公开(公告)号：WO2021130638A1

公开(公告)日：2021-07-01

申请号：PCT/IB2020/062229

申请日：2020-12-18

Applicant: CARNA BIOSCIENCES, INC. ,  GILEAD SCIENCES, INC.

Inventor： SAWA, Masaaki ,  ARAI, Mai ,  NAKAI, Ryoko ,  MATSUMOTO, Hirokazu ,  PUGH, Catherine ,  HU, Eric ,  GUERRERO, Juan ,  JACOBSEN, Jesse ,  MEDLEY, Jonathan William ,  XU, Jie ,  LAD, Latesh ,  PATEL, Leena ,  GRAUPE, Michael ,  ZHU, Qingming ,  HOLMBO, Stephen ,  KOBAYASHI, Tetsuya ,  WATKINS, Will ,  MOAZAMI, Yasamin ,  YEUNG, Suet C. ,  CODELLI, Julian A. ,  WEAVER, Heath A.

IPC: A61P31/12 ,  A61P31/14 ,  A61P31/16 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  A61K31/5415

Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

公开(公告)号：WO2004096236A2

公开(公告)日：2004-11-11

申请号：PCT/US2004/013143

申请日：2004-04-26

Applicant: GILEAD SCIENCES, INC. ,  CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  DESAI, Manoj ,  FARDIS, Maria ,  HUANG, Alan, X. ,  KIRSCHBERG, Thorsten, A. ,  LEE, Christopher, P. ,  MACKMAN, Richard, L. ,  NELSON, Peter, H. ,  PYUN, Hyung-Jung ,  RAY, Adrian, S. ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will ,  ZHANG, Jennifer, R.

Inventor： CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  DESAI, Manoj ,  FARDIS, Maria ,  HUANG, Alan, X. ,  KIRSCHBERG, Thorsten, A. ,  LEE, Christopher, P. ,  MACKMAN, Richard, L. ,  NELSON, Peter, H. ,  PYUN, Hyung-Jung ,  RAY, Adrian, S. ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will ,  ZHANG, Jennifer, R.

IPC: A61K31/662

CPC classification number: A61K31/662 ,  A61K47/548 ,  C07D205/04 ,  C07D211/58 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07D487/04 ,  C07F9/4075 ,  C07F9/5728 ,  C07F9/582 ,  C07F9/588 ,  C07F9/60 ,  C07F9/65037 ,  C07F9/650941 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655354 ,  C07F9/6561

Abstract: The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及具有免疫调节活性的膦酸酯取代的化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2005039552A2

公开(公告)日：2005-05-06

申请号：PCT/US2004/035136

申请日：2004-10-25

Applicant: GILEAD SCIENCES, INC. ,  CHO, Aesop ,  KIRSCHBERG, Thorsten, A. ,  WATKINS, Will ,  FARDIS, Maria ,  CHONG, Lee, S.

Inventor： CHO, Aesop ,  KIRSCHBERG, Thorsten, A. ,  WATKINS, Will ,  FARDIS, Maria ,  CHONG, Lee, S.

IPC: A61K31/00

CPC classification number: C07D307/88 ,  A61K47/548 ,  C07F9/65517 ,  C07F9/65586

Abstract: Phosphorus substituted mycophenolate derivatives with anti-cancer, anti-viral, anti-inflammatory and anti-tissue/organ transplant rejection properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit tumor growth, viral growth, inflammation, and tissue/organ transplant rejection and/or are useful therapeutically for the treatment or prevention of cancer, viral infection, inflammation and tissue/organ transplant rejection, as well as in assays for the detection of cancer, viral infection, inflammation and tissue/organ transplant rejection.

Abstract translation: 公开了具有用作治疗剂和用于其它工业目的的抗癌，抗病毒，抗炎和抗组织/器官移植排斥特性的磷取代霉酚酸衍生物。 组合物抑制肿瘤生长，病毒生长，炎症和组织/器官移植排斥和/或治疗用于治疗或预防癌症，病毒感染，炎症和组织/器官移植排斥以及用于检测的检测 癌症，病毒感染，炎症和组织/器官移植排斥。

公开(公告)号：WO2004096287A2

公开(公告)日：2004-11-11

申请号：PCT/US2004/013064

申请日：2004-04-26

Applicant: GILEAD SCIENCES, INC. ,  CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  KIRSCHBERG, Thorsten, A. ,  PYUN, Hyung-Jung ,  WATKINS, Will ,  ZHANG, Jennifer, R.

