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    Chemical compounds
    1.
    发明授权
    Chemical compounds 失效
    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

    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。

    Chemical compounds
    2.
    发明授权
    Chemical compounds 失效
    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

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

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

    IPC: C07D401/00

    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。

    Chemical Compounds
    4.
    发明申请
    Chemical Compounds 审中-公开
    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

    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）。

    Chemical Compounds
    5.
    发明申请
    Chemical Compounds 审中-公开
    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

    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）。

    Compounds
    10.
    发明授权
    Compounds 失效
    化合物

    公开(公告)号：US07674789B2

    公开(公告)日：2010-03-09

    申请号：US11389112

    申请日：2006-03-24

    Applicant: James F. Callahan ,  Zehong Wan ,  Hongxing Yan ,  Xichen Lin

    Inventor： James F. Callahan ,  Zehong Wan ,  Hongxing Yan ,  Xichen Lin

    IPC: A61K31/5355 ,  A61K31/519 ,  C07D487/04 ,  A61P29/00 ,  C07D239/30 ,  C07D239/38

    CPC classification number: C07D487/04

    Abstract: The present invention is directed to compounds of formula (I), (Ia),(Ic) and (Id), compositions, and uses thereof as an inhibitor of the p38 kinase, and wherein, inter alia R1 is C(Z)N(R10′)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10′)C(Z)(CR10R20)vRb; N(R10′)C(Z)N(R10′)(CR10R20)vRb; or N(R10′)OC(Z)(CR10R20)vRb; R3 is C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroarylC1-10 alkyl, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted; X is R2, OR2′, S(O)mR2′, (CH2)n′N(R10′)S(O)mR2′, (CH2)n′N(R10′)C(O)R2′, (CH2)n′NR4R14, (CH2)n′N(R2 ′)(R2″), or N(R10′)—Rh—NH—C(═N—CN)NRqRq′; and R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及作为p38激酶抑制剂的式（I），（Ia），（Ic）和（Id），其组合物和用途的化合物，其中除了其中R 1是C（Z）N （R10'）（CR10R20）vRb，C（Z）O（CR10R20）vRb，N（R10'）C（Z）（CR10R20）vRb; N（R 10'）C（Z）N（R 10'）（CR 10 R 20）v R b; 或N（R 10'）OC（Z）（CR 10 R 20）v R b; R 3是C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-10烷基，芳基，芳基C 1-10烷基，杂芳基C 1-10烷基或杂环基C 1-10烷基部分，并且其中这些部分中的每一个可以是任选的 取代 X是R2，OR2'，S（O）mR2'，（CH2）n'N（R10'）S（O）mR2'，（CH2）n'N（R10'）C（O）R2' ）n'NR4R14，（CH2）n'N（R2'）（R2“）或N（R10'） - Rh-NH-C（= N-CN）NRqRq' 和R 2是氢，C 1-10烷基，C 3-7环烷基，C 3-7环烷基烷基，芳基，芳基C 1-10烷基，杂芳基，杂芳基C 1-10烷基，杂环基或杂环基C 1-10烷基部分， ，不包括氢，可以任选被取代; 或其药学上可接受的盐。

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