公开(公告)号：WO2011073269A1

公开(公告)日：2011-06-23

申请号：PCT/EP2010/069787

申请日：2010-12-15

Applicant: EVOTEC AG ,  GREENHOUSE, Robert ,  HOGG, Joan Heather ,  LIN, Xiao-Fa ,  O'YANG, Counde ,  RAPTOVA, Lubica ,  TREJO-MARTIN, Teresa Alejandra

Inventor： GREENHOUSE, Robert ,  HOGG, Joan Heather ,  LIN, Xiao-Fa ,  O'YANG, Counde ,  RAPTOVA, Lubica ,  TREJO-MARTIN, Teresa Alejandra

IPC: C07D211/96 ,  C07D401/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  A61K31/451 ,  A61K31/4523 ,  A61P11/00 ,  A61P19/02 ,  A61P37/00

CPC classification number: C07D211/96 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

Abstract: Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with potassium channel modulation.

Abstract translation: 式（I）化合物或其药学上可接受的盐，其中m，R 1，R 2，R 3，R 4和R 5如本文所定义。 还公开了制备化合物和使用该化合物治疗与钾通道调节相关的疾病的方法。

公开(公告)号：WO2011073277A1

公开(公告)日：2011-06-23

申请号：PCT/EP2010/069801

申请日：2010-12-15

Applicant: EVOTEC AG ,  GREENHOUSE, Robert ,  HOGG, Joan Heather ,  LIN, Xiao-Fa ,  O'YANG, Counde ,  RAPTOVA, Lubica ,  TREJO-MARTIN, Teresa Alejandra

Inventor： GREENHOUSE, Robert ,  HOGG, Joan Heather ,  LIN, Xiao-Fa ,  O'YANG, Counde ,  RAPTOVA, Lubica ,  TREJO-MARTIN, Teresa Alejandra

IPC: C07D211/96 ,  C07D401/06 ,  C07D401/14 ,  C07D407/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/10 ,  A61K31/451 ,  A61K31/4523 ,  A61P11/00 ,  A61P19/02 ,  A61P37/00

CPC classification number: C07D401/06 ,  C07D211/96 ,  C07D401/14 ,  C07D405/12 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107

Abstract: Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein m, n, p, X, R 1 , R 2 , R 3 , R 4 R 5 and R 6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with potassium channel modulation.

Abstract translation: 式（I）化合物或其药学上可接受的盐，其中m，n，p，X，R 1，R 2，R 3，R 4 R 5和R 6如本文所定义。 还公开了制备化合物和使用该化合物治疗与钾通道调节相关的疾病的方法。

公开(公告)号：WO2009000663A1

公开(公告)日：2008-12-31

申请号：PCT/EP2008/057391

申请日：2008-06-12

Applicant: F. HOFFMANN-LA ROCHE AG ,  ELWORTHY, Todd Richard ,  HOGG, Joan Heather ,  KENNEDY-SMITH, Joshua ,  O YANG, Counde ,  SMITH, Mark ,  SWEENEY, Zachary Kevin ,  WU, Jeffrey

Inventor： ELWORTHY, Todd Richard ,  HOGG, Joan Heather ,  KENNEDY-SMITH, Joshua ,  O YANG, Counde ,  SMITH, Mark ,  SWEENEY, Zachary Kevin ,  WU, Jeffrey

IPC: C07D235/26 ,  C07D471/04 ,  C07D487/04 ,  C07C255/54 ,  A61K31/4166 ,  A61P31/18

CPC classification number: C07D235/26 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of formula (I), wherein R 1 , R 2 , R 3 , X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula (I) useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.

Abstract translation: 其中R 1，R 2，R 3，X和Ar如本文所定义的式（I）化合物或其药学上可接受的盐抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染的方法 和治疗艾滋病和/或ARC。 本发明还涉及含有用于预防和治疗HIV-1感染和治疗AIDS和/或ARC的式（I）化合物的组合物。

公开(公告)号：WO2011073276A1

公开(公告)日：2011-06-23

申请号：PCT/EP2010/069798

申请日：2010-12-15

Applicant: EVOTEC AG ,  HAN, Xiaochun ,  HAWLEY, Ronald Charles ,  HOGG, Joan Heather ,  LIN, Xiao-Fa ,  TREJO-MARTIN, Teresa Alejandra

Inventor： HAN, Xiaochun ,  HAWLEY, Ronald Charles ,  HOGG, Joan Heather ,  LIN, Xiao-Fa ,  TREJO-MARTIN, Teresa Alejandra

IPC: C07D265/36 ,  A61K31/538 ,  A61P11/00 ,  C07D498/04

CPC classification number: C07D265/36 ,  C07D498/04

Abstract: Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein E, Z, m, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with potassium channel modulation.

