公开(公告)号：WO2013041539A1

公开(公告)日：2013-03-28

申请号：PCT/EP2012/068380

申请日：2012-09-19

Applicant: F. HOFFMANN-LA ROCHE AG ,  LAI, Yingjie ,  LIANG, Jun ,  MAGNUSON, Steven, R. ,  ROBARGE, Kirk, D. ,  TSUI, Vickie, Hsaio-Wei ,  ZHANG, Birong

Inventor： LAI, Yingjie ,  LIANG, Jun ,  MAGNUSON, Steven, R. ,  ROBARGE, Kirk, D. ,  TSUI, Vickie, Hsaio-Wei ,  ZHANG, Birong

IPC: C07D471/04 ,  A61K31/437 ,  A61P29/00

CPC classification number: C07D471/04

Abstract: The invention provides TYK2 inhibitors of Formulas (la-lb), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R a , R 1 , R 2 , R 4 , R 5 and R 16 are defined herein, a pharmaceutical composition that includes a compound of Formulas (la-lb) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in the therapy of inflammatory diseases.

Abstract translation: 本发明提供式（Ia-1b）的TYK2抑制剂，其立体异构体或其药学上可接受的盐，其中A，X，Ra，R 1，R 2，R 4，R 5和R 16在本文中定义，药物组合物包括式 1a-1b）和药学上可接受的载体，佐剂或载体，以及在治疗炎性疾病中使用该化合物或组合物的方法。

公开(公告)号：WO2010142752A1

公开(公告)日：2010-12-16

申请号：PCT/EP2010/058128

申请日：2010-06-10

Applicant: F. HOFFMANN-LA ROCHE AG ,  GOODACRE, Simon Charles ,  LAI, Yingjie ,  LIANG, Jun ,  MAGNUSON, Steven R. ,  ROBARGE, Kirk D. ,  STANLEY, Mark S. ,  TSUI, Vickie Hsiao-Wei ,  WILLIAMS, Karen ,  ZHANG, Birong ,  ZHOU, Aihe

Inventor： GOODACRE, Simon Charles ,  LAI, Yingjie ,  LIANG, Jun ,  MAGNUSON, Steven R. ,  ROBARGE, Kirk D. ,  STANLEY, Mark S. ,  TSUI, Vickie Hsiao-Wei ,  WILLIAMS, Karen ,  ZHANG, Birong ,  ZHOU, Aihe

IPC: C07D213/75 ,  C07D401/12 ,  A61K31/506 ,  A61K31/495 ,  A61K31/4439 ,  A61K31/444 ,  A61P37/04

CPC classification number: C07D213/75 ,  C07D401/12

Abstract: The invention provides compounds of Formula (I), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R 1 , R 2 , R 4 and R 5 are defined herein, a pharmaceutical composition that includes a compound of Formula (I), methods of making those compounds as well as methods of use thereof

Abstract translation: 本发明提供式（I）化合物，其立体异构体或其药学上可接受的盐，其中A，B，D，R 1，R 2，R 4和R 5在本文中定义，药物组合物包含式（I）化合物， 使这些化合物及其使用方法

公开(公告)号：WO2009155551A1

公开(公告)日：2009-12-23

申请号：PCT/US2009/048017

申请日：2009-06-19

Applicant: GENENTECH, INC. ,  ZHU, Bing-Yan ,  SIU, Michael ,  MAGNUSON, Steven, R. ,  PASTOR, Richard ,  HAIYING, He ,  YISONG, Xiao ,  JIFU, Zheng ,  XING, Xu ,  JUNPING, Zhao

Inventor： ZHU, Bing-Yan ,  SIU, Michael ,  MAGNUSON, Steven, R. ,  PASTOR, Richard ,  HAIYING, He ,  YISONG, Xiao ,  JIFU, Zheng ,  XING, Xu ,  JUNPING, Zhao

IPC: A01N43/64 ,  A61K31/41

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

Abstract: A compound of Formula (I), enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula (I) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed. Formula (I).

