Bayer Aktiengesellschaft

Nycomed Imaging As

Amersham Health As

Hafslund Nycomed Pharma Aktiengesellschaft

Cambridge Bioclinical Limited

Robertson Towart

Egbert Wehinger

Horst Meyer

Friedrich Bossert

Kurt Stoepel

Stanislav Kazda

Wulf Vater

Arend Heise

Gerhard Franckowiak

Per Jynge

Gunter Thomas

Franz Rovenszky

Klaus Schlossmann

Peter Esch

Jan Olof Gustav Karlsson

Siegfried Goldmann

Jurgen Stoltefuss

Ulrich Rosentreter

Matthias Schramm

Horst Boshagen

Thomas Christoph

Michael Hartmann

Rudiger Sitt

Tudor Griffith

Derek Grant

Anke Bentlage

Benward Garthoff

Jan O G Karlsson

Stanislay Kazda

Jan O Karlsson

Reinhold Tacke

George Terence Evelyn Kealey

Bo Zieden

Hakan Malmgren

Rolf Goran Gustav Andersson

Friedrich Bosseret

Helge Refsum

Lars Goran Wistrand

Anders Olsson

Chelating agents, in particular dipyridoxyl and aminopolycarboxylic acid based chelating agents, and their metal chelates, when linked directly or indirectly to at least one nitric oxide releasing moiety, or when use in combination with nitric oxide or a nitric oxide releasing moiety have been found to be effective in treating a variety of disorders. In particular, such compounds may be used in treating conditions associated with the presence of free radicals in the body, e.g. reperfusion injuries, and in reducing the cardiotoxicity of anti-tumor agents, e.g. anthracyclines and/or paclitaxel.

Nitric oxide releasing chelating agents and their therapeutic use

Novel thienopyran compounds are disclosed, useful as anti-hypertensive agents and for asthma treatment. One group of the compounds has a heterocyclic ring spiro-connected at the 7-position of the thienopyran ring structure. Use of thienopyran compounds in hair growth modulation is described.

Potassium channel activators and their use

The invention provides the use of dipyridoxyl or aminopolycarboxylic acid based chelating agents, metal chelates and salts thereof, in the manufacture of a therapeutic agent for use in the treatment or prophylaxis of atherosclerosis and related conditions in the human or non-human animal body. Preferred compounds for use in the method of the invention are compounds of formula (I) or a metal chelate or salt thereof (wherein in formula (I) each R,independently represents hydrogen or &mdash;CH,COR,; R,represents hydroxy, optionally hydroxylated alkoxy, amino or alkylamido; each R,independently represents a group XYR,; X represents a bond, or a C,alkylene or oxoalkylene group optionally substituted by a group R,; Y represents a bond, an oxygen atom or a group NR,; R,is a hydrogen atom, a group COOR,, an alkyl, alkenyl, cycloalkyl, aryl or aralkyl group optionally substituted by one or more groups selected from COOR,, CONR,, NR,, OR,, &boxH;R,, &boxH;O, OP(O)(OR,)R,and OSO,M; R,is hydroxy, an optionally hydroxylated, optionally alkoxylated alkyl or aminoalkyl group; R,is a hydrogen atom or an optionally hydroxylated, optionally alkoxylated alkyl group; M is a hydrogen atom or one equivalent of a physiologically tolerable cation, e.g. an alkali or alkaline earth cation, an ammonium ion or an organic amine cation, such as a meglumine ion; R,represents a C,alkylene group, preferably a C,, e.g. a C,alkylene group, a 1,2-cycloalkylene group, or a 1,2-arylene group; each R,independently represents hydrogen or C,alkyl; and each R,independently may be absent or represents hydrogen, alkyl, hydroxyalkyl or carboxyalkyl).

