公开(公告)号：WO2016103155A1

公开(公告)日：2016-06-30

申请号：PCT/IB2015/059843

申请日：2015-12-21

Applicant: NOVARTIS AG ,  CHAN, Ho Man ,  GU, Xiang-Ju Justin ,  HUANG, Ying ,  LI, Ling ,  MI, Yuan ,  QI, Wei ,  SENDZIK, Martin ,  SUN, Yongfeng ,  WANG, Long ,  YU, Zhengtian ,  ZHANG, Hailong ,  ZHANG, Ji Yue (jeff) ,  ZHANG, Man ,  ZHANG, Qiong ,  ZHAO, Kehao

Inventor： CHAN, Ho Man ,  GU, Xiang-Ju Justin ,  HUANG, Ying ,  LI, Ling ,  MI, Yuan ,  QI, Wei ,  SENDZIK, Martin ,  SUN, Yongfeng ,  WANG, Long ,  YU, Zhengtian ,  ZHANG, Hailong ,  ZHANG, Ji Yue (jeff) ,  ZHANG, Man ,  ZHANG, Qiong ,  ZHAO, Kehao

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D487/04

Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R 1 , R 2 , R 3 , R 4 , R 5 , and n are as defined herein.

Abstract translation: 提供式（I）化合物或其药学上可接受的盐，其已被证明可用于治疗PRC2介导的疾病或病症：其中R1，R2，R3，R4，R5和n如所定义 于此。

公开(公告)号：WO2013038362A1

公开(公告)日：2013-03-21

申请号：PCT/IB2012/054775

申请日：2012-09-13

Applicant: NOVARTIS AG ,  CHEN, Chao ,  DENG, Haibing ,  GUO, Haibing ,  HE, Feng ,  JIANG, Lei ,  LIANG, Fang ,  MI, Yuan ,  WAN, Huixin ,  XU, Yao-Chang ,  YU, Hongping ,  ZHANG, Ji Yue (Jeff)

Inventor： CHEN, Chao ,  DENG, Haibing ,  GUO, Haibing ,  HE, Feng ,  JIANG, Lei ,  LIANG, Fang ,  MI, Yuan ,  WAN, Huixin ,  XU, Yao-Chang ,  YU, Hongping ,  ZHANG, Ji Yue (Jeff)

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/437 ,  A61P35/00 ,  A61P29/00

CPC classification number: A61K31/551 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5513 ,  A61K45/06 ,  C07D471/04 ,  C07D491/107 ,  C07D519/00

Abstract: The invention relates to compounds of formula (I) and salts thereof: Formula (I) wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).

Abstract translation: 本发明涉及式（I）化合物及其盐：式（I）其中取代基如说明书中所定义; 用于治疗人或动物体的式（I）化合物，特别是关于c-Met酪氨酸激酶介导的疾病或病症; 使用式（I）化合物制备用于治疗这些疾病的药物; 包含式（I）化合物，任选在组合配偶体存在下的药物组合物，以及制备式（I）化合物的方法。

公开(公告)号：WO2006052936A3

公开(公告)日：2006-05-18

申请号：PCT/US2005/040372

申请日：2005-11-07

Applicant: IRM LLC ,  WAN, Yongqin ,  MI, Yuan ,  FAN, Yi ,  CHENG, Dai ,  LIU, Yi ,  GRAY, Nathanael, Schiander ,  ALBAUGH, Pamela, A.

Inventor： WAN, Yongqin ,  MI, Yuan ,  FAN, Yi ,  CHENG, Dai ,  LIU, Yi ,  GRAY, Nathanael, Schiander ,  ALBAUGH, Pamela, A.

IPC: A61K31/4178 ,  C07D403/14

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC , Raf, ROCK-II, Rsk1, SGK, TrkA, TrkB and TrkC kinases.

公开(公告)号：WO2004113330A8

公开(公告)日：2006-03-30

申请号：PCT/US2004015699

申请日：2004-05-19

Applicant: IRM LLC ,  PAN SHIFENG ,  GRAY NATHANAEL S ,  MI YUAN ,  FAN YI ,  GAO WENQI

Inventor： PAN SHIFENG ,  GRAY NATHANAEL S ,  MI YUAN ,  FAN YI ,  GAO WENQI

IPC: A61K31/4725 ,  C07D217/16 ,  C07D217/24 ,  C07D413/04 ,  C07D413/10 ,  C07D498/04

CPC classification number: C07D413/04 ,  C07D217/16 ,  C07D217/24

Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

Abstract translation: 本发明涉及免疫抑制剂，其生产方法及其用途和含有它们的药物组合物。 本发明提供了一类新颖的化合物，其可用于治疗或预防由淋巴细胞相互作用介导的疾病或病症，特别是与EDG受体介导的信号转导相关的疾病。

