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1. 发明授权

US08354406B2 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US08354406B2
公开(公告)日：2013-01-15
申请号：US13273408
申请日：2011-10-14
申请人： Jianghe Deng , Jeffrey K. Kerns , Qi Jin , Guoliang Lin , Xichen Lin , Michael Lindenmuth , Christopher Neipp , Hong Nie , Sonia M Thomas , Katherine L. Widdowson
发明人： Jianghe Deng , Jeffrey K. Kerns , Qi Jin , Guoliang Lin , Xichen Lin , Michael Lindenmuth , Christopher Neipp , Hong Nie , Sonia M Thomas , Katherine L. Widdowson
IPC分类号： C07D401/04 , A61K31/445
CPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的吲哚甲酰胺衍生物。具体地说，本发明涉及式I化合物：其中R1，R2，R3，U和V定义如下，及其药学上可接受的盐。本发明的化合物是IKK2的抑制剂，并且可用于治疗与不适当的IKK2（也称为IKK＆bgr）活性相关的疾病，例如类风湿性关节炎，哮喘和COPD（慢性阻塞性肺疾病）。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制IKK2活性和与其相关的病症的治疗方法。

2. 发明申请

US20090143372A1 CHEMICAL COMPOUNDS 失效
标题翻译：化学化合物
公开(公告)号：US20090143372A1
公开(公告)日：2009-06-04
申请号：US11931189
申请日：2007-10-31
申请人： Jianghe Deng , Jeffrey K. Kerns , Qi Jin , Guoliang Lin , Xichen Lin , Michael Lindenmuth , Christopher Neipp , Hong Nie , Sonia M. Thomas , Katherine L. Widdowson
发明人： Jianghe Deng , Jeffrey K. Kerns , Qi Jin , Guoliang Lin , Xichen Lin , Michael Lindenmuth , Christopher Neipp , Hong Nie , Sonia M. Thomas , Katherine L. Widdowson
IPC分类号： A61K31/541 , C07D401/14 , A61K31/4545 , A61K31/496 , C07D413/14 , A61K31/5377 , C07D401/02 , A61P11/00 , A61P3/00 , A61P9/00 , A61P37/00 , A61P25/00 , A61P17/00 , A61P1/00 , A61K31/454 , C07D217/00 , A61K31/4725 , A61K31/506 , C07D417/14
CPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof.The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的吲哚甲酰胺衍生物。具体地说，本发明涉及式I化合物：其中R1，R2，R3，U和V定义如下，及其药学上可接受的盐。本发明的化合物是IKK2的抑制剂，并且可用于治疗与不适当的IKK2（也称为IKKβ）活性相关的疾病，例如类风湿性关节炎，哮喘和COPD（慢性阻塞性肺疾病）。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制IKK2活性和与其相关的病症的治疗方法。

3. 发明授权

US08063071B2 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US08063071B2
公开(公告)日：2011-11-22
申请号：US11931189
申请日：2007-10-31
申请人： Jeffrey K. Kerns , Qi Jin , Michael Lindenmuth , Sonia M Thomas , Katherine L. Widdowson
发明人： Jeffrey K. Kerns , Qi Jin , Michael Lindenmuth , Sonia M Thomas , Katherine L. Widdowson
IPC分类号： A61K31/445 , C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的吲哚甲酰胺衍生物。具体地说，本发明涉及式I化合物：其中R1，R2，R3，U和V定义如下，及其药学上可接受的盐。本发明的化合物是IKK2的抑制剂，并且可用于治疗与不适当的IKK2（也称为IKK＆bgr）活性相关的疾病，例如类风湿性关节炎，哮喘和COPD（慢性阻塞性肺疾病）。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制IKK2活性和与其相关的病症的治疗方法。

4. 发明授权

US07858796B2 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US07858796B2
公开(公告)日：2010-12-28
申请号：US11575416
申请日：2005-09-21
申请人： Jeffrey K. Kerns , Michael Lindenmuth , Xichen Lin , Hong Nie , Sonia M. Thomas
发明人： Jeffrey K. Kerns , Michael Lindenmuth , Xichen Lin , Hong Nie , Sonia M. Thomas
IPC分类号： C07D401/00
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的吲哚甲酰胺衍生物。具体地说，本发明涉及式I化合物：其中R1，R2，R3，U和V定义如下，及其药学上可接受的盐。本发明的化合物是IKK2的抑制剂，并且可用于治疗与不适当的IKK2（也称为IKK＆bgr）活性相关的疾病，例如类风湿性关节炎，哮喘和COPD（慢性阻塞性肺疾病）。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制IKK2活性和与其相关的病症的治疗方法。