Inventor： CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  KIRSCHBERG, Thorsten, A. ,  PYUN, Hyung-Jung ,  WATKINS, Will ,  ZHANG, Jennifer, R.

IPC: A61K47/48

CPC classification number: C07F9/4075 ,  A61K31/662 ,  A61K47/548 ,  C07D205/04 ,  C07D211/58 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07F9/5728 ,  C07F9/582 ,  C07F9/588 ,  C07F9/60 ,  C07F9/65037 ,  C07F9/650941 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655354 ,  C07F9/6561

Abstract: The invention is related to phosphorus substituted IMPDH inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及磷取代的IMPDH抑制化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2004096234A2

公开(公告)日：2004-11-11

申请号：PCT/US2004/013062

申请日：2004-04-26

Applicant: GILEAD SCIENCES, INC. ,  CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  DESAI, Manoj ,  FARDIS, Maria ,  KIRSCHBERG, Thorsten, A. ,  MACKMAN, Richard, L. ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will

Inventor： CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  DESAI, Manoj ,  FARDIS, Maria ,  KIRSCHBERG, Thorsten, A. ,  MACKMAN, Richard, L. ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will

IPC: A61K31/662

CPC classification number: A61K31/662 ,  A61K47/54 ,  A61K47/548 ,  C07F9/588 ,  C07F9/6561

Abstract: The invention is related to phosphorus substituted kinase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及磷取代的激酶抑制化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2004100960A2

公开(公告)日：2004-11-25

申请号：PCT/US2004/013198

申请日：2004-04-26

Applicant: GILEAD SCIENCES, INC. ,  CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  GIBBS, Craig ,  HIRSCHMANN, Ralph, F. ,  KIRSCHBERG, Thorsten, A. ,  LEE, Christopher, P. ,  LIN, Kuei-Ying ,  MACKMAN, Richard, L. ,  NELSON, Peter, H. ,  OARE, David ,  PYUN, Hyung-Jung ,  RAY, Adrian, S. ,  SHERLOCK, Rosemarie ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will ,  ZHANG, Jennifer, R.

Inventor： CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  GIBBS, Craig ,  HIRSCHMANN, Ralph, F. ,  KIRSCHBERG, Thorsten, A. ,  LEE, Christopher, P. ,  LIN, Kuei-Ying ,  MACKMAN, Richard, L. ,  NELSON, Peter, H. ,  OARE, David ,  PYUN, Hyung-Jung ,  RAY, Adrian, S. ,  SHERLOCK, Rosemarie ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will ,  ZHANG, Jennifer, R.

IPC: A61K31/662

CPC classification number: A61K31/662 ,  A61K47/548 ,  C07D205/04 ,  C07D211/58 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07D487/04 ,  C07F9/4075 ,  C07F9/5728 ,  C07F9/582 ,  C07F9/588 ,  C07F9/60 ,  C07F9/65037 ,  C07F9/650941 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655354 ,  C07F9/6561 ,  C07F9/65616

Abstract: The invention is related to phosphorus substituted anti-inflammatory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及磷取代的抗炎化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2004096286A2

公开(公告)日：2004-11-11

申请号：PCT/US2004/013063

申请日：2004-04-26

Applicant: GILEAD SCIENCES, INC. ,  BOOJAMARA, Constantine, G. ,  CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  JIN, Haolun ,  HIRSCHMANN, Ralph, F. ,  HUANG, Alan, X. ,  KIM, Choung, U. ,  KIRSCHBERG, Thorsten, A. ,  LEE, Christopher, P. ,  LEE, William, A. ,  MACKMAN, Richard, L. ,  MARKEVITCH, David, Y. ,  OARE, David ,  PRASAD, Vidya, K. ,  PYUN, Hyung-Jung ,  RAY, Adrian, S. ,  SHERLOCK, Rosemarie ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will ,  ZHANG, Jennifer, R.

Inventor： BOOJAMARA, Constantine, G. ,  CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  JIN, Haolun ,  HIRSCHMANN, Ralph, F. ,  HUANG, Alan, X. ,  KIM, Choung, U. ,  KIRSCHBERG, Thorsten, A. ,  LEE, Christopher, P. ,  LEE, William, A. ,  MACKMAN, Richard, L. ,  MARKEVITCH, David, Y. ,  OARE, David ,  PRASAD, Vidya, K. ,  PYUN, Hyung-Jung ,  RAY, Adrian, S. ,  SHERLOCK, Rosemarie ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will ,  ZHANG, Jennifer, R.

