公开(公告)号：US20070232599A1

公开(公告)日：2007-10-04

申请号：US11568909

申请日：2005-05-26

Applicant: Jakob Busch-Petersen ,  Christopher Neipp ,  Michael Palovich

Inventor： Jakob Busch-Petersen ,  Christopher Neipp ,  Michael Palovich

IPC: A61K31/535 ,  A61P11/00 ,  C07D265/36

CPC classification number: C07D498/08

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

公开(公告)号：US20120035164A1

公开(公告)日：2012-02-09

申请号：US13273408

申请日：2011-10-14

Applicant: Jianghe DENG ,  Jeffrey K. KERNS ,  Qi JIN ,  Guoliang LIN ,  Xichen LIN ,  Michael LINDENMUTH ,  Christopher NEIPP ,  Hong NIE ,  Sonia M. THOMAS ,  Katherine L. WIDDOWSON

Inventor： Jianghe DENG ,  Jeffrey K. KERNS ,  Qi JIN ,  Guoliang LIN ,  Xichen LIN ,  Michael LINDENMUTH ,  Christopher NEIPP ,  Hong NIE ,  Sonia M. THOMAS ,  Katherine L. WIDDOWSON

IPC: A61K31/541 ,  A61K31/4545 ,  A61K31/496 ,  C07D413/14 ,  A61K31/5377 ,  C07D401/04 ,  A61K31/454 ,  A61K31/4725 ,  C07D405/14 ,  C07D409/14 ,  A61K31/506 ,  C07D417/14 ,  A61K31/501 ,  A61P29/00 ,  A61P1/00 ,  A61P11/06 ,  A61P11/00 ,  A61P19/02 ,  A61P19/10 ,  A61P17/06 ,  A61P17/00 ,  A61P37/06 ,  A61P25/00 ,  A61P25/28 ,  A61P9/10 ,  A61P9/00 ,  A61P3/10 ,  A61P13/12 ,  A61P37/00 ,  A61P35/00 ,  A61P21/00 ,  A61P43/00 ,  C07D401/14

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20090143372A1

公开(公告)日：2009-06-04

申请号：US11931189

申请日：2007-10-31

Applicant: Jianghe Deng ,  Jeffrey K. Kerns ,  Qi Jin ,  Guoliang Lin ,  Xichen Lin ,  Michael Lindenmuth ,  Christopher Neipp ,  Hong Nie ,  Sonia M. Thomas ,  Katherine L. Widdowson

Inventor： Jianghe Deng ,  Jeffrey K. Kerns ,  Qi Jin ,  Guoliang Lin ,  Xichen Lin ,  Michael Lindenmuth ,  Christopher Neipp ,  Hong Nie ,  Sonia M. Thomas ,  Katherine L. Widdowson

IPC: 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 classification number: C07D401/04 ,  C07D401/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20070293531A1

公开(公告)日：2007-12-20

申请号：US11573097

申请日：2005-08-05

Applicant: Jakob Busch-Petersen ,  Roderick Davis ,  Dramane Laine ,  Christopher Neipp ,  Michael Palovich

Inventor： Jakob Busch-Petersen ,  Roderick Davis ,  Dramane Laine ,  Christopher Neipp ,  Michael Palovich

IPC: A61K31/439 ,  C07D221/22

CPC classification number: C07D451/14

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract translation: 毒蕈碱乙酰胆碱受体拮抗剂及其使用方法。

公开(公告)号：US20070249664A1

公开(公告)日：2007-10-25

申请号：US11774867

申请日：2007-07-09

Applicant: Damane Laine ,  Michael Palovich ,  Brent McCleland ,  Christopher Neipp ,  Sonia Thomas

Inventor： Damane Laine ,  Michael Palovich ,  Brent McCleland ,  Christopher Neipp ,  Sonia Thomas

IPC: A61K31/4745 ,  C07D453/02

CPC classification number: C07D453/02 ,  A61K31/439

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

公开(公告)号：US20070173646A1

公开(公告)日：2007-07-26

申请号：US11568930

申请日：2005-05-10

Applicant: Dramane Laine ,  Brent McCleland ,  Christopher Neipp ,  Michael Palovich

Inventor： Dramane Laine ,  Brent McCleland ,  Christopher Neipp ,  Michael Palovich

IPC: C07D451/02

CPC classification number: C07D453/02

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

公开(公告)号：US08354406B2

公开(公告)日：2013-01-15

申请号：US13273408

申请日：2011-10-14

Applicant: Jianghe Deng ,  Jeffrey K. Kerns ,  Qi Jin ,  Guoliang Lin ,  Xichen Lin ,  Michael Lindenmuth ,  Christopher Neipp ,  Hong Nie ,  Sonia M Thomas ,  Katherine L. Widdowson

Inventor： Jianghe Deng ,  Jeffrey K. Kerns ,  Qi Jin ,  Guoliang Lin ,  Xichen Lin ,  Michael Lindenmuth ,  Christopher Neipp ,  Hong Nie ,  Sonia M Thomas ,  Katherine L. Widdowson

IPC: C07D401/04 ,  A61K31/445

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20070185155A1

公开(公告)日：2007-08-09

申请号：US11568330

申请日：2005-04-27

Applicant: Damane Laine ,  Michael Palovich ,  Brent McCleland ,  Christopher Neipp ,  Sonia Thomas

Inventor： Damane Laine ,  Michael Palovich ,  Brent McCleland ,  Christopher Neipp ,  Sonia Thomas

IPC: A61K31/46 ,  C07D451/02

CPC classification number: C07D453/02 ,  A61K31/439

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract translation: 毒蕈碱乙酰胆碱受体拮抗剂及其使用方法。