公开(公告)号：JP2015091806A

公开(公告)日：2015-05-14

申请号：JP2014232987

申请日：2014-11-17

Applicant: PORTOLA PHARM INC

Inventor： ZHAOZHONG J JIA ,  CHANDRASEKAR VENKATARAMANI ,  WOLIN HUANG ,  MUKUND MEHROTRA ,  SONG YONGHONG ,  XU QING ,  SHAWN M BAUER ,  PANDEY ANJALI ,  BRIAN KANE ,  JACK W ROSE

IPC: C07D239/48 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P3/10 ,  A61P7/00 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: 【課題】sykキナーゼを阻害する化合物及びそれらの互変異性体又はそれらの薬学的に許容される塩、エステル及びプロドラッグの提供。【解決手段】sykキナーゼを阻害する化合物の製造における中間体、前記化合物の製剤、前記化合物を含む医薬組成物、sykキナーゼ活性の阻害方法、血小板凝集阻害の方法、及び、例えば望ましくない血栓症及び非ホジキンリンパ腫のような、少なくとも一部にsykキナーゼ活性化が関わっている多くの病態の予防又は治療方法。sykキナーゼを阻害する化合物の一例として、以下の構造で表される化合物が挙げられる。【選択図】なし

公开(公告)号：WO2006055951A2

公开(公告)日：2006-05-26

申请号：PCT/US2005042293

申请日：2005-11-21

Applicant: PORTOLA PHARM INC ,  SONG YONGHONG ,  ZHU BING-YAN ,  WANG SHUMEI ,  BAUER SHAWN ,  SCARBOROUGH ROBERT M

Inventor： SONG YONGHONG ,  ZHU BING-YAN ,  WANG SHUMEI ,  BAUER SHAWN ,  SCARBOROUGH ROBERT M

IPC: A61K31/4743

CPC classification number: C07D209/44 ,  C07D217/26 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D495/04

Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

Abstract translation: 本发明涉及由式I表示的化合物及其作为因子Xa抑制剂的药学上可接受的盐，溶剂合物，水合物和前药。 本发明还涉及用于制备这种化合物的中间体，含有这些化合物的药物组合物，预防或治疗多种不想要的血栓形成特征的病症的方法以及抑制血液样品凝固的方法。

公开(公告)号：WO2012061418A3

公开(公告)日：2012-08-02

申请号：PCT/US2011058826

申请日：2011-11-01

Applicant: PORTOLA PHARM INC ,  JIA ZHAOZHONG J ,  SONG YONGHONG ,  XU QING ,  KANE BRIAN ,  BAUER SHAWN M ,  PANDEY ANJALI

Inventor： JIA ZHAOZHONG J ,  SONG YONGHONG ,  XU QING ,  KANE BRIAN ,  BAUER SHAWN M ,  PANDEY ANJALI

IPC: C07D213/82 ,  A61K31/455 ,  A61P35/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D495/04

CPC classification number: C07C237/42 ,  C07C237/30 ,  C07C2601/14 ,  C07D209/08 ,  C07D209/40 ,  C07D213/74 ,  C07D213/82 ,  C07D231/12 ,  C07D231/38 ,  C07D233/56 ,  C07D239/48 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D261/14 ,  C07D275/03 ,  C07D277/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

Abstract translation: 本发明涉及作为Syk激酶抑制剂的式I化合物及其药学上可接受的盐，酯和前药。 本发明还涉及用于制备这类化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制Syk激酶活性的方法，抑制血小板聚集的方法以及预防或治疗一些 至少部分由Syk激酶活性介导的病症，如非霍奇金淋巴瘤。

公开(公告)号：EP2782580A4

公开(公告)日：2015-10-07

申请号：EP12851734

申请日：2012-11-23

Applicant: PORTOLA PHARM INC

Inventor： JIA ZHAOZHONG J ,  KANE BRIAN ,  XU QING ,  BAUER SHAWN M ,  SONG YONGHONG ,  PANDEY ANJALI ,  DICK RYAN

IPC: A61K31/506 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07H13/12

CPC classification number: C07H15/26 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07H13/12

公开(公告)号：WO2014058921A3

公开(公告)日：2014-10-23

申请号：PCT/US2013063942

申请日：2013-10-08

Applicant: PORTOLA PHARM INC

Inventor： BAUER SHAWN M ,  JIA ZHAOZHONG J ,  SONG YONGHONG ,  PANDEY ANJALI

IPC: C07D239/02 ,  C07D239/48

CPC classification number: C07D405/14 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

Abstract: Provided are substituted pyrimidinyl compounds for inhibition of JAK and/or Syk kinase, pharmaceutical compositions thereof, methods for inhibiting JAK and/or Syk kinase activity, and methods for treating conditions mediated at least in part by JAK and/or Syk kinase activity.

