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：US20090069318A1

公开(公告)日：2009-03-12

申请号：US11908440

申请日：2006-03-24

Applicant: James Francis Callahan ,  Jeffrey C. Boehm ,  Anthony William James Cooper ,  Stefano Livia ,  Neysa Nevins ,  Zehong Wan ,  Beth A. Norton ,  Xichen Lin

Inventor： James Francis Callahan ,  Jeffrey C. Boehm ,  Anthony William James Cooper ,  Stefano Livia ,  Neysa Nevins ,  Zehong Wan ,  Beth A. Norton ,  Xichen Lin

IPC: A61K31/5377 ,  C07D471/04 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.

公开(公告)号：US20080262040A1

公开(公告)日：2008-10-23

申请号：US12091491

申请日：2006-10-20

Applicant: James Francis Callahan ,  Jeffrey K. Kerns ,  Xichen Lin

Inventor： James Francis Callahan ,  Jeffrey K. Kerns ,  Xichen Lin

IPC: A61K31/4535 ,  C07D211/06 ,  A61P25/28 ,  A61P3/10 ,  A61P31/18 ,  A61P11/06

CPC classification number: C07D231/56 ,  C07D401/04 ,  C07D401/14

Abstract: 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).

Abstract translation: 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）。

公开(公告)号：US20080242685A1

公开(公告)日：2008-10-02

申请号：US12091488

申请日：2006-10-20

Applicant: Jeffrey K. Kerns ,  Xichen Lin

Inventor： Jeffrey K. Kerns ,  Xichen Lin

IPC: A61K31/519 ,  A61K31/437 ,  C07D471/04 ,  A61P35/00 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: 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).

Abstract translation: 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）。

公开(公告)号：US20070254873A1

公开(公告)日：2007-11-01

申请号：US11575416

申请日：2005-09-21

Applicant: Jeffrey Kerns ,  Michael Lindenmuth ,  Xichen Lin ,  Hong Nie ,  Sonia Thomas

Inventor： Jeffrey Kerns ,  Michael Lindenmuth ,  Xichen Lin ,  Hong Nie ,  Sonia Thomas

IPC: A61K31/535 ,  A61K31/405 ,  A61P11/06 ,  C07D265/28 ,  C07D401/00 ,  C07D209/04 ,  A61K31/445

CPC classification number: C07D409/14 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  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：US08354416B2

公开(公告)日：2013-01-15

申请号：US12132793

申请日：2008-06-04

Applicant: James F. Callahan ,  Jeffrey C. Boehm ,  Anthony William James Cooper ,  Stefano Livia ,  Paul Bamborough ,  Neysa Nevins ,  Zehong Wan ,  Beth A. Norton ,  Xichen Lin

Inventor： James F. Callahan ,  Jeffrey C. Boehm ,  Anthony William James Cooper ,  Stefano Livia ,  Paul Bamborough ,  Neysa Nevins ,  Zehong Wan ,  Beth A. Norton ,  Xichen Lin

IPC: C07D471/04 ,  A61K31/519 ,  A61P29/00 ,  A61P9/10

CPC classification number: C07D487/04

Abstract: Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.

Abstract translation: 新型取代的2,4,8-三取代8H-吡啶并[2,3-d]嘧啶-7-酮的化合物和组合物，以及它们在CSBP / RK / p38激酶抑制剂治疗中的用途。

公开(公告)号：US20130012491A1

公开(公告)日：2013-01-10

申请号：US13635499

申请日：2011-03-16

Applicant: Xichen Lin ,  Feng Ren ,  Haibo Zhang

Inventor： Xichen Lin ,  Feng Ren ,  Haibo Zhang

IPC: C07D239/26 ,  C07D401/04 ,  A61P25/00 ,  A61K31/506 ,  C07D401/10 ,  A61K31/505 ,  C07D403/10

CPC classification number: C07D239/26 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10

Abstract: Disclosed are pyrimidine derivatives for use as a sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or diseases mediated by S1P1 receptors, particularly multiple sclerosis.

Abstract translation: 公开了用作鞘氨醇1-磷酸1（S1P1）受体激动剂的嘧啶衍生物，其制备方法，含有它们的药物组合物及其用于治疗由S1P1受体，特别是多发性硬化症介导的病症或疾病的用途。

公开(公告)号：US20120101136A1

公开(公告)日：2012-04-26

申请号：US13379498

申请日：2010-06-24

Applicant: Guanghui Deng ,  Xichen Lin ,  Feng Ren ,  Jia-Ning Xiang

Inventor： Guanghui Deng ,  Xichen Lin ,  Feng Ren ,  Jia-Ning Xiang

IPC: A61K31/433 ,  A61K31/425 ,  C07D285/08 ,  C07D271/06 ,  C07D233/61 ,  A61P9/00 ,  A61P25/00 ,  A61P37/00 ,  A61P29/00 ,  A61P41/00 ,  A61P19/02 ,  A61P1/00 ,  A61P17/06 ,  A61P35/00 ,  A61P35/04 ,  A61P3/10 ,  A61K31/4245

CPC classification number: A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  C07D263/32 ,  C07D271/06 ,  C07D271/107 ,  C07D277/30 ,  C07D285/08 ,  C07D285/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: 5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.

Abstract translation: 公开了式（I）的5元杂芳基衍生物或其盐，其制备方法，含有它们的药物组合物及其在治疗由S1P1受体介导的各种疾病中的用途。

公开(公告)号：US20120101123A1

公开(公告)日：2012-04-26

申请号：US13379170

申请日：2010-06-17

Applicant: Chengyong Li ,  Xichen Lin ,  Qinghua Meng ,  Haibo Zhang

Inventor： Chengyong Li ,  Xichen Lin ,  Qinghua Meng ,  Haibo Zhang

IPC: A61K31/437 ,  A61P25/00 ,  A61P37/00 ,  A61P29/00 ,  A61P11/06 ,  A61P19/02 ,  A61P41/00 ,  A61P1/00 ,  A61P17/06 ,  A61P35/00 ,  A61P35/04 ,  A61P7/00 ,  A61P31/12 ,  A61P3/10 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

Abstract translation: 本发明涉及具有药理活性的新化合物，其制备方法，含有它们的药物组合物及其在治疗各种疾病中的用途。