公开(公告)号：WO2005082089A2

公开(公告)日：2005-09-09

申请号：PCT/US2005/006311

申请日：2005-02-24

Applicant: IRM LLC ,  LU, Wenshou ,  PAN, Shifeng ,  MARSILJE, Thomas, H. ,  GAO, Wenqi ,  GRAY, Nathanael, Schiander ,  HE, Yun ,  LIU, Yahua ,  MI, Yuan ,  XIE, Yongping

Inventor： LU, Wenshou ,  PAN, Shifeng ,  MARSILJE, Thomas, H. ,  GAO, Wenqi ,  GRAY, Nathanael, Schiander ,  HE, Yun ,  LIU, Yahua ,  MI, Yuan ,  XIE, Yongping

CPC classification number: C07D401/04 ,  C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D211/22 ,  C07D213/74 ,  C07D237/22 ,  C07D239/46 ,  C07D295/108 ,  C07D295/15 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/10 ,  C07D417/10

Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

公开(公告)号：WO03099192A8

公开(公告)日：2005-02-17

申请号：PCT/EP0305510

申请日：2003-05-26

Applicant: NOVARTIS AG ,  NOVARTIS PHARMA GMBH ,  IRM LLC ,  FAN YI ,  GAO WENQI ,  GRAY NATHANAEL S ,  HINTERDING KLAUS ,  LEFEBVRE SOPHIE ,  MI YUAN ,  NUSSBAUMER PETER ,  PAN SHIFENG ,  WANG WEI ,  ZECRI FREDERIC ,  PEREZ LAWRENCE BLAS ,  LA MONTAGNE KENNETH RICHARD ,  ETTMAYER PETER

Inventor： FAN YI ,  GAO WENQI ,  GRAY NATHANAEL S ,  HINTERDING KLAUS ,  LEFEBVRE SOPHIE ,  MI YUAN ,  NUSSBAUMER PETER ,  PAN SHIFENG ,  WANG WEI ,  ZECRI FREDERIC ,  PEREZ LAWRENCE BLAS ,  LA MONTAGNE KENNETH RICHARD ,  ETTMAYER PETER

IPC: A61K31/137 ,  A61K31/15 ,  A61K31/18 ,  A61K31/277 ,  A61K31/36 ,  A61K31/381 ,  A61K31/42 ,  A61K31/423 ,  A61K31/661 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P5/14 ,  A61P7/00 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P17/08 ,  A61P17/14 ,  A61P19/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  A61P37/06 ,  C07C215/28 ,  C07C215/32 ,  C07C215/46 ,  C07C215/68 ,  C07C217/48 ,  C07C217/54 ,  C07C237/30 ,  C07C251/40 ,  C07C251/48 ,  C07C255/13 ,  C07C255/32 ,  C07C255/43 ,  C07C255/58 ,  C07C255/59 ,  C07C271/22 ,  C07C309/66 ,  C07C311/08 ,  C07C311/13 ,  C07D261/04 ,  C07D261/08 ,  C07D263/56 ,  C07D263/57 ,  C07D317/58 ,  C07D333/20 ,  C07F9/09 ,  A61K31/133

CPC classification number: C07D263/57 ,  C07C215/28 ,  C07C215/46 ,  C07C217/54 ,  C07C237/30 ,  C07C251/48 ,  C07C255/13 ,  C07C255/43 ,  C07C255/58 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07D261/08 ,  C07D317/58 ,  C07D333/20 ,  C07F9/094

Abstract: The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract translation: 本发明涉及联苯衍生物，其制备方法及其用途和含有它们的药物组合物。

公开(公告)号：WO2004071442A3

公开(公告)日：2004-10-28

申请号：PCT/US2004004006

申请日：2004-02-11

Applicant: IRM LLC ,  PAN SHIFENG ,  GRAY NATHANAEL ,  MI YUAN ,  GAO WENQI ,  FAN YI ,  LEFEBVRE SOPHIE

Inventor： PAN SHIFENG ,  GRAY NATHANAEL ,  MI YUAN ,  GAO WENQI ,  FAN YI ,  LEFEBVRE SOPHIE

IPC: A61K20060101 ,  A61K31/15 ,  A61K31/18 ,  A61K31/277 ,  A61K31/42 ,  A61K31/421 ,  A61K31/537 ,  C07C251/48 ,  C07C251/52 ,  C07C251/54 ,  C07D213/30 ,  C07D261/02 ,  C07D263/30 ,  C07D307/42 ,  C07D333/16 ,  C07F9/09 ,  C07F9/6553

CPC classification number: C07D213/30 ,  C07C251/48 ,  C07C251/52 ,  C07C251/54 ,  C07D307/42 ,  C07D333/16 ,  C07F9/094 ,  C07F9/655345

Abstract: The present invention relates to bicyclic derivatives, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG/S1P receptor mediated signal transduction.

