公开(公告)号：US20140121213A1

公开(公告)日：2014-05-01

申请号：US14128704

申请日：2012-07-03

Applicant: Jeffrey Charles Boehm ,  Roderick S. Davis ,  Jeffrey Kerns ,  Guoliang Lin ,  Robert D. Murdoch ,  Hong NIE

Inventor： Jeffrey Charles Boehm ,  Roderick S. Davis ,  Jeffrey Kerns ,  Guoliang Lin ,  Robert D. Murdoch ,  Hong NIE

IPC: C07D409/14 ,  C07D405/14 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D213/80

CPC classification number: C07D409/14 ,  A61K31/497 ,  C07D213/80 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/12

Abstract: In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases.In particular, the present invention also relates to methods and uses for treatment of respiratory or respiratory tract diseases, which comprises administering to a subject in need thereof an effective amount of a compound of the present invention.

Abstract translation: 通常，本发明涉及电压门控钠通道阻断剂化合物的用途，其包括相应的前体，中间体，单体和二聚体，相应的药物组合物，用于呼吸和呼吸道疾病的化合物制备和治疗方法。 特别地，本发明还涉及治疗呼吸道或呼吸道疾病的方法和用途，其包括向有需要的受试者施用有效量的本发明化合物。

公开(公告)号：US20120040958A1

公开(公告)日：2012-02-16

申请号：US13279434

申请日：2011-10-24

Applicant: Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

Inventor： Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

IPC: 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 classification number: C07D409/04 ,  C07D409/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08084449B2

公开(公告)日：2011-12-27

申请号：US12365930

申请日：2009-02-05

Applicant: James Francis Callahan ,  Guoliang Lin ,  Zehong Wan ,  Hongxing Yan

Inventor： James Francis Callahan ,  Guoliang Lin ,  Zehong Wan ,  Hongxing Yan

IPC: A61K31/496 ,  A61K31/551 ,  A61K31/437 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use as dual chromaphores having inhibitory activity against PDE4 and muscarinic acetylcholine receptors (mAChRs), and thus being useful for treating respiratory diseases.

Abstract translation: 本发明涉及新型式（I）化合物及其药学上可接受的盐，药物组合物及其作为对PDE4和毒蕈碱性乙酰胆碱受体（mAChR）具有抑制活性的双重染色体的用途，因此可用于治疗呼吸系统疾病。

公开(公告)号：US08071584B2

公开(公告)日：2011-12-06

申请号：US12532773

申请日：2008-03-20

Applicant: Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

Inventor： Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

IPC: A61K31/397 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/4436 ,  A61K31/404 ,  C07D409/14 ,  C07D413/14 ,  C07D209/04

CPC classification number: C07D409/04 ,  C07D409/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100130468A1

公开(公告)日：2010-05-27

申请号：US12532773

申请日：2008-03-20

Applicant: Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

Inventor： Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

IPC: A61K31/405 ,  C07D209/04 ,  C07D409/14 ,  A61K31/55 ,  C07D403/02 ,  A61K31/497 ,  C07D413/02 ,  A61K31/535

CPC classification number: C07D409/04 ,  C07D409/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。