Portola Pharmaceuticals, Inc.

Millennium Pharmaceuticals Limited

Cor Therapeutics, Inc.

Hans-Michael Jantzen

Robert M Scarborough

Pamela B Conley

Wolin Huang

Charles K Marlowe

David M Sedlock

David J Julius

Kim A Kane-Maguire

Larry J Fretto

Alan M Laibelman

Kim A Kane-McGuire

Gunther Hollopeter

Vanitha Ramakrishnan-DuBridge

Novel compounds of formulae (I) and (VIII), 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) to (VIII), or a pharmaceutically acceptable salt thereof.

Platelet ADP receptor inhibitors

Novel compounds of formulae (I) to (VIII), 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) to (VIII), or a pharmaceutically acceptable salt thereof.

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.

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)&#x2013;(VI), or a pharmaceutically acceptable salt thereof.

The present invention includes a novel subtype of the P2-purinergic receptor, referred to as the P2Y receptor. This receptor is expressed selectively in the platelets and brain, and couples to a pertussis toxin-sensitive G protein (Gi). Nucleic acids encoding the receptor and associated screening and therapeutic methods are also disclosed.

Methods of identifying agents that modulate P2Y12 receptor activity

A novel subtype of the P -purinergic receptor, referred to as the P receptor, is disclosed. This receptor is activated by four of its agonists in the following order of specificity: UTP>UDP>ADP>ATP. Nucleic acids encoding the receptor, antibodies that bind to the receptor and associated screening and therapeutic methods also are disclosed.

P2U2 receptor antibodies

A novel subtype of the P.sub.2 -purinergic receptor, referred to as the P.sub.2U2 receptor, is disclosed. This receptor is activated by four of its agonists in the following order of specificity: UTP&gt;UDP&gt;ADP&gt;ATP. Nucleic acids encoding the receptor and associated screening and therapeutic methods also are disclosed.

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San Francisco, CA, United States of America

Hans-Michael Jantzen