公开(公告)号：US08067408B2

公开(公告)日：2011-11-29

申请号：US12365934

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

Abstract: The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

Abstract translation: 本发明涉及式（I）的新型化合物，其药物组合物及其在治疗中的用途，例如作为IV型磷酸二酯酶（PDE4）的抑制剂和毒蕈碱性乙酰胆碱受体（mAChR）的拮抗剂，用于治疗和/ 或预防呼吸系统疾病，包括抗炎和/或过敏性疾病如慢性阻塞性肺疾病（COPD），哮喘，鼻炎（例如过敏性鼻炎），特应性皮炎或牛皮癣。

公开(公告)号：US20090203677A1

公开(公告)日：2009-08-13

申请号：US12365933

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: A61K31/437 ,  C07D471/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61P11/06

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

Abstract translation: 本发明涉及式（I）的新化合物及其在治疗呼吸系统疾病中的应用，包括抗炎和过敏性疾病如慢性阻塞性肺病（COPD），哮喘，鼻炎（例如过敏性鼻炎），特应性皮炎 或牛皮癣。

公开(公告)号：US20090197871A1

公开(公告)日：2009-08-06

申请号：US12365934

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: A61K31/437 ,  C07D471/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61P11/06

CPC classification number: C07D471/04

Abstract: The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

Abstract translation: 本发明涉及式（I）的新型化合物，其药物组合物及其在治疗中的用途，例如作为IV型磷酸二酯酶（PDE4）的抑制剂和毒蕈碱性乙酰胆碱受体（mAChR）的拮抗剂，用于治疗和/ 或预防呼吸系统疾病，包括抗炎和/或过敏性疾病如慢性阻塞性肺疾病（COPD），哮喘，鼻炎（例如过敏性鼻炎），特应性皮炎或牛皮癣。

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：US08071588B2

公开(公告)日：2011-12-06

申请号：US12365933

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 relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.

Abstract translation: 本发明涉及式（I）的新化合物及其在治疗呼吸系统疾病中的应用，包括抗炎和过敏性疾病如慢性阻塞性肺病（COPD），哮喘，鼻炎（例如过敏性鼻炎），特应性皮炎 或牛皮癣。

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：US20130023541A1

公开(公告)日：2013-01-24

申请号：US13522183

申请日：2011-01-13

Applicant: Jeffrey Charles Boehm ,  Roderick S. Davis ,  Jeffrey K. Kerns ,  Guoliang Lin ,  Hong Nie

Inventor： Jeffrey Charles Boehm ,  Roderick S. Davis ,  Jeffrey K. Kerns ,  Guoliang Lin ,  Hong Nie

IPC: A61K31/496 ,  A61P11/00 ,  C07D401/04

CPC classification number: C07D213/80 ,  C07D213/74 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

Abstract: 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.

Abstract translation: 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。

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：US20090264498A1

公开(公告)日：2009-10-22

申请号：US12424761

申请日：2009-04-16

Applicant: Dramane Ibrahim Laine ,  Guoliang Lin ,  Brent W. McCleland ,  Michael R. Palovich

Inventor： Dramane Ibrahim Laine ,  Guoliang Lin ,  Brent W. McCleland ,  Michael R. Palovich

IPC: A61K31/40 ,  C07D207/14

CPC classification number: C07D207/14

Abstract: This invention relates to compounds of formula (I) which are useful for treating chronic obstructive pulmonary disease, and the like.

Abstract translation: 本发明涉及可用于治疗慢性阻塞性肺病的式（I）化合物等。

公开(公告)号：US20090203657A1

公开(公告)日：2009-08-13

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: A61K31/56 ,  C07D471/02 ,  A61K31/437 ,  C07D401/14 ,  A61K31/496 ,  C07D243/08 ,  A61K31/551 ,  A61P11/00

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。