Use of chelating agents in the treatment of atherosclerotic conditions

The invention provides the use of a compound of formula (I) or a metal chelate or salt thereof in the manufacture of a therapeutic agent for use in the treatment of prophylaxis of conditions resulting from the presence of free radicals in the human or non-human animal body (wherein in formula (I): each R,independently represents hydrogen or &mdash;CH,COR,; R,represents hydroxy, optionally hydroxylated alkoxy, amino or alkylamido; each R,independently represents a group XYR,; X represents a bond, or a C,alkylene or oxoalkylene group optionally substituted by a group R,; Y represents a bond, an oxygen atom or a group NR,; R,is a hydrogen atom, a group COOR,, an alkyl, alkenyl, cycloalkyl, aryl or aralkyl group optionally substituted by one or more groups selected from COOR,, CONR,, NR,, OR,, &boxH;NR,, &boxH;O, OP(O)(OR,)R,and OSO,M; R,is hydroxy, an optionally hydroxylated, optionally alkoxylated alkyl or aminoalkyl group; R,is a hydrogen atom or an optionally hydroxylated, optionally alkoxylated alkyl group; M is a hydrogen atom or one equivalent of a physiologically tolerable cation; R,represents a C,alkylene group, a 1,2-cycloalkylene group, or a 1,2-arylene group; and each R,independently represents hydrogen or C,alkyl). Such compounds are particularly effective in relieving symptoms associated with reperfusion of ischemic tissue and in treating or preventing radiation-induced injury.

Chelating agents and their metal chelates for treating free radical induced conditions

The invention relates to the use of certain chelating agents and their metal chelates and to the use of certain manganese containing compounds, in particular manganese chelates, in the manufacture of a therapeutic agent for use in reducing the cardiotoxicity of an antitumor agent. Such compounds are particularly effective in reducing the side-effects of anthracycline drugs and/or paclitaxel.

Reduction of cardiotoxicity of an antitumor agent using manganese

The invention relates to heterocyclic amides of the formula ##STR1## in which the radicals A, Z, A.sub.1, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, to a process for the preparation of these amides and to their use as active substances for the curing and amelioration of disorders and diseases which can be treated by exerting influence on potassium channels.

Heterocyclic amides

The invention relates to optically active 1,4-dihydropyridine compounds of Formulas Ia and Ib as defined hereinabove which are effective for influencing circulation. Also included in the invention are compositions containing said optically active compounds and methods for the use of said compounds and compositions.

Optically active 1,4-dihydropyridine esters useful for treating

The compound,

A method of treating a patient suffering from asthma which comprises administering to such patient an asthma-relieving amount of a 5-sulphonyl-1,4-dihydropyridine of the formula ##STR1## in which R.sup.1 is aryl having 6 or 10 C atoms, optionally substituted by 1 to 3 identical or different substituents from the group: halogen, cyano, nitro, trifluoromethyl, trifluoromethoxy, alkoxycarbonyl (up to 4 C atoms), carboxyl, alkoxy (up to 4 C atoms) or straight-chain or branched alkyl having up to 4 C atoms, or is heteroaryl,

Use of sulphonyldihydropyridines as medicaments for the treatment of

1,4-Dihydropyridines of the formula ##STR1## in which n is 0,1 or 2, and

Method of combatting coronary and vascular diseases

1,4-Dihydro-2,6-dimethyl-4-(2'-chlorophenyl)-3,5-dicarboxylic

The invention relates to substituted 2-amino-3,4-dihydropyridine derivative compounds useful, for example as lipid absorption inhibitors. Also included in the invention are methods for the manufacture of said active compounds, compositions containing them and methods for the use of said compounds and compositions.

Substituted 2-amino-3,4-dihydropyridine derivatives, their production

The invention includes new 1,4-dihydropyridazine compounds, compositions containing said 1,4-dihydropyridazine compounds and methods for the use of said compounds and compositions. Also included in the invention are methods for preparing the new 1,4-dihydropyridazine compounds.

1,4-Dihydropyridazine compounds, and their medicinal use

The invention includes, as novel compounds, 1,4-dihydropyridazines and methods for their preparation. Also included are compositions containing said compounds and methods for the use of said compounds and compositions. The compounds of the invention are active as circulation-influencing and spasmolytically active agents.

1,4-Dihydropyridazine compounds

The invention relates to 1,4-dihydro-pyridazine-3-carboxylic acid derivatives and compositions containing said derivatives. Also included in the invention are methods for the manufacture and use of said compounds and compositions. The derivatives of the invention influence the circulation and have a spasmolytic and anti-inflammatory action.

1,4-Dihydropyridazine-3-carboxylic acid derivatives, a process for their

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Wuppertal, Germany

Robertson Towart