公开(公告)号：CA2876945A1

公开(公告)日：2013-12-27

申请号：CA2876945

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 ,  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.

公开(公告)号：MX315135B

公开(公告)日：2013-11-07

申请号：MX2012011444

申请日：2010-10-15

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

公开(公告)号：ZA201007046B

公开(公告)日：2013-09-25

申请号：ZA201007046

申请日：2010-10-04

Applicant: PORTOLA PHARM INC

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

IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101

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：CA2856301A1

公开(公告)日：2013-05-30

申请号：CA2856301

申请日：2012-11-23

Applicant: PORTOLA PHARM INC

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

IPC: C07D403/12 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/506 ,  C07D239/48 ,  C07D401/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D495/04

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

公开(公告)号：NZ588830A

公开(公告)日：2012-11-30

申请号：NZ58883009

申请日：2009-04-22

Applicant: PORTOLA PHARM INC

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

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

Abstract: Disclosed are compounds of formula (Ia) and pharmaceutically acceptable salts, thereof which are inhibitors of syk and/or JAK kinase. Examples of compounds of formula(I) are: N-(4-(4-(5-aminopentylamino)-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)phenyl)-N-methylacetamide; N-(4-(4-(5-aminopentylamino)-5,6-dibromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)phenyl)-N-methylacetamide and 4-(4-(cyclopropylamino)-5-(pyridin-4-yl)-7Hpyrrolo[2,3-d]pyrimidin-2-ylamino)benzamide Also disclosed are pharmaceutical compositions and kits of parts containing such a compound, the use of the compound in the manufacture of a medicament for inhibiting syk and/or JAK kinase activity and platelet aggregation, and medicaments 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.

公开(公告)号：NZ589314A

公开(公告)日：2012-10-26

申请号：NZ58931409

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

Inventor： BAUER SHAWN M ,  JIA ZHAOZHONG J

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

Abstract: The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of Spleen tyrosine kinase (syk) and/or Janus (JAK) kinases. Also disclosed are 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. These compounds are suitable for treating 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.

公开(公告)号：AU2009251863A2

公开(公告)日：2011-06-09

申请号：AU2009251863

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

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.

公开(公告)号：AU2004278030C1

公开(公告)日：2010-12-02

申请号：AU2004278030

申请日：2004-09-29

Applicant: PORTOLA PHARM INC

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

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

Abstract: 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C 1-6 alkyl; R 1 is a member selected from the group consisting of H, C 1-6 alkyl, C 1-6 haloalkyl, C 3-5 cycloalkyl and C 3-5 cycloalkyl-alkyl; R 2 is a member selected from the group consisting of H, halogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 1-6 alkoxy, cyano and -C(O)R 2a , wherein R 2a is a member selected from the group consisting of C 1-6 alkoxy and (C 1-6 alkyl) 0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of -CH 2 -, -CH(CH 3 )-, -CH 2 CH 2 -, -CH 2 CH(CH 3 )- and -CH 2 CH 2 CH 2 -; L 1 is a linking group selected from the group consisting of a bond and -CH 2 -; L 2 is a linking group selected from the group consisting of a bond, -NH- and -CH 2 -; and Ar 1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided. The compounds are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.

公开(公告)号：AU2009251863A1

公开(公告)日：2009-12-03

申请号：AU2009251863

申请日：2009-04-16

Applicant: PORTOLA PHARM INC

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

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.

公开(公告)号：AU2004278030A1

公开(公告)日：2005-04-14

申请号：AU2004278030

申请日：2004-09-29

Applicant: PORTOLA PHARM INC

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

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

Abstract: 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C 1-6 alkyl; R 1 is a member selected from the group consisting of H, C 1-6 alkyl, C 1-6 haloalkyl, C 3-5 cycloalkyl and C 3-5 cycloalkyl-alkyl; R 2 is a member selected from the group consisting of H, halogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 1-6 alkoxy, cyano and -C(O)R 2a , wherein R 2a is a member selected from the group consisting of C 1-6 alkoxy and (C 1-6 alkyl) 0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of -CH 2 -, -CH(CH 3 )-, -CH 2 CH 2 -, -CH 2 CH(CH 3 )- and -CH 2 CH 2 CH 2 -; L 1 is a linking group selected from the group consisting of a bond and -CH 2 -; L 2 is a linking group selected from the group consisting of a bond, -NH- and -CH 2 -; and Ar 1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided. The compounds are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.