公开(公告)号：US20120101124A1

公开(公告)日：2012-04-26

申请号：US13379214

申请日：2010-06-17

Applicant: Xichen Lin ,  Feng Ren ,  Yugui Si

Inventor： Xichen Lin ,  Feng Ren ,  Yugui Si

IPC: A61K31/437 ,  A61K31/4439 ,  C07D413/14 ,  C07D413/10 ,  A61K31/4245 ,  A61P25/00 ,  A61P29/00 ,  A61P11/06 ,  A61P19/02 ,  A61P1/00 ,  A61P17/06 ,  A61P35/00 ,  A61P35/04 ,  A61P31/12 ,  A61P3/10 ,  A61P9/00 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D413/04 ,  C07D413/14

Abstract: 1,2,4-Oxadiazol derivatives represented by formula (I) useful as sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated via S1P1 receptor are disclosed.

Abstract translation: 可用作鞘氨醇1-磷酸1（S1P1）受体激动剂的式（I）表示的1,2,4-恶二唑衍生物，其制备方法，含有它们的药物组合物及其用于治疗通过S1P1受体介导的各种病症的用途 披露

公开(公告)号：US08071584B2

公开(公告)日：2011-12-06

申请号：US12532773

申请日：2008-03-20

Applicant: Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

Inventor： Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

IPC: A61K31/397 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/4436 ,  A61K31/404 ,  C07D409/14 ,  C07D413/14 ,  C07D209/04

CPC classification number: C07D409/04 ,  C07D409/14 ,  C07D417/14

Abstract: The invention is directed to novel indole carboxamide derivatives. 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.

Abstract translation: 本发明涉及新的吲哚甲酰胺衍生物。 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IKK＆bgr）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活性和与其相关的病症的治疗方法。

公开(公告)号：US20110269738A1

公开(公告)日：2011-11-03

申请号：US13096641

申请日：2011-04-28

Applicant: Guanghui Deng ,  Xichen Lin ,  Feng Ren ,  Baowei Zhao

Inventor： Guanghui Deng ,  Xichen Lin ,  Feng Ren ,  Baowei Zhao

IPC: A61K31/433 ,  A61K31/454 ,  A61P25/00 ,  A61P29/00 ,  A61P11/06 ,  A61P9/00 ,  A61P17/06 ,  A61P35/00 ,  A61P35/04 ,  A61P31/12 ,  A61P3/10 ,  C07D417/10 ,  A61P19/02

CPC classification number: C07D417/10

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。

公开(公告)号：US20110086839A1

公开(公告)日：2011-04-14

申请号：US12999091

申请日：2009-06-18

Applicant: Jose Luis Castro Pineiro ,  Xichen Lin ,  Quan Liu ,  Kevin Meng ,  Feng Ren ,  David R. Vesey ,  Baowei Zhao

Inventor： Jose Luis Castro Pineiro ,  Xichen Lin ,  Quan Liu ,  Kevin Meng ,  Feng Ren ,  David R. Vesey ,  Baowei Zhao

IPC: A61K31/4245 ,  C07D413/10 ,  C07D413/14 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4439 ,  A61P25/00

CPC classification number: C07D413/04 ,  C07D413/14

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

公开(公告)号：US20100130468A1

公开(公告)日：2010-05-27

申请号：US12532773

申请日：2008-03-20

Applicant: Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

Inventor： Jeffrey Charles Boehm ,  Jakob Busch-Petersen ,  Wei Fu ,  Qi Jin ,  Jeffrey K. Kerns ,  Huijie Li ,  Guoliang Lin ,  Xichen Lin ,  Christopher E. Neipp

IPC: A61K31/405 ,  C07D209/04 ,  C07D409/14 ,  A61K31/55 ,  C07D403/02 ,  A61K31/497 ,  C07D413/02 ,  A61K31/535

CPC classification number: C07D409/04 ,  C07D409/14 ,  C07D417/14

Abstract: The invention is directed to novel indole carboxamide derivatives. 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.

Abstract translation: 本发明涉及新的吲哚甲酰胺衍生物。 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IKK＆bgr）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活性和与其相关的病症的治疗方法。

公开(公告)号：US20100093766A1

公开(公告)日：2010-04-15

申请号：US12618933

申请日：2009-11-16

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

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

IPC: A61K31/519 ,  C07D475/06 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.