Abstract translation: 式（I）的化合物，其对映体，非对映体，互变异构体或其药学上可接受的盐，其中R1，R2，R3，R4和R5如本文所定义，可用作JAK激酶抑制剂。 公开了包含式（I）化合物和药学上可接受的载体，佐剂或媒介物的药物组合物，以及治疗或减轻对患者中JAK激酶活性抑制作出反应的疾病或病症的严重性的方法。 式（I）。

公开(公告)号：WO2003027112A1

公开(公告)日：2003-04-03

申请号：PCT/US2002/030176

申请日：2002-09-23

Applicant: BAYER CORPORATION ,  WANG, Yamin ,  GUNN, David, E. ,  LIU, Qingjie ,  LIANG, Sidney, X. ,  BULLOCK, William, H. ,  LIU, Donglei ,  MAGNUSON, Steven, R. ,  LI, Tindy ,  MULL, Eric, S. ,  WOOD, Jill, E. ,  QI, Ning

Inventor： WANG, Yamin ,  GUNN, David, E. ,  LIU, Qingjie ,  LIANG, Sidney, X. ,  BULLOCK, William, H. ,  LIU, Donglei ,  MAGNUSON, Steven, R. ,  LI, Tindy ,  MULL, Eric, S. ,  WOOD, Jill, E. ,  QI, Ning

IPC: C07D471/04

CPC classification number: A61K45/06 ,  A61K31/44 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  C07D471/04 ,  A61K2300/00

Abstract: The invention relates generally to naphthyridine derivatives of the formula wherein one of U, X, Y and Z is nitrogen and the others are C-R, where R is hydrogen or a substituent. More specifically, the invention relates to 1,8-naphthyridine derivatives and pharmaceutical compositions containing such derivatives. Methods of the invention comprise administration of a naphthyridine derivative of the invention for the treatment of diabetes and related disorders.

Abstract translation: 本发明一般涉及下式的萘啶衍生物，其中U，X，Y和Z中的一个为氮，其余为C-R，其中R为氢或取代基。 更具体地，本发明涉及1,8-萘啶衍生物和含有这些衍生物的药物组合物。 本发明的方法包括施用本发明的萘啶衍生物用于治疗糖尿病和相关疾病。

公开(公告)号：WO2016055028A1

公开(公告)日：2016-04-14

申请号：PCT/CN2015/091614

申请日：2015-10-10

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC. ,  ROMERO, F. Anthony ,  MAGNUSON, Steven R. ,  PASTOR, Richard ,  TSUI, Vickie Hsiao-Wei ,  MURRAY, Jeremy ,  CRAWFORD, Terry ,  BURDICK, Daniel J. ,  ALBRECHT, Brian K. ,  COTE, Alexandre ,  TAYLOR, Alexander M. ,  NASVESCHUK, Christopher G. ,  LEBLANC, Yves ,  HEWITT, Michael Charles ,  LAI, Kwong Wah ,  CHEN, Kevin

Inventor： ROMERO, F. Anthony ,  MAGNUSON, Steven R. ,  PASTOR, Richard ,  TSUI, Vickie Hsiao-Wei ,  MURRAY, Jeremy ,  CRAWFORD, Terry ,  BURDICK, Daniel J. ,  ALBRECHT, Brian K. ,  COTE, Alexandre ,  TAYLOR, Alexander M. ,  NASVESCHUK, Christopher G. ,  LEBLANC, Yves ,  HEWITT, Michael Charles ,  LAI, Kwong Wah ,  CHEN, Kevin

IPC: C07D223/16 ,  C07D243/12 ,  C07D267/14 ,  C07D281/10 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  A61P29/00 ,  A61P37/00 ,  A61P35/00

CPC classification number: A61K31/55 ,  A61K31/337 ,  A61K31/5513 ,  A61K45/06 ,  C07D223/16 ,  C07D243/12 ,  C07D243/24 ,  C07D267/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/10 ,  C07D471/04 ,  C07D495/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

Abstract translation: 本发明涉及式（I）的化合物及其盐，其中A具有说明书中定义的任何值，以及其组成和用途。 该化合物可用作CBP和/或EP300的抑制剂。 还包括包含式（I）化合物或其药学上可接受的盐的药物组合物，以及在治疗各种CBP和/或EP300介导的病症中使用这些化合物和盐的方法。

公开(公告)号：WO2009155565A1

公开(公告)日：2009-12-23

申请号：PCT/US2009/048041

申请日：2009-06-19

Applicant: GENENTECH, INC. ,  ZHU, Bing-yan ,  SIU, Michael ,  MAGNUSON, Steven, R. ,  PASTOR, Richard ,  HAIYING, He ,  YISONG, Xiao ,  JIFU, Zheng ,  XING, Xu ,  JUNPING, Zhao ,  LIU, Wendy

Inventor： ZHU, Bing-yan ,  SIU, Michael ,  MAGNUSON, Steven, R. ,  PASTOR, Richard ,  HAIYING, He ,  YISONG, Xiao ,  JIFU, Zheng ,  XING, Xu ,  JUNPING, Zhao ,  LIU, Wendy

