公开(公告)号：WO2005102989A1

公开(公告)日：2005-11-03

申请号：PCT/EP2005/004048

申请日：2005-04-15

Applicant: F. HOFFMANN-LA ROCHE AG ,  DUNN, James, Patrick ,  HIRSCHFELD, Donald, Roy ,  SILVA, Tania ,  VORA, Harit

Inventor： DUNN, James, Patrick ,  HIRSCHFELD, Donald, Roy ,  SILVA, Tania ,  VORA, Harit

IPC: C07C235/38

CPC classification number: C07C311/46 ,  C07C311/08 ,  C07C311/51 ,  C07C317/32 ,  C07C317/40 ,  C07C317/44 ,  C07C323/49 ,  C07C323/62 ,  C07C2601/14 ,  C07D207/325 ,  C07D213/75 ,  C07D213/82 ,  C07D213/84 ,  C07D295/108 ,  C07D295/13 ,  C07D295/135 ,  C07D295/26 ,  C07D307/79

Abstract: The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula (I) where Ar, R 1 -R 5 , R 11c and X 1 are as defined herein.

Abstract translation: 本发明提供了用于治疗或预防HIV感染或治疗AIDS或ARC的化合物，其包括给予式（I）化合物，其中Ar，R 1 -R 5，R 11c和X 1， 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：WO2006010545A1

公开(公告)日：2006-02-02

申请号：PCT/EP2005/007893

申请日：2005-07-20

Applicant: F. HOFFMANN-LA ROCHE AG ,  DUNN, James, Patrick ,  ELWORTHY, Todd, Richard ,  STEFANIDIS, Dimitrios ,  SWEENEY, Zachary, Kevin

Inventor： DUNN, James, Patrick ,  ELWORTHY, Todd, Richard ,  STEFANIDIS, Dimitrios ,  SWEENEY, Zachary, Kevin

IPC: C07D249/12

CPC classification number: C07D249/12

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 where R 1 , R 2 , R 3 , R 4 , R 5 , 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 公式其中R

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。

公开(公告)号：WO2004074257A1

公开(公告)日：2004-09-02

申请号：PCT/EP2004/001477

申请日：2004-02-17

Applicant: F. HOFFMANN-LA ROCHE AG ,  DUNN, James, Patrick ,  HOGG, Joan, Heather ,  MIRZADEGAN, Taraneh ,  SWALLOW, Steven

Inventor： DUNN, James, Patrick ,  HOGG, Joan, Heather ,  MIRZADEGAN, Taraneh ,  SWALLOW, Steven

IPC: C07D231/20

CPC classification number: C07D231/20 ,  C07D403/06 ,  C07D409/06

Abstract: This invention relates to novel pyrazole derivatives of formula (I) wherein R1 to R4 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibits or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula (I) and pharmaceutical compositions of formula (I) admixed with at least one solvent, carrier or excipient. The compounds are useful for treating disorders in which HIV and genetically related viruses are implicated (formula I).

Abstract translation: 本发明涉及式（I）的新型吡唑衍生物，其中R 1至R 4如概述中所定义及其药学上可接受的盐和溶剂合物，用式（I）化合物抑制或调节人类免疫缺陷病毒（HIV）逆转录酶的方法， 和式（I）的药物组合物与至少一种溶剂，载体或赋形剂混合。 该化合物可用于治疗涉及HIV和遗传相关病毒的疾病（式I）。

公开(公告)号：WO2004092144A2

公开(公告)日：2004-10-28

申请号：PCT/EP2004/003779

申请日：2004-04-08

Applicant: F. HOFFMANN-LA ROCHE AG ,  DUNN, James, Patrick ,  GOLDSTEIN, David, Michael ,  STAHL, Christoph, Martin ,  TREJO-MARTIN, Teresa Alejandra

Inventor： DUNN, James, Patrick ,  GOLDSTEIN, David, Michael ,  STAHL, Christoph, Martin ,  TREJO-MARTIN, Teresa Alejandra

IPC: C07D239/84

CPC classification number: C07D239/84 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention relates to compounds of formula (I), wherein R4, R5, R6, R7, Q, m and n are as defined in the specification. The compounds are useful as p38 kinase inhibitors, and therefore, may be used for treatment of p38-mediated disorder.

Abstract translation: 本发明涉及式（I）化合物，其中R4，R5，R6，R7，Q，m和n如说明书中所定义。 该化合物可用作p38激酶抑制剂，因此可用于治疗p38介导的病症。

公开(公告)号：WO2004092144A3

公开(公告)日：2005-03-24

申请号：PCT/EP2004003779

申请日：2004-04-08

Applicant: HOFFMANN LA ROCHE ,  DUNN JAMES PATRICK ,  GOLDSTEIN DAVID MICHAEL ,  STAHL CHRISTOPH MARTIN ,  TREJO-MARTIN TERESA ALEJANDRA

Inventor： DUNN JAMES PATRICK ,  GOLDSTEIN DAVID MICHAEL ,  STAHL CHRISTOPH MARTIN ,  TREJO-MARTIN TERESA ALEJANDRA

IPC: A61P19/02 ,  C07D239/84 ,  C07D401/12 ,  C07D405/12 ,  A61K31/517 ,  C07D403/12 ,  C07D407/12

CPC classification number: C07D239/84 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention relates to compounds of formula (I), wherein R4, R5, R6, R7, Q, m and n are as defined in the specification. The compounds are useful as p38 kinase inhibitors, and therefore, may be used for treatment of p38-mediated disorder.

Abstract translation: 本发明涉及式（I）化合物，其中R4，R5，R6，R7，Q，m和n如说明书中所定义。 该化合物可用作p38激酶抑制剂，因此可用于治疗p38介导的病症。