公开(公告)号：US20100093765A1

公开(公告)日：2010-04-15

申请号：US12618927

申请日：2009-11-16

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

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

IPC: A61K31/519 ,  C07D475/06 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.

Abstract translation: 新型取代的1,5,7-三取代-3,4-二氢嘧啶并[4,5-d]嘧啶-2-（1H） - 酮化合物及其组合物及其在CSBP / RK / p38激酶抑制剂治疗中的用途 。

公开(公告)号：US20100010053A1

公开(公告)日：2010-01-14

申请号：US12486853

申请日：2009-06-18

Applicant: Jose Luis Castro Pineiro ,  Xichen Lin ,  Qian Liu ,  Kevin Meng ,  Feng Ren ,  David R. Vesey ,  Baowei Zhao

Inventor： Jose Luis Castro Pineiro ,  Xichen Lin ,  Qian Liu ,  Kevin Meng ,  Feng Ren ,  David R. Vesey ,  Baowei Zhao

IPC: A61K31/4245 ,  C07D271/06 ,  A61P37/06 ,  A61P29/00 ,  A61P35/00 ,  A61P1/00

CPC classification number: C07D413/04 ,  C07D413/14

Abstract: The present invention relates to novel oxadiazole derivatives 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型恶二唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种病症中的用途。

公开(公告)号：US08217028B2

公开(公告)日：2012-07-10

申请号：US12999091

申请日：2009-06-18

Applicant: Jose Luis Castro Pineiro ,  Xichen Lin ,  Qian Liu ,  Kevin Meng ,  Feng Ren ,  David R Vesey ,  Baowei Zhao

Inventor： Jose Luis Castro Pineiro ,  Xichen Lin ,  Qian Liu ,  Kevin Meng ,  Feng Ren ,  David R Vesey ,  Baowei Zhao

IPC: A61K31/4245 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4439 ,  A61P25/00 ,  C07D413/14 ,  C07D413/10

CPC classification number: C07D413/04 ,  C07D413/14

Abstract: The present invention relates to novel oxadiazole derivatives 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型恶二唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种病症中的用途。

公开(公告)号：US08207176B2

公开(公告)日：2012-06-26

申请号：US11908440

申请日：2006-03-24

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 ,  C07D409/06

CPC classification number: C07D487/04

Abstract: The present invention is directed to novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds, compositions, and use in therapy as CSBP/RK/p38 kinase inhibitors of Formulas (V) and (Va) wherein inter alia, G5 and G6 are nitrogen and CH, provided that only one of G5 or G6 is nitrogen and the other is CH; 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; R1′ is independently selected at each occurrence from halogen, C1-4 alkyl, halo-substituted-C1-4 alkyl, cyano, nitro, (CR10R20)v′NRdRd′, (CR10R20)v′C(O)R12, SR5, S(O)R5, S(O)2R5, or (CR10R20)v′OR13; Rb is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or heterocyclylC1-10 alkyl moiety, which moieties, excluding hydrogen, may all 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′)RhNH—C(═N—CN)NRqRq′; and R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted.

Abstract translation: 本发明涉及新型取代的2,4,8-三取代8H-吡啶并[2,3-d]嘧啶-7-酮，其含有化合物，组合物和用于治疗作为CSBP / RK / p38激酶抑制剂的式 V）和（Va）其中G5和G6特别是氮和CH，条件是G5或G6中只有一个是氮，另一个是CH; R1是C（Z）N（R10'）（CR10R20）vRb，C（Z）O（CR10R20）vRb，N（R10'）C（Z）（CR10R20）vRb，N（R10'）C（Z） （R10'）（CR10R20）vRb或N（R10'）OC（Z）（CR10R20）vRb; 卤素，C 1-4烷基，卤素取代的C 1-4烷基，氰基，硝基，（CR 10 R 20）v'NR d R d'，（CR 10 R 20）v'C（O）R 12，SR 5， S（O）R 5，S（O）2 R 5或（CR 10 R 20）v'OR 13; R b是氢，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，杂芳基C 1-10烷基，杂环基或杂环基C 1-10烷基部分， 可以任选地被取代; 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'）RhNH-C（= N-CN）NRqRq' 并且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，杂芳基C 1-10烷基，杂环基或杂环基C 1-10烷基部分， 这些部分可以任选被取代。