IPC: A61K47/48

CPC classification number: C07F9/65616 ,  A61K31/662 ,  A61K31/7072 ,  A61K31/7076 ,  A61K47/548 ,  C07D205/04 ,  C07D211/58 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07F9/4075 ,  C07F9/5728 ,  C07F9/582 ,  C07F9/588 ,  C07F9/60 ,  C07F9/65037 ,  C07F9/650941 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655354 ,  C07F9/6561 ,  C07H15/00 ,  C07H17/00 ,  C07H19/056 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  Y02A50/393 ,  Y02A50/465

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及具有抗病毒活性的磷取代的化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2004096237A2

公开(公告)日：2004-11-11

申请号：PCT/US2004/013146

申请日：2004-04-26

Applicant: GILEAD SCIENCES, INC. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  KIRSCHBERG, Thorsten, A. ,  KRAWCZYK, Steven ,  PYUN, Hyung-Jung ,  WATKINS, Will

Inventor： CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  KIRSCHBERG, Thorsten, A. ,  KRAWCZYK, Steven ,  PYUN, Hyung-Jung ,  WATKINS, Will

IPC: A61K31/662

CPC classification number: A61K31/662 ,  A61K47/548

Abstract: The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及具有用于治疗代谢疾病和/或病症（例如糖尿病和高胆固醇血症）的活性的磷取代的化合物，以及含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于 制备此类化合物。

公开(公告)号：WO2004096235A2

公开(公告)日：2004-11-11

申请号：PCT/US2004/013121

申请日：2004-04-26

Applicant: GILEAD SCIENCES, INC. ,  BOOJAMARA, Constantine, G. ,  CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  HUANG, Alan, X. ,  KIM, Choung, X. ,  KIRSCHBERG, Thorsten, A. ,  KRAWCZYK, Steven ,  LEE, Christopher, P. ,  LIN, Kuei-Ying ,  MACKMAN, Richard, L. ,  MARKEVITCH, David, Y. ,  NELSON, Peter, H. ,  OARE, David ,  PRASAD, Vidya, K. ,  PYUN, Hyung-Jung ,  RAY, Adrian, S. ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will ,  ZHANG, Lijun

Inventor： BOOJAMARA, Constantine, G. ,  CANNIZZARO, Carina, E. ,  CHEN, James, M. ,  CHEN, Xiaowu ,  CHO, Aesop ,  CHONG, Lee, S. ,  FARDIS, Maria ,  HUANG, Alan, X. ,  KIM, Choung, X. ,  KIRSCHBERG, Thorsten, A. ,  KRAWCZYK, Steven ,  LEE, Christopher, P. ,  LIN, Kuei-Ying ,  MACKMAN, Richard, L. ,  MARKEVITCH, David, Y. ,  NELSON, Peter, H. ,  OARE, David ,  PRASAD, Vidya, K. ,  PYUN, Hyung-Jung ,  RAY, Adrian, S. ,  SWAMINATHAN, Sundaramoorthi ,  WATKINS, Will ,  ZHANG, Lijun

IPC: A61K31/662

CPC classification number: A61K31/662 ,  A61K47/548 ,  C07D205/04 ,  C07D211/58 ,  C07D239/94 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07D487/04 ,  C07F9/4075 ,  C07F9/5728 ,  C07F9/582 ,  C07F9/588 ,  C07F9/60 ,  C07F9/65037 ,  C07F9/650941 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655354 ,  C07F9/6561

Abstract: The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及磷取代的抗癌化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2005063258A1

公开(公告)日：2005-07-14

申请号：PCT/US2004/043595

申请日：2004-12-22

Applicant: GILEAD SCIENCES, INC. ,  WATKINS, Will

Inventor： WATKINS, Will

IPC: A61K31/662

CPC classification number: C07F9/6561 ,  A61K47/548

Abstract: The invention is related to phosphorus substituted kinase inhibitory compounds and conjugates, compositions containing such compounds and conjugates, and therapeutic methods that include the administration of such compounds and conjugates, as well as to processes and intermediates useful for preparing such compounds and conjugates.

Abstract translation: 本发明涉及磷取代的激酶抑制化合物和缀合物，含有这些化合物和缀合物的组合物，以及包括施用这些化合物和缀合物的治疗方法以及可用于制备这些化合物和缀合物的方法和中间体。