5. 发明申请

US20120040958A1 INDOLE CARBOXAMIDES AS IKK2 INHIBITORS 失效
标题翻译：将碳酰胺作为IKK2抑制剂
公开(公告)号：US20120040958A1
公开(公告)日：2012-02-16
申请号：US13279434
申请日：2011-10-24
申请人： Jeffrey Charles Boehm , Jakob Busch-Petersen , Wei Fu , Qi Jin , Jeffrey K. Kerns , Huijie Li , Guoliang Lin , Xichen Lin , Christopher E. Neipp
发明人： Jeffrey Charles Boehm , Jakob Busch-Petersen , Wei Fu , Qi Jin , Jeffrey K. Kerns , Huijie Li , Guoliang Lin , Xichen Lin , Christopher E. Neipp
IPC分类号： A61K31/404 , C07D409/14 , A61K31/4439 , A61K31/55 , A61K31/416 , C07D417/14 , A61K31/427 , C07D413/14 , A61K31/5377 , A61K31/553 , A61K31/496 , C07D495/08 , A61P29/00 , A61P11/06 , A61P11/00 , C07D409/04
CPC分类号： C07D409/04 , C07D409/14 , C07D417/14
摘要： The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein.The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的吲哚羧酰胺化合物。具体地，本发明涉及式（I）的化合物：其中R 1，R 2，R 3，R 4和m如本文所定义。本发明的化合物是IKK2的抑制剂，并且可用于治疗与不适当的IKK2（也称为IKK＆bgr）活性相关的疾病，例如类风湿性关节炎，哮喘，鼻炎和COPD（慢性阻塞性肺疾病）。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制IKK2活性和与其相关的病症的治疗方法。

6. 发明授权

US08071584B2 Indole carboxamides as IKK2 inhibitors 失效
标题翻译：吲哚甲酰胺作为IKK2抑制剂
公开(公告)号：US08071584B2
公开(公告)日：2011-12-06
申请号：US12532773
申请日：2008-03-20
申请人： Jeffrey Charles Boehm , Jakob Busch-Petersen , Wei Fu , Qi Jin , Jeffrey K. Kerns , Huijie Li , Guoliang Lin , Xichen Lin , Christopher E. Neipp
发明人： Jeffrey Charles Boehm , Jakob Busch-Petersen , Wei Fu , Qi Jin , Jeffrey K. Kerns , Huijie Li , Guoliang Lin , Xichen Lin , Christopher E. Neipp
IPC分类号： A61K31/397 , A61K31/55 , A61K31/5377 , A61K31/4436 , A61K31/404 , C07D409/14 , C07D413/14 , C07D209/04
CPC分类号： C07D409/04 , C07D409/14 , C07D417/14
摘要： The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的吲哚甲酰胺衍生物。具体地，本发明涉及式（I）的化合物：其中R 1，R 2，R 3，R 4和m如本文所定义。本发明的化合物是IKK2的抑制剂，并且可用于治疗与不适当的IKK2（也称为IKK＆bgr）活性相关的疾病，例如类风湿性关节炎，哮喘，鼻炎和COPD（慢性阻塞性肺疾病）。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制IKK2活性和与其相关的病症的治疗方法。

