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1. 发明申请

WO2004074438A2 CCR8 ANTAGONISTS 审中-公开
公开(公告)号：WO2004074438A2
公开(公告)日：2004-09-02
申请号：PCT/US2004/004394
申请日：2004-02-13
申请人： SMITHKLINE BEECHAM CORPORATION , JIN, Jian , KERNS, Jeffrey, K. , SHI, Dongchuan , WANG, Feng , WANG, Yonghui
发明人： JIN, Jian , KERNS, Jeffrey, K. , SHI, Dongchuan , WANG, Feng , WANG, Yonghui
IPC分类号： C12N
CPC分类号： C07D405/12 , C07D243/08
摘要： The invention relates to certain substituted bicyclicaryl-benzenesulfonamide and their use for inhibiting the chemokine receptor nominated CCR8. The generic structure for these compounds, as defined herein is that of a benzenesulfonamide of Formula (I).
摘要翻译：本发明涉及某些取代的双环芳基 - 苯磺酰胺及其用于抑制趋化因子受体被提名的CCR8的用途。如本文所定义的这些化合物的一般结构是式（I）的苯磺酰胺的一般结构。

2. 发明申请

WO2004073619A2 CCR8 ANTAGONISTS 审中-公开
公开(公告)号：WO2004073619A2
公开(公告)日：2004-09-02
申请号：PCT/US2004/004256
申请日：2004-02-13
申请人： SMITHKLINE BEECHAM CORPORATION , JIN, Jian , KERNS, Jeffrey, K. , WANG, Feng , WANG, Yonghui
发明人： JIN, Jian , KERNS, Jeffrey, K. , WANG, Feng , WANG, Yonghui
IPC分类号： A61K
CPC分类号： C07D295/192 , C07D243/08 , C07D409/12
摘要： This invention relates to certain substituted benzenesulfonamide and their use for inhibiting the chemokine receptor nominated CCR8. The generic structure for these compounds, as defined herein is that of a benzenesulfonamide of formula (I).
摘要翻译：本发明涉及某些取代苯磺酰胺及其用于抑制趋化因子受体被提名的CCR8的用途。这些化合物的通式结构如本文所定义为式（I）的苯磺酰胺的一般结构。

3. 发明申请

WO2004032856A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2004032856A2
公开(公告)日：2004-04-22
申请号：PCT/US2003/031795
申请日：2003-10-07
申请人： SMITHKLINE BEECHAM CORPORATION , JIN, Jian , KERNS, Jeffrey, K. , WANG, Feng , WANG, Yonghui
发明人： JIN, Jian , KERNS, Jeffrey, K. , WANG, Feng , WANG, Yonghui
IPC分类号： A61K
CPC分类号： C07D413/14 , C07D471/04
摘要： Oxazolidin-2-one of the formula as further defined herein are useful for inhibiting the chemokine receptor nominated CCR8, resulting in treatment of diseases such as asthma and the like.
摘要翻译：本文进一步定义的式的恶唑烷-2-酮可用于抑制趋化因子受体指定的CCR8，导致治疗诸如哮喘等疾病。

4. 发明申请

WO2007102883A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2007102883A2
公开(公告)日：2007-09-13
申请号：PCT/US2006/060098
申请日：2006-10-20
申请人： SMITHKLINE BEECHAM CORPORATION , CALLAHAN, James, Francis , KERNS, Jeffrey, K. , LIN, Xichen
发明人： CALLAHAN, James, Francis , KERNS, Jeffrey, K. , LIN, Xichen
IPC分类号： A61K31/416
CPC分类号： C07D231/56 , C07D401/04 , C07D401/14
摘要： 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).
摘要翻译：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，特别是用于治疗和预防包括炎症和组织修复紊乱在内的IKK2机制介导的病症。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）。

5. 发明申请

WO2005000247A3 4-CARBOXAMIDO QUINOLINE DERIVATIVES FOR USE AS NK-2 AND NK-3 审中-公开
公开(公告)号：WO2005000247A3
公开(公告)日：2005-01-06
申请号：PCT/US2004/020333
申请日：2004-06-23
申请人： SMITHKLINE BEECHAM CORPORATION , KERNS, Jeffrey, K. , NIE, Hong
发明人： KERNS, Jeffrey, K. , NIE, Hong
IPC分类号： A61K31/496
摘要： Compounds of the formula (I) are disclosed which are NK2 and NK3 receptor antagonists and are useful in the treatment of respiratory diseases: or a pharmaceutically acceptable salt thereof.

