公开(公告)号：WO2005032488A3

公开(公告)日：2005-05-12

申请号：PCT/US2004032921

申请日：2004-09-29

Applicant: PORTOLA PHARM INC ,  SCARBOROUGH ROBERT M ,  HUANG WOLIN ,  PANDEY ANJALI ,  BAUER SHAWN M ,  ZHANG XIAOMING ,  JIA ZHAOZHONG J

Inventor： SCARBOROUGH ROBERT M ,  HUANG WOLIN ,  PANDEY ANJALI ,  BAUER SHAWN M ,  ZHANG XIAOMING ,  JIA ZHAOZHONG J

IPC: A61K20060101 ,  A61K31/517 ,  A61P7/02 ,  C07D409/12 ,  C07D409/14

CPC classification number: C07D409/12 ,  C07D409/14

Abstract: 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.

Abstract translation: 提供了2,4-二氧代-3-喹唑啉基芳基磺酰脲化合物，其用于抑制ADP-血小板聚集，特别是在治疗血栓形成和血栓形成相关病症或病症中。

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：WO2008137809A3

公开(公告)日：2009-01-22

申请号：PCT/US2008062584

申请日：2008-05-02

Applicant: PORTOLA PHARM INC ,  SHARP EMMA ,  QUEGAN LOUISA JANE ,  PANDEY ANJALI ,  WANG JUAN ,  NIEDER MATTHEW ,  HUANG WOLIN

Inventor： SHARP EMMA ,  QUEGAN LOUISA JANE ,  PANDEY ANJALI ,  WANG JUAN ,  NIEDER MATTHEW ,  HUANG WOLIN

IPC: C07D409/12 ,  A61K31/517

CPC classification number: C07D409/12

Abstract: The present invention provides novel sulfonylurea salts of a salt of formula (I) and polymorph forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a salt of formula (I) or a pharmaceutically acceptable form thereof.

Abstract translation: 本发明提供式（I）的盐的新型磺酰脲盐及其多晶型形式。 各种形式的化合物是有效的血小板ADP受体抑制剂，可用于各种药物组合物中，并且特别有效预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病。 本发明还提供了一种制备此类化合物和形式并用于预防或治疗哺乳动物血栓形成和血栓形成相关病症的方法，包括施用治疗有效量的式（I）的盐或其药学上可接受的形式的步骤。

公开(公告)号：WO2007056219A3

公开(公告)日：2007-12-27

申请号：PCT/US2006043093

申请日：2006-11-03

Applicant: PORTOLA PHARM INC ,  SCARBOROUGH CARROLL ANNA CREW ,  HUANG WOLIN ,  MEHROTRA MUKUND ,  ZHANG XIAOMING ,  CANNON HILARY ,  GRANT CRAIG M

Inventor： HUANG WOLIN ,  MEHROTRA MUKUND ,  ZHANG XIAOMING ,  CANNON HILARY ,  GRANT CRAIG M ,  SCARBOROUGH ROBERT M

IPC: A61K31/5513 ,  A61K31/44 ,  C07D257/04

CPC classification number: C07D409/12

Abstract: The present invention provides novel sulfonylurea compounds of formula (I) and pharmaceutically acceptable derivatives and polymorph and amorphous forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or forms thereof.

Abstract translation: 本发明提供了式（I）的新型磺酰脲化合物及其药学上可接受的衍生物和多晶型物及其无定形形式。 各种形式的化合物是有效的血小板ADP受体抑制剂，并且可以用于各种药物组合物中，并且特别有效用于预防和/或治疗心血管疾病，特别是与血栓形成相关的疾病。 本发明还提供了用于制备这些化合物和形式以及用于预防或治疗哺乳动物的血栓形成和血栓形成相关病症的方法，其包括施用治疗有效量的式（I）化合物或其药学上可接受的盐或其形式 。

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：EP1951254A4

公开(公告)日：2009-05-27

申请号：EP06827506

申请日：2006-11-03

Applicant: PORTOLA PHARM INC

Inventor： HUANG WOLIN ,  MEHROTRA MUKUND ,  ZHANG XIAOMING ,  CANNON HILARY ,  GRANT CRAIG M ,  SCARBOROUGH ROBERT M

IPC: C07D409/12 ,  A61K31/517 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10

CPC classification number: C07D409/12

公开(公告)号：EP1668002A4

公开(公告)日：2006-12-20

申请号：EP04789522

申请日：2004-09-29

Applicant: PORTOLA PHARM INC

Inventor： SCARBOROUGH ROBERT M ,  HUANG WOLIN ,  PANDEY ANJALI ,  BAUER SHAWN M ,  ZHANG XIAOMING ,  JIA ZHAOZHONG J

IPC: C07D409/12 ,  A61K20060101 ,  A61K31/517 ,  A61P7/02 ,  C07D409/14

CPC classification number: C07D409/12 ,  C07D409/14

公开(公告)号：CA2960692C

公开(公告)日：2019-09-24

申请号：CA2960692

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

IPC: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12

Abstract: The present specification is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present specification is also directed to intermediates used in making such compounds, the preparation of such a compound, methods for inhibition of syk and/or JAK kinase activity, methods for inhibition of 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. The present specification is also directed to pharmaceutical compositions containing such a compound and which are formulated for topical administration.

公开(公告)号：CY1118559T1

公开(公告)日：2017-07-12

申请号：CY161101026

申请日：2016-10-13

Applicant: PORTOLA PHARM INC

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

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

Abstract: ΗπαρούσαεφεύρεσηαναφέρεταισεενώσειςτουτύπουΙ-ΙΙκαιταφαρμακευτικάαποδεκτάταυτομερή, άλατα, ήταστερεοϊσομερήαυτών, ταοποίαείναιαναστολείςτηςκινάσης Syk και/ή JAK. Ηπαρούσαεφεύρεσηεπίσηςαναφέρεταισεενδιάμεσαπουχρησιμοποιούνταιστηνσύνθεσητέτοιωνενώσεων, τηνπαρασκευήμίαςτέτοιαςένωσης, τιςφαρμακευτικέςσυνθέσειςπουπεριέχουνμίατέτοιαένωση, τιςμεθόδουςαναστολήςτηςδραστικότηταςτηςκινάσης Syk και/ή JAK, τιςμεθόδουςαναστολήςτηςσυσσωμάτωσηςτωναιμοπεταλίων, καιτιςμεθόδουςγιατηνπρόληψηή τηθεραπείαενόςαριθμούπαθήσεωνπουπροκαλούνταιτουλάχιστονενμέρειαπότηνδραστικότητατηςκινάσης Syk και/ή JAK, όπωςη καρδιαγγειακήνόσος, ηφλεγμονώδηςνόσος, ηαυτοάνοσηνόσοςκαιη πολλαπλασιαστικήδιαταραχήκυττάρων, ηθρόμβωση, ηαλλεργία, τοάσθμα, ηρευματοειδήςαρθρίτιδα, ηλευχαιμία, ήτολέμφωμαμη-Hodgkin.

公开(公告)号：CA2723205C

公开(公告)日：2017-03-14

申请号：CA2723205

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

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

Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers 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 cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder, thrombosis, allergy, asthma, rheumatoid arthritis, leukemia, or non-Hodgkin's lymphoma.