公开(公告)号：AU2009244897A1

公开(公告)日：2009-11-12

申请号：AU2009244897

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

IPC: C07D239/48 ,  A61K31/506 ,  A61P9/00 ,  A61P35/00 ,  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 tautomers thereof or 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 undesired thrombosis and Non Hodgkin's Lymphoma.

公开(公告)号：CA2627719A1

公开(公告)日：2007-05-18

申请号：CA2627719

申请日：2006-11-03

Applicant: PORTOLA PHARM INC

Inventor： GRANT CRAIG M ,  ZHANG XIAOMING ,  CANNON HILARY ,  MEHROTRA MUKUND ,  HUANG WOLIN ,  SCARBOROUGH ROBERT 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：AU2001236644B2

公开(公告)日：2006-05-04

申请号：AU2001236644

申请日：2001-02-05

Applicant: PORTOLA PHARM INC

Inventor： JANTZEN HANS-MICHAEL ,  SEDLOCK DAVID M ,  HUANG WOLIN ,  SCARBOROUGH ROBERT M JR ,  MARLOWE CHARLES K

IPC: C07D239/48 ,  C07D417/12 ,  A61K31/381 ,  A61K31/4035 ,  A61K31/4365 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D239/22 ,  C07D239/50 ,  C07D333/34 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D495/04

Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives 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 relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.

公开(公告)号：DE60114994D1

公开(公告)日：2005-12-22

申请号：DE60114994

申请日：2001-02-05

Applicant: PORTOLA PHARM INC

Inventor： SCARBOROUGH M ,  JANTZEN HANS-MICHAEL ,  HUANG WOLIN ,  SEDLOCK M ,  MARLOWE K

IPC: C07D239/48 ,  A61K31/381 ,  A61K31/4035 ,  A61K31/4365 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D239/22 ,  C07D239/50 ,  C07D333/34 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D495/04 ,  C07D411/12 ,  C07D417/14 ,  A61K31/40 ,  A61K31/38 ,  A61K31/44 ,  A61K31/495 ,  A61K31/425 ,  A61K31/55

Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives 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 relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.

公开(公告)号：BRPI0910921B1

公开(公告)日：2022-06-21

申请号：BRPI0910921

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

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

Abstract: inibidores de proteína syk quinase, composição faramacêutica, kit e usos dos referidos inibidores. a presente invenção refere-se a compostos de fórmula i-v e tautômeros dos mesmos ou sais, ésteres, e profármacos farmaceuticamente aceitáveis dos mesmos que são inibidores de syk quinase. a presente invenção está também refere-se a intermediários usados na preparação de tais compostos, à preparação de um tal composto, composições farmacêuticas contendo um tal composto, métodos de inibição atividade de syk quinase, métodos de inibição de agregação de plaqueta, e métodos para prevenir ou tratar diversas condições mediadas pelo menos em parte pela atividade de syk quinase, tais como trombose indesejada e linfoma de não hodgkin.