7. 发明申请

US20100130468A1 INDOLE CARBOXAMIDES AS IKK2 INHIBITORS 失效
标题翻译：将碳酰胺作为IKK2抑制剂
公开(公告)号：US20100130468A1
公开(公告)日：2010-05-27
申请号：US12532773
申请日：2008-03-20
申请人： Jeffrey Charles Boehm , Jakob Busch-Petersen , Wei Fu , Qi Jin , Jeffrey K. Kerns , Huijie Li , Guoliang Lin , Xichen Lin , Christopher E. Neipp
发明人： Jeffrey Charles Boehm , Jakob Busch-Petersen , Wei Fu , Qi Jin , Jeffrey K. Kerns , Huijie Li , Guoliang Lin , Xichen Lin , Christopher E. Neipp
IPC分类号： A61K31/405 , C07D209/04 , C07D409/14 , A61K31/55 , C07D403/02 , A61K31/497 , C07D413/02 , A61K31/535
CPC分类号： C07D409/04 , C07D409/14 , C07D417/14
摘要： The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein.The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的吲哚甲酰胺衍生物。具体地，本发明涉及式（I）的化合物：其中R 1，R 2，R 3，R 4和m如本文所定义。本发明的化合物是IKK2的抑制剂，并且可用于治疗与不适当的IKK2（也称为IKK＆bgr）活性相关的疾病，例如类风湿性关节炎，哮喘，鼻炎和COPD（慢性阻塞性肺疾病）。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物来抑制IKK2活性和与其相关的病症的治疗方法。

8. 发明申请

US20130023541A1 VOLTAGE-GATED SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译：电压门控通道阻塞器
公开(公告)号：US20130023541A1
公开(公告)日：2013-01-24
申请号：US13522183
申请日：2011-01-13
申请人： Jeffrey Charles Boehm , Roderick S. Davis , Jeffrey K. Kerns , Guoliang Lin , Hong Nie
发明人： Jeffrey Charles Boehm , Roderick S. Davis , Jeffrey K. Kerns , Guoliang Lin , Hong Nie
IPC分类号： A61K31/496 , A61P11/00 , C07D401/04
CPC分类号： C07D213/80 , C07D213/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： The present invention relates to voltage-gated sodium channel blocker intermediates, compounds and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory or respiratory tract diseases.
摘要翻译：本发明涉及电压门控钠通道阻断剂中间体，化合物和二聚体，相应的药物组合物，用于呼吸或呼吸道疾病的化合物制备和治疗方法。

9. 发明申请

US20080262040A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20080262040A1
公开(公告)日：2008-10-23
申请号：US12091491
申请日：2006-10-20
申请人： James Francis Callahan , Jeffrey K. Kerns , Xichen Lin
发明人： James Francis Callahan , Jeffrey K. Kerns , Xichen Lin
IPC分类号： A61K31/4535 , C07D211/06 , A61P25/28 , A61P3/10 , A61P31/18 , A61P11/06
CPC分类号： C07D231/56 , C07D401/04 , C07D401/14
摘要： The invention is directed to novel indazole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): where R1 and R2 are as defined below. These compounds are useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, in particular in the treatment and prevention of disorders mediated by IKK2 mechanisms including inflammatory and tissue repair disorders. Such disorders include rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease).
摘要翻译：本发明涉及新的吲唑甲酰胺衍生物。具体地，本发明涉及式（I）的化合物：其中R 1和R 2如下所定义。这些化合物可用于治疗与不适当的IKK2（也称为IKKβ）活性相关的疾病，特别是治疗和预防包括炎性和组织修复障碍在内的IKK2机制介导的疾病。这些疾病包括类风湿性关节炎，哮喘和COPD（慢性阻塞性肺疾病）。

10. 发明申请

US20080242685A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20080242685A1
公开(公告)日：2008-10-02
申请号：US12091488
申请日：2006-10-20
申请人： Jeffrey K. Kerns , Xichen Lin
发明人： Jeffrey K. Kerns , Xichen Lin
IPC分类号： A61K31/519 , A61K31/437 , C07D471/04 , A61P35/00 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention is directed to novel azaindole and azaindazole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): where R1, R2, T1, T2 and T3 are defined below. These compounds are useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, in particular in the treatment and prevention of disorders mediated by IKK2 mechanisms including inflammatory and tissue repair disorders. Such disorders include rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease).
摘要翻译：本发明涉及新颖的氮杂吲哚和氮杂唑类甲酰胺衍生物。具体地，本发明涉及式（I）化合物：其中R1，R2，T1，T2和T3如下定义。这些化合物可用于治疗与不适当的IKK2（也称为IKKβ）活性相关的疾病，特别是治疗和预防包括炎性和组织修复障碍在内的IKK2机制介导的疾病。这些疾病包括类风湿性关节炎，哮喘和COPD（慢性阻塞性肺疾病）。

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