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1. 发明授权

US08754103B2 Fused heterocyclic compounds as ion channel modulators 有权
公开(公告)号：US08754103B2
公开(公告)日：2014-06-17
申请号：US12843702
申请日：2010-07-26
申请人： Britton Corkey , Elfatih Elzein , Robert Jiang , Rao Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Gregory Notte , Eric Parkhill , Thao Perry , Jeff Zablocki
发明人： Britton Corkey , Elfatih Elzein , Robert Jiang , Rao Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Gregory Notte , Eric Parkhill , Thao Perry , Jeff Zablocki
IPC分类号： A01N43/42 , A61K31/44 , C07D491/02
摘要： The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

2. 发明申请

US20130012521A1 APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS 有权
标题翻译：抗病毒信号调节激酶抑制剂
公开(公告)号：US20130012521A1
公开(公告)日：2013-01-10
申请号：US13618841
申请日：2012-09-14
申请人： Britton Corkey , Michael Graupe , Keith Koch , Lawrence S. Melvin, JR. , Gregory Notte
发明人： Britton Corkey , Michael Graupe , Keith Koch , Lawrence S. Melvin, JR. , Gregory Notte
IPC分类号： A61K31/4439 , C07D471/04 , A61K31/444 , A61K31/4709 , A61K31/4545 , A61K31/496 , A61K31/506 , A61P9/00 , A61P3/10 , A61P13/12 , A61P11/00 , A61P1/16 , A61P25/28 , A61P29/00 , C07D401/14
CPC分类号： A61K31/444 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/585 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
摘要翻译：本发明涉及式（I）的化合物：其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，X 8，R 1，R 2，R 3如上所定义。该化合物具有凋亡信号调节激酶（ASK1）抑制活性，因此可用于治疗ASK1介导的病症，包括自身免疫疾病，炎性疾病，心血管疾病和神经变性疾病。本发明还涉及包含一种或多种式（I）化合物的药物组合物和制备式（I）化合物的方法。

3. 发明授权

US09371329B2 Fused heterocyclic compounds as ion channel modulators 有权
公开(公告)号：US09371329B2
公开(公告)日：2016-06-21
申请号：US14274422
申请日：2014-05-09
申请人： Britton Corkey , Elfatih Elzein , Robert Jiang , Rao Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Gregory Notte , Eric Parkhill , Thao Perry , Jeff Zablocki
发明人： Britton Corkey , Elfatih Elzein , Robert Jiang , Rao Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Gregory Notte , Eric Parkhill , Thao Perry , Jeff Zablocki
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

4. 发明申请

US20140303158A1 FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS 有权
标题翻译：熔融杂环化合物作为离子通道调节剂
公开(公告)号：US20140303158A1
公开(公告)日：2014-10-09
申请号：US14274422
申请日：2014-05-09
申请人： Britton Corkey , Elfatih Elzein , Robert Jiang , Rao Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Gregory Notte , Eric Parkhill , Thao Perry , Jeff Zablocki
发明人： Britton Corkey , Elfatih Elzein , Robert Jiang , Rao Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Gregory Notte , Eric Parkhill , Thao Perry , Jeff Zablocki
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译：本发明涉及钠通道抑制剂及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的化合物。在具体实施方案中，化合物的结构由式I给出：其中W1，W2，W3，R1，Q，X1，X2和X3如本文所述，用于制备和使用化合物和药物组合物的方法含有相同的

5. 发明授权

US08598360B2 Apoptosis signal-regulating kinase inhibitors 有权
标题翻译：细胞凋亡信号调节激酶抑制剂
公开(公告)号：US08598360B2
公开(公告)日：2013-12-03
申请号：US13618841
申请日：2012-09-14
申请人： Britton Corkey , Michael Graupe , Keith Koch , Lawrence S. Melvin, Jr. , Gregory Notte
发明人： Britton Corkey , Michael Graupe , Keith Koch , Lawrence S. Melvin, Jr. , Gregory Notte
IPC分类号： A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4545 , A61K31/496 , A61K31/506 , A61P9/00 , A61P3/10 , A61P13/12 , A61P11/00 , A61P1/16 , A61P25/28 , A61P29/00 , C07D401/14 , C07D471/04
CPC分类号： A61K31/444 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/585 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
摘要翻译：本发明涉及式（I）的化合物：其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，X 8，R 1，R 2，R 3如上所定义。该化合物具有凋亡信号调节激酶（“ASK1”）抑制活性，因此可用于治疗ASK1介导的病症，包括自身免疫性疾病，炎性疾病，心血管疾病和神经变性疾病。本发明还涉及包含一种或多种式（I）化合物的药物组合物和制备式（I）化合物的方法。

