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D277/30 , C07D417/04 , C07D417/14
摘要： The present invention comprises compounds of Formula I wherein: R1, R2, R3, R4, R5, R7, R8, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
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公开(公告)号：US20160120850A1
公开(公告)日：2016-05-05
申请号：US14927501
申请日：2015-10-30
发明人： Steven Goldberg , Christoph Steeneck , Christian Gege , Olaf Kinzel , Gerald Kleymann , Thomas Hoffmann
IPC分类号： A61K31/426 , A61K31/427 , A61K45/06 , C07D417/14 , A61K31/506 , A61K31/4725 , A61K31/454 , A61K31/433 , C07D277/30 , C07D417/04 , A61K31/5377
CPC分类号： A61K31/426 , A61K31/427 , A61K31/433 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D277/30 , C07D417/04 , C07D417/14
摘要： The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R7, R8, and are defined in the specification.The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
摘要翻译： 本发明包括式I化合物，其中：R1，R2，R3，R4，R5，R7，R8，并在说明书中定义。 本发明还包括治疗或改善综合征，病症或疾病的方法，其中所述综合征，病症或疾病是类风湿性关节炎或牛皮癣。 本发明还包括通过施用治疗有效量的至少一种权利要求1的化合物来调节哺乳动物的RORγt活性的方法。
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公开(公告)号：US10080744B2
公开(公告)日：2018-09-25
申请号：US15812528
申请日：2017-11-14
发明人： Steven Goldberg , Christoph Steeneck , Christian Gege , Olaf Kinzel , Gerald Kleymann , Thomas Hoffmann , Anne M. Fourie , Xiaohua Xue
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/4725 , A61K31/454 , A61K31/433 , A61K31/427 , A61K31/426 , C07D277/30 , C07D417/14 , A61K45/06 , C07D417/04
CPC分类号： A61K31/426 , A61K31/427 , A61K31/433 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D277/30 , C07D417/04 , C07D417/14
摘要： The present invention comprises compounds of Formula I wherein: R1, R2, R3, R4, R5, R7, R8, and {circle around (A)} are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
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公开(公告)号：US20180064690A1
公开(公告)日：2018-03-08
申请号：US15812528
申请日：2017-11-14
发明人： Steven Goldberg , Christoph Steeneck , Christian Gege , Olaf Kinzel , Gerald Kleymann , Thomas Hoffmann , Anne M. Fourie , Xiaohua Xue
IPC分类号： A61K31/426 , A61K31/506 , C07D277/30 , A61K31/433 , A61K31/454 , A61K31/4725 , C07D417/14 , A61K45/06 , A61K31/427 , C07D417/04 , A61K31/5377
CPC分类号： A61K31/426 , A61K31/427 , A61K31/433 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D277/30 , C07D417/04 , C07D417/14
摘要： The present invention comprises compounds of Formula I wherein:R1, R2, R3, R4, R5, R7, R8, and are defined in the specification.The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
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公开(公告)号：US09850236B2
公开(公告)日：2017-12-26
申请号：US14927499
申请日：2015-10-30
发明人： Steven Goldberg , Hariharan Venkatesan , Virginia Tanis , Olaf Kinzel , Christian Gege , Christoph Steeneck , Gerald Kleymann , Thomas Hoffmann , Anne M. Fourie , Xiaohua Xue
IPC分类号： A61K31/426 , C07D277/56 , C07D417/06 , A61K31/454 , A61K45/06 , C07D487/08 , A61K31/427 , C07D495/10 , C07D417/14 , A61K31/4709 , A61K31/541 , A61K31/4439
CPC分类号： C07D417/06 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/541 , A61K45/06 , C07D277/56 , C07D417/14 , C07D487/08 , C07D495/10
摘要： The present invention comprises compounds of Formula I. wherein: X, A1, A2, A3, A4, R1, R2, and R3 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
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公开(公告)号：US20170327492A1
公开(公告)日：2017-11-16
申请号：US15664673
申请日：2017-07-31
发明人： Steven Goldberg , Hariharan Venkatesan , Olaf Kinzel , Christian Gege , Christoph Steeneck , Gerald Kleymann , Thomas Hoffmann
IPC分类号： C07D417/06 , C07D487/08 , C07D417/14 , C07D277/56 , A61K31/541 , A61K31/426 , A61K31/4709 , A61K31/454 , A61K31/4439 , A61K31/427 , C07D495/10 , A61K45/06
CPC分类号： C07D417/06 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/541 , A61K45/06 , C07D277/56 , C07D417/14 , C07D487/08 , C07D495/10
摘要： The present invention comprises methods of making 5-(2,3-dichloro-4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2-hydroxy-2-methylpropyl)-4-(R1-1-carbonyl)thiazole-2-carboxamide, wherein R1 is defined in the specification.
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公开(公告)号：US20160122336A1
公开(公告)日：2016-05-05
申请号：US14927499
申请日：2015-10-30
发明人： Steven Goldberg , Hariharan Venkatesan , Virginia Tanis , Olaf Kinzel , Christian Gege , Christoph Steeneck , Gerald Kleymann , Thomas Hoffmann
IPC分类号： C07D417/06 , A61K45/06 , C07D487/08 , A61K31/427 , A61K31/4439 , A61K31/426 , C07D495/10 , C07D417/14 , A61K31/4709 , A61K31/541 , A61K31/454 , C07D277/56
CPC分类号： C07D417/06 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/541 , A61K45/06 , C07D277/56 , C07D417/14 , C07D487/08 , C07D495/10
摘要： The present invention comprises compounds of Formula I. wherein: X, A1, A2, A3, A4, R1, R2, and R3 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
摘要翻译： 本发明包括式I化合物，其中X，A 1，A 2，A 3，A 4，R 1，R 2和R 3在本说明书中定义。 本发明还包括治疗或改善综合征，病症或疾病的方法，其中所述综合征，病症或疾病是类风湿性关节炎或牛皮癣。 本发明还包括通过施用治疗有效量的至少一种权利要求1的化合物来调节哺乳动物的RORγt活性的方法。
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公开(公告)号：US20160122335A1
公开(公告)日：2016-05-05
申请号：US14927502
申请日：2015-10-30
发明人： Steven Goldberg , Hariharan Venkatesan , Virginia Tanis , Maud Urbanski , Aihua Wang , David Kummer , Christoph Steeneck , Christian Gege , Olaf Kinzel , Gerald Kleymann , Thomas Hoffmann
IPC分类号： C07D417/04 , A61K45/06 , A61K31/4545 , A61K31/454 , A61K31/4439 , A61K31/427 , C07D417/14
CPC分类号： C07D417/04 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D417/06 , C07D417/14
摘要： The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R5, A1, A2, and are defined in the specification.The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
摘要翻译： 本发明包括式I化合物，其中：R1，R2，R3，R5，A1，A2，并在说明书中定义。 本发明还包括治疗或改善综合征，病症或疾病的方法，其中所述综合征，病症或疾病是类风湿性关节炎或牛皮癣。 本发明还包括通过施用治疗有效量的至少一种权利要求1的化合物来调节哺乳动物的RORγt活性的方法。
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