IPC: A01N43/64 ,  A61K31/41

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

Abstract translation: 其中R 1，R 2，R 3，R 4和R 5在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作JAK激酶抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及治疗或减轻对患者中JAK激酶活性的抑制作用的疾病或病症的严重程度的方法。

公开(公告)号：WO2013113669A1

公开(公告)日：2013-08-08

申请号：PCT/EP2013/051613

申请日：2013-01-29

Applicant: F. HOFFMANN-LA ROCHE AG ,  GENENTECH, INC ,  CHEN, Huifen ,  CRAWFORD, Terry ,  MAGNUSON, Steven, R. ,  NDUBAKU, Chudi ,  WANG, Lan

Inventor： CHEN, Huifen ,  CRAWFORD, Terry ,  MAGNUSON, Steven, R. ,  NDUBAKU, Chudi ,  WANG, Lan

IPC: C07D217/22 ,  C07D217/26 ,  C07D401/04 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/472 ,  A61K31/4725 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D217/22 ,  C07D217/26 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/12

Abstract: The invention provides novel compounds having the general formula (I) wherein A, R 1 and R 2 are as described herein, compositions including the compounds and use of the compounds for inhibiting angiogenesis by inhibition of MAP4K4.

Abstract translation: 本发明提供具有通式（I）的新化合物，其中A，R 1和R 2如本文所述，包括该化合物的组合物和通过抑制MAP4K4抑制血管生成的化合物的用途。

公开(公告)号：WO2011113802A2

公开(公告)日：2011-09-22

申请号：PCT/EP2011053826

申请日：2011-03-15

Applicant: HOFFMANN LA ROCHE ,  LAI YINGJIE ,  LIANG JUN ,  MAGNUSON STEVEN R ,  TSUI VICKIE H ,  ZHANG BIRONG ,  ROBARGE KIRK

Inventor： LAI YINGJIE ,  LIANG JUN ,  MAGNUSON STEVEN R ,  TSUI VICKIE H ,  ZHANG BIRONG ,  ROBARGE KIRK

IPC: A61K31/437 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P17/06 ,  A61P29/00 ,  C07D471/04 ,  C07D473/34 ,  C07D491/107

CPC classification number: C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D519/00

Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.

Abstract translation: 本发明提供式Ia-Ib的化合物，其立体异构体或其药学上可接受的盐，其中A，X，R 1，R 2，R 4，R 5和R 16如本文所定义，药物组合物包括式Ia-Ib的化合物和药学上可接受的盐 可接受的载体，佐剂或载体，以及在治疗中使用该化合物或组合物的方法。

公开(公告)号：WO2011003065A3

公开(公告)日：2011-05-19

申请号：PCT/US2010040906

申请日：2010-07-02

Applicant: GENENTECH INC ,  GIBBONS PAUL ,  HANAN EMILY ,  LIU WENDY ,  LYSSIKATOS JOSEPH P ,  MAGNUSON STEVEN R ,  MENDONCA ROHAN ,  PASTOR RICHARD ,  RAWSON THOMAS E ,  SIU MICHAEL ,  ZAK MARK E ,  ZHOU AIHE ,  ZHU BING-YAN

Inventor： GIBBONS PAUL ,  HANAN EMILY ,  LIU WENDY ,  LYSSIKATOS JOSEPH P ,  MAGNUSON STEVEN R ,  MENDONCA ROHAN ,  PASTOR RICHARD ,  RAWSON THOMAS E ,  SIU MICHAEL ,  ZAK MARK E ,  ZHOU AIHE ,  ZHU BING-YAN

IPC: C07D487/04 ,  A61K31/437 ,  A61P35/00 ,  C07D403/12

CPC classification number: C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

Abstract translation: 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。

公开(公告)号：WO2011113802A3

公开(公告)日：2011-09-22

申请号：PCT/EP2011/053826

申请日：2011-03-15

Applicant: F. HOFFMANN-LA ROCHE AG ,  LAI, Yingjie ,  LIANG, Jun ,  MAGNUSON, Steven R. ,  TSUI, Vickie H. ,  ZHANG, Birong ,  ROBARGE, Kirk

Inventor： LAI, Yingjie ,  LIANG, Jun ,  MAGNUSON, Steven R. ,  TSUI, Vickie H. ,  ZHANG, Birong ,  ROBARGE, Kirk

IPC: A61K31/437 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/541 ,  C07D471/04 ,  C07D473/34 ,  C07D491/107 ,  A61P1/00 ,  A61P17/06 ,  A61P29/00

Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R 1 , R 2 , R 4 , R 5 and R 16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy., as an inhibitor of TYK2 kinase and conditions related, such as inflammatory illenesses, inflammatory bowel disease or psoriasis.