Orion-yhtyma Oy

Orion Corporation

Orion Corporation/orion Pharmaceutica

Jarmo J Pystynen

Erkki J Honkanen

Aino K Pippuri

Anne M Luiro

Reijo J Backstrom

Heimo O Haikala

Pentti Pohto

Erkki A Nissinen

Inge-Britt Y Linden

Pentti T Nore

Kalevi E Heinola

Pekka J Kairisalo

Martti Ovaska

Seppo K Kaakkola

Jouko Levijoki

Eija Tiainen

Juha Kaivola

Timo Lotta

Pekka I Mannisto

Kari K Lonnberg

Petri Kaheinen

Jukka Vidgren

Paivi A Aho

Reijo Bäckström

Kari L&ouml;nnberg

Marko Ahlmark

Arto J Karjalainen

David Din Belle

Anssi Haikarainen

Piero Pollesello

Seppo Parhi

Carola Tilgmann

Matti Vaismaa

Reijo B&auml;ckstr&ouml;m

Jukka Tenhunen

Marjo Yliperttula-Ikonen

Antti Pohjakallio

Irma O Ojala

Tord K Langenskiold

Josef Messinger

Taina Pajunen

Mika Kauppala

Lawrence Sellin

Pekka T Mannisto

Esa Kumpulainen

Shouming Wang

Ismo Ulmanen

Jyrki Taskinen

Compounds of formula I, wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2, or 3 N, O, or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.

2-(1-heteroarylpiperazin-4-yl)methyl-1,4-benzodioxane derivatives as alpha2C antagonists

Compounds of formula (I), wherein Ris as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

Catechol O-methyltransferase activity inhibiting compounds

Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. 

Pharmaceutical compounds

Compounds of formula I'wherein the two &#x2014;OH substituents in the phenyl moiety are in a position ortho to one another and Rin a position ortho to one of the hydroxy groups; and X, Rto Rare as defined in disclosure. The compounds exhibit COMT enzyme inhibiting activity, so are useful as COMT inhibitors.

Coumarin derivatives with COMT inhibiting activity

Compounds of formula (I'), wherein A, Rto Rand t are as defined in the disclosure, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.

Derivatives of naphthalene with COMT inhibiting activity

Pyridazinyl phenyl hydrazones useful against congestive heart failure

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

Catechol derivatives

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 compound according to formula 1 ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, carbamoyl which is substituted by an alkyl of 1 to 4 carbon atoms, alkylcarbonyl of 2 to 5 carbon atoms or phenyl carbonyl, X represents halogen nitro or cyano and R.sub.3 represents ##STR2## wherein R.sub.4 represents cyano or alkylcarbonyl of 2 to 5 carbon atoms and R.sub.5 represents carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms or which is substituted with hydroxyalkyl of 1 to 8 carbon atoms or pharmaceutically acceptable esters and salts thereof, and a pharmaceutically acceptable carrier therefor, as well as pharmaceutical compositions containing said compounds as COMT inhibitors.

Pharmacologically active catechol derivatives

Compound of formula ##STR1## wherein n is 0 or 1, R.sub.1 and R.sub.2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.

Substituted .beta.-diketones and their use

Catechol compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3 and X are as described herein are effective Catechol-O-methyltransferase inhibitors.

Pharmacologically active compounds, methods for the preparation thereof

New heterocyclic compounds of formula I ##STR1## In which Het means one of following groups; ##STR2## wherein R.sub.11, R.sub.13 and R.sub.14 mean independently hydrogen, hydroxymethyl or lower alkyl group, Z means S, O or NH; A means valency bond, --CH.dbd.CH--, or --CH.sub.2 --CH.sub.2 --group; R.sub.1 and R.sub.2 independently mean nitro, cyano, halogen, amino, carboxamido, aryl, aroyl, pyridyl, alkoxycarbonyl, acyl or one of following groups; ##STR3## wherein R.sub.6 means hydrogen or lower alkyl group, R.sub.8 means lower alkyl, R.sub.7 means cyano or COOR.sub.10, wherein R.sub.10 means hydrgen or lower alkyl or R.sub.1 and R.sub.2 together form a susbtituted or unsubstituted 5 or 6 membered ring which may contain 1 to 2 heteroatom N; R.sub.3, R.sub.4, and R.sub.5 means independently hydrogen, hydroxy or lower alkyl group; Y means N or CH. The compounds may be used in the treatment of congestive heart failure.

Thiadiazines and pharmaceutical compositions thereof as well as method

Substituted benzylideneiminophyenylpyridazinones or dihydropyridazinones of formula I ##STR1## in which R.sub.1 and R.sub.8 independently mean hydrogen or lower alkyl, R2 is hydrogen, lower alkyl, trifluoromethyl, hydroxy alkyl, halogen alkyl, alkoxy alkyl, pyridyl, furyl, thienyl or cycloalkyl or one of optionally substituted groups; aryl, aralkyl, aralkenyl or nitrogen containing heterocyclic ring joining through an alkyl or alkenyl group and R.sub.3, R.sub.4 and R.sub.5 independently mean hydrogen, lower alkyl, hydroxy alkyl, halogen, hydroxy, alkoxy, acyloxy, aroyloxy, formyl, acyl, cyano, amino, carboxy or trifluoromethyl, R.sub.6 and R.sub.7 independently mean hydrogen, amino, lower alkyl, hydroxy, nitro or cyano or R.sub.2 and R.sub.7 together form a --CH.sub.2 --NH-- or --CH.dbd.N-- group and A means phenyl, naphtyl or a nitrogen containing heterocyclic ring. The compounds may be used in the treatment of congestive heart failure.

Substituted pyridazinones

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Espoo, Finland

Jarmo J Pystynen