Abstract translation: 提供用于抑制JAK和/或Syk激酶的取代的嘧啶基化合物，其药物组合物，用于抑制JAK和/或Syk激酶活性的方法，以及用于治疗至少部分由JAK和/或Syk激酶活性介导的疾病的方法。

公开(公告)号：WO2012061428A3

公开(公告)日：2012-10-11

申请号：PCT/US2011058838

申请日：2011-11-01

Applicant: PORTOLA PHARM INC ,  BAUER SHAWN M ,  SONG YONGHONG ,  XU QING ,  ROSE JACK W ,  JIA ZHAOZHONG J ,  KANE BRIAN ,  HUANG WOLIN ,  PANDEY ANJALI ,  MEHROTRA MUKUND

Inventor： BAUER SHAWN M ,  SONG YONGHONG ,  XU QING ,  ROSE JACK W ,  JIA ZHAOZHONG J ,  KANE BRIAN ,  HUANG WOLIN ,  PANDEY ANJALI ,  MEHROTRA MUKUND

IPC: C07D213/82 ,  A61K31/455 ,  A61P35/00 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

CPC classification number: C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods ofinhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract translation: 本发明涉及作为JAK激酶抑制剂的式I化合物及其药学上可接受的盐，酯和前药。 本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗多种 至少部分由JAK激酶活性介导的病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

公开(公告)号：WO2009131687A3

公开(公告)日：2010-01-07

申请号：PCT/US2009002512

申请日：2009-04-22

Applicant: PORTOLA PHARM INC ,  SONG YONGHONG ,  XU QING ,  BAUER SHAWN M ,  JIA ZHAOZHONG J ,  MEHROTRA MUKUND ,  PANDEY ANJALI

Inventor： SONG YONGHONG ,  XU QING ,  BAUER SHAWN M ,  JIA ZHAOZHONG J ,  MEHROTRA MUKUND ,  PANDEY ANJALI

IPC: C07D239/48 ,  A61K31/506 ,  A61K31/52 ,  A61P9/00 ,  A61P29/00 ,  A61P35/00 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/04 ,  C07D473/16

CPC classification number: C07D471/04 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D473/16

Abstract: The present invention is directed to compounds of formula (I)-(II) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract translation: 本发明涉及作为syk和/或JAK激酶抑制剂的式（I） - （II）化合物及其药学上可接受的盐，酯和前药。 本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制性syk和/或JAK激酶活性的方法，抑制血小板聚集的方法以及预防方法 或治疗至少部分通过syk和/或JAK激酶活性介导的许多病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

公开(公告)号：WO2009136995A2

公开(公告)日：2009-11-12

申请号：PCT/US2009002401

申请日：2009-04-16

Applicant: PORTOLA PHARM INC ,  JIA ZHAOZHONG J ,  VENKATARAMANI CHANDRASEKAR ,  HUANG WOLIN ,  MEHROTRA MUKUND ,  SONG YONGHONG ,  XU QING ,  BAUER SHAWN M ,  PANDEY ANJALI

Inventor： JIA ZHAOZHONG J ,  VENKATARAMANI CHANDRASEKAR ,  HUANG WOLIN ,  MEHROTRA MUKUND ,  SONG YONGHONG ,  XU QING ,  BAUER SHAWN M ,  PANDEY ANJALI

IPC: C07D239/48 ,  A61K31/506 ,  A61P9/00 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention is directed to compounds of formula I-V and tattooers thereof or pharmaceutically acceptable salts, esters, and pro drugs thereof which are inhibitors of sky kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract translation: 本发明涉及作为天sky素抑制剂的式I-V化合物及其纹身或其药学上可接受的盐，酯和其前体药物。 本发明还涉及用于制备这种化合物的中间体，这种化合物的制备，含有这种化合物的药物组合物，抑制syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗数字的方法 至少部分通过syk激酶活性介导的病症，例如不期望的血栓形成和非霍奇金淋巴瘤。

公开(公告)号：WO2014051654A3

公开(公告)日：2014-05-22

申请号：PCT/US2013000225

申请日：2013-09-27

Applicant: PORTOLA PHARM INC

Inventor： PANDEY ANJALI ,  SONG YONGHONG ,  XU QING

IPC: A61K31/5365

CPC classification number: C07D498/04

Abstract: Provided are bicyclic oxa-lactam compounds for inhibition of JAK/Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting JAK/Syk kinase activity, and methods for treating conditions mediated at least in part by JAK/Syk kinase activity.

Abstract translation: 提供用于抑制JAK / Syk激酶的双环氧杂内酰胺化合物，用于制备此类化合物的中间体，其制备方法，其药物组合物，抑制JAK / Syk激酶活性的方法以及治疗至少部分 通过JAK / Syk激酶活性。

公开(公告)号：WO2013192049A3

公开(公告)日：2014-02-13

申请号：PCT/US2013046006

申请日：2013-06-14

Applicant: PORTOLA PHARM INC

Inventor： JIA ZHAOZHONG J ,  KANE BRIAN ,  ROSE JACK ,  BAUER SHAWN M ,  SONG YONGHONG ,  XU QING ,  PANDEY ANJALI

IPC: A01N43/64 ,  A01N43/707 ,  A61K31/53

CPC classification number: C07D253/075 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04

Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

Abstract translation: 提供用于抑制Syk激酶的三嗪化合物，用于制备这种化合物的中间体，其制备方法，其药物组合物，抑制Syk激酶活性的方法，以及至少部分地通过Syk激酶活性介导的病症的治疗方法。