Orion Corporation

Juha Kaivola

Heimo O Haikala

Jouko Levijoki

Piero Pollesello

Jarmo J Pystynen

Martti Ovaska

Carola Tilgmann

Jukka Tenhunen

Petri Kaheinen

Pentti T Nore

Timo Lotta

Jukka Vidgren

Marjo Yliperttula-Ikonen

Kari L&ouml;nnberg

Arto J Karjalainen

Aino K Pippuri

Anne M Luiro

Eija Tiainen

Seppo Parhi

Reijo B&auml;ckstr&ouml;m

Ismo Ulmanen

This invention relates to determining the three-dimensional structure of the cytosolic domain of phospholamban (PLB) and its active site from NMR data of sufficiently high resolution for the three-dimensional structure determination. The invention also relates to methods for rational drug design enabling the design of phospholamban inhibitors based on using the three-dimensional structure data provided on computer readable media, as analyzed on a computer system having suitable computer algorithms. The invention also relates to phospholamban inhibiting compounds with certain structural, physicochemical and spatial characteristics that allow for the interaction of said compounds with specific residues of the active site of phospholamban.

Compounds for deactivating phospholamban function on Ca-ATPase (phospholamban inhibitors)

Pyridazinyl phenyl hydrazones useful against congestive heart failure

This invention relates to determining the three-dimensional structure of the cytosolic domain of phospholamban (PLB) and its active site from NMR data of sufficiently high resolution for the three-dimensional structure determination. The invention also relates to methods for rational drug design enabling the design of phospholamban inhibitors based on using the three-dimensional structure data provided on computer readable media, as analyzed on a computer system having suitable computer algorithms. The invention also relates to phospholamban inhibiting compounds with certain structural, phsicochemical and spatial characteristics that allow for the interaction of said compounds with specific residues of phospholamban.

Compounds for deactivating phospholamban function on Ca-ATPase (phopholamban inhibitors)

A method for obtaining direct dilatation of the coronary arteries by administering a therapeutically effective amount of a phospholamban inhibitor is described. Compounds which are effective in relieving the inhibitory effects of phospholamban on cardiac sarcoplasmic reticulum Ca,-ATPase are also described.

Phospholamban inhibitors and a method for increasing coronary flow

A method for the prevention and treatment of stunning of the heart subsequent to ischemia-reperfusion is described. The method comprises administering a therapeutically effective amount of a phospholamban inhibitor to a patient. Phospholamban inhibitors relieve the inhibitory effect of phospholamban on cardiac sarcoplasmic reticulum Ca.sup.2+ -ATPase.

Method for the prevention and treatment of stunned myocardium

A method for the treatment of neurohumoral imbalance caused by alterations of cardiac function to prevent the development of heart failure comprises administering an effective amount of (R)-�4-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)phenyl!acetamide to a mammal in need of such treatment.

Use of a pyridazinone derivative

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Helsinki, Finland

Juha Kaivola