公开(公告)号：AU2013205326A1

公开(公告)日：2013-05-09

申请号：AU2013205326

申请日：2013-04-11

Applicant: PORTOLA PHARM INC

Inventor： LU GENMIN ,  PHILLIPS DAVID R ,  ANDRE PATRICK ,  SINHA UMA

IPC: A61P7/02 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/715 ,  A61K31/727 ,  A61K38/36 ,  A61K38/48 ,  A61K39/00 ,  A61K39/395 ,  A61K47/48 ,  A61P7/04 ,  C07H21/00 ,  C07K14/00 ,  C07K16/00 ,  C12N5/10 ,  C12N9/64 ,  C12P21/00

Abstract: The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or 5 have reduced intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.

公开(公告)号：AU2011323484A1

公开(公告)日：2013-05-09

申请号：AU2011323484

申请日：2011-11-01

Applicant: PORTOLA PHARM INC

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

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.

公开(公告)号：AU2011295909A1

公开(公告)日：2013-04-04

申请号：AU2011295909

申请日：2011-08-31

Applicant: PORTOLA PHARM INC

Inventor： CAPODANNO VINCENT R ,  CORCORAN LIAM ,  MCNEVIN MICHAEL ,  ARROYO ITZIA ZORAIDA ,  WENSLOW ROBERT M ,  BALL RICHARD G ,  MARGELEFSKY ERIC L ,  MAHER TIMOTHY K ,  PANDEY ANJALI

IPC: C07D213/75 ,  A61K31/44 ,  A61P7/02

Abstract: Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof.

公开(公告)号：NZ589315A

公开(公告)日：2012-11-30

申请号：NZ58931509

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

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

Abstract: The present disclosure is directed to 2,6-diamino-pyrimidin-5-yl-carboxamide derivatives of formula (I) and tautomers thereof or pharmaceutically acceptable salts thereof which are inhibitors of Spleen tryosine kinase (syk) or Janus kinase (JAK). The disclosure 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 or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions such as undesired thrombosis and Non Hodgkin's Lymphoma which are mediated at least in part by syk kinase or JAK kinase activity. These compounds are used in the preparation of a medicament for inhibiting syk or JAK kinase or a signal transduction pathway mediated at least in part by syk kinase activity, wherein the medicament is suitable for treating a condition or disorder selected from the group consisting of cardiovascular disease, inflammatory disease and autoimmune disease and cell proliferative disorder.

公开(公告)号：HK1158179A1

公开(公告)日：2012-07-13

申请号：HK11112350

申请日：2011-11-16

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: C07D20060101 ,  A61K20060101 ,  A61P20060101

公开(公告)号：BRPI0618210A2

公开(公告)日：2011-08-23

申请号：BRPI0618210

申请日：2006-11-03

Applicant: PORTOLA PHARM INC

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

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

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.

公开(公告)号：IL201885D0

公开(公告)日：2011-08-01

申请号：IL20188509

申请日：2009-11-02

Applicant: PORTOLA PHARM INC

IPC: C12N20060101

Abstract: The present invention provides new methods of treating thrombosis and cardiovascular diseases using of antithrombotic agents, as well as methods of determining therapeutically effective amounts of antithrombotic agents and unit dose formulations thereof.

公开(公告)号：MX2011004907A

公开(公告)日：2011-07-29

申请号：MX2011004907

申请日：2009-11-11

Applicant: PORTOLA PHARM INC

Inventor： LU GENMIN ,  SINHA UMA

IPC: A61K38/48 ,  A61K35/14 ,  A61K35/16 ,  A61K38/16 ,  A61P7/04

Abstract: La presente invención se refiere a los antídotos de los anticoagulantes dirigidos contra el factor Xa los cuales son usados en combinación con agentes de coagulación de sangre u otros antídotos tipo heparina para prevenir o reducir el sangrado en un sujeto. Los antídotos aquí descritos tienen o no reducida su actividad anticoagulante intrínseca. Aquí se manifiestan métodos para detener o prevenir el sangrado en un paciente que es o será sometido a terapia de anticoagulantes con un inhibidor del factor Xa.

公开(公告)号：MA32442B1

公开(公告)日：2011-07-03

申请号：MA33302

申请日：2010-11-01

Applicant: PORTOLA PHARM INC

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

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

Abstract: L'invention concerne des composés représentés par les formules i-v et des tautomères de ceux-ci, ou des sels pharmaceutiquement acceptables, des esters et des promédicaments de ceux-ci qui constituent des inhibiteurs de la syk kinase. L'invention concerne aussi des produits intermédiaires utilisés dans la fabrication de tels composés, la préparation d'un tel composé, des compositions pharmaceutiques contenant un tel composé, des procédés d'inhibition de l'activité de la syk kinase, des procédés d'inhibition de l'agrégation plaquettaire et des procédés destinés à prévenir ou à traiter des états pathologiques dus au moins en partie à l'activité de la syk kinase, tels qu'une thrombose indésirable et un lymphome malin non hodgkinien.

公开(公告)号：AU2009313867A1

公开(公告)日：2011-06-30

申请号：AU2009313867

申请日：2009-11-13

Applicant: PATHEON INC ,  PORTOLA PHARM INC

Inventor： CHANDIR RAMANI ,  JUAN WANG ,  ANIL KANE ,  KWOK CHOW ,  JOE LAMBING

IPC: A61K9/20 ,  A61K31/19 ,  A61K31/192 ,  A61K31/405 ,  A61K31/517 ,  A61P7/02 ,  A61P9/00

Abstract: A novel solid composition and methods for making and using the solid composition are provided. The solid composition comprises: (a) at least one active agent with a solubility of less than about 0.3 mg/ml in an aqueous solution with a pH of at most about 6.8 at a temperature of about 37C; and (b) a hydrophilic polymer matrix composition comprising: i) a hydrophilic polymer selected from the group consisting of METHOCELTM, POLYOX WSR 1105 and combinations thereof; and optionally ii) a hydrophobic polymer selected from the group consisting of Ethocel 20 premium; and (c) an alkalizer selected from the group consisting of calcium carbonate, magnesium oxide heavy and sodium bicarbonate; wherein the composition provides at least about 70% release of the active between about 7 to about 12 hours following oral administration.