6. 发明申请

WO2007114848A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2007114848A2
公开(公告)日：2007-10-11
申请号：PCT/US2006/060099
申请日：2006-10-20
申请人： SMITHKLINE BEECHAM CORPORATION , KERNS, Jeffrey, K. , LIN, Xichen
发明人： KERNS, Jeffrey, K. , LIN, Xichen
IPC分类号： A61B8/14
CPC分类号： C07D487/04 , C07D471/04
摘要： 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).
摘要翻译：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，特别是用于治疗和预防包括炎症和组织修复紊乱在内的IKK2机制介导的病症。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）。

7. 发明申请

WO2007076286A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2007076286A2
公开(公告)日：2007-07-05
申请号：PCT/US2006/062058
申请日：2006-12-14
申请人： SMITHKLINE BEECHAM CORPORATION , KERNS, Jeffrey, K.
发明人： KERNS, Jeffrey, K.
IPC分类号： A61K31/454 , A61K31/404
CPC分类号： C07D209/08 , C07D209/12 , C07D209/42
摘要： The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I). 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.
摘要翻译：本发明涉及新的吲哚甲酰胺衍生物。具体地，本发明涉及根据式（I）的化合物。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活性和与之相关疾病的治疗方法。

8. 发明申请

WO2004017911A2 PROTEASE INHIBITORS 审中-公开
标题翻译：蛋白酶抑制剂
公开(公告)号：WO2004017911A2
公开(公告)日：2004-03-04
申请号：PCT/US2003/026358
申请日：2003-08-22
申请人： SMITHKLINE BEECHAM CORPORATION , BONDINELL, William, E. , HALL, Ralph, F. , JIN, Qi , KERNS, Jeffrey, K. , NIE, Hong , WIDDOWSON, Katherine, L.
发明人： BONDINELL, William, E. , HALL, Ralph, F. , JIN, Qi , KERNS, Jeffrey, K. , NIE, Hong , WIDDOWSON, Katherine, L.
IPC分类号： A61K
CPC分类号： H04L27/2601 , C07D223/08 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： This invention relates 4-amino-azepan-3-ones of formula (1) which are useful as protease inhibitors, particularly of cathepsin S, and as such are useful for preventing a number of diseases amongst which are atherosclerotic lesions and pulmonary diseases such as asthma and allergic reactions.
摘要翻译：本发明涉及式（1）的4-氨基 - 氮杂环庚烷-3-酮，其可用作蛋白酶抑制剂，特别是组织蛋白酶S，并因此可用于预防许多疾病，其中是动脉粥样硬化病变和肺部疾病，如哮喘和过敏反应。

9. 发明申请

WO2008118724A1 INDOLE CARBOXAMIDES AS IKK2 INHIBITORS 审中-公开
标题翻译：将碳酰胺作为IKK2抑制剂
公开(公告)号：WO2008118724A1
公开(公告)日：2008-10-02
申请号：PCT/US2008/057583
申请日：2008-03-20
申请人： SMITHKLINE BEECHAM CORPORATION , BOEHM, Jeffrey, Charles , BUSCH-PETERSEN, Jakob , FU, Wei , JIN, Qi , KERNS, Jeffrey, K. , LI, Huijie , LIN, Guoliang , LIN, Xichen , NEIPP, Christopher, E.
发明人： BOEHM, Jeffrey, Charles , BUSCH-PETERSEN, Jakob , FU, Wei , JIN, Qi , KERNS, Jeffrey, K. , LI, Huijie , LIN, Guoliang , LIN, Xichen , NEIPP, Christopher, E.
IPC分类号： A01N43/38 , A61K31/405
CPC分类号： C07D409/04 , C07D409/14 , C07D417/14
摘要： 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.
摘要翻译：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IKKβ）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活性和与之相关疾病的治疗方法。

10. 发明申请

WO2007062318A3 CHEMICAL COMPOUNDS 审中-公开
公开(公告)号：WO2007062318A3
公开(公告)日：2007-05-31
申请号：PCT/US2006/061018
申请日：2006-11-17
申请人： SMITHKLINE BEECHAM CORPORATION , KERNS, Jeffrey, K. , BUSCH-PETERSEN, Jakob , LI, Huijie , BOEHM, Jeffrey, Charles , NIE, Hong , TAGGART, John, J.
发明人： KERNS, Jeffrey, K. , BUSCH-PETERSEN, Jakob , LI, Huijie , BOEHM, Jeffrey, Charles , NIE, Hong , TAGGART, John, J.
IPC分类号： A61K31/54
摘要： The invention is directed to novel indolecarboxamide derivatives, Specifically, the invention is directed to compounds according to formula (I), where R1 , R2, R3 and X 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).

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