Millennium Pharmaceuticals Limited

Portola Pharmaceuticals, Inc.

Kim A Kane-Maguire

Robert M Scarborough

Charles K Marlowe

Bing-Yan Zhu

Wolin Huang

Penglie Zhang

Ting Su

Xiaoming Zhang

Yonghong Song

Zhaozhong Jon Jia

Mark Stephen Smyth

Hans-Michael Jantzen

David M Sedlock

Daniel E Levy

Lane Clizbe

Willy Teng

Brandon Doughan

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

Isoquinolinone 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.

Substituted isoquinolinones

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.

The present invention relates to derivatives and analogues of adenine of the formula:wherein L, A, Y and Z are those defined herein. Compounds of the present invention are useful in inhibiting adenylyl cyclase activity. The present invention also relates to a method of preventing and inhibiting a patient's fibroproliferative vasculopathy following vascular injury or a vascular surgical operation which includes administering to the patient, an effective amount of a compound according to the invention subsequent to a vascular injury, or subsequent to a vascular surgical operation, for one to two weeks after the injury or surgical operation, effective to treat or prevent a patient's fibroproliferative vasculopathy such as chronic allograft rejection or vascular restenosis following vascular trauma. The present invention also relates to a method for measuring the inhibition of adenylyl cyclase activity and a method for treating congestive heart failure.

Adenine based inhibitors of adenylyl cyclase, pharmaceutical compositions, and method of use thereof

Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Inhibitors of factor Xa

Oxindole inhibitors of factor Xa

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Belmont, CA, United States of America

Kim A Kane-Maguire