公开(公告)号：ES2597441T3

公开(公告)日：2017-01-18

申请号：ES09755219

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

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

Abstract: Un compuesto que tiene la fórmula I:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que: D1 es cicloalquilo C3-8, opcionalmente sustituido con 1 a 4 sustituyentes seleccionados independientemente entre el grupo que consiste en: alquilo C1-8, amino, hidroxi, alquilcarbonilo C1-8, aminocarbonilo, alcoxicarbonilamino C1- 8, arilalcoxicarbonilamino C1-8, fenilo y heterociclil-alquileno C1-8; R1 se selecciona entre el grupo que consiste en H, alquilo C1-8, amino, aminocarbonilo, hidroxilo, alcoxi C1-8, haloalquilo C1-8, alquenilo C2-8, alquinilo C2-8, oxo, ciano, alcoxicarbonilo C1-8, cicloalquilo C3-8, arilo y heterociclilo; y cada heterociclilo está opcionalmente sustituido con 1 a 4 sustituyentes seleccionados entre el grupo que consiste en: alquilo C1-8, halo, oxo, amino, alcoxi C1-8, alquilcarbonilo C1-8, arilalcoxicarbonilo C1-8, aminocarbonilo, arilalquilenocarbonilo C1-8 y alquilsulfonilo C1-8; Y1 se selecciona entre el grupo que consiste en (a) arilo; opcionalmente sustituido con 1 a 3 sustituyentes, R4a, independientemente seleccionados entre el grupo que consiste en alquilo C1-8, alcoxi C1-8-alquilo C1-8, aminocarbonil-, hidroxilo, oxo, halógeno, hidroxi, alcoxi C1-8 y alquilsulfonilo C1-8; (b) heteroarilo, opcionalmente sustituido con 1 a 3 sustituyentes, R4a, independientemente seleccionados entre el grupo que consiste en alquilo C1-8, alcoxi C1-8-alquilo C1-8, aminocarbonil-, hidroxilo, oxo, halógeno, hidroxi, alcoxi C1-8 y alquilsulfonilo C1-8; R2 es un heterociclilo o heteroarilo sustituido con al menos un grupo, R3, seleccionado entre el grupo que consiste en aminoalquil C1-8-, alcoxi C1-8-alquil C1-8-, oxo-, alquilcarbonilo C1-8, cicloalquilcarbonilo C3-8, heterociclilcarbonilo, alquilcarbonilamino C1-8, cicloalquilcarbonilamino C3-8, heterociclilcarbonilamino, alquilsulfonilo C1-8, cicloalquilsulfonilo C3-8 y heterociclilsulfonilo; y en la que R2 está opcionalmente sustituido adicionalmente con 1 a 2 sustituyentes, R4c, independientemente seleccionados entre el grupo que consiste en alquilo C1-8, alcoxi C1-8, halo, aminocarbonilo, oxo, hidroxilo, aminoalquileno C1-8, alcoxi C1-8-alquileno C1-8, alquilcarbonilo C1-8, cicloalquilcarbonilo C3-8, heterociclilcarbonilo, alquilcarbonilamino C1-8, cicloalquilcarbonilamino C3-8, heterociclilcarbonilamino, alquilsulfonilo C1-8, cicloalquilsulfonilo C3-8, heterociclilsulfonilo, cicloalquilo C3-8, alquilcicloalquileno C1-8, heteroarilo; donde cicloalquilo se refiere a un grupo hidrocarburo mono o policíclico alquilo, alquenilo o alquinilo que puede formar un anillo puenteado o un anillo espiro, y que puede tener uno o más dobles o triples enlaces.

公开(公告)号：CY1112826T1

公开(公告)日：2016-02-10

申请号：CY121100393

申请日：2012-04-04

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

Abstract: Ηπαρούσαεφεύρεσηπαρέχεινέεςενώσειςσουλφονυλουρίαςτουτύπου (Ι) καιφαρμακευτικώςαποδεκτάπαράγωγακαιπολύμορφεςκαιάμορφεςμορφέςαυτών. ΟιενώσειςστιςδιάφορεςμορφέςτουςείναιαποτελεσματικοίαναστολείςυποδοχέαΑDΡαιμοπεταλίωνκαιμπορείναχρησιμοποιούνταισεδιάφορεςφαρμακευτικέςσυνθέσεις, καιείναιιδιαιτέρωςαποτελεσματικέςγιατηνπρόληψηή/καιθεραπευτικήαγωγήκαρδιαγγειακώνασθενειών, ιδιαιτέρωςεκείνωντωνασθενειώνπουσχετίζονταιμετηθρόμβωση. Ηεφεύρεσηπαρέχειεπίσηςμιαμέθοδογιατηνπαρασκευήτέτοιωνενώσεωνκαιμορφώνκαιγιατηνπρόληψηή θεραπευτικήαγωγήθρόμβωσηςκαισχετιζόμενωνμετηθρόμβωσηκαταστάσεωνσεέναθηλαστικό, ηοποίαπεριλαμβάνειτοστάδιοχορήγησηςμιαςθεραπευτικώςαποτελεσματικήςποσότηταςμιαςένωσηςτουτύπου (Ι) ήενόςφαρμακευτικώςαποδεκτούάλατοςή μορφέςαυτού.

公开(公告)号：PT2323993E

公开(公告)日：2015-10-12

申请号：PT09742982

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

公开(公告)号：BRPI0810800A2

公开(公告)日：2014-10-29

申请号：BRPI0810800

申请日：2008-05-02

Applicant: PORTOLA PHARM INC

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

IPC: C07D409/12 ,  A61K31/517

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.

公开(公告)号：AU2009251863B2

公开(公告)日：2014-09-25

申请号：AU2009251863

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

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.