6. 发明授权

US08378108B2 Apoptosis signal-regulating kinase inhibitors 有权
标题翻译：细胞凋亡信号调节激酶抑制剂
公开(公告)号：US08378108B2
公开(公告)日：2013-02-19
申请号：US12834673
申请日：2010-07-12
申请人： Britton Corkey , Michael Graupe , Keith Koch , Lawrence S. Melvin, Jr. , Gregory Notte
发明人： Britton Corkey , Michael Graupe , Keith Koch , Lawrence S. Melvin, Jr. , Gregory Notte
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/4725 , A61K31/437 , A61K31/5377 , C07D401/14 , C07D401/12 , C07D471/04 , C07D413/14 , A61P37/00 , A61P25/28 , A61P9/00
CPC分类号： A61K31/444 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/585 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of Formula (I): where in X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
摘要翻译：本发明涉及式（I）化合物：其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，X 8，R 1，R 2，R 3如上所定义。该化合物具有凋亡信号调节激酶（ASK1）抑制活性，因此可用于治疗ASK1介导的病症，包括自身免疫疾病，炎性疾病，心血管疾病和神经变性疾病。本发明还涉及包含一种或多种式（I）化合物的药物组合物和制备式（I）化合物的方法。

7. 发明授权

US08952034B2 Fused heterocyclic compounds as ion channel modulators 有权
标题翻译：稠合杂环化合物作为离子通道调节剂
公开(公告)号：US08952034B2
公开(公告)日：2015-02-10
申请号：US12843702
申请日：2010-07-26
申请人： Britton Corkey , Elfatih Elzein , Robert Jiang , Rao Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Gregory Notte , Eric Parkhill , Thao Perry , Jeff Zablocki
发明人： Britton Corkey , Elfatih Elzein , Robert Jiang , Rao Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Gregory Notte , Eric Parkhill , Thao Perry , Jeff Zablocki
IPC分类号： A01N43/42 , A61K31/44 , C07D491/02
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译：本发明涉及钠通道抑制剂及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的化合物。在具体实施方案中，化合物的结构由式I给出：其中W1，W2，W3，R1，Q，X1，X2和X3如本文所述，用于制备和使用化合物和药物组合物的方法含有相同的

8. 发明授权

US08703759B2 Fused heterocyclic compounds as ion channel modulators 有权
标题翻译：稠合杂环化合物作为离子通道调节剂
公开(公告)号：US08703759B2
公开(公告)日：2014-04-22
申请号：US13174587
申请日：2011-06-30
申请人： Tetsuya Kobayashi , Dmitry Koltun , Gregory Notte , Eric Parkhill , Jeff Zablocki
发明人： Tetsuya Kobayashi , Dmitry Koltun , Gregory Notte , Eric Parkhill , Jeff Zablocki
IPC分类号： A61K31/437 , C07D519/00 , A61K31/506 , A61K31/4985 , A61P25/02 , A61K31/501 , A61P9/06 , A61P9/04 , A61P9/10 , A61P9/12 , A61P3/10 , C07D471/04
CPC分类号： C07D471/04 , C07D519/00
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译：本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。在具体实施方案中，化合物的结构由式I给出：其中R 1，R 2，R 3，R 4和R 5如本文所述，用于制备和使用化合物的方法以及含有该化合物的药物组合物。

9. 发明授权

US08440665B2 Apoptosis signal-regulating kinase inhibitors 有权
标题翻译：细胞凋亡信号调节激酶抑制剂
公开(公告)号：US08440665B2
公开(公告)日：2013-05-14
申请号：US13174459
申请日：2011-06-30
申请人： Britton Corkey , Gregory Notte , Jeff Zablocki
发明人： Britton Corkey , Gregory Notte , Jeff Zablocki
IPC分类号： A61K31/535 , C07D239/42 , C07D401/04
CPC分类号： C07D409/14
摘要： The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
摘要翻译：本发明涉及式（I）的化合物：其中X1，X2，X3，X4，X5，R，R1，R2如上定义。这些化合物具有凋亡信号调节激酶（“ASK1”）抑制活性，因此可用于治疗ASK1介导的病症，包括自身免疫性疾病，炎症性疾病，心血管疾病，糖尿病，糖尿病性肾病，心脏肾病，包括肾脏疾病，纤维化疾病，呼吸系统疾病，COPD，特发性肺纤维化，急性肺损伤，急性和慢性肝病和神经变性疾病。本发明还涉及包含一种或多种式（I）化合物的药物组合物和制备式（I）化合物的方法。

10. 发明申请

US20120289493A1 FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS 有权
标题翻译：熔融杂环化合物作为离子通道调节剂
公开(公告)号：US20120289493A1
公开(公告)日：2012-11-15
申请号：US13466995
申请日：2012-05-08
申请人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Gregory Notte , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
发明人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Gregory Notte , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
IPC分类号： A61K31/53 , C07D401/10 , C07D403/10 , C07D413/06 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/501 , A61K31/506 , C07D265/22 , A61K31/536 , C07D498/10 , A61K31/4725 , C07D417/06 , A61K31/5415 , A61P9/00 , A61P9/10 , A61P9/12 , A61P3/10 , A61P25/08 , A61P25/00 , C07D253/08
CPC分类号： C07D498/10 , C07D217/26 , C07D237/32 , C07D239/88 , C07D239/90 , C07D253/08 , C07D263/58 , C07D265/22 , C07D279/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译：本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。在具体实施方案中，化合物的结构由式I给出：其中Q，R 1，X 1，X 2，Y和R 2如本文所述，用于制备和使用该化合物的方法以及含有该化合物的药物组合物。

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