Abstract translation: 式（I）化合物或其药学上可接受的盐，其中E，Z，m，R 1，R 2，R 3，R 4和R 5如本文所定义。 还公开了制备化合物和使用该化合物治疗与钾通道调节相关的疾病的方法。

公开(公告)号：WO2011073273A1

公开(公告)日：2011-06-23

申请号：PCT/EP2010/069793

申请日：2010-12-15

Applicant: EVOTEC AG ,  HAN, Xiaochun ,  HAWLEY, Ronald Charles ,  HOGG, Joan Heather ,  LIN, Xiao-Fa ,  TREJO-MARTIN, Teresa Alejandra

Inventor： HAN, Xiaochun ,  HAWLEY, Ronald Charles ,  HOGG, Joan Heather ,  LIN, Xiao-Fa ,  TREJO-MARTIN, Teresa Alejandra

IPC: C07D265/36 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D498/04 ,  A61K31/538 ,  A61K31/5383 ,  A61P11/00

CPC classification number: C07D413/14 ,  C07D265/36 ,  C07D413/04 ,  C07D417/04 ,  C07D498/04

Abstract: Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, n, p, E, X, R 1 , R 2 , R 3 , R 4 R 5 and R 6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with potassium channel modulation.

Abstract translation: 式（I）化合物或其药学上可接受的盐，其中m，n，p，E，X，R 1，R 2，R 3，R 4 R 5和R 6如本文所定义。 还公开了制备化合物和使用该化合物治疗与钾通道调节相关的疾病的方法。

公开(公告)号：WO2008138920A1

公开(公告)日：2008-11-20

申请号：PCT/EP2008/055807

申请日：2008-05-13

Applicant: F. HOFFMANN-LA ROCHE AG ,  ABBOT, Sarah C. ,  BOICE, Genevieve N. ,  BUETTELMANN, Bernd ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HOGG, Joan Heather ,  IYER, Pravin ,  MCCALEB, Kristen Lynn ,  TAN, Yun-chou

Inventor： ABBOT, Sarah C. ,  BOICE, Genevieve N. ,  BUETTELMANN, Bernd ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HOGG, Joan Heather ,  IYER, Pravin ,  MCCALEB, Kristen Lynn ,  TAN, Yun-chou

IPC: C07D215/48 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04 ,  C07F7/18 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/47 ,  A61P37/00 ,  A61P29/00 ,  A61P3/00 ,  A61P25/00

CPC classification number: C07D215/48 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04

Abstract: Compounds of formula I or a pharmaceutically acceptable salt thereof are effective modulators of JNK: (formula) wherein X, Y, Z, R 4 , R 5 , R 6 and R 7 are as defined herein.

Abstract translation: 式I化合物或其药学上可接受的盐是JNK的有效调节剂：（式）其中X，Y，Z，R 4，R 5，R 5， 6和R 7和R 7如本文所定义。

公开(公告)号：WO2009138340A1

公开(公告)日：2009-11-19

申请号：PCT/EP2009/055443

申请日：2009-05-06

Applicant: F. HOFFMANN-LA ROCHE AG ,  ARZENO, Humberto Bartolome ,  DUNN, James Patrick ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HAN, Xiaochun ,  HOGG, Joan Heather ,  JAHANGIR, Alam ,  PALMER, Wylie Solang ,  REUTER, Deborah Carol ,  SILVA, Tania ,  TIVITMAHAISOON, Parcharee ,  TREJO-MARTIN, Teresa Alejandra ,  WU, Shao-Yong

Inventor： ARZENO, Humberto Bartolome ,  DUNN, James Patrick ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HAN, Xiaochun ,  HOGG, Joan Heather ,  JAHANGIR, Alam ,  PALMER, Wylie Solang ,  REUTER, Deborah Carol ,  SILVA, Tania ,  TIVITMAHAISOON, Parcharee ,  TREJO-MARTIN, Teresa Alejandra ,  WU, Shao-Yong