Abstract translation: 本发明涉及双环衍生物，其制备方法，其用途和含有它们的药物组合物。 本发明提供了一类新型化合物，用于治疗或预防由淋巴细胞相互作用介导的疾病或病症，特别是与EDG / S1P受体介导的信号转导相关的疾病。

公开(公告)号：WO2003099192A2

公开(公告)日：2003-12-04

申请号：PCT/EP2003/005510

申请日：2003-05-26

Applicant: NOVARTIS AG ,  NOVARTIS Pharma GmbH ,  IRM LLC ,  FAN, Ying ,  GAO, Wenqi ,  GRAY, Nathanael, S. ,  HINTERDING, Klaus ,  LEFEBVRE, Sophie ,  MI, Yuan ,  NUSSBAUMER, Peter ,  PAN, Shifeng ,  WANG, Wei ,  ZECRI, Frédéric ,  PEREZ, Lawrence, Blas ,  LA MONTAGNE, Kenneth, Richard ,  ETTMAYER, Peter

Inventor： FAN, Ying ,  GAO, Wenqi ,  GRAY, Nathanael, S. ,  HINTERDING, Klaus ,  LEFEBVRE, Sophie ,  MI, Yuan ,  NUSSBAUMER, Peter ,  PAN, Shifeng ,  WANG, Wei ,  ZECRI, Frédéric ,  PEREZ, Lawrence, Blas ,  LA MONTAGNE, Kenneth, Richard ,  ETTMAYER, Peter

IPC: A61K

CPC classification number: C07D263/57 ,  C07C215/28 ,  C07C215/46 ,  C07C217/54 ,  C07C237/30 ,  C07C251/48 ,  C07C255/13 ,  C07C255/43 ,  C07C255/58 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07D261/08 ,  C07D317/58 ,  C07D333/20 ,  C07F9/094

Abstract: The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract translation: 本发明涉及联苯衍生物，其制备方法及其用途和含有它们的药物组合物。

公开(公告)号：WO2011018454A1

公开(公告)日：2011-02-17

申请号：PCT/EP2010/061609

申请日：2010-08-10

Applicant: NOVARTIS AG ,  FU, Xingnian ,  HE, Feng ,  LI, Yue ,  LIU, Lei ,  MI, Yuan ,  XU, Yao-chang ,  XUN, Guoliang ,  YU, Zhengtian ,  ZHANG, Ji Yue (Jeff) ,  DAI, Miao

Inventor： FU, Xingnian ,  HE, Feng ,  LI, Yue ,  LIU, Lei ,  MI, Yuan ,  XU, Yao-chang ,  XUN, Guoliang ,  YU, Zhengtian ,  ZHANG, Ji Yue (Jeff) ,  DAI, Miao

IPC: C07D487/04 ,  A61K31/4985 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D487/04

Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).

Abstract translation: 本发明涉及式（I）的化合物及其盐：其中取代基如说明书中所定义; 用于治疗人或动物体的式（I）化合物，特别是关于c-Met酪氨酸激酶介导的疾病或病症; 使用式（I）化合物制备用于治疗这些疾病的药物; 包含式（I）化合物，任选在组合配偶体存在下的药物组合物，以及制备式（I）化合物的方法。

公开(公告)号：WO2008073480A1

公开(公告)日：2008-06-19

申请号：PCT/US2007/025447

申请日：2007-12-11

Applicant: IRM LLC ,  MI, Yuan ,  ALBAUGH, Pamela ,  FAN, Yi ,  CHOI, Ha-Soon ,  LIU, Zuosheng ,  HUANG, Shenlin

Inventor： MI, Yuan ,  ALBAUGH, Pamela ,  FAN, Yi ,  CHOI, Ha-Soon ,  LIU, Zuosheng ,  HUANG, Shenlin

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/404 ,  A61P35/00

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly TrkA, TrkB, TrkC, PDGFR and c-kit.

Abstract translation: 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是TrkA，TrkB，TrkC，PDGFR和c-kit。