IPC: C07D401/14 ,  A61K31/506 ,  A61P29/00

CPC classification number: C07D401/14

Abstract: The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula (I), wherein m, n, p, q, Q, r, R 1 , R 2 , R 3 , X, X 1 , X 2 , X 3 , X 4 , X 5 , Y 1 , Y 2 , Z 1 , and Z 2 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

Abstract translation: 本发明涉及JNK抑制剂的前药以及用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。 本申请公开了如下式（I）所述的JNK抑制剂的前药，其中m，n，p，q，Q，r，R1，R2，R3，X，X1，X2，X3，X4，X5， Y2，Z1和Z2如本文所定义。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。

公开(公告)号：WO2008068171A9

公开(公告)日：2008-06-12

申请号：PCT/EP2007/062920

申请日：2007-11-28

Applicant: F. HOFFMANN-LA ROCHE AG ,  DUNN, James Patrick ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HOGG, Joan Heather ,  MICHOUD, Christophe ,  PALMER, Wylie Solang ,  SIDDURI, Achyutharao ,  SILVA, Tania ,  TIVITMAHAISOON, Parcharee ,  TREJO-MARTIN, Teresa Alejandra

Inventor： DUNN, James Patrick ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HOGG, Joan Heather ,  MICHOUD, Christophe ,  PALMER, Wylie Solang ,  SIDDURI, Achyutharao ,  SILVA, Tania ,  TIVITMAHAISOON, Parcharee ,  TREJO-MARTIN, Teresa Alejandra

IPC: C07D403/04 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4178 ,  A61K31/506 ,  A61P29/00 ,  A61P35/00 ,  A61P25/00

Abstract: The invention is concerned with novel JNK modulator of formula (I) wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , R, R 1 , Z and n are as defined in the description and the claims, as well as physiologically acceptable salts thereof.

公开(公告)号：WO2008068171A1

公开(公告)日：2008-06-12

申请号：PCT/EP2007062920

申请日：2007-11-28

Applicant: HOFFMANN LA ROCHE ,  DUNN JAMES PATRICK ,  GOLDSTEIN DAVID MICHAEL ,  GONG LEYI ,  HOGG JOAN HEATHER ,  MICHOUD CHRISTOPHE ,  PALMER WYLIE SOLANG ,  SIDDURI ACHYUTHARAO ,  SILVA TANIA ,  TIVITMAHAISOON PARCHAREE ,  TREJO-MARTIN TERESA ALEJANDRA

Inventor： DUNN JAMES PATRICK ,  GOLDSTEIN DAVID MICHAEL ,  GONG LEYI ,  HOGG JOAN HEATHER ,  MICHOUD CHRISTOPHE ,  PALMER WYLIE SOLANG ,  SIDDURI ACHYUTHARAO ,  SILVA TANIA ,  TIVITMAHAISOON PARCHAREE ,  TREJO-MARTIN TERESA ALEJANDRA

IPC: C07D403/04 ,  A61K31/4178 ,  A61K31/506 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D403/04 ,  C07D471/04 ,  C07D487/04

Abstract: The invention is concerned with novel JNK modulator of formula (I) wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , R, R 1 , Z and n are as defined in the description and the claims, as well as physiologically acceptable salts thereof.

Abstract translation: 本发明涉及式（I）的新型JNK调节剂，其中X 1，X 2，X 3，X 4， / SUP>，X 5，X 6，R 1，R 1，Z和n如说明书和权利要求中所定义，如 以及其生理上可接受的盐。

公开(公告)号：WO2005090317A1

公开(公告)日：2005-09-29

申请号：PCT/EP2005/002779

申请日：2005-03-16

Applicant: F.HOFFMANN-LA ROCHE AG ,  DUNN, James, Patrick ,  ELWORTHY, Todd, Richard ,  HOGG, Joan, Heather ,  STEFANIDIS, Dimitrios

Inventor： DUNN, James, Patrick ,  ELWORTHY, Todd, Richard ,  HOGG, Joan, Heather ,  STEFANIDIS, Dimitrios

IPC: C07D237/14

CPC classification number: C07D237/14 ,  Y10S514/85

Abstract: The present invention relates to a compounds according to formula (I), methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula (I) and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula (I) where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein.

Abstract translation: 本发明涉及式（I）化合物，通过给予根据式（I）的化合物治疗由人免疫缺陷病毒介导的疾病的方法和用于治疗由含有根据本发明的化合物的化合物的人类免疫缺陷病毒介导的疾病的药物组合物 式（I）其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义。